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Volume - 1

Chief Editor
Dr. Kavita Chahal
Assistant Professor (Botany), Government College, Bichhua, Chhindwara,
Madhya Pradesh, India

Integrated Publications
New Delhi
Published By: Integrated Publications

Integrated Publications
H. No. - 3 Pocket - H34, Sector - 3,
Rohini, Delhi-110085, India

Chief Editor: Dr. Kavita Chahal

The author/publisher has attempted to trace and acknowledge the materials


reproduced in this publication and apologize if permission and
acknowledgements to publish in this form have not been given. If any material
has not been acknowledged please write and let us know so that we may rectify
it.

© Integrated Publications
Publication Year: 2021
Pages: 137
ISBN:
Book DOI:
Price: ` 747/-
Contents

Chapters Page No.


1. Phenolics & Alkaloids Based Phyto-Secondary Metabolites &
Their Pharmacological Application 01-17
(Anil Kumar Koshal and Sadiya Patel)

2. Allergy and Antihistamine: The Significance of Medicinal


Plants and Their Relevance in Drug Repurposing 19-36
(Dr. Shalini Nema and Dr. Shobha Shrivastava)

3. Xylaria: The Natural Warehouse of Bioactive Potential


Compounds in the Recent Past Decades 37-60
(V. Ramesh and V. Siva)

4. Examples of Plant-Derived Drugs 61-84


(Dr. Sweta Prakash and Dr. Kamini Dubey)

5. Plant Based Drugs: New Era for Cancer Treatment 85-99


(Krati Singh and Shobhit Gupta)

6. Recent Approaches for Plant-Derived Drug Discovery 101-137


(Dr. Aarti Chouhan and Dr. Rajmal Singh Rao)
Chapter - 1
Phenolics & Alkaloids Based Phyto-Secondary
Metabolites & Their Pharmacological
Application

Authors
Anil Kumar Koshal
Assistant Professor, Department of Chemistry, Govt. College
Lateri, Vidisha, Madhya Pradesh, India
Sadiya Patel
Assistant Professor, Department of Chemistry, Government
College Timarni, Harda, Madhya Pradesh, India

Page | 1
Page | 2
Chapter - 1
Phenolics & Alkaloids Based Phyto-Secondary Metabolites
& Their Pharmacological Application
Anil Kumar Koshal and Sadiya Patel

Abstract
The comprehensive and multipurpose medicinal properties of
phytopharmacophores of the plants are basically reliant on their
phytochemical constituents. Commonly, the plant phytopharmacophores
ingredients are classified into two classes based on their role in basic
metabolic phenomenon, namely primary and secondary metabolites. Primary
metabolite is a kind of metabolite that is directly involved in normal life
functions such as growth, development and reproduction of the plants. It
generally accomplishes a physiological function in the organism. It is also
discussed as a fundamental metabolite; therefore, they are more or less similar
in all living organism of the plants.
However, Secondary metabolites are ingredients that are not necessary
for a cell organism to live, but play a vital role by the interaction of the cell
organism with its environment. These constituents are regularly involved in
plants protection against biotic or abiotic stresses.
In the sequence of perusal, the pharmacophore effects of herbals are
concerned with the secondary plant metabolites. Secondary plant metabolites
played an important role in diminishing several ailments in the traditional
pharmacophore and mutual uses. In series of contemporary pharmacophores,
they provided central ingredients for the production of drugs for treating
various ailments from minor up to heart attack, cancer etc. Secondary plant
metabolites are categorized according to their chemical structures into various
groups and sub groups. In this chapter, we will be proposing numerous classes
of secondary plant metabolites, their dispersal in diverse plant families and
their pharmacological applications.
Keywords: phyto-secondary metabolites, alkaloids, phenolics and
phytopharmacophore

Page | 3
1. Introduction
Throughout the ages, people have dependent on nature for their
elementary needs, for the production of food from crops and fruit,
accommodations, clothing, manures, flavours, fragrances and drugs for
treating of various ailments. Plants play an important role in conventional as
well as modern herbal Phyto-pharmacophores [1].
According to the WHO (Worlds Health Organization), any herb, plant,
vegetable, which encompasses the ingredients that can be used for therapeutic
purposes or which are precursors agents of pharmacophore, semi-synthetic
new drug is referred to as medicinal plants [2]. Recently, there has been a
transition in universal trend from synthetic to photochemotherapeutic, which
can be said return to nature. Plant-isolated drugs have been a part of the
evolution of human healthcare for thousands of years. Phytochemistry is the
foundation of the chemotherapeutic uses of medicinal herbs [3]. A good
knowledge of the composition of associate ingredients of medicinal plants
leads to a better understanding of its possible therapeutic worth.
Metabolites are the end products of metabolic processes in plants and
intermediates gradients formed during metabolic processes [4]. Phytochemistry
has pronounced role of primary phytometabolites in elementary life functions
such as cell development, growth, respiration and reproduction [5]. It includes
the various components formed during different phenomena such as
glycolysis, Krebs, photosynthesis and many associate path ways. Primary
phytometabolites include small molecules such as carbohydrates, amino acids,
starch, proteins, nucleic acids etc. In conclusion, the primary phytometabolites
are similar in all alive cells of plants [6].
Secondary metabolites are not necessary as primary metabolites as these
are not directly involved physiological and biological activity of plant cell.
They are organic ingredients which are indirectly play a vital role in survival
of plants but they produce some chemical ingredients which assist them in
their physiological and biological growth and development [7]. Plant secondary
metabolites are organic compounds biosynthetically produce from plant
primary metabolites [8].
Plants secondary metabolites are known to possess various physiological
and biological effects, which assign the scientific base for the use of medicinal
plants in the traditional chemotherapeutic agents in many communities [9].
They have been described as antimicrobial and anticancer and many more
activity against pathogen, therefore they are able to shield plants from
pathogens. Besides, they prevent various stem, fruit and leaf to damage from
the UV light [10].

Page | 4
Secondary plant metabolites are classified according to their chemical
structures into a lot of categories. In this section, the nature of secondary plant
metabolites will be deliberated as a foundation for a review of the main classes
of constituents considered to be of therapeutic importance. Each section
describes an overview of a class of the plant secondary metabolites concerning
structure, botanical spreading in nature and generalizations about
chemotherapeutic uses, followed by examples of representative secondary
metabolites. The category of secondary plant metabolites include:

2. Alkaloids
Alkaloids are primarily found in plants and generally in certain classes of
flowering plants. In fact, one fourth of higher plants are assessed to contain
alkaloids ingredients, among which numerous and different types have been
identified [10]. They occur mostly in seed-bearing plants mainly in berries,
bark, fruits, roots and leaves. Alkaloids often contain at least one nitrogen
atom in heterocyclic ring. These are basic in nature and thus referred as
alkaloid (alkali-like) [11].
Opium poppy (Papaver somniferum) and the ergot fungus (Claviceps)
individually contain about 30 types of different ingredients of alkaloids. The
Ranunculaceae, Solanaceae and Amaryllidaceae are other leading alkaloid-
ingredients containing families. Ergot and few other fungi species also
produce alkaloid [12].
Alkaloids are the important classes of secondary metabolites which are
found to possess important biological properties like analgesic, muscle
relaxant, antioxidant and many more [13]. These are used for the help of
mankind and found beneficial for life-threatening diseases. Some important
phyto-alkaloid described in this chapter are as follow:

Page | 5
2.1 Morphine
Morphine is the first alkaloid compound to be isolated and crystallized in
1804, was the potent active ingredient of the opium poppy, morphine [14]. The
molecular formula for morphine and its hydrate form is respectively
C17H19NO3 and C17H19NO3.H2O, are less soluble in water or lipids. It is a
benzyl isoquinoline alkaloid [15].

Opium poppy morphine


Morphine is used mainly to treat both acute and chronic severe pain. Its
period of analgesia is nearby three to seven hours. It is used for the treatment
of pain due to myocardial infarction and for labor pains also it is beneficial.
Morphine has also been traditionally used in the treatment of acute pulmonary
edema and effective in relieving cancer pain [16].
2.2 Cocaine
Cocaine is a naturally occurring stimulant Phyto-drug which is isolated
from the leaves of the coca plant (Erythroxylon coca). Coca leaves possesses
only about ½-1% cocaine. Chemically the molecular formula of cocaine is
C17H21NO4 and it is the ester of benzoylecgonine with methyl and is also
known as 3β-hydroxy-1αH,5α-H-tropane-2β-carboxylic acid methyl ester
benzoate [17].

Coca leaves cocaine


Cocaine is a tropane alkaloid with central nervous systems stimulating
and shows local anaesthetic efficiency. Cocaine obstruct the dopamine,

Page | 6
serotonin and norepinephrine passage and prevents the re-uptake of serotonin,
dopamine and norepinephrine into pre-synaptic neurons system [18]. This leads
the way to aggregation of the respective neurotransmitters in the synaptic cleft
and may result in improved postsynaptic receptor activation. Cocaine is a
prescribed pharmacological drug used to treat the symptoms of Anaesthesia
of the Nasal Cavity and Mucous Membrane. Cocaine may be used as pure
drug or mix with other medications in constant percentage. Cocaine belongs
to a class of medication known as local anaesthetics, esters [19].
2.3 Colchicine
One of the best known biologically active compounds from ancient times
is colchicine, an alkaloid naturally occurring in Colchicum autumnale a plant
of Liliaceae family and also in Gloriosa superba. It was isolated for the first
time in 1820 from Colchicum autumnale plant (autumn crocus) [20].
Colchicine is an alkaloid compound possessing the molecular formula
C22H25NO6 and chemical name N-[(7S)- 5,6,7,9-tetrahydro-l, 2,3,10-
tetramethoxy-9-oxobenzo(a)heptalen-7-yl)acetamide]. Colchicine contains
three rings, A-ring which is trimethoxy phenyl ring), B-ring which is a
saturated seven membered ring and C-ring which is tropolone ring.

Colchicum autumnale colchicine


Colchicine is pharmacologically used to treat in gout and behçet's disease.
In gout disease, it is less preferred to NSAIDs or steroids. At lower doses, it is
well tolerated, in a review it was mentioned in low-quality evidence that low-
dose colchicine reduced gout symptoms and pain both whereas high-dose
colchicine was effective against only pain. Colchicine is also used as an anti-
inflammatory agent for long-term treatment of Behçet's disease [21].
2.4 Nicotine
Nicotine, an organic phyto secondary metabolite compound that is the
principal alkaloid of tobacco which is isolated from Nicotiana tabacum L.
plant of solanaceae family, is a perennial herbaceous plant. Nicotine occurs

Page | 7
throughout the tobacco plant and especially big amount in the leaves. It is
found only in cultivation, where it is the most commonly grown of all plants
in the Nicotiana genus, and its leaves are commercially grown in many
countries to be produced into tobacco [22].
Nicotine is also known as 3-(1-methyl-2-pyrrolidinyl)pyridine according
to the IUPAC nomenclature. It is a bicyclic compound with a pyridine cycle
and a pyrrolidine cycle with nitrogen as a heteroatom. The molecule possesses
an asymmetric carbon and so exists in two enantiomeric compounds [23].

Nicotiana tabacum leaves nicotine


Nicotine has been used as an pesticide and insecticide since at least the
1690s, in the form of tobacco extracts. But now days chemists have prospered
in using genetically modified tobacco plants to produce drugs for several
autoimmune and inflammatory ailments, comprising diabetes [24].
The primary chemotherapeutic use of nicotine is to treat addiction of
nicotine by eliminating smoking habits and the reduces the damage it does to
health. Controlled levels of nicotine are given to patients through gums,
dermal patches, lozenges, inhalers or nasal sprays to dissuade them off their
dependence [25].
3. Phenolics
Phenolic organic ingredients are plant secondary metabolites, which are
formed in the shikimic acid of plants and pentose phosphate via
phenylpropanoid metabolization. They bear six membered carbon aromatic
rings, with one or more than hydroxyl substituents and range from simple
phenolic molecules to highly polymerized compounds [26].

Page | 8
Phenol
Phenolics compounds probably constitute the versatile group of phyto-
secondary metabolites. They share the presence of one or more phenol groups
as a common characteristic of phenolics and range from simple one aromatic
ring to highly complex secondary plant metabolites ingredients [27].
They are widely available in various phyto families where they contribute
significantly to the taste, colour and flavour of many herbs, foods and drinks.
Some phenolics are preciouses chemotherapeutically for their anti-
inflammatory activities such as quercetin or antihepatotoxic features such as
silybin. Many of the phenolic molecules are also show antioxidants, especially
flavonoids. Phenolics compounds can be broadly classified according to their
structure or biosynthetic mechanism. According to their structures, phenolics
can be classified into some simple phenolics. Some important of them such as
flavonoid, coumarins, xanthones are pharmacological utility discussed in this
chapter [28].
3.1 Flavonoid
Flavonoids are a large subgroup of plant secondary metabolites as
phenolic ingredients compounds, widely available throughout various plants
family and various prokaryotes species.
The general structure of flavonoids is a 15-carbon skeleton, containing 2
benzene rings connected by a 3-carbon linking chain 2-phenyl-1,4-
benzopyrone is basic back bone of flavonoid this is also known as Isoflavan
[29]
.

Flavonoid isoflavone
They represent various class of polyphenolic phyto-secondary
metabolites ingredients with known chemotherapeutic activity. The flavonoid

Page | 9
has also been described to exhibited other useful medication utility such as
antiatherosclerotic, anti-tumour, antioxidant, coronary disorder, anti-micro
pathogens and anti-inflammatory activities [30].
3.1.1 Hesperidin
In the series of various derivatise of flavonoids Hesperidin is an important
organic ingredient of flavonoid isolated from citrus family lemon. Mainly
hesperidin isolated from citrus fruits [31].
Chemically the name and molecular formula of hesperidin is respectively
Hesperitin-7-rhamnoglucoside and C28H34O15 and it is a yellow to brown
powder with a molecular weight of 610.56.

Lemon fruit Hesperidin


A large number of citrus plant pharmacophore contain Hesperidin
ingredients derivative of flavonoids, which have been isolated by many
scientist as having anti-tumour, antibacterial, anti-fungal, anti-inflammatory,
antiviral, antineoplastic, and heart disorder activity. Pharmacological effects
are connected to antioxidant activity of hesperidin, appears through their
ability to scavenge radicals. It has been reported to protect against DNA
damage, lipid peroxidation [32].
3.2 Coumarins
Coumarins are secondary metabolites widely spread in nature, being
found in green plants, fungi, bacteria, in some animal species, in fruits
(bilberry, cloudberry), green tea and other foods and spices. Coumarin was
first isolated from tonka beans in 1820 by A. Vogel [33].
Coumarin (1,2-benzopyrone, 2H-1-benzopyran-2-one, cis-o-coumarinic
acid lactone) is a naturally occurring compound belonging to a large class of
phenolic substances which present an aromatic ring fused to a condensed 6-
member lactone ring. Coumarin is a colourless crystalline solid with a
sweet odour resembling the scent of vanilla and a bitter taste [34].

Page | 10
Coumarin
Coumarin and Coumarin-related organic compounds have proved for
many years having significant therapeutic potential in treating of various
aliments arise due to various pathogens and other agents [35].
These are many important secondary plant metabolites which bearing
classes of coumarin organic compounds. In the series of the coumarin
containing secondary plant metabolites Osthole play an important role.
3.2.1 Osthole
Osthole, is a natural photo-secondary metabolites containing coumarin
first time extracted from Cnidium plant. High content of Osthole is found the
mature fruit of Cnidium monnieri, which is commonly applied in medical
practice of Traditional Chinese Medicine, while it is also broadly found in
other medicinal plants including Angelica, Archangelica, citrus etc. [36]
Chemically the name and molecular formula of osthole is respectively 7-
methoxy-8-(3-methyl-2- butenyl)-2H-1-benzopyran-2-one and C15H16O3.

Cnidium Plant Osthole


Plenty of experimental results demonstrated that osthole exhibits a variety
of pharmacological benefits including neuroprotection, osteogenesis,
immunomodulation and cancer combating properties, making it a potential
multitarget complementary medicine and functional food [37].
3.3 Xanthones
Xanthones are natural occurring polyphenols with the basic molecular
formula C13H8O2 that are commonly found in lichens, fungi and seven major
genera of higher plants: Anacardiaceae, Gentianaceae and Guttiferae etc.

Page | 11
Chemically general structure of xanthone having three fused six membered
aromatic ring in which centred ring bearing oxygen as a heteroatom.

Xanthones
Plants belonging to the family Gentianaceae are known for their bitter
taste due to the bearing of xanthones and are used in traditional remedies
against loss of appetite and fever and are still included in many “tonic”
preparation [38].
Xanthones isolated from natural sources are classified into six main
groups, namely, simple xanthones, xanthone glycosides, prenylated
xanthones, xanthonolignoids, bisxanthones and miscellaneous xanthones [39].
Xanthones are testified to give CNS stimulation and have strong
hypoglycemic and anti-inflammatory activity. A crude extract of Swertia
which bearing xanthones moiety has been assigned to insect repellent activity.
In the series of Xanthone derivatise Mangostin is a important ingredients [40].
3.3.1 Mangostin
Mangostin is an important natural occurring plant-secondary metabolite
of xanthones derivative. The main source of mangostin is Mangosteen
(Garcinia mangostana Linn.) is a tropical plant from India, Myanmar,
Malaysia, Philippines, Sri Lanka and Thailand. Mangostin isolated from the
pericarp of mangosteen-fruit. Mangosteen Garcinia mangostana Linn
commonly called “Queen of fruits and Food of Gods” [41].

Mangosteen fruit mangostin


In this chapter, medicinal assistances of mangosteen are categorized into
numerous distinct areas including anti-cancer, anti-micro-pathogen and anti-

Page | 12
diabetes. Furthermore, its protection against damages and disorders in various
humanoid organs such as liver, skin, joint, eye, neuron, bowel and
cardiovascular tissues [42].
Conclusion
This chapter contains the importance of phyto-secondary metabolites
organic ingredients from various plants species, with their classification, and
pharmacological applications.
Since there is a persistent and crucial requirement for new medication
agents to fight against tumour, cardiac aliments, cytotoxic, pathogen
infectious diseases and autoimmune disorders of both animals and plants. The
fight against any aliments is a vibrant symmetry between modern
chemotherapy and natural selection on infectious or invasive agents. If the
scientific circle is to put endless importance in this never-ending effort, then
novel sources of bioactive phyto-secondary metabolites with new activities
must be discovered. Phyto-secondary metabolites with noteworthy
pharmacological activity are considered as an alternative to most of the
synthetic pharmacophore and other commercially valuable components.
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39. Andri Cahyo Kumoro, Annisa Sholikhati. Dissolution Rates of
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Ibarra, Jazmin M Pérez-Rojas. Medicinal properties of mangosteen
(Garcinia mangostana), J Pedraza-Chaverri et al./Food and Chemical
Toxicology. 2008; 46:3227-3239.
42. Ali Ghasemzadeh, Hawa ZE Jaafar, Ali Baghdadi, Amin Tayebi-
Meigooni. Alpha-Mangostin-Rich Extracts from Mangosteen Pericarp:
Optimization of Green Extraction Protocol and Evaluation of Biological
Activity, Molecules. 2018; 23(1852):1-16.
doi:10.3390/molecules23081852
43. Fabiola Gutierrez-Orozco, Mark L Failla. Biological Activities and
Bioavailability of Mangosteen Xanthones: A Critical Review of the
Current Evidence, Nutrients. 2013; 5:3163-3183.
doi:10.3390/nu5083163.

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Chapter - 2
Allergy and Antihistamine: The Significance of
Medicinal Plants and Their Relevance in Drug
Repurposing

Authors
Dr. Shalini Nema
Assistant Professor, Govt. MGM PG College, Department of
Botany, Itarsi, Hoshangabad, Madhya Pradesh, India
Dr. Shobha Shrivastava
Professor and Head, Department of Botany, Sarojini Naidu
Government Girls PG College, Bhopal, Madhya Pradesh, India

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Chapter - 2
Allergy and Antihistamine: The Significance of Medicinal
Plants and Their Relevance in Drug Repurposing
Dr. Shalini Nema and Dr. Shobha Shrivastava

Abstract
Allergic disorders encompass skin, food and respiratory allergies. Study
present here includes plant metabolites like Polyphenols, Quercetin,
Gossypin, Saponin, Steroidal lactone, alkaloids and many others are such
class of compounds that are found in foods and plant sources and have been
investigated for their anti‐allergic, antihistamine and anti-inflammatory
properties. These plants display their antiallergic potential through affecting
mast cell, immunoglobulin, histamine and inhibiting different cytokines and
interleukins. Research into repositioning known drugs to treat off target
diseases other than the originally intended disease continues to grow and
develop for therapeutic purposes. Phytoconstituents and the recent
knowledge about SARS-CoV and SARS-CoV-2 pathology, profess their use
in the prevention and management of COVID-19 pandemic. It is, therefore,
believed to be an emerging strategy where existing plant metabolites having
already been tested safe in humans, are redirected based on a valid target
molecule to combat particularly, rare, neglected and difficult-to-treat
diseases.
Aim: This review provides an overview of antallergic and antihistamine
potential of respective plant extracts and also assess their use in drug
repurposing against viral infections with focus on prevalent corona virus
disease.
Keywords: Plant metabolites, Antiallergy, Antihistamine, Antiviral, Drug
repurposing, SARS-CoV-2, Coronavirus.
Introduction
An allergy is an immune response, or reaction to substances that are
usually not harmful. In someone with allergies, the immune response is
oversensitive when it recognizes an allergens and induces the release of
histamine. The substances that trigger the overreaction are called allergens.

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The symptoms that result are called an allergic reaction. Histamine causes
vessels to swell and dilate, leading to allergy symptoms.
The physiological mechanism of allergic reactions is the same in
everyone. Allergens enter the body-either through ingestion, inhalation or
contact with the skin or mucous membranes. This causes white blood cells to
release an antibody which then binds to w mast cells. The mast cells rupture-
and in the process, release biochemical substances including histamine.
Anaphylaxis and Allergen
Anaphylaxis is an allergic disease that occurs when the body is exposed
to specific allergen. It could be caused by a variety of exogenous substances
like allergens that include heterologous serum (such as tetanus antitoxin),
certain animal proteins (such as that of fish, shrimp, and crabs), bacteria,
viruses, parasites, animal fur, plant pollen, dust mites in the air, and
chemicals and drugs. Allergens could stimulate human B cells to produce
immunoglobulin E, which combines with antibodies on human mast cells
and sensitized cells, damages the cell membrane and leads to degranulation,
and releases histamine.
Histamine and its receptors
Histamine is synthesized and released by different human cells,
especially basophils, mast cells, platelets, histaminergic neurons,
lymphocytes, and enterochromaffin cells. It is stored in vesicles or granules
released on stimulation. Histamine exerts its effects on target cells in various
tissues by binding to its four receptors: histamine receptor (HR)1, HR2, HR3,
and HR4.These receptors belong to the G protein-coupled receptors family
(GPCRs) (Jutel, M. et al. 2005). H1 receptor (HR1) is codified in the human
chromosome 3 and is responsible for many symptoms of allergic diseases,
such as pruritus, rhinorrhea, bronchospasm, and contraction of the intestinal
smooth. The presence of histamine stabilizes the receptor in its active form.
Antihistamines
Antihistamines are used in the management of allergic conditions. They
are useful for treating the itching that results from the release of histamine.
There fore, antihistamine are medicines that treat allergy symptoms by
blocking the effects of histamine by stabilizing the inactive form of the
receptor.
Mechanisms of action
Antihistamines are competitive inverse agonists at the H1 receptor that
have preferential affinity for the inactive state of the receptor and stabilize it

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in this conformation. Therefore, they are ‘inverse agonists’ that reduce the
basal level of constitutive activity at histamine H1 receptors as well as
blocking the agonist effects of histamine.
Antihistamines effects
1) Suppression of many of the vascular effects of histamine, with a
reduction of vasodilation and oedema.
2) Inhibition of the accumulation of inflammatory cells in tissues.
3) Suppression of the immune response to antigens.

Fig 1: Mechanism of Action of active and inactivehistamine receptor

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Importance of medicinal plants: A review
Plant-derived substances have recently become of great interest owing
to their versatile applications. Medicinal plants are the richest bioresource of
drugs of traditional systems of medicine, modern medicines, nutraceuticals,
food supplements, folk medicines, pharmaceutical intermediates and
chemical entities for synthetic drugs.
Antihistamine have many drawbacks including side effects of
drowsiness and significant anticholinergic side effects. As a result, many
patients with chronic allergic conditions, such as asthma, seek
complementary alternative medicine (CAM) in order to achieve better
control of symptoms. CAM is a set of healing resources that includes herbs
that are used in traditional medicine (Slader, C.A. 2007). Bioactive natural
products have played a key role in discovery of many important drug
molecules and therefore medicinal plants are considered as potential sources
a of new chemical entities (NCE) including viral drugs.
Singh, et al. (2011), highlight the presence of polyphenols in the daily
diet confer them a safety profile and justifies their recognition as anti-
allergic agents. It is known that polyphenols can form insoluble complexes
with allergenic proteins changing their structure or rendering it less
bioavailable.
Okunade, et al. (2004) have observed that plant alkaloids have
considerable biological activity. They are known to have pharmacological
effects and are used in medication.
Flavonoids are a class of natural product that is most extensively found
in food associated with anti-allergic activity (Kempuraj, et al. 2005). On the
other hand, saponins which are frequently found in several food plants such
as soybeans, peas, spinach, quinoa, licorice, ginseng, capsicum peppers,
eggplant and yam, present glucocorticoid-like activity and have huge
biologic potential (Francis, et al., 2002).
Tannin contributes various medicinal properties such as antimicrobial,
anti-inflammatory and astringent activity. They have been also reported to
have anti-viral, antibacterial and anti-parasitic effect (Holvoet, et al. 2012).
Thymoquinone (TQ) is a chief bioactive constituent of black seed oil
(Nigella sativa). TQ holds promising pharmacological properties against
several diseases. It exhibits outstanding antioxidant, anti-inflammatory,
anticancer, and other important biological activities, (Rahman, et al. 2020).

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Drug Repurposing/drug repositioning
Drug repurposing is a process of identifying new uses for approved or
investigational drugs and it is considered as a very effective strategy for drug
discovery as it involves less time and cost to find a therapeutic agent in
comparison to the de novo drug discovery process. Drug repositioning
utilizes the combined efforts of activity-based or experimental and in silico-
based or computational approaches to develop/identify the new uses of drug
molecules on a rational basis. It is, therefore, believed to be an emerging
strategy where existing medicines, having already been tested safe in
humans, are redirected based on a valid target molecule to combat
particularly, rare, difficult-to-treat diseases and neglected diseases.
Challenges
Drug repositioning is a complex process involving multiple factors such
as technology, commercial models, patents, and investment and market
demands. Another important issue is related to patent application and
intellectual property rights (IPR). There are no provisions of IP protection of
drug discovery by repositioning approach as per the IP and patent laws. For
repositioned drugs, IP protection is limited (Rudrapal. M., 2020).
Significance and Benefits
This process do not require the initial processes of testing and approval
thus saving time and resources. Most importantly, the already existing
approved drugs have a known safety profile, which makes it an attractive
proposition.
Drug repurposing has numerous advantages over conventional drug
discovery approaches, including:
1) Considerably cuts research and development (R&D) costs.
2) Reduces the drug development timeline, as various existing
compounds have already demonstrated safety in humans, it does not
require Phase 1 clinical trials.
3) Potential for reuse despite evidence of adverse effects and failed
efficacy in some indications.
Some popular drug repurposing approaches include
1) Repurposing oncology drugs.
2) Repositioning drugs across therapeutic areas.
3) Aspirin: Is a powerful drug that is not only being evaluated in the
oncology field, but also in cardiac-related indications such as
myocardial infarction.

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4) Repurposing drugs to treat COVID-19: Drugs are also being
repurposed as a treatment strategy against COVID-19, the disease
caused by SARS-CoV-2. Several drugs are being evaluated
including Lopinavir/ritonavir, Danoprevir plus Ritonavir and other
combinations, Remdesivir etc.
Why phytoconstituents are a proven significant source?
Reasons
1) Demonstrate a broad spectrum of activity against pathogenic
species.
2) Rarely have severe side effects.
3) Often possess the immunomodulatory action in humans.
Mechanism of action
Secondary Metabolites can affect the microbial cell in several different
ways. These include the disruption of cytoplasmic membrane function and
structure, interaction with the membrane proteins, interruption of DNA/RNA
synthesis and function, destabilization of the proton motive force with
leakage of ions, prevention of enzyme synthesis, induction of coagulation of
cytoplasmic constituents, and interruption of normal cell communication
([Anand U. et al., 2019; Radulovic, et al., 2013). For example, Berberine
(alkaloid group) from Berberis spp., can severely damage the structure of
bacterial cell membranes and inhibit the synthesis of proteins and DNA
under interaction with Streptococcus agalactiae.
Obviously, each compound that is extracted from a plant is not ready to
be instantly used in routine clinical practice. We need antibacterial with
sufficiently low inhibitory concentrations, minimal toxicity, and ease
bioavailability for efficient and safe use in humans. Current advances in bio
screening research, including the omics technologies, first of all
metabolomics, will enable us to both catch and identify even very low-
quantity active phytochemicals and clarify the specific molecular
mechanisms underlying their effect(s) on bacterial targets (Cyrill. et al.,
2020).
Ethnomedicinal plants: Their role in Antiallergy and Drug
Repositioning.
Given below is a brief description of some potential ethnomedicinal
plants which are known to exhibit anti allergic and antihistamine activity and
are used in Chinese traditional system of medicine, Ayurvedic system, Unani

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and as Prophetic medicines. These plants are explored further for drug
discovery and repurposing drugs for other ailments. (Table: 1).
Methodology
The available informations on the medicinal plants which characterized
antimicrobial potential were collected from electronic scientific databases:
Pub Med, Science Direct, Scopus, Web of Science and Google Scholar. A
total of 11 plants were included in the present review. Reviews from Various
researchers regarding natural compounds from various medicinal plants were
studied (Table: 1).

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Table 1: Antiallergic Effects of Plant Species, Biological Response and reproposition

Important
S. No. Plants Drug effect Reference Repurposing drug Reference
phytoconstituents
Allium cepa, Malus Inhibition of histamine e
domestica, Camellia release, decrease in pro- -Zhang D.H. et
Quercetin Mlcek. J. et
1. sinensis and inflammatory cytokinesis Against SARS-CoV-2 al., 2020 Lee H.
(flavonoid) al., 2016
Fagopyrum suppressed interleukin IL-4 et al., 2015
esculentum. production.
Inhibit antiprurities,
Hibiscus vitifolius (Gossypin) systemic anaphylaxis Ganapaty S, Lee j. et al.,
2. Against Herpes simplex virus
Linn Bioflavonoid reactions reduced the et al., 2010 1999
histamine release
Mast cell membrane
Aristolochia Chitme et al. Broad spectrum of
3. Chloroform extract stabilization, Inhibiting Negi, et al. 2003
bracteolate Lamk. 2010 antibacterial activity
histamine pathway.
High antiviral activity on
Lee J-H, et
Camellia japonica L. porcine epidemic diarrhea Yang J.-L., et
4. Ethanol Degradation of mast cell al.,
Theaceae Leaf. virus (PEDV) of corona virus al., 2015
2008
family
Camellia sinensis Morikawa T. In various antivirus vaccines Sharma R. et al.,
5. Saponin Decrease histamine level
(L.) O. Kuntze et al., 2007. (saponin based adjuvants) 2020
Antiviral activity on herpes
Cordia verbenacea Fernandes et Hayasi K et al.,
6. Sesquiterpene Decrease edema simplex virus type 1 (Cordia
D.C. al., 2007 1990
salicifolia)
Decrease the expression
Withania somnifera Malik F. et Against SARS-CoV-2 S Dhawam m. et
7 Steroidal lactone of IFN-IL-2 and decreases
(L.) Dunal. al., 2007 protein al., 2021
IL-4 level

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Treatment for
neurogenerative disease like
Fungicidal, antihistamine Naik. M. et (Dash et al.,
8 Azadirachta indica Nimbin (Triterpene) Alzheimer’s and Parkinson’s
and antiseptic properties. al., 2014. 2017)
disease, Type 2 Diabetes
Mellitus and Polycythemia
Alkaloid, cinnamic
9 Solanum nigrum Cai X-F, et Anti-Hepatitis c virus v et al., Javed et al.,
acid ester, steroid Degranulation of mast cell
L. al., 2010. Accine 2011
derivative (spirostan)
Cao. w. et al. Against AIDS. Hatori. T. et al.,
10 Glycyrrhiza uralensis glycyrrhizin Antihistamines
2020 (inhibit HIV replication). 1989.
Reducing the release of Alsamarai
inhibit SARS-CoV-2 Rahman, M.T.
11 Nigella sativa Thymoquinone (TQ) histamine and leukotrienes, A.M, et al.,
replication. 2020
anti-inflammatory. 2014

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Combating covid-19: Impact of antiallergic bioactive compounds on
viral activity
Camellia sinensis (L.) O. kuntze
Saponin-based adjuvants selectively stimulate Th1 and cytotoxic T cell
responses because they direct antigens into endogenous processing pathways
and enhance IFN-γ release by dendritic cells. As a result, a robust antibody
and cell-mediated immune response is activated. Therefore, more research is
needed to develop saponin adjuvanted recombinant spike or RBD protein
subunit vaccine. Development of a saponin adjuvanted subunit vaccine for
SARS-COV-2 would also help us in tackling future pandemics associated
with other novel coronaviruses (Sharma R. et al., 2020).
Withania somnifera
The medicinal attributes of W. somnifera are owing to a broad range of
bioactive secondary metabolites including steroidal lactones [withanone,
withanolide D, withanolide A, and withaferin A (WFA)]. Among these,
WFA is one of the most interesting naturally occurring bioactive compounds
that possess potent anti-tumorigenic, anti-inflammatory, pro-apoptotic, anti-
angiogenic, and anti-invasive activities. WFA might bind to SARS-CoV-2 S
protein and alter the S protein, thereby hindering its access into the host
cells. Withanone and Withanoside V can impede the functional activities of
SARS-CoV-2 main protease (Mpro). Withanolides have been found to
control cytokine secretions during infection and could alleviate the cytokine
storm in the lungs. The combined use of withanolides are several other drugs
or therapeutic modalities, such as hydroxychloroquine and dexamethasone,
has been demonstrated as an efficient strategy to improve the effectiveness
of therapeutic regime for COVID-19 treatment (Dhawam. et al.,2021).
Glycyrrhiza uralensis
Licorice root (Glycyrrhiza uralensis) has shown strong antiviral activity.
It was observed that extracted substance, glycyrrhizin sulphate, inhibit HIV
replication, interfere with virus-to-cell binding and cell-to-cell infection, and
induce IFN activity (Hatori. T. et al., 1989).
Nigella sativa (black seed)
Nigella sativa could be considered for its bioactive components such as
thymoquinone which was proven to have anti-viral activity. Further benefits
to use N. sativa could be augmented by Zn supplement. Notably, Zn has
been proven to improve innate and adaptive immunity in course of microbial
infection. The effectiveness of the Zn salt supplement can be enhanced with

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N. sativa as its major bioactive component might work as ionophore to allow
Zn2+ to enter pneumocytes and inhibit SARS-CoV-2 replication by stopping
its replicase enzyme system (Rahman, M.T. 2020).
Allium cepa, Malus domestica, Camellia sinensis and Fagopyrum
esculentum
During the SARS-CoV-2 pandemic, Research based on molecular
docking models with pharmacological network analysis for testing bioactive
compounds have shown that quercetin from onions (Allium cepa), apples
(Malus domestica), green tea (Camellia sinensis) and buckwheat
(Fagopyrum esculentum) can inhibit the 6LU7 and 6Y2E proteases of
SARS-CoV-2 by binding to them (Zhang D.H. et al., 2020 and Lee H. et al.,
2015).
Cordia salicifolia extract
Partially purified extract from whole plant of Cordia salicifolia showed
an inhibitory effect on herpes simplex virus type 1 (HSV-1). The activity of
on different steps of HSV-1 replication in HeLa cells was investigated.
Under single-cycle replication conditions, extract exerted a greater than
99.9% inhibition in virus yield. The extract has been shown to have a direct
virucidal activity (Hayasi K et al., 1990).
Azadirachta indica
Nimbin (triterpene) has shown to have antipyretic, fungicidal,
antihistamine and antiseptic properties. Also Nimbin is associated with anti-
inflammatory and antioxidant effects, therefore reducing damage by
mitigating the production of reactive oxygen species. Their metabolites
found in Neem extracts are: limonoids, tannins, alkaloids, terpenoids,
reducing sugar, catechins, sterols and gallic acid. Biochemical analysis done
on leaf extracts has revealed high presence of proline, which is a current
treatment for neurodegenerative diseases like Alzheimer’s and Parkinson’s
disease, Type 2 Diabetes Mellitus and Polycythemia (Dash et al., 2017).
Solanum nigrum
Hepatitis c virus (HCV) infection is a serious global health problem
necessitating effective treatment. Currently, there is no vaccine available for
prevention of HCV infection due to high degree of strain variation.
Methanolic and chloroform extract of Solanum nigrum seeds play a role in
viral clearance during natural HCV infection. These data also suggest that
therapeutic induction of extracts might represent an alternative approach for
the treatment of chronic HCV infection or the present study leads to the

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development of more potent and orally available HCV therapeutic drug
(Javed et al., 2011).
Hibiscus vitifolius Linn
The inhibitory effects of 12 flavonoids including gossypin against
plaque formation of Herpes simplex virus type 2 (HSV-2) and 1 (HSV-1)
was evaluated. It was found potent against HSV-1 and HSV-2 respectively
(Lee j. et al., 1999).
Conclusion
Study here suggests that all the compounds and plants identified for
allergy and antihistamine also showed antiviral potential when reproposed,
hence unlocking a close relationship between ethnobotanical research and
antiviral properties in plants.
Viruses can develop resistance through mutation to current antimicrobial
agents, and this increases the need for the discovery and development of new
effective compounds against old and new viral infections, especially against
SARS-CoV-2. Secondary metabolites such as terpenes, flavonoids,
alkaloids, saponins and stilbenes have been characterized through antiviral
activity assays (Liu A. et al., 2012).
Plants secondary metabolites: Future perspectives
Research shows that some secondary metabolites of plants possess high-
levels of intrinsic antimicrobial activity. However, it should keep in mind
that, even in the case when a plant-derived substance reveals strong
antibacterial, antifungal and antiviral effects, there is always the possibility
that microorganism will appear to be non-susceptible or develop resistance
to it. Therefore, a way to combine plant metabolites with conventional
antibiotics might be the most profitable. Such combinations act at different
target sites in bacterial cells and lead to high levels of efficacy, especially in
suppressing the development of resistance. A detailed understanding of the
molecular mechanisms underlying the action of phytochemicals, or of those
underlying phytochemical-antibiotic interactions, is required for developing
a successful therapeutic approach. The versatility of secondary metabolites
and their low toxicity may provide novel antibiotics to tackle MDR (Multi-
Drug Resistant) microbes too.
Today, advanced and rapid acting extraction, purification, and
characterization techniques are needed for studying plant metabolites as well
as multidisciplinary expertise and funding are very essential for novel drug
discovery.

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Chapter - 3
Xylaria: The Natural Warehouse of Bioactive
Potential Compounds in the Recent Past Decades

Authors
V. Ramesh
Department of Botany, Vivekananda College, Tiruvedakam
West, Madurai, Tamil Nadu, India
V. Siva
PG and Research Department of Microbiology, VHNSN
College, Virudhunagar, Tamil Nadu, India

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Chapter - 3
Xylaria: The Natural Warehouse of Bioactive Potential
Compounds in the Recent Past Decades
V. Ramesh and V. Siva

Abstract
Xylaria is a large and the first described genus of the family Xylariaceae
and reported to be promising and significant natural source of bioactive
compounds. Bioactive novel natural compounds discovery and invention is a
multidisciplinary endeavor that includes the search for new potent
pharmaceuticals. Xylaria produce enormous diversified bioactive
compounds with anticancer, antioxidant, antimicrobial, immune-stimulatory
as a secondary metabolite via natural fruiting bodies as well as fermentation
process and can be inexhaustible and sustainable resource. Researchers
reported so far Xylaria as macro fungi as well as endophytic forms natural
ware houses of biologically active compounds. Recent research and
development technologies has opened new avenue on fungal research for
highly sustainable and economically feasible novel natural products which
are the frontiers of new drug invention. In this present review, we compiled
the detailed reports of diverse class of novel secondary metabolites produced
by the fungal species of Xylaria of its pharmaceutical importance.
Keywords: biological activity, endophytic Xylaria, macro fungi, novel
natural products
Introduction
Nature has proven to be an endless source of abundant diversity of
chemical entities with varying biological activities. The world health
organization estimates that 80% of the world's population depends on
traditional medicine for treating their everyday health problems. Natural
products play a major role as active substances, model molecules for the
discovery and validation of drug targets. Natural product researchers from
fungal metabolite were revolutionized by the discovery of penicillin. It has
factually saved millions of lives and sparked an era of fungal derived
medicines (Tulp & Bohlin, 2004). This discovery of penicillin is still a front-

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line antibiotic for some common bacterial infections, although its
effectiveness is now limited by the development of drug resistant gram-
negative bacteria. The phenomenal success of penicillin led to the intensive
search for other antibiotic producing fungi.
Plant kingdom harbors different kinds of microbes such as bacteria and
fungi which are potent to producing biologically unique and diverse range of
novel natural products (Rai et al., 2021). Fungi have been shown to be one
source of a variety of useful natural products. They were common in nature
and considered as good antimicrobial agents (Lindequist et al., 2005; Abad
et al., 2007; Muhsin et al., 2011). As of 2010 approximately half a million
natural products were known of which 60000 - 80000 are estimated to be of
fungal origin. Approximately half of the latter display some kind of
biological activity. Important discoveries other than antibiotics have
included cyclosporine, an immunosuppressive drug used to prevent rejection
of transplanted organs, produced by Tolypocladium inflatum (Hyde, 1996).
The anticancer agent paclitaxel which was commonly known as taxol
provides an interesting case. Initially it was thought to be produced solely
from the bark of Taxus brevifolia Nutt, but it was later found to also be
produced by the fungus Taxomyces andreanae (Katz, 2002; Strobel & Daisy,
2003). Macro fungi have been proved to be one of the most productive
sources for producing a large and diverse variety of secondary metabolites
with significant bioactivities (Mugdha et al., 2010). These are krestin from
the cultured mycelium of Trametes versicolor, lentinan from the fruiting
bodies of Lentinus edodes and schizophyllan from the culture fluid of
Schizophyllum commune (Mizuno, 1993). Their previous successes in
yielding useful natural products, their extensive habitat range and number of
species yet to be discovered imply that fungi will continue to be a promising
source of novel antibiotics. Endophytic fungal species are also recorded as
natural ware house of potential bioactive compounds with pharmaceutical
importances (Newman & Cragg, 2016).
The Xylariaceae is a large and relatively well-known ascomycete family
found in most countries (Whalley, 1996) and it contains 35 genera (Eriksson
& Hawksworth, 1993). It is characterized by perithecial ascocarps bearing
paraphyses and periphyses that are embedded in a stroma. The asci of most
species bear a ring at the apex that appears as a characteristic amyloid ascal
plug when stained with iodine. Many species of Xylaria actively decay wood
of living or dead angiosperms and are known to be saprobic in most cases
(Rogers, 1979). They are saprobic or sometimes weakly to strongly parasitic
on woody plants. Although they are found mostly on wood, some species are

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found on sawdust, leaf and dung or soil. Moreover, Species of Xylaria living
inside the plant tissues like stem, leaf and bark of both angiosperms and
Gymnosperms as an Endophytic fungi (Boonphong et al., 2001). Families of
Xylariaceae (for illustrations of representative species see Fig. 1, 1a & 1b)
represented one of the most important and prolific lineages of secondary
metabolite producers among the fungal kingdom (Becker & Stadler, 2021).
In this review, we divided this into two major parts, the first one is dealing
with isolation & identification and second the part consists of interesting
novel bioactive compounds from the large genus of Xylaria of the family
Xylariaceae.

a) X. melanura b) X. telfairii c) X. grammica d) X. primorskensis e) Xylaria sp.


(JF795290), f) X. curta (JF795289) g) Xylaria sp. (KC405623) h) X. digitata & i) X.
persicaria (Kevin Becker & Marc Stadler 2021); (Mohd Adnan et al., 2018);
(Ramesh et al., 2012)
Fig 1: Fruiting bodies of some species of Xylaria

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a) X. apiculata b) X. carpophila c) X. cubensis d) X. curta e) X. feejeensis f) X.
filliformis (Koyani et al., 2016)
Fig 1a: Fruiting bodies of some species of Xylaria

a) X. gigantea b) X. longipes c) X. nigripes d) X. polymorpha (Karun & Sridhar, 201)


Fig 1b: Fruiting bodies of some species of Xylaria

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Isolation and Identification
Isolation of Xylaria as a macro fungus
The fruiting body or stromata of the Xylaria spp. was washed
thoroughly with sterile distilled water and was thereafter aseptically broken
with aid of a sterile forceps. A small piece of 2×2 mm of the fruiting body
was aseptically transferred onto plates containing PDA with 50 μg/mL of
streptomycin to suppress bacterial growth. The plates were incubated at 30
°C for three weeks for the development of fruiting body (Fig. 2). The fungi
growing out from the fruiting bodies were subsequently transferred onto
fresh PDA plates without antibiotics (Ramesh et al., 2012).

Fig 2: Graphical representation of mycelial cultivation macro fungal species of


Xylaria
Isolation of Xylaria as an endophytic fungus
Commonly Xylaria sp., which are common endophytic inhabitants of
most tropical plants, have been previously investigated for their production
of new metabolites and have proven to be a good source of bioactive
compounds (Espada et al., 1997). For isolation of endophytic fungi, any one
of the asymptomatic healthy plant materials such as stem, leaf and bark were
thoroughly washed in running tap water, and then it is surface sterilized by a
slightly modified standard protocol of Raviraja (2005). The selected plant
tissue were immersed in 95% ethanol for 30 s, 4% sodium hypochlorite
solution for 60s and 95% ethanol for 30 s followed by rinsing with sterile
distilled water three times for 10 s and allowed to surface dry under sterile
conditions. After drying, each plant material segment was cut into
approximately 0.2-0.5cm squares and placed on Petri plates containing basic
fungal culture medium such as potato dextrose agar medium (PDA)

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supplemented with streptomycin (100 mg/L) to suppress bacterial growth.
Petri plates were sealed with cling film and incubated at 30 °C in a light
chamber for up to one week. They were monitored every day for growth of
endophytic fungal colonies. Fungi growing out from the samples were
subsequently transferred onto fresh PDA plates. The procedure of
transferring to fresh PDA plates was carried out several times in order to
isolate pure colonies (Fig. 3). Morphological characteristics such as size,
shape and color of the fruiting bodies allow the identification of the fungal
species of Xylaria (Sutton and Cundell, 2004) and it was reinforced by
molecular confirmed by rRNA sequence comparisons (Altschul et al., 1990).

Fig 3: Graphical representation of Isolation of Endophytic Xylaria


Screening of bioactive novel natural products
Owing to the fungal bioactive metabolic unique versatility, ecological
diversity and essential role in nature, fungi have been attracted the attention
of various interdisciplinary researchers such as biologists, chemists,
biochemists, geneticists, ecologists and naturalists in myriad ways (Tkacz &
Lange, 2004). The use of Xylaria species for the production of
pharmaceutically important products has a long tradition, but it has increased
rapidly over the past half century (Papagianni, 2004). Secondary metabolites
from the genus of Xylaria have broad spectrum of biological activities. Since
the discovery antibiotic agent penicillin from Penicillium (Fleming, 1929),
interest to find bioactive compounds from fungal genus has increased

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considerably. Many important secondary metabolites that are potential leads
for treatment of human diseases such as antioxidants, antimicrobial agents,
immunomodulatory agents and anticancer agents, etc., have been identified
from this genus (Song et al., 2011; Wu et al., 2011; Ko et al., 2009; Yin et
al., 2011).
Xylaria as a source of anticancer agents
Based on the report of world health organization, 80% of the world’s
population predominantly in the developing countries rely on plant based
natural products as therapeutic agent for the health care (Gurib-Fakim et al.,
2006). Bioactive Natural products and their derivatives represent one of the
important and more than 50% of all the drugs in clinical use of the world.
Almost 60% of the drugs approved for cancer treatment are of natural origin.
Moreover, as per the research report says that, more than 70% of the
anticancer and antimicrobial bioactive compounds were derived from fungal
origin (Newman & Cragg, 2020).
In the unremitting search for novel bioactive compounds from the
species of Xylaria led to abundant natural products with bioactivities. In the
Table 1, xylarichalasin A from endophytic Xylaria sp. isolated from roots of
Damnacanthus officinarum showed the strongest activity against human
cancer cell lines MCF-7 with IC50 value of 6.3 μM and SMMC-7721 with
IC50 value of 8.6 μM (Wang et al., 2020). Likewise, cytochalasans
derivatives from solid-state rice fermentation extract of X. longipes was
reported by Wang et al., (2019). It is a novel compounds and exhibited
cytotoxicity of IC50 > 40 μg/mL against human cancer cell lines like HL-60.
Noppawan et al., (2020) reported and cultivated wood decaying macro
fungal species of Xylaria. It has also cytochalasin named cytochalasin (Fig.
4) found to be active against HeLa cells (IC50 57 μg/mL), HT29, HCT116,
MCF-7 (IC50 90 to >100 μg/mL). Similarly, curtachalasins A and B are
bioactive cytochalasans from xylariaceae were found in the species of
endophytic Xylaria cf. curta isolated from the potato stem tissue. These
metabolites have promising bioactivities in its initial screenings for
cytotoxicity and antimicrobial activities (Wang et al., 2018). A patent was
published and dealing with a macrolide compound of clonostachydiol from
X. curta, which showed cytotoxic effects against several human cancer cell
lines (Ai et al., 2018). It was also the same compounds were isolated and
reported from the Xylaria sp. and exhibited moderate cytotoxicity against
diverse human cancer cell lines like HL-60 and A-549 with IC50 values of
4.9 and 25.6 μM, respectively (Ojima et al., 2018). Selective cytotoxic of a
novel cytochalasin was isolated from a marine-derived Xylaria sp. and

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named cytochalasin P1 (Fig. 4). It is chemically know as 19, 20-epoxide of
the known cytochalasin P. It has significant cytotoxicity against human
tumor cell lines like SF-268 and MCF-7 with the IC50 values of 1.37 and
0.71 μM (Chen et al., 2017).
Moreover, Ramesh et al., (2015a, & 2015b) studied and reported
significant antitumor activity of both natural fruiting bodies and cultural
filtrate crude extract as well as partial purified fraction against human cancer
cell lines such as MDA-MB-231 (Breast carcinoma cells), A549 (Lung
carcinoma cells) and MCF-7 (Breast carcinoma cells). Wei et al., (2015)
isolated bioactive cytochalasins C, D and Q from the Xylaria sp. NC1214, a
fungal endophyte of the moss Hypnum sp. (Table 1). They have investigated
for their cytotoxic activity against five tumors cell lines. Among the above
cytochalasins, cytochalasin D showed significant cytotoxicity against all five
cell lines, with IC50s ranging from 0.22 to 1.44 lM, whereas cytochalasins C
and Q exhibited moderate, but selective cytotoxicity. Isaka et al., (2011)
isolated novel cytotoxic compounds of three new sesquiterpenoids and a new
pimarane-type diterpenoid from the fermentation broth of the wood-decay
fungus Xylaria sp. BCC 5484. Similarly, Yin et al., (2011) studied the
cytotoxic activities of the compounds isolated from X. carpophila. These
chemical compounds such as cyclopeptide cyclo (N-methyl-L-Phe31 L-Leu-
D-Ile-L-Val), five new sesquiterpenes named as xylocarpus A-E and another
known compound had cytotoxicity against human cancer cell lines. These
compounds showed an effective antiproliferative activity. Moreover, earlier
reports revealed that the novel anticancer compound of cytochalasins was
extracted from the species of Xylaria (Pongcharoen et al., 2007;
Rukachaisirikul et al., 2009; Zhang et al., 2010). Shiono et al., (2009)
reported the cytotoxicity of the isopimarane diterpene glycosides extracted
from the fruiting bodies of the ascomycete X. polymorpha. IC50 value of the
compound ranged from 71 to 607 μM.
Table 1: Some of the reported bioactive natural products isolated from endophytic
Xylaria

Name of the
Bioactive Compounds Host Plants Bioactivity
species
Damnacanthus
Xylarichalasin A Xylaria sp. Anticancer Activity
officinarum
Cytotoxicity &
Curtachalasins A and B X.cf. curta Solanum tuberosum
Antimicrobial activities
Cytochalasins C, D and Xylaria sp.
Hypnum sp. Cytotoxicity
Q NC1214

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Ethyl acetate extract Xylaria sp. Mussaenda luteola Antioxidant activity
Methanol extract X. feejeensis Tectona grandis Antioxidant activity
Pentapeptides Xylaria sp. Sophora tonkinensis Antibacterial activities
Amazonian forest
Xyolide X. feejeensis Antifungal activity
plant
Proline containing
Xylaria sp. Endolichenic Antifungal activity
cyclopentapeptides
Immunosuppressive
Xylaria diterpenes A–R X. longipes Fomitopsis betulina
activities

Xylaria as a source of Antioxidants agents


Among the many bioactive secondary metabolites recovered from the
kingdom fungi, natural products that possess antioxidant potential occupy a
major proportion. Antioxidants are compounds that obstruct free radical
reactions and slow down cellular deterioration. Mohd Adnan et al., 2018
reported that the pharmacological properties of a potent and major bioactive
compound like xylaranic acid from X. primorskensis (X. primorskensis). The
terpenoids nanoparticles from xylaranic acid showed significant antioxidant
potential against DPPH & H2O2 radicals and also its showed antibacterial
and anticancer activity against human bacterial pathogens and human lung
cancer cells. Rupesh D Divate et al., (2017) studied the Protective effect of
medicinal fungus X. nigripes mycelia extracts against hydrogen peroxide-
induced apoptosis in PC12 cells. They reported that, ethanol extract showed
higher antioxidant activity by scavenging DPPH radicals, inhibiting lipid
peroxidation, and reducing power. Hence, they said that, the macro fungal
species of X. nigripes has high phenolic content and antioxidant activity may
provide the neuroprotective effects. In the same year, Shylaja et al., (2017)
studied and reported that the ethyl acetate extract of endophytic fungal
species of Xylaria showed moderate antioxidant activity when compared to
other endophytic fungal isolates isolated from Mussaenda luteola. Similarly,
Durga & Rajagopal (2016) reported the methanol extract of X. feejeenis
exhibited high antioxidant potential compared to ethyl acetate and
chloroform extracts. They also studied the optimization of antioxidant
potential of X. feejeensis by the statistical optimization by Plackett-Burman
design and Central Composite Design. In this method, they found the
increased antioxidant yield of X. feejeenis by 23%-75%. Fernando et al.,
(2016) investigated and reported that the antioxidant properties of terrestrial
X. feejeenis harvested from the dry zone forest reserves in Dambulla and
Mahiyanganaya areas of Sri Lanka for the first time. That species also
exhibited a strong antioxidant capacity and high contents of phenolic and

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flavonoid substances implying that studied forms possess an effectual
antioxidative system.
Moreover, Liu et al., (2007) investigated the antioxidant activity of
cultivated fruiting bodies of Xylaria sp. The results revealed that the
methanol extract exhibited strong antioxidant activity in both DPPH and β-
carotene-linoleic acid model system. Total phenolic and flavonoid contents
were also highest in methanol extract of fruiting bodies. The results showed
that total phenolic and flavonoid contents were the highest in methanol
extract (54.51±1.05 mg gallic acid equivalent/g dry weight and 86.76±0.58
mg rutin equivalent/g dry weight), while the hexane extract was the lowest
(9.71±0.57 mg GAE/g dw and 10.14±0.76 mg RE/g dw, respectively).
Furthermore, the spectroscopic studies revealed that the extract of Xylaria
sp. had bioactive compounds like esters, phenolics, alkanes, carboxylates
and alcohols.
Xylaria as a source of immunomodulatory agents
Immunomodulators are the group of chemical substances that help to
regulate and boost the immune system. The basic mechanisms by which the
natural products of fungal species defend the body against infection caused
by microorganisms have two probable ways one by destroying pathogens
and other by enhance by stimulating the body immunity. In clinical practice,
they are usually classified into three categories such as immunosuppressants,
immunostimulants, and immunoadjuvants (El Enshasy & Hatti-Kaul 2013).
Their market share has increased day by day rapidly in recent past due to
wide-ranging pharmaceutical applications for patients that require human
immune system modulations. They are also widely used as a prophylactic
medicine for an increasing number even in healthy people (Reis et al., 2017
& Himanshi et al., 2017). However, most immunomodulators are in market
were synthetic or semi-synthetic compounds, there has been a growing
interest in natural immunomodulators. Indeed, most of the currently used
chemical immunomodulatory drugs have negative side effects and the
market share of natural immunomodulators is increasing rapidly with an
annual growth rate of 8.6% (Shukla et al., 2014).
Recently, Chen et al., (2020a & 2020b) isolated Xylaria diterpenes A-R
and two isopimarenes designated xylarilongipins A and B from the
fungicolous species of X. longipes, growing on fruiting bodies of the
basidiomycete Fomitopsis betulina. These both terpenoids products showed
immunosuppressive activities against cell proliferation of concanavalin A-
induced T-lymphocytes and LPS-induced B-lymphocytes. Rupesh D Divate

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& Yun Chin Chung, (2017) studied the in vitro and in vivo assessment of
anti-inflammatory and immunomodulatory activities of hot water and 70%
ethanol extracts of X. nigripes mycelium. They reported that, both the
extracts effectively reduced the concentration of NO, TNF-α and IL-6 in
culture medium, and Cox-2 enzyme activity. The phagocytic activity of
RAW264.7 cells was enhanced upon treatment with X. nigripes extracts for
24 h. X. nigripes extract exhibited increased anti-inflammation effects,
phagocytic activity, and secretion of anti-inflammatory cytokine IL-10. The
X. nigripes mycelium exhibited immunomodulatory activities by enhancing
splenocytes proliferation, cytokine inductions, and the cytotoxicity of splenic
natural killer cells. Ko et al., (2011) investigated that the immunomodulatory
properties of X. nigripes in peritoneal macrophage cells of Balb/c mice. The
hexane and methanol extracts showed a dose dependent inhibitory effect on
NO, PGE2, IL-1β, IL-6, TNF-α and IFN-γ production in LPS-stimulated
macrophages. RT-PCR assay also showed that hexane extract possessed a
greater inhibition than ethanol extract on iNOS and COX-2 RNA expression.
Furthermore, hexane extract also showed a significant suppression effect
than ethanol extract. Finally, these results conclude that hexane extract
possessed a stronger anti-inflammatory activity than ethanol extract.
Similarly, Liu et al., (2006) studied the immunomodulatory effect of X.
hypoxylon. They reported that lectin of X. hypoxylon (XHL) showed the
excellent Inhibition proliferation of HepG2 cells. Likewise, X. nigripes
(Koltz.) SACC. also known as wu ling shen, is a high value medicinal fungus
belonging to the family of xylariaceae. It is found growing in wilds around
the abandoned termite nests. In traditional Chinese medicine, it is known to
enhance immunity and hematopoiesis (Xu, 1997). Moreover, the wild X.
nigripes was also used for treatment of insomnia, trauma and as a diuretic
and nerve tonic (Dai & Yang, 2008).
Xylaria as a source of Antimicrobial agents
The accelerating haunt for new antimicrobial drugs to provide assistance
in medical community to combat drug resistance microorganism, the
appearance of life-threatening bacteria, and the tremendous increase in the
incidence of fungal infections in the world’s population. Devaraju Rakshith
et al., (2020) studied the antimicrobial potential of culture broth of Xylaria
sp. FPL-25(M) against human bacterial and fungal pathogens by bioactivity
guided fractionation using bioautography and chromatography. The isolated
xylobovide-9-methyl ester exhibited broad-spectrum antimicrobial activity.
Similarly, Yu et al., (2019) isolated and reported two known compounds of
penixylarins C & D from the fungal species of Xylaria under axenic

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condition. Its bioactivity exhibited against Mycolicibacterium phlei with the
minimum inhibitory concentrations of 6.25 μg/mL and 12.5 μg/mL against
Vibrio parahaemolyticus. Liang et al., (2019) isolated a number of
antibacterial compounds, including a new eremophilane sesquiterpenoid
named xylareremophil, from a Xylaria sp. it exhibited weak antibacterial
activity with the minimal inhibitory values of 25 μg/mL against Micrococcus
luteus and Proteus vulgaris.
Occurrence of antibacterial metabolites was reported from Xylaria sp.
within two publications: in the first work (Zheng et al., 2018a), a new
pyranone, 6-heptanoyl-4-methoxy-2H-pyran-2-one, was reported, while the
second publication gave account on a novel phthalide named xylarphthalide
A (Zheng et al., 2018b). Both these compounds showed antibacterial
activities with the minimum inhibitory concentrations value of 44 μg/mL, 50
μg/mL & 12.5 μg/mL against E. coli, S. aureus and Bacillus subtilis
respectively. The cyclic pentapeptides were isolated and reported from the
endophytic Xylaria sp. of the chinese medicinal plant Sophora tonkinensis
(Xu et al., 2017). These compounds were commonly known as xylapeptide
and exhibited selective antibacterial activities with minimum inhibitory
concentrations of 12.5 μg/mL against Bacillus sp. also showed moderate
antibacterial activity against various bacteria including the pathogenic S.
aureus (MIC 6.25-12.5 μg/mL). Furthermore, xylapeptide B showed
moderate antifungal activity against Candida albicans with a MIC of
12.5μg/mL. The antifungal agent griseofulvin (Fig. 4) which was originally
found in P. griseofulvum is well studied and even clinically applied against
dermatophytosis. However, in order to research for more potent derivatives
is ongoing using the novel X. cubensis as an alternative producer for the
same antifungal agent. Hence, the research group of Paguigan et al., (2017)
reported and isolated semisynthetically the griseofulvin derivatives of 7-
fluoro-7-dechlorogriseofulvin showed an activity similar to griseofulvin
against the skin infection causing Microsporum gypseum.

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(Kevin Becker & Marc Stadler 2021)
Fig 4: Recently reported bioactive Compounds obtained from the species of Xylaria
The broad spectrum of infections due to multidrug-resistant S. aureus
(MRSA) varies from mild skin infections to serious and invasive diseases
such as septicaemia, pneumonia, endocarditic, deep-seated abscesses
including food poisoning, and toxic shock syndrome (Tenover et al., 2000;
Holmes et al., 2005). Over the past few years, a notable increase in antibiotic
resistance among Gram-negative bacteria recovered from hospitalized
patients has been reported, especially for critically ill patients (Fridkin et al.,
2001). Infections caused by multidrug-resistant Gram-negative bacteria,
especially multidrug-resistant P. aeruginosa (MRPA), have been associated
with increased morbidity, mortality, and costs. P. aeruginosa strains are
frequently resistant to multiple antimicrobial agents, and the morbidity and
mortality of infections (Niederman 2001, Paladino et al., 2002). In this
regard, Ramesh et al., (2016, 2015a; 2015b, and 2012a; 2012b) studied and
reported significant antibacterial activity of both natural fruiting bodies and
cultural filtrate crude extract as well as partial purified fraction against
multidrug resistant bacterial pathogens of S. aureus and P. aeruginosa.
Likewise, Surup et al., (2014) sporotrichosis of xylarialean fungus
shows very strong antifungal effects against fungal pathogens. Ezra G
Baraban et al., (2013) studied and reported that an antifungal agent xyolide
which was isolated from an Amazonian endophytic fungus X. feejeensis
(Table 4). They tested its bioactive nonenolide called xyolide and it has
exhibited an antifungal activity with the MIC value of 425 μM against
Pythium ultimum. Hacioglu et al., (2011) reported that the ethanol extract of
fruiting bodies in X. polymorpha inhibited the growth of E. coli, S. aureus,
P. aeruginosa and Candida albicans.

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Wu et al., (2011) reported the isolation and structural elucidation of
antifungal proline containing cyclopentapeptides from an endolichenic
Xylaria sp. They were isolated 10 bioactive compounds such as two new
cyclic pentapeptides and the known blazein, ganodesterone, ergosterin,
cerevisterol, 24-methylcholesta-4,6,8, 22-tetraen-3-one, 5,8-epidioxyergosta-
6,22-dien-3-ol, 16-R-D-mannopyranosyloxyisopimar-7-en-19-oic acid and
16-hydroxy isopimar-7-en-19-oic acid. Further, all the compounds were
evaluated for synergistic activity with ketoconazole against fungal
pathogens. Among them, cyclic pentapeptide exhibited an effective
synergistic antifungal activity with 0.004 μg/mL ketoconazole against C.
albicans. Gloger’s group found that extracts from cultures of Xylaria sp.
showed moderate antifungal and antiinsecticidal activity. Subsequent
chemical studies of this extract led to the isolation of four triterpenoid
glycosides named as kolokosides A to D. The kolokosides appear to be
members of the fernane class of triterpenoids. Among these compounds,
kolokosides A exhibited antibacterial activity against gram positive bacteria
(Deyrup et al., 2007). Jang et al., (2007) isolated xylarinic acids A and B
from the fruiting bodies X. polymorpha. These novel compounds had
antifungal activity against plant pathogenic fungi. Park et al., (2005)
reported that novel dechlorogriseofulvin and griseofulvin metabolites of the
Xylaria sp. F0010 displayed potent antifungal activity against plant
pathogenic fungi with lower IC50 value of 30 μg/ml. Similarly, Healy et al.,
(2004) reported that the xanthones isolated from Xylaria had an effective
antibacterial activity against E. coli, Streptococcus pneumoniae,
Enterococcus faecalis, P. aeruginosa and S. aureus.
Future prospective of Xylaria
A vast study reported and envisioned that Xylaria as an endophytic as
well as macro fungus forms a store house of diverse biologically active
natural products. Whereas the number of compounds extracted and purified
from the species of Xylaria entering in the field and clinical trials is said to
be limited. Some of the future requirements for avenues in research and
development are certainly optimization of growth condition at standard
laboratory set up is a crucial stage in isolation of bioactive compounds from
Xylaria research, widest possible screening for bioactive compounds,
extraction of bioactive compounds with the organic solvents, purification of
crude extract by chromatographic methods, in-vitro as well as in-vivo
pharmacological screening of purified fraction and finally development of
commercial bioactive products.

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Conclusion
The chemical diversity bearing pharmaceutical potential thus implied
reaches beyond the plant kingdom. Most of these compounds exhibit
excellent pharmacological activities and are helpful for the invention and
discovery of bioactive compounds in future. Moreover, Xylaria actually
comprises several thousands of species of which the majority remains to be
recognized and also to be an untapped and formally described for its
bioactive natural products and its will be presumed to push forward to the
frontiers of drug discovery.
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Chapter - 4
Examples of Plant-Derived Drugs

Authors
Dr. Sweta Prakash
School of Studies in Botany, Jiwaji University, Gwalior,
Madhya Pradesh, India
Dr. Kamini Dubey
Assistant Professor of Botany, Department of Botany, Govt.
P.G. College, Narsinghgarh, Madhya Pradesh, India

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Page | 62
Chapter - 4
Examples of Plant-Derived Drugs
Dr. Sweta Prakash and Dr. Kamini Dubey

Abstract
Plant obtained compounds that have recently undergone development
include the anticancer agents, taxol and camptothecin, the Chinese,
antimalarial, artemisinin drug and the Ayurvedic drug forskolin. These and
lots of other examples serve for instance the sustained value of plant-derived
secondary metabolites as useful compounds for drug development. Plant
derived natural products have long been and can still be extremely important
as sources of medicinal agents and models for the synthesis and semi-
synthesis of novel substances for treating many diseases. Many of the
medicinally important plant derived pharmaceuticals are essential in
introducing the age of modern medicine and therapeutics and a few of this
substance. Medicinal plants became the most objects of chemists,
biochemists, and pharmaceutics. Their investigation plays a crucial role in
discovering and developing new drugs that probably have more efficacy and
no side actions like the latest drugs.
Keywords: ayurvedic, medicinal plants, natural products, drugs
Introduction
Medicinal plants have historically proven their significance as a source
of molecules with healing potential and present days so far describe a crucial
tool for the recognition of novel drug leads. India is one of the countries
where various traditional systems of medicines are used. Ayurveda, Siddha,
Unani, Homeopathy and Tibetan system of medicines are essential ones.
These systems have a stimulating task in bioprospecting new medicines.
Many modern drugs have their origin in traditional medicines. An outsized
part of the Indian population even today depends on the Ayurvedic system of
medicine. ‘An ancient science of life’ the documented treaties in Ayurveda
are Charaka and Sushruta Samhita.
Medicinal plants are in use for untold centuries and have provided
authentic and effective sources in treating and preventing diseases.

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Medicinal plants are a vital tool of usual and uncostly new drugs for people
ubiquitously in the planet. There is a need for suitable recognition of drugs
and collecting them at accurate times and grading them for attributes.
The great need of collecting good herbarium material for taxonomic
identification of the collected species must be stressed. The base of the
pharmacognostic profile of the plants will help in standardization which can
help within the identification of plants. There is a requirement for the
protection of all usable plant species and also its cultivation, preservation
and evaluation of germplasm for use in future. Primarily among the foremost
vulnerable plant species in India, the predominant over-exploited are the
medicinal plants. The East Indian snakeroot Rauvolfia serpentina (L.) Benth.
ex Kurz has been used for hundred years as a native East Indian medicinal
plant, and its main active principle reserpine is now utilized in western
medicine as an antihypertensive and tranquilizer. Accordingly, other
bioactive and poisonous plants with vast folklore histories have yielded
cardiac (Digitalis) glycosides.
Natural products as drug: a historical perspective
The first written records on medicinal plants date back to about 2600 BC
and report the presence of the medicinal system in Mesopotamia, which
includes about 1000 plant-derived medicines. Traditional Chinese medicine
has been broadly documented over thousands of years (Unschuld, 1986) and
therefore the documentation of the Indian Ayurveda system dates back to the
first millennium BC (Patwardhan, 2005).
Collection of drugs
The time of the collection of vegetable drugs is of prime need and until
we may not be able to make extensive generalizations, still the following
general rules for the collection of various drugs may be given:
1) Roots, rhizomes and barks should be collected immediately before
the vegetative life-processes begin (in the spring) or immediately
after the vegetative processes cease (usually in the fall).
2) Leaves should be collected when the C02 assimilation process is
most active; usually about the time of development of the flowers
and before mature development of fruit and seed.
3) Flowers should be collected before or just about the time of
pollination.
4) Fruits should be collected near the ripening period (i.e., full-grown
but unripe).
5) Seeds should be collected when fully matured.

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The valuation of drugs
In the identification of medicinal drugs few traits are taken under
consideration, like color, aroma general appearance, structure, texture, etc.,
these at the equivalent time depicting during a greater or less degree the
qualitative value of the drug. While these characteristics may enable the
expert to explore very slight variations in quality and to calculate
approximately the value of a given drug, still the true value is based upon the
quantity of the medicinal principles or so-called active constituents. The
methods employed within the valuation of drugs may be grouped as follows:
1) Chemical methods: They are more generally applied and generally
involve the isolation and estimation of the active principles.
2) Physical methods: It involves such processes as the determination
of specific gravity of the drug as of jalap or the assessment of the
elasticity or measurement of the fibers as of cotton and still other
special methods applied to individual drugs giving indirectly their
valuation.
3) Microscopical methods: It valuated may oftentimes be used when
other methods fail as, for ex: when foreign starches are added to
starchy products within the cereals and spices. Microchemical
reaction can also be depended upon in some instances to point the
value of a drug as in Strophanthus where the value of the drug
depends directly upon the number of seeds giving a green
coloration with sulphuric acid.
4) Biological methods: It includes the importance of the effects of
drugs upon animals or plants.
5) Ethnopharmacological methods: It includes the selection of the
test samples based on traditional medicinal usage of the plant
species.
6) Ecological methods: It involves the choice of samples that
supported the interactions between organisms and their natural
world on the entire that plant secondary metabolites affect
ecological functions from which a probable medicinal uses for
humans are often derived.

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Table 1: Some Examples of Economically Important Plant-Derived Drugs (Lewis et
al., 1977; Tyler et al., 1988; Farnsworth, 1973, 1966)
S.
Plant sources Drugs/Alkaloid Family Product Activity
N.
1. Acacia senegal Arabin Combretaceae Evecare Dental problem
Achyranthes Ecdysterone,
2. Amaranthaceae Cystone tablet Astringent, diuretic
aspera Saponins C, D
a) Adonis Adonis Anti-asthmatic,
3. Adonis vernalis Ranunculaceae
b) Adonidine vernalis cardiac disorder
a) Visnaga Lukoskin oral Muscle relaxant
4. Ammi visnaga Umbelliferae
b) Khellin drops Anti-asthmatic
5. Artemisia annua Artemisinin Asteraceae Artekin Anti-malaria
Andrographis Baccillary
6. Andrographolide Acanthaceae Sage liverex
paniculata dysentery
7. Berberis vulgaris Berberine Berberidaceae Berberis Antidysentric
8. Betula alba Betulinic acid Betulaceae Birch oil Anticancerous
Constivac,
Sennoside A, Laxative,
9. Cassia acutifolia Leguminosae Isova powder,
Sennoside B carminatives
Kultab tablet
a) Vincristine
Antileukaemic
b) Ajmalthine
Catharanthus Antiarrhythmic
10. c) Serpentine Apocynaceae Cytocristin
roseus Tranquilizer
d) Vinblastine
Antitumor
e) Ajmalicine
Cephaelis a) Emetine Amoebicide,
11. Rubiaceae Ipecac syrup
ipecacuanha b) Pscychotrines emetic, Anti-HIV
Chondodendron Skeletal muscle
12. Curare Menispermaceae Tubocurarine
tomentosum relaxant
Chrysanthemum
13. Pyrethrin Compositae Pyrethrin Insecticide
cinerariaefolium
Dioscorea Lanoxin
14. Diosgenin Dioscoreaceae Antifertility
deltoidea tablets
a) Digoxin
b) Lanatoside A,
15. Digitalis lanata Scrophulariaceae Acetyldigoxin Cardiotonic
B, C
c) Acetyligitoxin
a) Atropine Stomach disorders,
Duboisia
16. b) Hyoscyamine Solanaceae Duboisia 30C pre-surgical muscle
myoporoides
c) Scopolamine relaxant
Galantamine
hydrobromide Dementia
Galanthus Razadyne,
17. Amaryllidaceae extended associated with
caucasicus Galantamine
release Alzheimer's disease
capsules
Gomine
Helianthus Inulin as helianthus Antidiabetic,
18. Compositae
tuberosus fructosan tuberosus antirheumatism
powder
19. Ocimum sanctum Eugenol, citral, Labiatae Nomarks, Antidiabetic,

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epigenin Sualin antipyretic
Rauwolfia Antihypertensive,
Rauvolfia
20. Reserpine Apocynaceae serpentine psychotropic,
serpentina
tablets tranquilizer
Pilocarpus Cholinergic, dilate
21. Pilocarpine Rutaceae Jaborandi
jaborandi pupils
Erythroxylum Fluid extract
22. Cocaine Erythroxylaceae Local anesthetic
coca coca

Table 2: Drugs derived from Allopathy

S.N. Plant Name Drug/Alkaloid Family Product Activity


Camptotheca Ovarian, lung
1. Camptothecin Nyssaceae Irinotecan
acuminata cancer, antitumor
Lemon peel, Luteolin Carminative,
Ultra doux
2. Citrus limon (Flavone), Naringin Rutaceae stimulant, vit C
conditioner
(Flavanone) source
Coleus
3. Forskolin Lamiaceae Forskolin forte Anti-glaucoma
forskohlii
Quidine, quinine,
Cinchona Antimalarial,
4. cinchonine, Rubiaceae Quinalaquin
calisaya antidiarrhoeal
cinchonidine
a) Quinidine Cardiac
Herbipyrin
C. b) Cinchonidine depressant,
5. Rutaceae tablet, M.P. 6
ledgeriana Rheumatism,
Capsules
anti-malarial
Cough
Papaver
6. Morphine, Codeine Papaveraceae Oxycontin suppressant, anti-
somniferum
cancer
Psoralea Purim, Arena,
7. Psoralea Leguminosae Aphrodisiac
corylifolia Purodil
Santalum Diuretic,
8. Sandal Santalaceae Abana, Lukol
album, cardiotonic,
Smilax Purodil Chronic skin
9. Sarsaparilla Liliaceae
ornata capsules diseases
Analgesic,
10. Salix alba Salicin Salicaceae Aspirin
Antipyretic
Tricosanthes
Anti-cancer, anti-
Tricosanthes kirilowi dried
11. Tricosanthin Cucurbitaceae inflammation,
kirilowi fruit liquid
anti-bronchial
extract

Table 3: Drugs derived from Homeopathy

S.N. Plant Name Drug/Alkaloid Family Product Activity


Abrus Treatment of
1. Abrol, abasine Fabaceae Jequirity
precatorius eyes
Ailanthus
2. Ailanthone Simaroubaceae Ailanthus Anthelmintic
glandulosa

Page | 67
Anti-
Anemone rheumatism,
3. Anemonin Ranunculaceae Pulsatila
pulsatilla gastric
disorders
Cucurbitacin Bronchitis, dry
4. Bryonia dioica Cucurbitaceae Bryonia
glucosides cough
Calendula Wounds, burn,
5. Coumarins Asteraceae Calendula
officinalis soothes skin
Roundworm,
Chenopodium
6. Ascaridole Amaranthaceae Chenopodium tapeworm
anthelminticum
infection
Cimicifuga Cimicifugic acid, Amenorrhoea,
7. Ranunculaceae Cimicifuga
racemosa Fucinolic acid Neuralgic
Conium N-methylconiine, Paralysis,
8. Apiaceae Conium
maculatum conhydrine cancer
Eugenia
9. Myricetin Myrtaceae Jambul Anti-diabetic
jambolana
Bed sores,
10. Quercus alba Quercitannic acid Fagaceae Quercus
astringent
Ringworm,
11. Thymus vulgaris Carvacrol, thymol Labiatae Thymol
antiparasitic

Table 4: Drugs derived from Ayurvedic


S.N. Plant Name Drug Family Product Medicinal use
Aegle Chyawanprash,
1. Bael Rutaceae Diarrhoea, Dysentry
marmelos Bilwadi churna
Vasaka vasicinol,
Adhatoda Vasavaleha, Respiratory
2. vasicinone, Acanthaceae
vasica vasaka capsule disorders
adhatonine
Areca Himplasia, Anthelmintic,
3. Arecoline Palmaceae
catechu khadiradi bati aphrodisiac
Asparagus Satavari kalp, Aphrodisiac,
4. Shatavari Liliaceae
racemosus Diabecon laxative
Brahmoside, Tonic, improve
Centella Geriforte,
5. brahminoside, Umbelliferae memory,
asiatica Menosan, Mentat
asiaticoside immunomodulator
Cinnamomum Chyawanprash,
6. Cinnamon Lauraceae Carminative
zeylanicum Sutsekhar ras
7. C. camphora Camphene Lauraceae Dabur balm Antipruritic
Citrus Bitter orange Dabur vatica
8. Rutaceae Stomachic
vulgaris peel body shampoo
Cymbopogon a) Lemongrass
9. Poaceae Sage lion balm Mosquito repellant
flexuosus b)Lonones
a) Hyoscine Jatifaladi Bati,
10. Datura metel Solanaceae Anticholinergic
b)Scopolamine. Jatyadi tail
Datura
11. Scopolamine Solanaceae Maharasayan vati Antispasmodic
stramonium

Page | 68
Skin and hair
12. Eclipta alba Ecliptal Asteraceae Eclipta
disorders
Hyoscyamus Sarpagandhaghan
13. Hyoscyamine Solanaceae Anticholinergic
niger vati, Brahmi vati
Mentha Dabur lal tooth
14. Peppermint Labiatae Stimulant, Nausea
piperita powder
15. M. spicata Pudina Labiatae Rheumatic gel Carminative
Picrorhiza
16. Katurohini Plantaginaceae Purim, Aptikid Hepatoprotective
kurroa
Plantago Laxative, anti-
17. Ispaghula Plumbaginaceae Isabgol, Trifgol
ovata diarrhoeal
Semecarpus Sanjivani vati, Leprous affections,
18. bhilawanol Anacardiaceae
anacardium Patrangasava nervous debility
Swertia Safi, Mehmudgar Appetite stimulant,
19. Chirayita Gentianaceae
chirayta bati ophthalmic appetizer
Tinospora Guduchi, Guduchi tablet, Rejuvenator,
20. Menispermaceae
cordifolia tinocordifolisoide Abana antioxidant

Table A: Drugs derived from Flowering plant part (Seeds)


S.N. Plant Name Drug/Alkaloid Family Product Activity
Delphinium
Delphinium Toothache, genitor-
1. Staphisagria Ranunculaceae staphisagria
staphisagria urinary
remedia globuli
Elettaria
2. Cineole Zingiberaceae Koflet Stomachic
cardamomum
3. Garcinia indica Kokum Guttiferae Bioslim Cosmetic
Gossypium
4. Linoleic Malvaceae J.P. Message oil Emollient
harbaceum
Linum Linseed oil, Canisep and
5. Linaceae Gonorrhoea
usitassimum Linamarin Scavon
Myristica
6. Nutmeg Myristicaceae Kumaryasava Flatulence
fragrans
Nigellimin, Antiinflammatory,
Anti-dandruff
7. Nigella sativa nigellidin, Ranunculaceae antihypertensive,
shampoo
nigellicin. antidiarrhoeal
Prunus Badam roghan
8. Almond oil Rosaceae Emollient
amygdalus oil
Ricinus Lip balm, Laxative,
9. Ricinoleic acid Euphorbiaceae
communis muscle joint rub antitumorous
Strophanthus Chronic
10. Strophanthus Apocynaceae
kombe heartproblems
Nuxvomica,
Strychnos nux Laxative, Nervous
11. Strychnine, Loganiaceae Neo tablet
vomica disorder, paralysis
Brucine
Trachyspermum
12. Aptikid Apiaceae Aptikid Antispasmodic
ammi

Page | 69
Table 5: Drugs derived from Plant part (Roots and rhizomes)

S.N. Plant Name Drug/Alkaloid Family Product Activity


a) Aconite
1. Aconitum napellus Ranunculaceae J.P. Painkill oil Rheumatism, neuralgia
b) Aconitine
2. Acorus calamus Acorus Arecaceae Mahamarichadi tel Expectorant
a) Belladonna
3. Atropa belladonna Solanaceae Belladonna plaster Anticholinergic
b) Atropine
4. Brassica nigra Mustard oil, Allyl isothiocyanate Brassicaceae Dabur mustard oil Rubefacient
5. Carthamus tinctorius Safflower oil, oleomargarine Compositae Saaf organic eraser body Oil Edible, artherosclerosis
6. Colchicum luteum Colchicum Liliaceae Aujai capsules Gout
Curcumin I, II, III, Curcuminoids, Respinova, J.P. Nikhar oil, Antinflammatory, anticancer,
7. Curcuma longa Zingiberaceae
Tetrahydrocurcuminoides Diabecon, Purian Antioxidants, antiinflammatory
8. Glycyrrhiza glabra Glycyrrhiza, Licorice Leguminosae Herebolex, Yasti madhu Bronchitis, skin whitening
9. Nardostachys jatamansi Nardostachone Valerianaceae Dashmularishta Antirrhythmic
a) Podophyllum Antiviral,
10. Podophyllum peltatum Berberidaceae Podowart, Podophyllotoxin
b) Etoposide Anticancer
11. Polygala senega Senega Polygalaceae Senega snakeroot Expectorant
Confido, Lukol, Antihypertensive, blood
12. Rauwolfia serpentina Rauwolfia, ajmalicine Apocynaceae
Serpina,Sarpagandhan bati pressure
13. Sesamum indicum Sesame oil, oleic, linoleic acid Pedaliaceae Dabur lal tel Antioxidant, insecticidal
14. Valeriana wallichi Valerian Valerianacee Anxocare, Mentat Blood pressure
15. Zingiber officinale Gingerol Zingiberaceae Hajmola, Strepsils Antiemetic, antioxidant

Page | 70
Table 6: Drugs derived from Plant part (Stems)

S.N. Plant Name Drugs/Alkaloids Family Product Activity


Compound
Liquidambar Antiseptic,
1. Storax Hamamelidaceae Benzoin
orientalis parasiticide
Tincture
Aubrey
Organics
Myroxylon
2. Balsam of Peru Papilionaceae Natural sun Miticide
balsamum
SPF 12
Vitamin C
Rosmarinus Anti-dandruff Gastric
3. Cornosolic acid Lamiaceae
officinalis shampoo debility
Styrax Ciniferyl Friar’s
4. Styraceae Antioxidative
tonkinensis benjoate Balsam
Styrax Friar’s
5. Sumatra benzoin Styraceae Diuretic
benzoin Balsam

Table 7: Drugs derived from Plant part (Pith, wood and bark)
S.N. Plant Name Drugs/Alkaloids Family Product Activity
Phlobatannin
1. Acacia catechu Leguminosae Koflet lozenge Astringent
catechutannic acid
Cassia Gastric
2. Cassia bark Lauraceae Madhudoshantak
aromaticum debility
Cinchona Cinchona officinalis Treatment of
3. Quinine Rubiaceae
officinalis 30C malaria.
Commiphora Arogyavardhini Lowers LDL
4. Guggul Burseraceae
mukul gutika and VLDL
Mahamanjishthadi
Holarrhena
5. Kurchi Apocynaceae kwath, Purodil Antidysentric
antidysenterica
capsules
Pterocarpus
6. Kinotannic acid Leguminosae Diabecon Astringent
marsupium
7. Saraca indica Ashoka, Anthocyanin Leguminosae Ashokarisht Uterine tonic
Symplocos Red, yellow
8. Lodh Symplocaceae Evecare, Styplon
racemosa dye
Terminalia Geriforte, Liv 52, Angina,
9. Arjunic acid Combretaceae
arjuna Arjun churna hypertensive

Table 8: Drugs derived from Plant part (Flowers)

S.N. Plant Nmae Drugs/Alkaloids Family Product Activity


Arnica Arnica Anti-
1. Arnicin Compositae
montana montana 30X inflammation
Calendula
Calendula Antimicrobial,
2. Calendulin Compositae officinalis
officinalis antioxidant
ointment

Page | 71
a) Cannabidiol
Cannabis Bilwadi Muscle relaxant,
3. b) Cannabidolic Cannabinaceae
sativa churna hallucinogenic
acid
Capsicum a) Capsicin Postherpetic
4. Solanaceae Capsigyl-D
annum b) Casanthin neuralgia
Citrullus The body Gastralgia,
5. Colocynth Cucurbitaceae
colocynthis pure diarrhea

Table 9: Drugs derived from Plant part (Fruits)

Plant
S.N. Drug/Alkaloids Family Product Activity
Name
Anethum Woodward’s
1. Dill, D-limonene Umbelliferae Flatulence
graveolens gripe water
Reduce
Carica
2. β-Cryptoxanthin Caricaceae Papain incidence of
papaya
blood clots
Carum
3. Caraway, Carvene Umbelliferae Gripe water Dyspepsia
carvi
Carum Bilwadi
4. Umbelliferone Umbelliferae Rheumatism
carvi churna
Cuminum
5. Cumin aldehyde Umbelliferae Hajmola Carminative
cyminum
Diakof,
Embelia Anthelmintic,
6. Viranga, vilangin Myrisinaceae Herbolax,
ribes contraceptive
Koflet
Triphala
Emblica Phyllantidine, Improves
7. Euphorbiaceae churna,
officinalis phyllantine memory
Chyawanprash
Dabur
Estrogen like
Foeniculum hajmola,
8. Anethole Umbelliferae activity,
vulgare Dabur janum
lactation
Gunti
Olea Olive oil, Oleic acid, Laxative,
9. Oleaceae Figaro oil
europoea Luteolin (Flavone) demulcent
a) Dextromethorphan Analgesic,
b) Verapamil antitussive
Papaver c) Codeine Morphine, Angina
10. Papaveraceae
somniferum d) Noscapine codeine Sedative
e) Papaverine Cough
suppressant
Pimpinella Umbelliferone, Pimpinella Antispasmodic,
11. Umbelliferae
anisum scopoletin anisum carminative
Haritakh
churna, Antiviral,
Terminalia Haritaki, chebulinic
12. Combretaceae Triphala bleeding gums,
chebula acid
churna, Antiasthmatic
Tentex forte

Page | 72
Terminalia Triphala Dyspepsia,
13. Gallic acid Combretaceae
bellerica churna diarrhoea
Bonnisan,
Tribulus
14. Tribulustrine Zygophyllaceae Dhatupoushtik Aphrodisiac
terrestris
churna

Table 10: Drugs derived from Plant part (Leaves)

Plant
S.N. Drug/Alkaloids Family Product Activity
Name
Diabecon, Purgative,
1. Aloe vera Aloin, emodin Liliaceae
kumariasava antiviral
Bacopa Memory
2. Bacoside Plantaginaceae Brahmi
monnieri enhancement
Mahamarichadi
3. Cassia tora Chrysophanol Caesalpiniaceae Skin diseases
Tail
Celastrus Geriforte, Aphrodisiac, brain
4. Malkangni Celastraceae
paniculatus Himcolin tonic
Eucalyptus Canisep, cold
5. Eucalyptol Myrtaceae Febrifuge
globulus balm
Copernicia Cosmetics,
6. Carnaubic acid Palmae Carnauba wax
prunifera deodorants
Digitalis a) Digitoxin
7. Scrophulariaceae Lanoxin tablets Cardiotonic
purpurea b) Gitalin
Gaultheria Methyl Diuretic,
8. Ericaceae Dabur balm
procumbens salicylate rubefacient
Tylophorine, Antiinflammatory,
Tylophora
9. Tylophorinine, Asclepiadaceae Geriforte Aqua antidiarrhoeal,
indica
Tylophorinidin antidysentry
a) Withanolides Anticancer,
Geriforte,
b) Withaferin A Parkinson’s
Withania Ashvagandha
10. Solanaceae disorder,
somnifera tablet,
Alzheimer’s
Balarishta
disorder

Table 11: Drugs derived from Plant part (Exudations, juices and other plant
products)

S.N. Plant Name Drug/Alkaloids Family Product Activity


Allicin, Alliin,
Allium Lashunadi Carminative,
1. Quercetin Liliaceae
sativum bati antiinflammatory
(Flavonols)
Ananas
2. Bromelain Bromeliaceae Bromelain Fabrinolytic
comosus
Cocos Lip balm,
3. Coconut oil Palmae Dietary
nucifera Evecare
Crocus Tentex
4. Saffron Iridaceae Spasmolytic
sativus forte

Page | 73
Eugenia Himsagar Local an
5. Eugenol Myrtaceae
caryophyllus tail aesthetic
Hevea
6. Caoutchouc Euphorbiaceae
braziliensis
Esoban
7. Zea mays Corn oil Gramineae Dermatitis
ointment

Table 12: Drugs derived from Pteridophyte

S.N. Plant Name Drug/Alkaloids Family Product Activity


Antibacterial,
Asplenium Scolopendrium
1. Gallic acid Aspleniaceae digestive
scolopendrium vulgare
disorders
Dryopteris Phloroglucinol Paratrex, Flix Gastric
2. Dryopteraceae
filix-mas Filicic acid max disorders
Equisetum Equisetum
3. Palustrine Equisetaceae Stop bleeding
arvense arvense
Equisetum
4. E. hyemale Kaempferol Equisetaceae Antioxidant
hyemale
Lycopodium Antidiarrhoeal,
5. Apigenin Lycopodiaceae Lycopodium
clavatum stomach ache
Huperzia
6. Huperzine A Lycopodiaceae Huperzine A Alzheimer’s
serrata
Selaginella Control fever,
7. Selaginellins Selaginellaceae Selacin
flabellate menstruation

Page | 74
Table 13: Drugs derived from Gymnosperm

S.N. Plant Nmae Drug/Alkaloid Family Product Activity


1. Abies balsamea Camphor Pinaceae Canada balsam Antidysentric
a) Synribo
2. Cephalotaxus harringtonia Cephalotaxaceae Cephalotaxus Anti-cancer, Leukemia
b) Cephalotoxine
3. C. circinalis Amentoflavone Cycadaceae Anodyne Narcotic
4. Chamaecyparis lawsoniana Terpinen-4-ol Cupressaceae Cupressus lawsoniana Antioxidant, antiviral
5. Ephedra distachya Ephedrine Ephedraceae Ephedra
a) Ephedrine
6. Ephedra sinica Ephedraceae Bronchial asthama, cold Antihistamine
b) Pseudoephedrine
a) Ephedra Antiallergenic
7. Ephedra gerardiana b) Pseudoephedrine Ephedraceae Ephedrine sulphate Coughsuppressant
c) Norpseudoephedrine Vasodilator
8. Ferula asafoetida Asafoetida Apiaceae Madhudoshantak Antispasmodic
Antiasthmatic, antioxidant,
9. Ginkgo biloba Ginkgolides A, B, C Ginkgoaceae Ginkgo
memory enhancer
10. Juniperus communis Gallocatechin Cupressaceae Juniperus communis Antioxidant, antiinflammatory
11. J. virginianan Cupressuflavone Cupressaceae Juniperus virginiana Antimicrobial
12. J. sabina Siderin Cupressaceae Savin oil, Sabina Abortifacient
13. Macrozamia spiralis Macrozamin Zamiaceae Macrozamia Toxic
14. Panax ginseng Ginsenosides Araliaceae Ginseng Anticancer
15. Picea mariana ɑ-terpineol Pinaceae Abies nigra Antiseptic
16. Pinus lambertiana Lambertianic acid Pinaceae Pinus lambertiana Laxative
17. Pinus longifolia Turpentine Pinaceae Oleoresin, Rubefacient

Page | 75
Rumalaya gel
18. P. pinaster Procyanidins Pinaceae Pycnogenol Antioxidant
19. P. sylvestris Terpinolene Pinaceae Pinus sylvestris Expectorant
20. Pseudotsuga manzeisii Bornyl acetate Pinaceae Pseudotsuga manzeisii Antiseptic, sore throat
Sequoitol, pinitol, Sequoia & blue lily
21. Sequoia sempervirens Taxodiaceae Anti-ageing, antiwrinkle
myoinositol antiwrinkle
22. Taxus baccata Taxanes Taxodiaceae Taxus baccata Anticancer
23. Taxus brevifolia Taxol (Paclitaxel) Taxaceae Taxus brevifolia Anticancer
24. Thuja occidentalis Thujone Cupressaceae Thuja occidentalis Anti-inflammatory, Anti-HIV
25. T. plicata ɑ-thujone, β-thujone Cupressaceae Thuja lobbi Bronchodilator
26. Tsuga canadensis ɑ pinene, myrcene Pinaceae Abies canadensis Digestive disorder

Page | 76
Table 14: Drugs derived from Fungi
S.N. Fungi Name Drugs/Alkaloids Class Product Activity
Acremonium
1. β-lactam Ascomycetes Cephalosporin Bactericidal
chrysogenum
Amanita
2. Muscimol Agariomycetes Muscarine Analgesic
pantherina
Aspergillus Spirotryprostatin Fumagillin,
3. Ascomycetes Anticancer
fumigatus B gliotoxin
Aflatoxin B1,
4. A. flavus Kojic acid Ascomycetes Pesticides
B2, M1
Antibiotic
5. A. fumigatus Fumagillin Ascomycetes Antifungal
fumagillin
6. A. gallomyces Galactomannan Ascomycetes Gallic acid Antioxidant
Riboflavin
7. Ashbya gossypii Ergosterol Ascomycetes Antiallergic
(vit B2)
8. A. oryzae Asperfuran Ascomycetes Kojic acid Anti-allergic
Citric acid,
Bicoumanigrin, Disinfectant,
9. A. niger Ascomycetes gluconic acid,
Aspernigrin B Neuroprotective
oxalic acid
Lovastatin,
10. A. terreus Mevinolin Ascomycetes Antifungal
Gliotoxin
Torula yeast,
11. Candida utilis Cholesterol Ascomycetes Proteolytic
vit D
12. Cephalosporium β-lactam Ascomycetes Cephalosporin Antibacterial
a) Ergometrine Lysergic acid
Claviceps Uterus contraction,
13. b) Bromocryptine Ascomycetes (LSD),
purpurea Parkinson’s disease
c) Ergotamine Ergosterol
Cordyceps
14. Sterol Ascomycetes Cordyceps Anti-ageing
sinensis
Clitocybe
15. Nebularine Basidiomycetes Muscarine Antiglaucoma
nebularis
Cordyceps
16. Myriocin Ascomycetes Gilenya Immunosuppressant
sinclairii
Fusidium
17. β-glucogallin Sordariomycetes Fusidic acid Bacteriostatic
coccineum
Digitoxigenin,
18. Fusarium lini Lactones Deuteromycetes Cardiac disorder
digoxigenin
Ganoderma
19. Ganoderic acid β Basidiomycetes Ganoderma Anti-HIV
lucidum
Gibberella
20. Gibberellic acid Ascomycetes Gibberellins Phyto hormone
fujikuroi
Glyscavins A, B,
21. Mycelia sterilia Deuteromycetes Myriocin Immunisuppresant
C
Penicillium Mycophenolic
22. Ascomycetes Compactin Immunosuppressive
brevicompatcum acid
Penicillium Citrinin, Cholesterol
23. Lovastatin Ascomycetes
citrinum Compactin lowering

Page | 77
24. P. expansum Patulin Ascomycetes Patulin Antibiotic
25. P. griseofulvin Penifulvin A Ascomycetes Griseofulvin Antifungal
26. P. islandicum Islanditoxin Ascomycetes Emodin Antiinflammatory
Penicillin,
6-
griseofulvin,
27. P. notatum aminopenicillanic Ascomycetes Immunosuppressant
mycophenolic
acid
acid
Mycophenolic Mycophenolic
28. P. stoloniferum Ascomycetes Antibacterial
acid acid
Pencillium Ochratoxin A, B, Nephrotoxin,
29. Ascomycetes Ochratoxin
viridicatum C carcinogenic
Pleurotus
30. β-glucan Basidiomycetes Lovastatin Cholestrol lowering
ostreatus
Psilocybe
31. Psilosin Basidiomycetes Psilocybin Hallucinogenic
mexicana
Fumaric acid,
Rhizopus
32. d-lactic acid Phycomycetes Lactic acid, Food acidulant
stolonifer
cortisone
Farnesene,
Lactic acid,
Saccharomyces zymase,
33. Ascomycetes succinic acid, Antibacterial
cerevisae Artemisinic acid,
vit D, Invertase
Paclitaxel
Tolypocladium
34. Tolypocladin Sordariomycetes Cyclosporin A Immunosuppressant
inflatum
Yarrowia
35. ɑ-ketoglutarate Ascomycetes Isocitric acid Anticoagulant
lipolytica

Table 15: Drugs derived from Algae

Name of
S.N. Drug/Alkaloid Family Product Activity
Algae
Chlorella
1. Uronic acid Chlorophyta Chlorellin Antibacterial
vulgaris
Chondria Anthelmintic,
2. Domoic acid Rhodophyceae Domoic acid
armata antiparasitic
Kappa-
Chondrus carrageenin, Carrageenan,
3. Rhodophyceae Antiinflammatory
crispus lambda- Agar
carrageenin
Chondria
4. Chondriol Rhodophyceae Cycloeudesmol Antibiotics
oppositicladia
Dictyopteris Zonorol,
5. Phaeophyceae Zonarol Antifungal
zonoroid isozonorol
Digenia
6. α-Kainic acid Rhodophyceae α-Kainic acid Anthelmintic
simplex
Fucus
7. kelp Phaeophyceae Iodine Anticoagulant
vesiculosus
Gracilaria
8. Prostaglandins Rhodophyceae Agar Laxative
lichenoides

Page | 78
Gambierdiscus Ciguatoxin, Ciguatoxin
9. Dinophyceae Fish poisoning
toxicus Maitotoxin CTX
Gonyaulax
10. Saxitoxin 1 Dinophyceae Saxitoxin Neurotoxin
catenella
Iridaea Galactan
11. Galactan Rhodophyceae Anticoagulant
laminarioides sulphuric acid
Alginic acid, Dilate cervix,
Laminaria Fucoidan,
12. Phaeophyceae mannitol, HIV, Herpes
digitala Laminine, kelp
iodine simplex viruses.
Laurencia
13. Prepacifenol Rhodophyceae Laurencia Antibacterial
johnstonii
14. L. filiformis Chondriol Rhodophyceae Chondriol Antibacterial
Lyngbya Curacin A, Lyngbyatoxin Contact dermatitis,
15. Cyanophyceae
majuscule Dolastatin A Antiproliferative
Spirulina
16. vit A, vit E Cyanophyceae Spirulina Immunostimulant
platensis

Table 16: Drugs derived from Bryophytes and Lichens

S.N. Plant Name Drug/Alkaloid Family Product Activity


Cetraria lichenin and nauseous
1. Lichenan Parmeliaceae
islandica isolichenin medicines
Cladonia
2. Usnic acid Cladoniaceae Usnic acid Antibiotic
substellata
Plagiochin E,
Marchantia Lunularic Pulmonary
3. marchantins A, Marchantiaceae
polymorpha acid tuberculosis
B
Antitumor,
Polytrichum dissolve stones of
4. Luteolin Polytrichaceae Polytrichum
commune kidney, gall
bladder
P. Communins
5. Polytrichaceae Polytrichum Anticancer
juniperinum A(1), B(2)
Sphagnum Antiseptic,
6. Sphagnum acid Polytrichaceae Sphagnol
strictum anticandidal

Page | 79
Table 17: Drugs derived from Bacteria

S.N. Plant Nmae Drug/Alkaloid Family Product Activity


1. Bacillus polymyxa Bacillomycin D, L Paenibacillaceae Polymyxin B, Collistin Bactericidal
2. B. subtilis Fengycin Paenibacillaceae Bacitracin, Amicoumacin Antibiotics
3. Lactobacillus acidophillus Lactic acid Lactobacillaceae Probiotics Vaginal infections
Clindamicin, Antibacterial, Antibiotic,
4. Escherichia coli Shiga toxin Enterobacteriaceae
Ciprofloxacin, Vancomycin Intestinal inflammation
5. Micromonospora purpurea Gentamicin C1 Micromonosporaceae Gentamicin Meningitis
Antibacterial, Intestinal
6. Pseudomonas aeruginosa Phenazines Pseudomonadaceae Tobramycin, Vancomycin
inflammation
7. Streptomyces spp. Actinomycin D Streptomycetaceae Actinomycin D Sarcoma and gall tumors
8. Streptomyces avermitilis Ivermectin B1a, B1b Streptomycetaceae Avermectin Antinematodal
9. Streptomyces aureofaciens Tetracycline Streptomycetaceae Aureomycin Antibacterial
10. S. caespitosus Mitomycins A, B, C Streptomycetaceae Mitomycin C Gastric, colorectal cancer
11. S. carbophilus Pravastatin Streptomycetaceae Compactin Hypocholesterolemic
12. S. capreolus Capreomycin sulphate Streptomycetaceae Capreomycin Antituberculosis
13. S. coeruleorubidus Daunomycin Streptomycetaceae Daunomycin Antileukemic
14. Antimicrobial, respiratory
Streptomyces clavuligerus Clavulanic acid Streptomycetaceae Clavulanic acid
tract infections
Pneumonia, whooping
15. S. erythreus Erythromycin A Streptomycetaceae Erythromycin
cough
16. S. fradiae Tylosin, Fosfomycin D Streptomycetaceae Neomycin Wounds, ulcers, burn
Pulmonary tuberculosis,
17. S. griseus Streptomycin Streptomycetaceae Streptomycin, actidine
plague, Antimicrobial

Page | 80
18. S. lincolinensis Lincomycin Streptomycetaceae Clindmycin Antibacterial
19. S. mediterranei Rifampin Streptomycetaceae Rifampicin Oral contraceptives
20. S, nodosus Amphotericin B Streptomycetaceae Amphotericin B Antifungal
21. S. noursei Nystatin Streptomycetaceae Nystatin Antifungal
Doxorubicin, Epirubicin,
22. S. pneuceticus Epirubicin Streptomycetaceae Lymphoma, breast cancer
Idarubicin
23. S. rapamycinicus Nigericin Streptomycetaceae Rapamycin Anticancer
24. S. roseosporus Daptomycin Streptomycetaceae Daptomycin Blood, skin infections
25. S. rimosus Tetracycline Streptomycetaceae Oxytetracycline Antibacterial
Istamycin A R1, Istamycin
26. Streptomyces tenjimariensis Istamycin A, B Streptomycetaceae Antibiotic
B R1
Prevent young children
27. S. thermophilus Gamma aminobutyric acid Streptomycetaceae Streptococcus thermophilus
from diarrhoea
28. Streptomyces tsukubaensis Tacrolimus Streptomycetaceae Tacrolimus Immunosuppressant
Chloramphenicol, Antibacterial, Typhoid
29. S. venezualae Pikromycin Streptomycetaceae
Pikromycin fever
30. S. verticillus Bleomycin Streptomycetaceae Bleomycin Head and Neck cancer

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Role of plants in drug development
Medicinal plants are used as a major source of drugs for thousands of
years in human history and even at present times they are the basis of the
systematic traditional medicine practices in many countries. The primary
recorded literature on medicinal plants are often traced back to an earlier age
of human history like the Atharvaveda (2000 BC) in India, the Divine
Farmer’s Herb- Root Classic (3000 BC) in China and therefore the Eber
Papyrus (1550 BC) in Egypt. The modern drug industry has been developed
to a substantial degree as a result of plant-based traditional medicines. A
number of these plant-derived curative agents like atropine (anticholinergic),
codeine (cough suppressant), colchicine (antigout), ephedrine
(bronchodilator), morphine (analgesic) and physostigmine (cholinesterase
inhibitor) are still being extensively used nowadays (Sneader, 1996). Active
constituents extracted from plants can use directly as treatment in clinical
use, like morphine, atropine, quinine and paclitaxel or as prototype
biologically active “lead” compounds allow many structural analogs as new
pharmaceutical agents like artemisinin and so the opiate derivatives. Besides
their medicinal use some secondary metabolites from plants are also used as
powerful “pharmacological tools” to help explain the mechanisms of basic
human diseases (Principe, 1989; Cabnillas, 1979). Today drug discovery
from plants is predicated mainly on bioactivity-guided isolation and groups
of scientists with different research backgrounds including botany,
biochemistry, pharmacology, pharmaceutics, pharmacognosy, medicinal
chemistry, organic chemistry and toxicology are during this enterprise
(Geisman 1969).
In addition to the biologically active plant-derived secondary
metabolites which have been found to use as drug entities, many other
bioactive plant compounds have proven usable as model compounds. β-
carotene, a plant primary metabolite that can be useful within the prevention
or treatment of various types of cancers. It is repeatedly forgotten that plant
secondary compounds can use as templates for the design and total synthesis
of the latest drug entities. For ex: belladonna alkaloids (e.g., atropine),
physostigmine, quinine, cocaine, opiates (codeine and morphine),
papaverine, and salicylic acid have served as models for the design and
synthesis of anticholinergics, anticholinesterases, antimalarial drugs,
benzocaine, procaine and other local anesthetics the analgesics pentazocine
(Talwin), verapamil (Papaver and papaverine), and aspirin (acetylsalicylic
acid), respectively. These examples and lots of others serve for instance the
value and importance of plant-derived secondary metabolites as model
compounds for contemporary drug development.

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Conclusion
It may be concluded from this chapter that plants have vast uses in
forming drugs for humans and animals. The survival of life highly depends
upon various products extracted from these plants. Plant fulfills the need for
foods, medicines, shelter, clothes and luxuries for humans. If the present
trends of destruction and exploitation of forests continue at their present
rates, scientists interested and involved in medicinal plant research may have
only a couple of decades during which to investigate much of the rich
diversity of the plant kingdom for useful secondary metabolites and lots of
chances for successful drug invention will almost surely be lost.
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Chapter - 5
Plant Based Drugs: New Era for Cancer
Treatment

Authors
Krati Singh
Dr. Bhimrao Ambedkar University, Agra, Uttar Pradesh, India
Shobhit Gupta
Dr. Bhimrao Ambedkar University, Agra, Uttar Pradesh, India

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Page | 86
Chapter - 5
Plant Based Drugs: New Era for Cancer Treatment
Krati Singh and Shobhit Gupta

Abstract
Cancer is a major public health challenge. According to WHO 2020
report, 10 million death of people were listed as cancer. DNA damage
triggered by ultraviolet radiations, environmental agents, ionizing radiations,
etc. Almost all cancers are frequently diagnosed cancers are lung (12.7%),
colorectal (9.7%), breast (10.9%), and gastric cancer (7.81%). Natural
compounds are most favourable against cancer on their anti-cancerous ability,
easy to avail and efficient. There is an urgent need for new effective anti-
cancer drugs with fewer side effects, and plants show promising results for
making drugs. In this chapter, we focus on some plant-derived drugs against
cancer. These include 5-fluorouracil, artemisinin, polysaccharide, curcumin,
etc. Also discussed uses and future prospects for the development of plant-
derived substances with anti-cancer activity.
Keyword: anti-cancer, drugs, natural compounds, cancer
Introduction
Cancer is one of the deadliest ailments worldwide. It is one of the prime
reason of deaths and morbidity round the world and is getting frequent
increase in its cases and been expected to reach about 21 million by the end of
2030 [1, 2]. The reason now also includes the lifestyle change [3]. People are
working hard to minimalize the destructing drug effects in the cancer therapy
procedure on tissues and cells, and ultimately cumulating the lesion worth and
drug growth for targeting systems and new drug distribution [4]. Several
approaches are being used to treat cancer such as radiotherapy, chemotherapy,
tumor surgery, cancer vaccinations, stem cell transformation, photodynamic
therapy. But these therapies might include toxicity, fast clearance, non-
specificity etc. [5, 6].
Plants are the good source for medicine from many years. Plant consists
of many medicinal plants which are the finest source for developing drug.
Hence, there’s a serious need to search for some improved action for this

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disease. We need to work on new agents because chemotherapy and radiation
therapy which is widely being used for cancer treatment induce side effects on
scale. The compounds obtained from plants are beneficial over the chemical
ones as they are less or non-toxic to human and more endured. According
many studies plants can constrain the sequence and expansion of cancer [3].
Action of plants showing anticancer property
The plants with anticancer activity include the polyphenols, flavonoids,
alkaloids, saponins, triterpenes, tannins, and quinones. These bioactive
compounds used as antiproliferative, cytostatic, cytotoxic, antimetastatic,
apoptotic and antioxidative properties that inhibited angiogenesis and reduced
cancer cell viability.
Polyphenols
Studies show that polyphenols have antioxidant and cytotoxic activities
against cancer cells [7-9]. Polyphenols regulate the accumulation of copper ions
on chromatin, stimulated by the polyphenols such as to elicit DNA
disintegration, resveratrol [7].
Flavonoids
Natural flavonoids a wide class of polyphenolic compounds, chief sources
of flavonoids are fruits, seeds, vegetables, beverages, and flowers, different
type of foods has different quantity of anti-cancerous flavonoids. The known
biological properties of natural flavonoids are anticipation against cancer,
cardio-protective, inhibition of bone resorption and hormonal action.
Flavonoids possess anti-inflammation, antioxidant, along with anti-cancerous
activities through multiple pathways, they induce apoptosis in breast,
colorectal, and prostate cancers. Flavonoids can also bind with the ATP-
binding proteins including mitochondrial ATPase, protein kinase C, protein
kinase A, calcium plasma membrane ATPase, and topoisomerase. The
flavonoids delayed NF-ĸB expression. NF-ĸB is a protein complex required
for the proliferation, angiogenesis and existence of cancer cells [10].
Alkaloids
The bioactive compounds disturbed tumorigenesis as well as the
progression of tumor cell growth [11-13]. These bioactive compounds decrease
cellular glutathione (GSH) levels by intermingling directly with GSH, hence
stimulated the generation of ROS [15-18]. The alkaloids are complicated in the
inhibition of NF-κB activation [11, 14].

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Saponins
Saponins showed immunomodulatory activities through cytokine
interaction [11]. Cytostatic and cytotoxic actions were shows the major
anticancer mechanisms of saponins [19, 20]. The steroidal saponins promoted
cancer cell cycle arrest and induced apoptosis, and acted as antitumor agents
[21]
.
Triterpenes
Triterpenes such as 3-O-acetyl-11-keto-β-boswellic acid started tumor
cell apoptosis over stimulation of the death receptor DR-5 signaling pathway
[22, 23]
. This class of bioactive compounds induced tumor angiogenesis by
preventing the emission of the angiogenic factors: VEGF-A and bFGF and the
vascular endothelial growth factor [24, 25]. The cancer cell triggering enzymes,
proteins, and signalling pathways like CDK2, CDK4, Cdc2 kinases
cyclooxygenase, topoisomerase enzyme, COX-2(cyclooxygenase), PI3K,
Bcl-2, cytokines, Akt, MAPK/ERK, TNK, MMP could be achieved by most
the plants products like as flavonoids, saponins, vitamins, taxanes, alkaloids,
oils, minerals, gums etc which triggers DNA repair procedure (p53, p21, p51,
p27 genes and commodities of protein by targeting the rapamycin. (Figure1) [26].

Fig 1: Impact of anticancer phytochemicals after activating expression of various


genes, proteins, enzymes and signaling cascades in order to block cancer initiation
and progression [26]
Certain proteins like BAX, BAK, Bid tempts antioxidant effect,
protective enzymes development (Caspase-3, 7, 8, 9, 10, 12) and hence display
strong anticancer effects and worthful on proteins, enzymes and signalling
pathways (Figure-2) [26-28].

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Fig 2: Impact of anticancer phytochemicals after inhibiting expression of various
genes, proteins, enzymes and signaling cascades in order to block cancer initiation
and progression [26]
After going through the certain researches, we found that there are many
plants that shows anti- cancerous activity as follows-
S. No. Plant Common Name Component Cancer Reference
Ovary, cervix,
Zingiber [29]
01 Ginger Ginger colon, liver and
officinale
urinary caner.
Withania Human cervical [30]
02 Ashwagandha 5-Fluorouracil
somnifera cancer cell.
Sweet
Artemisia wormwood, [31]
03 Artemisinin Breast cancer
annua sweet annie and
sweet sagewort
Astragalus Mongolian [32]
04 Polysaccharide Liver cancer
membranaceus milkvetch
Curcuma [33]
05 Turmeric Curcumin Colon cancer
longa
Garcinia [34]
06 Kokum Garcinol Colon cancer
indica
Bing Ling Cao,
Blushred
Rabdosia [35]
07 Rabdosia and Oridonin Gallbladder cancer
rubescens
Isodon
Rubescens

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Tinospora [36]
08 Guduchi Dichloromethane Brain tumor
cordifolia
White leadwort,
Plumbago [37]
09 chitrak and Naphthoquinone Prostate cancer
zeylanica
Ceylon leadwort
Hodgkin’s
Colchicum lymphoma, chronic [38]
10 Autumn crocus Colchicine
autumnale granulocytic
leukemia.
In our paper our major focus is on one plant Curcuma longa.
Curcuma longa
Curcumin is the most important component of the rhizomes of Curcuma
longa L. (turmeric) [39]. The current literature has found that new anticancer
mechanism for curcumin by inhibiting the lactate production (Warburg effect)
glucose uptake and in cancer cells by downregulation of pyruvate kinase M2
(PKM2). The inhibition of PKM2 was achieved by defeating the mammalian
target of rapamycin-hypoxia-inducible factor 1α (TOR-HIF1α) [40]. Studies
shows the ability of curcumin and its derivatives to defeat multiple different
carcinomas by networking with different molecular targets (figure. 3) [41].

Fig 3: Molecular targets of curcumin in cancer cells. ↑: Increase; ↓: Decrease; MMP:


Matrix metalloproteinase; AP-1: Activation pro1 [41]

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Both in vitro and in vivo studies show that curcumin has strong capability
to induce apoptosis and inhibit proliferation in prostate cancer [42] by
interfering with cellular pathways, including epidermal growth factor receptor
(EGFR), nuclear factor κ (NFκB) and mitogen-activated protein kinase
(MAPK) [43, 44].
A current study says the ability of curcumin to activate protein kinase D1
(PKD1), leading to a decrease in the oncogenic signalling by MAPK and
catenin and resulting in inhibition of prostate cancer. Likewise, PKD1 was
found to be down structured following progression from androgen-
independent from androgen-dependent prostate cancer [45] and E-cadherin
affects the invasion and motility of prostate cancer [46] and considered as a new
therapeutic target for prostate cancer [47]. Studies show that Dimethyl
curcumin (ASC-J9) shown good results in androgen-dependent prostate
cancer by enhancing androgen receptor degradation [48, 49].
After prostate cancer and lung cancer, colorectal cancer is the most
common form of cancer [50]. After diagnosing this cancer removed by surgery
and chemotherapy, most of the patients suffer from relapses [51]. Studies found
that to reduce M (1) G levels without changing COX-2 protein levels in the
malignant colorectal cells [52].
In vitro research of curcumin in different head and neck cancer cell lines
has confirmed its ability to inhibit cell growth that affects cellular pathways
involved in cell propagation, especially STAT3 and NF-κB, which are
overexpressed in some neck and head carcinomas [53, 54]. Curcumin remained
shown downregulate NF-κB and suppress the interleukin-6 (IL-6)-mediated
phosphorylation of STAT3, thus inhibiting the cancer cells [54, 55].
In research on MCF-10A human mammary epithelial cells and MCF-7
breast cancer cells, telomerase activity was observed in tangible drops as a
consequence of treatment with curcumin in a concentration-dependent manner
which was associated to downregulation of Telomerase reverse transcriptase
(hTERT) via curcumin but not with the c-Myc mRNA pathway [56]. In contrast
with the previous literature, this study showed curcumin's ability to
downregulate NF-κB, leading to an antiproliferative effect with breast cancer
cell lines [57, 58]. Dimethyl curcumin (ASC-J9) has also been reported to be
effective against inhibiting several types of steroid receptors in estrogen-
dependent breast cancer [59, 60].
Therefore, alternative therapies using naturally derived compounds such
as curcumin shows promising results and fewer side effects via conventional
treatment. Curcumin has shown multiple molecular targets (Figure. 3),

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consequently, combating brain tumours may take different cellular pathways
autophagy, including apoptosis, invasion, angiogenesis, and metastasis [61].
Future of plant-based drugs
Subsequently, from primordial time turmeric is the most basic and
significant medicine in Ayurveda, and currently scientists are showing keen
interest in bringing the treatment of diseases from plant based natural
products. Studies are still in progress but not exactly a drug development have
been carried out till now. In case of curcumin, it is vastly auspicious
antioxidant and non-hazardous. Curcumin is easily available and can be tested
properly to develop drug for studying its action mechanism and medicinal
effects. It is believed that Curcumin has a very wide purpose in novel drug to
regulate different diseases, oxidative stress and disorders.
Conclusion
Cancer is one of the most dangerous problem around the globe. Many
therapies are also been practised to treat cancer. But as these therapies utilise
chemical compounds, they exhibit many long-term side-effects too. Hence,
here in our paper we are reviewing about the use of plants for treating this
disease which are even less toxic to human beings and plant based organic
compounds like alkaloid, flavonoids etc are used for this purpose. There are
so many plants showing anticancerous effects but in our review the major
focus is on Curcuma longa. We chose this plant as it exhibits antioxidant.
Anti-inflammatory, and anticancer effects. This plant has shown effects over
breast cancer, pancreatic cancer, neck and hand cancer etc. After going
through the latest research, we went to the conclusion that Curcuma longa has
highest drug efficacy and few varied effects. Although there are certain
alterations that makes it difficult to increase its efficacy but working in it might
help us in overcoming this event.
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Chapter - 6
Recent Approaches for Plant-Derived Drug
Discovery

Authors
Dr. Aarti Chouhan
Assistant Professor of Botany, SBN Government P.G. College,
Barwani, Madhya Pradesh, India
Dr. Rajmal Singh Rao
Assistant Professor of Botany, SBN Government P.G. College,
Barwani, Madhya Pradesh, India

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Chapter - 6
Recent Approaches for Plant-Derived Drug Discovery
Dr. Aarti Chouhan and Dr. Rajmal Singh Rao

Abstract
At present, challenges before the world to develop and maintain our
available natural resources-based technologies specially related to drug
discovery approaches in the context, over growth of population and over
exploitation of natural resources. In India, the plants use in a therapeutic
healing both traditionally and medicinally up to ancient periods. In Charak
samhita, 340 drug origin from vegetable plants species used for the
therapeutic treatments of human’s disease. The locally available plant has a
much and more medicinal values we have collect these literatures and
summarized in this type of plant and highlight their medicinal capacity and
combinations for the recent approaches of drug discovery. Already isolated
drug and their therapeutic combination shown in table-1, and in the table-2
shown various part of the plants use in treatments and table-3 shown various
plants locally people use in antiviral activates recent Covid-19 pandemic
duration, after that discovered have two vaccines, Covaxin and Covisheild to
empirical cure or a vaccination for this potentially fatal disease. Mention
traditional and current technical methods for recent approach plants drug
design, highlight positioning and repurposing for drug and its outlines charts.
The pharmacological uses of plants and diagrammatic shown the chemical
structure of primitive and modern drug compound and molecules. The
material is used for the study and research regarding fields.
Keywords: Ayurveda, Covaxin and Covisheild, drug-repositioning, drug-
discovery, herbal-medicines, compound, therapeutic agent, natural-products
Introduction
Systematic and practical medical knowledge in India is called Ayurveda.
Medicinal knowledge gained over trial and error over the thousands of years
in India and neighboring regions of Asia/south Asia has been systematized
some four thousand years ago in a system of medicine called Ayurveda.
Ayurveda (pronounced, I-your-vay-da), the science of life prevention and

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longevity is the oldest and most holistic or comprehensive medical system
available. It was placed in written from over 2000 year ago in India, it is said
to be a world medicines before the advent to writing, the ancient wisdom of
healing, prevention and longevity was a part of the spiritual tradition of a
universal religious. Medical knowledge from all area of the world gathered
in India and the famous sage Vyasa, put into writing the complete
knowledge of Ayurveda along with the more directly spiritual insights of
ethics, virtue and self-realization. In Ayurvedic the method used to acute this
knowledge of the uses of herbs, foods, aromas, gems, colors, yoga mantras
lifestyle and surgery. the sage physician or surgeon of the time were the
same sages or seers, deeply devoted holy people who saw health as an
integral part of spiritual life. it is said that they received their training of
Ayurveda through direct cognition during meditation. In other words, the
knowledge of the use of the various methods of healing, prevention,
longevity and surgery come through divine revelation; there was no guessing
of testing and harming animals. These revelations were transcribed from the
oral tradition into book from interspersed with the other aspects of life and
spiritually.
The vedas: Rik, Soma Yajur and Atharva. Ayurveda was used in
conjunction with Vedic astrology (Jyotish-inner light). Ayurveda was
organized into its on compact system of health and considered an auxiliary
branch of the Vedas called an Upaved (Limb of the Veda), because it dealt
with the healing aspect of spiritually, and not directly discussing spiritual
development. Ayurveda from the various Vedas and made separate books,
dealing only with; Ayurveda. Among the Rik Veda’s 10,572 hymns, are
found discussion of the three doshas Vayu, Pitta, Kapha: organ transplant
and artificial limbs the use of herbs to heal the disease of the mind and body
and to faster longevity. within the Atharva Veda’s 5,977 hymns, are
discussion of anatomy physiology and surgery. Around 1500 B.C. Ayurveda
was delineated into eight specific branches of medicines. There were two
main school of Ayurveda at that time Atreya-the school of physicians; and
Dhanvantari-the school of surgeon.
Origin ethics: The origin of this system of course is lost in time. In
legend it is said to have been taught by the creator to the Prajapati Daksh
(one of the lards of animals) who taught to the divine twins called the
Aswins.
Great concept of Ayurveda: Vyaadhi or disease in Ayurveda is due to
an imbalance of three fundamental element of the body. These are VATA,
PITTA and KAPHA. The entire universe is made of five Mahabhootas or

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great elements these are called; 1. Akaasa (space) 2. Vaayu (air) 3. Tejas
(light) 4. Ap (water) 5. Prithvi (earth).
Description of this thee Vaata, Pitta and Kapha.
The Vaata: Humans body are mainly made of AkasaVaayu, with a
little of Teja, Ap and Prithvi. Vaata is what allow one to interact with
environment. Briefly vaata transmit sense impression to the mind and
response to various place of the body maintain the integrity of the body and
proper functioning of its various constituent elements the sensory organ of
touch and sound depend on Vaata.
The Pitta: In the primary constituents of the living body whose
structure is Tejas (luminouslight) its function is balancing and
transformative. Its function in particular are-“vision, digestion, production of
heat, hunger, thirst softness and suppleness of body, lustre, cheerfulness and
intelligence.
The Kapha: Is one of the primary constituents of body having “water”
and “earth” as elements. Function of pitta is conserving and stabilizing. It
organizes the tissue.
Influence of Ayurveda: Other system of medicines such as chine’s,
Tibetan and Islamic tradition have their roots in Ayurveda. The buddha born
550 B.C. was follower of Ayurveda and spread of Buddhism into Tibet
during and Buddhism countries. The ancient civilization was liked to one
another by trade ruts campaign and war Arab trade spreads knowledge of
Indian plants and Ayurvedic was studied by Arad physicians who include
Indian plant and their Material Medica, and the knowledge was spreads on
the ancient Greek and Romans.
Foreign herbs and synthesized drugs
The growing use of foreign herbs in the 17th prompted heated debate
about the relative value of indigenous European herbs, but for the majority
of the population this was irrelevant as the imported herb were well out of
their price range. Herbal medicine uses rural people used locally while
affluent city dwellers and aristocrats purchased plants foreign origin,
prescribed by university-trained physicians. In beginning of 18th century
approximately 75 percent of plants medicines stock by European countries
were imported. In the 19th century it becomes to practice herbalists known as
Komboyannites, were persecuted.
In India
The name Ayurveda derived from two Indian words; ayur meaning life
and Veda means knowledge of science. Ayurvedic medicines is more than a

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system of healing. It is way of encompassing science, religious and
philosophy that enhance well -being, increased longevity and ultimately self-
realization. it aims to bring about a union of physical, emotional and spiritual
health known as Swasthya.
In China medicines
Uses of traditional Chinese medicines of the herbal tradition the part of
developed separately for Chinese folk medicines. Its tradition for thousands
of years. Its idea recorded between 200 BC. and AD.100 in the yellow
Emperor’s.Encyclopedia of tradition Chinese medicinal substance which has
about 5,757 and most of them are herbs. The communist revolution in 1949
help the swell number of plants used in traditional Chinese medicines, uses
mainly for chronic condition. Because herb that had previously only
employed in folk medicines. Influence by idea of traditional Chinese
medicine in Japan and Korea.
New frontiers and herbal medicines
European settled during the great migration of the 18th and 19th
centuries-North American, South, America, Southern Africa or Australia-
much of the European medicine familiar from home was either unavailable
or prohibitively expensive. Settler came to learn that native people were a
wellspring of information about the medicine virtues of indigenous plants.
For example, European settlers in southern Africa learned about the diuretic
properties of Buchu (Barosma betulina) from native peoples and Australian
shelters came to understand the remarkable antiseptic properties of tea tree
(Melaleuca alternifolia) from observing the medicine as it exists today is a
bland of Aztec, Mayan and Spanish herbs and practices. In northern
America, Native herbalist were particularly adept at healing external wounds
and bites, being superior in many respects to their European counterparts to
their area of medicine. This is not surprising given the range of highly
effective medicinal plants native American had discovered including well
known herbs such as Echinacea (Echinacea angustifolia) goldenseal
(Hydrastis canadensis) and lobelia (Lobelia inflata)
Brief history of the plant utilization
History of the plant one most go back to the history of utilization of
plant and pharmacology for until the last century medicinal plant were still
being process for general use. The history of discovery of the curative and
therapeutic prosperities of plant these are must have sprung from some
human instinct uses. Primitive man used plants for the food and medicine.
He would have learnt after perhaps many unfortunate experiences that some

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plant contained curtained prosperities and able to identify them by the results
they induced. He would also have observed which plants animals utilize
when they were sick. After seeing an injured deer robbing itself against the
geom. He might have discovered for instance they this plant would hell his
own wounds and realized that dog tooth grass would act as an emetic as it
did with the cat. Many remarkable example of animal institutively knowing
how to treat with appropriate plants are quoted by numerous writers Cicero
for example mentioned.
Early origin of the 19 Century
Medicinal plants have been maintained to sustainable the health and
well-being of mankind. Humans knew the importance of linseed oil Linum
usitatissimum oil as nutritious cooking oil, fuel, a cosmetic balm for the skin
and treatment of some disease’s bronchitis, respiratory and digestion
disorders. 60000, years old burial site excavated in Iraq to be found different
medicinal plants, for the medicinal purpose including Ephedra plant. In
many civilizations’ plants were considered to have souls. Even Aristotle, the
4th, century BC Greek Philosopher, through the plant had a psyche, albeit of
a lesser order than the human’s soul. In medieval Europe the doctrine of
signature stated there was a connection between how a plant looked Gods,
signature and how it might be used medicinally for example the mottled
leaves of lungwort (Pulmonaria officinalis), were thought to resemble lung
tissue and the plant is still used to treat ailment of the respiratory tract.
Similar in western culture it is a belief that plant sprits linger. In Britain
people do not cut down elder trees for fear of arousing the anger of the elder
mother the sprit that lived in and protected the tree. In Hindu culture plant
are sacred to specific divinities. For example, the bale tree Aegle marmelos is
said to s helter “Lard Shiva, the God of health, beneath and branches. In
South America believe that the coca plant (Erythroxylon coca) is protected
by Mama Coca, a sprit who must be respected and placated it the leaves are
to be harvested and used. In many traditions’ societies illness is through to
stem from malignant plant have healing power. In Egypt the Middle East
India and China civilization grew from 3000 BC. On words therefore the use
of herbs becomes more sophisticated. They made first written account of
medicinal plants.
In India, the Vedas the epic poem had written 1500 BC. This volume
contended rich material on herbal lore of that time. The Vedas were followed
in about 700 BC. By the Charaka Samhita, written by the physician Charaka.
He is known as is known Father of medicine of India. This medical treatise
includes details of around 350 herbal medicines. Amongst them are Visnaga

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(Ammi visnaga) an herb of middle east Eastern origin that has recently
proven effective in the treatment of asthma and Gotu, kola (Centella
asiatica) which has been long used to treat leprosy.
Indian Islamic medicine AD500-1500
In the Arabic culture AD. 500-1500 gained the classical Greek and
Roman ideas for medicinal plants. They preserved and elaborated them. The
spread of Islamic cultural along North Africa and present Day Italy, Spain
and Portugal led to the founding of renowned medical schools notably at
Cordoba in Spain. The Arabs were expert pharmacist, blending and mixing
herbs to improve their medicinal effects and their tastes. Their contract with
both Indians and Chinese medical tradition meant that they had remarkable
range of medical and herbal knowledge to draw on and develop.
Medical plants in European countries AD-1000-1400
The classical Greek Roman and Egyptian literature were preserved in
the libraries of Constantinople which filtered back to Europe. This
encouraged European scholar to established hospitals medical scholars and
universities the medical school at Salerno on the west coast of Italy is one of
the prime institutes. It not only allowed from all faiths-Christian Moslem and
Jewish- to study medicine but it also allowed women to train as physicians.
In 12th century, trade with Asia expanding and new herbs species were being
regularly imported into Europe. Hildegard of Bingen (1098-1179) the
famous German mystic and herbal authority, considered galangal (Alpinia
officinarum), used in Asia as a warming and nourishing spice for the
digestive system-to be the “spice of life “given by God to provide health and
to product against illness.
Development in Asia
Macro Polo’s travels to China in the 14th century coincided with the
unification of the whole of Asia from the Yellow Sea in China to the Black
Sea in South-eastern Europe by Genghis Khan and his grandson Kublai
Khan, whose capital was in China, not far from Beijing. Neither the Chinese
nor Ayurvedic medicine medical tradition were directly threatened by this
conquest. The ruler of Mongol tried to stop use of a few toxic plants like
aconite (Aconitum napellus). The people were using aconite as alternative of
arrow poison-one that could have been used against the ruling powers.
Mongols have tried to make unification between the two medical disciplines.
In other part of Asia, such Vietnam and Japan, Chinese culture and medicine
exerted the primary influence. While kampo-the traditional herbal medicines
of Japan are distinctive to that country.

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The trading of medicinal plants
In 15th century onwards an explosion in trade led to a cornucopia of a
new herbs becoming readily available in Europe. They include plants such as
ginger (Zingiber officinalis) Cardamom (Eletoria cardamomum) nutmeg
Myristica fragrans turmeric (Curcuma longa) cinnamon (Cinnamomum
verum) and senna (Cassia senna) the trade is herb was not entirely one way.
The European herb sage the example come into use in China where it was
considered to be a valuable yin tonic. In 1942 ships of Columbus arrived in
the Caribbean which was followed in the rapid conquest and colonization of
central and South Africa by the Spanish and Portuguese. Along with their
booty plundered gold the conquistadores returned to the old world with
previously unheard-of medicinal plants various herb from the Americans had
highly potent medicinal action. They soon become available in the
apothecaries of the major European cities. Plant such as lignum vitae
(Guaiacum officinale) cinchona were used for treatment of fever malaria,
syphilis, smallpox and other serious illness. The natural communities tried to
foreign plants for medical and food valve. In the other country’s Potatoes
(Solanum tuberosum) and Maize both native to south America become
common food for all. These plants clear medical as well as nutritional
benefits. Potato juice is a valuable remedy for arthritis, while corn silk makes
effective decoction problem such as cystitis.
1.1 Identified plants drug and their chemical compounds.
The plant use as a foods and medicines about 6-7% of the out of 250000
angiosperms plants but some plants have extra potentially capacity for the
therapeutic treatment for many humans’ disease those are screening by some
surveyor. Most of the observer about 15-20% have been evaluated for
phytochemically. These are all useable plants identified and screened for the
therapeutic and ayurvedically useable. Plants have an advantage this area
based and their long-term use by the humans expect any bio active
compounds obtained from such plant to maintained and minimize toxicity.
Some plants may be toxic within a given endemic pandemic culture that
have no reporting system of these effects. Plants have much medicinally
properties we should try and attempt this to modified and converted as a
useable therapeutic use for the particular diseases, most of the large
pharmaceutical manufacturer and biotechnological Industries and drug
company able to screening for identified plants uses as a therapeutic
medicine it is thousand and more plants to identified and isolate for their
valuable biochemicals but the challenges of the all these firms forthcoming
viral pandemics. Most of the important plant drugs occur and isolates by the
following plant.

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Table 1: Drugs derived from plants, with their ethnomedical importance and sources

Drug Action or Clinical use Plant Source


Acetyldigoxin Cardiotonic Digitalis lanata Ehrh
Adoniside Cardiotonic Adonis vernalis L.
Aescin Anti-inflammatory Aescus hippocastanum L.
Aesculetin Antidysentery Fraxinus rhynchophylla Hance
Agrimophol Anthelmintic Agrimonia eupatoria L.
Rauvolfia serpentina (L) benthex
Ajmalicine Circulatory disorder
Kurz
Allyl isothiocyanate Rubenfacient Brassica nigra (L) Koch
Andrographolide Bacillary dysentery Andrographis paniculate Nees
Anisodus tanguticus (Maxim)
Anisodamine Anticholinergic
Pascher
Anisodus Tanguticus (Maxim)
Anisodine Anticholinergic
Pascher
Arecoline Anthelmintic Areca catechu L.
Asiaticoside Vulnerary Centella asia cica (L) Urban
Atropine Anticholinergic Atropa belladona L.
Berberine Bacillary dysentery Berberis vulgaris L.
Bergenin Antitussive Ardisia japonica BL.
Anti-inflammatory;
Bromelain Ananas comosus (L.) Merrill
proteolytic agent
Caffeine CNS stimulant Camellia sinensis (L.) Kuntze
± Catechin Haemostatic Potentilla fragaroides L.
Chymopapain Proteolytic; mucolytic Carica papaya L.
Cocaine Local anaesthetic Erythroxylum coca Lamk.
Codeine Analgesic; antitussive Papaver somniferum L.
Colchicine Antitumor agent; antigout Colchicum autumnale L.
Convallotoxin Cardiotonic Convallaria majalis L.
Curcumin Choleretic Cucurma longa L.
Cynarin Choleretic Cynara scolymus L.
Danthron Laxative Cassia spp.
Antihypertensive;
Deserpidine Rauwolfia canescens L.
tranqualizer
Deslanoside Cardiotonic Digitalis lanata Ehrh.
Digitalin Cardiotonic Digitalis purpurea L.
Digitoxin Cardiotonic Digitalis purpurea L.
Cephaelis ipecacuanha (Brotero)
Emetine Amebicide, emetic
A.

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Ephedrine Sympathomimetic Ephedra sinica Stapf.
Etoposide Antitumor agent Podophyllum peltatum
Gitalin Cardiotonic Digitalis purpurea L.
Glaucaroubin Amoebicide Simarouba glauca DC.
Glycyrrhizin Sweetener Glycyrrhiza glabra L.
Gossypol Male contraceptive Gossypium spp.
Hemsleyadin Bacillary dysentery Helmsleya amabilis Diels
Hydrastine Hemostatic; astringent Hydrastis canadensis L.
Hyoscamine Antichlinergic Hyoscyamus niger L.
Kainic Acid Ascaricide Digenea simplex (Wuif) Agardh
Kawain Tranquilizer Piper methysicum Forst. f.
Khellin Bronchodilator Ammi visnaga (L.) Lamk.
Lenatosides A.B. Cardiotonic Digitalis lanata Ehrh.
Smoking deterrent;
Lobeline Lobelia inflata L.
Respiratory stimulant
Monocrotaline Antitumor agent Crotalaria sessiliflora L.
Morphine Analgesic Papaver sominiferum L.
Neoandrographolide Bacillary dysentery Andrographis paniculata Nees
Noscapine Antitussive Papaver sominiferum L.
Ouabain Cardiotonic Strophanthus grantus Baill.
Papain Proteolytic, mucolytic Carica papaya L.
Phyllodulcin Sweetener Hydrangea macrophylla (thumb)
Physostigmine Cholinestares inhibitor Physostigma venenosum Balf.
Picrotoxin Analeptic Anamirta cocculus (L.) W&A
Pilocarpine Parasimpathomimetic Pilocarpus jaborandi Holmes
Podophyllotoxin Cardylomata acuminata Podophyllum peltatum L.
Protoviratrines Antihypertensive Veratrum album L.
Pseudoephedrine Sympathomimetic Ephedra sinicastapf.
Cinchona lendgeriana Moens ex.
Quinine Antimalarial
Trimen
Quisqualic acid Anthelmintic Quisqual indica L.
Rauvolfia serpentina L. benth ex.
Reseinnamine Antihypertensive tranquliser
Kurz
Rauvolfia serpentina L. benth ex.
Reserpine Antihypertensive tranquliser
Kurz
Rhomitoxin Antihypertensive Rhododendron mole G. Don
Rorifone Antitussive Rorippa indica L.
Rotenone Piscicide Lonchocarpus Nicou (Abul)
Rotundine Analgesic sedative Stephania sinicadiels

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Salicin Analgesic Salix alba L.
Santonin Ascaricide Artemisia maritima L.
Scillarin A Cardiotonic Urginea maritima L. Baker
Scopolamine Sedative Dhaturametel L.
Sennosides A &B Laxative Cassia spp.
Silymarin Antihepatotoxic Silybum marianum L. Gaertn
Stevioside Sweetener Stevia rebaudiyana Bertoni
Strychinine CNS stimulant Stychnosnux vomica L.
Teniposide Antitumor agent Podophyllum peltatum L.
Tetrahydropalmatine Analgesic sedative Coridali ambigua (pallas)
Theobromine Diuretic bronchodilator Theobroma cacao L.
Theophylline Diuretic bronchodilator Camellia sinensis L. kuntze
Trichosanthin Abortifacient Thymus vulgaries L.
Tubocurarine Skeletal muscle relaxant Chondrodendron tomentosum
Valepotriates Sedative Valeriana officinalis L.
Vincamine Cerebral stimulant Vinca minor L.
Xanthotoxin Leukoderma vitiligo Ammi majus L.
Yohimbine Aphrodisiac Pausinystalia yohimbe
Yuanhuacine Abortifacient Daphne genkwa Seib & Zuce

The use of plant as a medicine for the therapeutic uses could be called
more accurately ethnobotanic medicines and Ethnomedicinally may be
defined as broadly and ethnopharmacology is a high diversified drug
discovery approach through the identification, observation, description,
experimental and investigation of indigenous drug discovery. The basic
criteria and involve discipline like botany, chemistry biochemistry,
pharmacology and others importance’s. Medicinal herbs are blessings from
nature towards entire humankind, which provide timely and adequate
remedies to several human’s health disorders. Medicinal herbs allow people
to increase their immunity in times of health problem like novel coronavirus
in pandemic periods. It is evident from the human history that medicinal
plants have been the treatment to cure a variety of diseases, including
diseases caused by, bacteria, viruses. Fungi and insects the effects shown by
the plants are due to the chemicals present in them, and they work in the
same manner as conventional therapeutic drugs. In the present time, we need
to understand the correlation between medicinal plants, immune systems,
and Covid-19. Recently, the world health organization (WHO) estimated that
80 percent of people worldwide esthetical depends on medicinal herbs for
their primary health care their needs. According to the WHO, around 21,000
plant species have the potential to be used as medicinal plants. Medicinal

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plants and the immune system: Scientists have focused on preventive
measurements and explored fast health remedies. Many of the plants &
herbal extract in the form of alkaloids, terpenoids, flavonoids,
polysaccharides, glycoside and lactone products are responsible for causing
alterations to the improved, boosting immunological responses. Ayurveda
experts have emphasized that medicinal herbs such as Aswgandha, Withania
somnifera, Glycyrrhiza glabra, Tinospora cordifolia, Andrographis
paniculata, Piper nigram etc. are advantageous in boosting the immune
system to combat against the deadly viruses. Severe acute respiratory
syndrome produces coronavirus-2 (SARS-CoV-2) that causes novel corona
virus disease 2019 (Covid-19), primarily effects on the lungs and the
respiratory tracts. The valuable prosperities of some therapeutic medicinal
plants given below summarizes with special reference to immunological
responses (Table-2).

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Botanical name Common name Family Uses
1. Root and other Antispasmodic, expectorant and carminative, used in epilepsy and other
underground part. Sweet flag Araceae therapeutic uses sedative and analgesic.
Acorus calamus
Source of the gum-resin, Ferula asafoetida, useful in the treatment of asthma
Ferula asafoetida Hing Apiaceae
cough and indigestion disease.
The drug Rauwolfia serpentina is used for relief from nervous disorder and
anxiety states, excitement, maniacal behavior associated with psychosis,
Rauvolfia serpentine Sarpagandha Apocynaceae
schizophrenia, insanity, insomnia, and epilepsy; used in high blood pressure
and hypertension treatments.
Yields colchicine’s, carminative, Laxative, and aphrodisiac; used in gout,
Colchicum autumnale Hirantutiya Liliacea
rheumatism and disease of liver and spleen treatment.
Emetic, diaphoretic, and expectorants, useful for the disease of allaying cough
Cephaelis ipecacuanha Ipecacunha Rubiacea and catarrhal affections, and irritable conditions of the membrane of urinary
organs.
Panax schinseng, P. guigue- Disorder of stimulants, stomachic, demulcent and expectorant and antipyretic,
Ginseng Araliacea
folium influences metabolic and prevents development of arthrosclerosis.
2. Bark The plant drug Podophyllum is therapeutic used as a purgative and an effective
Podophyllum hexandrum, Podophyllum Berberidaceae vermifuge also used for tumorous growth.
P. peltatum
Rheum officinales Rhubarb Polygonaceae Used as a purgative and astringent tonic stomach disorder.
Astringent, carminative and antiseptic; useful in asthma, diarrhea, fevers,
Myrica esculenta Kaiphal Myriaceae
chronic bronchitis, lung affections and dysentery and dieresis and disorder.
Plant extract tonic and anthelmintic; used in scrofula and cutaneous troubles;
Bauhinia variagata Kachnar Caesalpiniaceae
also used for ulcers and leprosy disease.

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Rhamnus purshiana Cascara Rhamnaceae Plant extract use in tonic and laxative.
3. Stem and wood Plant drug source of ephedrine; given for asthma and other respiratory troubles.
Ephedra Ephedraceae
Ehedraequistina, E. sinica
Source of galbanum; used for the stimulants, carminative, expectorant, and
Ferula galbaniflua gandhabiroja Apiaceae
antispasmodic.
Uses in Diuretic, diaphoretic, refrigerant and expectorant, used as a sedative
Santalum album Safed chandan Santalaceae
and cardiac tonic.
4. Leaves Used in the sedative, antispasmodic, and anodyne; used in ophthalmology to
Belladonna Solanaceae
Atropa belladonna dilate pupil.
The plant drug Vaska is used in bronchial troubles and consumption; also used
Adhatodavasica Vasaka Acanthaceae
in diarrhea, dysentery, glandular tumors and skin affections and others.
This plant uses cathartic and refrigerant; used in liver and spleen ailments and
Aloe barbandensis Ghee-kunvar Liliaceae for eye troubles; found useful in x-ray burns, dermatitis, cutaneous
leishmaniasis and other skin disease and disorder.
The medicines Digitalis is used as a cardiac stimulants and tonic; increase the
Digitalis purpurea Foxglove Scrophulariaceae force of systolic concentration and the efficiency of decompensate heart. It is a
diuretic useful in renal obstruction and dropsy disease.
Plant drug Henbane has anyone, narcotic and mydriatic properties; employed as
Khurasani
Hyoscyamus niger Solanaceae a sedative in nervous affections and irritable condition, such as asthma and
Ajwain
whooping cough.
Mentha arvensis, Uses in stimulants and carminative, used for allaying nausea and flatulence,
M. pipertia Pudina Lamiaceae and externally applied in rheumatism, neuralgia, congestive headache, and
M. longifolia toothache etc.
Holarrhena Plant Astringent, anthelmintic, stomachic, antipyretic, tonic and antidysentery
Kurchi Apocunaceae
antidysenterica used in amoebic dysentery diarrhea disease.
5. Flowers Laung Myrtaceae Pant dried unopened floral buds, known as ‘Clove’, are used as aromatic,

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Syzygium aromaticum stimulants and carminative; used for dyspepsia and gastric irritation and
inflammatory.
The plant drug used as an anthelmintic, particularly effective against
Artemisia maritime Wormseed Asteraceae
roundworm; stomachic laxative and febrifuge effects.
Treatment of stimulants, diaphoretic, laxative and anthelmintic used for cough
Leucas cephaloes Dronapushpi Lamiaceae
and cold.
6. Fruits and seeds The famous plant drug emollient, demulcent, and laxative used in chronic
Papaver somniferum constipation, dysentery and diarrhea, and inflammatory condition of
Opium poppy Papaveraceae
gastrointestinal and genitor-urinary tract. Poultice of crushed seeds applied to
rheumatic and glandular swelling disorder.
Medicines used as a tonic, stimulants and febrifuge; also used in preparation for
Strychnosnux-vomica nux-vomica Loganiaceae
nervous disorder.
These are use emollient, demulcent and laxative; and chronic consumption,
dysentery and diarrhea and inflammatory condition of gastrointestinal and
Plantago ovate Isubgol Plantaginaceae
genitor-urinary tract. Poultice of crushed seeds applied to rheumatic and
glandular swellings disorder.
The plant drug carminative, stimulants and diuretic, used in dropsy, disorder of
Junipers communis Haubera Cupressaceae
urinogenital tract cutaneous disease and disorder.
Croton tiglium Jamalgota Euphorbiaceae Plant drug used as a violent purgative and vesicant.
Chenopodium ambrosioides American Medicine used as an anthelmintic, especially for hookworm infections disease.
Chenopodiace
var. anthelminiticum wormseed
Strophanthus hispidus Strophanthus Apocynaceae Plant drug used as cardiac stimulant.
Taraktogenos Kurzii Chaulmugra Flacourtaceae Plant drug used as an external application in leprosy.
Citrulina colocynthis bitter apple Cucurbitaceae Plant uses as drastic hydragog, cathartic.
Used for the aromatic stimulants, local irritant, durotactic, carminative and
Piper cubeba Kababchini Piperaceae
sedative; used in rheumatism, gonorrhea, bronchial troubles etc.

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Many plants derived biochemical compound have been use as
therapeutic drug for the treatment of many human and animal diseases. The
plants extracted chemicals utilize as therapeutic medicine is called plant drug
and plants secondary metabolites can also serve as drug precursors,
prototypes drug, and pharmacological probes, these entire discovery by plant
screening technical methods. We attempt to discuss on the Present drug
discovery scenario and primitive and advanced plant drug discovery and its
development and related techniques. The plant identified and screening
methods to discovery of plant drug.
Natural Products are characterized by enormous scaffold diversity and
structural complexity. They typically have a higher molecular mass, a larger
number of sp3 carbon atoms and oxygen atoms but fewer nitrogen and
halogen atoms, higher numbers of H-bond acceptors and donors, lower
calculated octanol–water partition coefficients (cLogP values, indicating
higher hydrophilicity) and greater molecular rigidity compared with
synthetic compound libraries (Harvey Al.,et. al., 2008, Fabricant DS.,
2001and Smit HFet. al.,1995).
Over a million people in the worldwide are now confirmed to be
infected with COVID- 19; we have two in India like, Covaxin and
Covishields and others, empirical cure vaccines for this potentially fatal
disease. Drug repurposing is playing a vital role in combination recovering
of this disease. Drug repurposing or repositioning is a drug development
strategy which identifies new pharmacological applications of already
approved for the drugs. Drug repositioning is the discovery of new
indications for approved or failed drugs. Positioning opportunities exist
because drugs perturbing multiple biological entities and themselves
involved in the diversified biological process. The drug discovery focused on
one way of disease of interest, a therapeutic application for a drug to other
areas can be abide. The therapeutic plants have an advantage in this area
based on their long-time use by humans. One may expect any bioactive
compounds obtained from such medicinal plant to have low human health
toxicity. Obviously, these many plants may be toxic within a given of the
endemic culture that has no reporting to document these effects.
The covid19 life cycle involves a number of potentially targetable step
including endocytic entry into humans, host cells [Involving Angiotensin-
converting Enzyme 2 (ACE2) and Transmembrane Protease Serine 2
(TMPRSS2) both of them], RNA replication and transcription [Involving
Helicase and RNA-dependent RNA Polymerase (RdRP)], translation and
proteolytic processing of viral proteins virion assembly, and release of new

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viruses through the exocytic human cell systems. In addition to virally
encoded targets, numerous respiratory host targets are essential for viral
replication and disease progression, like covid19 use the endolysosomal
pathway to enter the cell before uncoating of the host.
1. Methods approaches through selection of candidates and species
screening
In silico is the term used to mean “performed on computer through
computer simulation”. In silico methods help in identifying drug targets in a
less time, cheapest and cost-effective manner. The use of computers and
computational methods is involvement in all aspects of drug designing,
development and repurposing.
There are two major types of drug design:
1) Ligand-based drug design these is based on the knowledge of other
molecules that bind to the biological target of interest. These other
molecules may be used to derive a pharmacophore model that
defines as the minimum necessary structural characteristics a
molecule must of the possess in order to bind to target.
2) Structure-based drug design these is based on the knowledge of the
three-dimensional structure of biological target obtained through
methods such a x-ray crystallography and NMR spectroscopy.

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There are many important methods for in-silico drug design research
such as homology modelling, molecular dockin virtual high-throughput
screening, quantitative structure activity relationship (QSAR) and hologram
quantitative structure activity relationship (HQSAR), comparative molecular
field analysis of (CoMFA), Comparative molecular similarity indices
analysis (CoMSIA), 3D pharmacophore mapping, microarray analysis and
conformational analysis techniques, Monte Carlo simulation and molecular
dynamic (MD) simulation ((Kubiyayi, H., 1997, Cramer RD., et. al.,1989
&Klebe G., 1994).

A. Random approaches B. Ethnopharmacology approaches C.


Traditional approaches D. Zoo-pharmacology
1) Observed out of 2.50 lakh angiosperms and gymnosperms plants
species recently 6% have been screened for biological activity and
about 15 percent have been screened for phytochemical activity
(Fabricant DS et al., 2001).
2) Random approaches have been followed for screening of plants
selection method through randomly for purpose of latest drug
discovery. The plant screening for selected class of plants product
like alkaloid flavonoidsetc.
3) Screening plants for selected bioassay, this is followed up to three
decades by Central Drug Research Institute and council of scientific
and industrial research of India, National Cancer Institute’s (NCI),
National Institutes of Health, USA.
4) The drug discovery approach of ethnopharmacology essentially
depend on empirical experience related to use of plants drug for the
biologically active NCEs this is through experimental,
investigation, description and observation.
5) Traditional system of medicine approach in India and China has a
rich heritage and well documented traditional system of medicines
and plant sources.

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6) Behavior of animals with a view for observation and identify the
candidate’s plants for view drug discovery, its observation straight
tail linked to cattle grazing habit in certain habit of South America
led to identification of a plant Cestrum diurinum and three other
plants members of family Solanaceae which probably are the
known plant sources of the derivatives of vitamin D, this is close
observation and monitoring under animal behavior (Katiyar. Et al.,
2015).
2. Other useable methods for the drug discovery
1) Drug chemical structure similarity.
2) Drug side- effect similarity.
3) Drug target similarity.
4) Gene ontology (GO) similarity of drug-related genes.
5) Disease phenotypic similarity.
6) Human phenotype (HPO) similarity.
7) GO similarity of disease-related genes.
8) Gold standard dataset.
9) Traditionally plants product used methods.
10) 10 Marine natural plants product isolate methods.
11) Bioinformatics methods.
3. Docking methods
Once we chose leader compounds from the previously mentioned list,
we used the COVID-19 Docking Server (https://ncov.schanglab.org.cn/), a
web server that predicts the binding modes between different COVID-19
targets and the ligands. A complete description of the algorithm used for
such could be found (Kong, R., et. al.,2020). We tested the targets: Main
protease, papain-like protease, Nsp3 (AMP site), Nsp3 (MES site), RdRp
(RTP site), RdRp (RNA site), Helicase (ADP site), Helicase (NCB site),
Nsp14 (ExoN), Nsp14 (N7-MTase), N protein (NCB site) with the selected
ligands, accordingly to the best conformation (emodin anthrone, kaempferol,
quercetin, aesculin, cichoriin, luteolin, matricin, riolozatrione, monocaffeoyl
tartaric acid and aucubin).
4. Pharmacokinetic assessment (PBPK Model building and evaluation)
The best compound according to docking results observe of the some
reviewed against SARS-CoV-2, developed a PBPK model to predict the

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pharmacokinetic potential of such compounds in an individual. In this
response, the PBPK’s models predict the concentration-time profile of
compounds in the body, giving an idea of such compounds’ to the
performance. The adult PBPK model was developed using PK-sim modeling
software (version 8.0, 2017, http://www. Systems biology.com/products/pk-
sim.html) and according to data from simulation from other coumarins.
(Miura, T., et al., 2020).
A brief update on the status of potential repurposed discovery of drugs
and/or combinations recently under clinical trials is following.

1) Anti-HIV drugs: The therapeutic, combination of lopinavir-


ritonavir is used in the USA to treat HIV infections and it has
selected because of its ability to inhibit protease of HIV and other
SARS-CoV-2.
2) Anti-ebola drug: The famous drug, Remdesivir (2-ethylbutyl-L-
alaninate phosphoramidate prodrug) is a novel nucleotide analogue
originally developed by GILEAD Sciences to treat Ebola virus. It’s
used in corona viral disease treatments.
3) Antimalarial drugs: The beneficial effects of repurposed drug
Chloroquine, Hydro-cloroquine it is anti-malarial drug used in the
treatment of covid-19.
4) Anti-influenza drugs: Favipiravir, is a new type of RdRp inhibitor
which is currently using clinical trial for the covid-19.
5) Anti-HIV & Anti-hepatitis drugs: The Ritonavir and Danoprevir
suspension is approved for the treatment this combination with or
without interferon nebulization for the treatment of COVID-19.
Caution: Above the entire drug only study purposes in this article
anybody should not directly apply and practices, without permission of
prescribed physician and experts. Otherwise the authors are not responsible
for any effects.

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Table 3: List of potential medicine plants possessing antiviral, anti-malarial and anti-bacterial activity

S. No. Name of the plant Family Important phytoconstituents Therapeutic uses

Gems, fungi and infection with


Eugenol, carvacrol, methyl anti-bacterial. The fresh mature
Ocimum sanctum
1. eugenol, caryophyllene, linalool, leaves are given to children with
(Holy Basil)
cineole. nasal catarrh and cough, asthma,
fever, constipation and worm.
Family: Lamiaceae

Nigella sativa Influenza Virus(H9N2),


2. (Black seed) Thymoquinone, Nigellimine Cytomegalovirus (MCMV),
Hepatitis C virus, HIV
Family: Ranunculaceae

Cinchona succirubra Quinine, Quinidine, Cinchonidine, Herpes simplex virus-1(HSV-1)


3.
(Cincona) Cinchonine influenza A virus (IAV)

Family: Rubiaceae

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Sambucus nigra Herpesvirus
4. Ursolic acid, Oleanolic acid
(Elderberry)

Family: Caprifoliaceae

Withanolides, somniferinine,
Withania somnifera
withaferins, Isopelletierine, Herpes Simplex Virus
5. (L.) Dunal
anaferine, sitoinroside, Influenza virus H1N1
(Ashwagandha)
anahygrine, visamine.
Family: Solanaceae

HIV-1 and Bola virus,


Prunella vulgaris Betulinicacid, Hyperoside,
6. Herpes Simplex Virus -1 & 2
(Self-heal) Delphinidin, Lupeol

Family: Lamiaceae

Used for diseases of the


respiratory tract (cough,
Piper nigrum ((Kali Piperine, Piperdine, Piperettine,
7. bronchitis, asthma), Increase
mirch, Maricha) Chavicine
total WBC and Bone marrow
cells.
Family: Piperaceae

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Used in high fever, strengthens
Berberin, columbin, chasmanthin, immune system and cures
Tinospora cordifolia
8. palmarin, tinosporon, tinosporic various infections like cold,
(Guduchi/Giloy)
acid and tinosporol. cough, swine flu and fever due
to any reason.
Family: Menispermaceae

HCV, Influenzavirus, HSV1


Glycyrrhiza glabra Glyrrhizin, Glycyrrhetic acid,
9.
(Licorice) Liquiritin, Isoliquiritin

Family: Fabaceae

Caesalpinia
Lupeol, β-amyrin, Peltoqinods,
10. pulcherrima Herpes viruses, adenovirus
Homoisoflavonoids
(Peacock flower)

Family: Leguminoseae

Curcumin, d-a-phellandrene, d-
Curcuma longa HSV-1, HIV, HCV
11. sabinene, cineol, borneol,
(Turmeric)
sesquiterpenes.
Family: Zingiberaceae

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Plant drug as considered
Cinnamomum astringent, stimulant and
12. zylanicum Cinnamic aldehyde, eugenol carminative, check nausea;
(dalchini, Darushila) useful in gastric troubles and
toothache.
Family: Lauraceae

Zingiber officinale
13. Gingerol, Shogaols, Zingerone Avian influenza virus (H9N2)
(Ginger)

Family: Zingiberaceae

Punica granatum
14. Punicalagins, Ellagitannin SARS-Co. V -19
(Pomegranate)
Family: Lythraceae

Andrographis Antiviral properties, HSV, HBV,


15. paniculate Andrographolide HCV, Chikungunya virus, HPV,
(green chireta) HIV
Family: Acanthaceae

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Antiviral properties, anti-
Methyl-amyl ketone, gallotamic
Syzygium aromaticum microbial activity, powerful anti-
16. acid, eugenol acetate, iso-eugenol,
(Laung, lavanga) septic, Phthisis, bronchial
vanillin, caryophyllin.
troubles and

Family: Myrtaceae

Aconitum
Biokhaconitine, indaconitine, Cardiac stimulants, arthritis,
17. heterophyllum
diacetyl pseudo-aconitine. scabies.
(Bish, Attis)
Family: Ranunculaceae

Neuralgia, inflammation,
Bacopa monnieri (L.) Brahmine, herpastive, hersaponin,
18. asthma. bronchitis, syphilis,
(Brami, Sarasvadi) bacogenin-A, monnierin
fever.
Family: Scrophullariaceae

Fruits are anti-diarrhoeal, anti-


dysenteric, the are used as a
Emblica officinalis
19. Emblicanin-A, Emblicanin-B, collyrium in eye complaints and
(Amlika, Anola)
their infusion is given in asthma,
bronchitis, and fever.
Family: Euphorbiaceae

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Fig 1: Chemical structure of some selected natural Products known to exhibit potent
antiviral activity
They identified some of the 13 natural products, which is occur in
traditional Chinese medicines and could cause antiCovid-19 activity. 125
herbs listed to contain at least two of these phytoconstituents while only 26
herbs are listed and categorically used to treat viral respiratory infections
(Zhang DH., et al., 2020). The identified chemicals include; Quercetin,
Kaempferol, Betulinic acid, Coumaryl tyramine, Cryptotanshinone, Sugiol
etc. The extra potential Chinese herbal plants containing these constituents
and possibly be used to treat for respiratory syndromes are Forsythiae
fructus, Liquorice, Mori cortex, Eriobotryae folium, Ardisia japonicae herba
etc.
screened a medicinal plant database containing 32,297 potential anti-
viral phytochemicals/traditional Chinese medicinal compounds and selected
the top nine hits that may inhibit SARS-CoV-2 3CLpro activity and hence
virus replication. Top ranked phytochemicals 5,7,3',4'-Tetrahydroxy2'-(3,3-
dimethylallyl) isoflavone from Psorothamnus arborescens, Myricitrin from

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Myrica cerifera, Methyl rosmarinate from Hyptisatrorubens poit,
Calceolarioside B from Fraxinus sieboldiana, Licoleafol from Glycyrrhiza
uralensis showed better binding affinity and docking scores than positive
control drugs, Nelfinavir and Prulifloxacin. They concluded that these
phytochemicals might serve as potential anti-COVID-19 lead molecules for
further optimization and drug development process to combat COVID-19
(Qamar MT., et. al.,2020). On the observe several efforts have been
performed to identify whether natural products possess antiviral disease
effects.
This instance, aqueous extracts of Ocimum basilicum have been proven
to be effective against enterovirus by inhibiting viral replication capacity
(Chiang, LC. Et al., 2005). In others observation Furthermore, saikosaponins
(Cheng, PW., 2006) identified phenolic compounds, amentoflavone,
myricetin and scutellarein isolated from Lycoris radiata, Artemisia annya,
Torreya nucifera and Lindera aggregata are active against SARS-CoV-1
disease (Li, SY., et al., 2005 &Yu, MS., Lee et al., 2012).
A brief review of herbal medicine, to (Huang, J. et al., 2014). Moreover,
other sources of antiviral compounds have shown to possess such important
properties for instance, Suwannarach et, al. (2020) observe that fungi are a
source of natural bioactive compounds that are potentially useful for
preventing viral infections and improving human immunomodulation;
against disease and additionally, natural products from marine plants species
have recently shown important antiviral properties (Teng, YF. Et al., 2020).
In the field plants therapeutic, Mexico is the fourth country with the large
biodiversity globally. It has been estimated that there are more than 35,000
species of plants; and after China, Mexico is the country with the second
largest number of medicinal plants (4000 spp., approximately). Moreover,
Mexican ethnomedicine has a deeply rooted tradition to use herbal remedies
to treat the most common health problems. In this sense, Mexican plants
have been studied phytochemically, pharmacologically and
anthropologically for more than 100 years, representing a significant
research line in Mexico and worldwide (Mata, R., et al., 2019).
Interestingly, the most frequently used plants accordingly to (Mata, R.,
et, al.,2019 & Valdivia-Correa et. al.,2016)are Opuntia Ficus, Scoparia
dulcis, Citrus aurantium, Prunus persica, Rosmarinus officinalis, Prunus
persica, Rosmarinus officinalis, Equisetum hyemale, Tiliamexicana, Mentha
piperita, Larrea divaricata, Taraxacum officinale, Morus alba, Verbascum
densiflorum, Matricariarecutita, Urtica dioica, Passiflora incarmata,
Tiliaeuropea and Aloa Vera most of which have shown several

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pharmacological properties such as antiparasitic, pain and menstrual pain
relief, issues of the nervous system, among others.
Conclusion
In Ayurveda 2000 plants species are considered to have medicinal
values while Chinese’s pharmacopoeia listed over 5700 traditional plants
medicines. Indian medicinal plant has a good contribution to the
development of material medica. The Charak Samhita is one of the earliest
treatises in Indian medicines it was recorded the use of over 340 vegetable
drugs. In European, Asian, Australian, American countries have a great plant
medicine produce system and they develop latest drug discovery institutions.
Liquorice, Zinger Turmeric, Green Chireyta, Winter Cherry are widely used
Indian system of medicines for upper respiratory infection since ancient
time. To the traditional plant therapeutic medicines system be implement in
future because our native traditional therapeutic plant medicines very
effective and cheapest available locally. India is greatest and largest country
in the context of biodiversity plant diversity and natural resources, in India
nearabout, absolutely important plant species found in naturally grown
condition we have much and more resources in compare to other develop
and developing countries of the world, our scientist, technologist, do great
effort to implementation of technologies for this. Covid-19 is worldwide
pandemic disease caused by novel corona viruses, SARS-CoV-2 these is
effects humans’ respiratory system. In the world nearabout 10 million people
causing death up-to April 2021, and worldwide crisis for the socio-economy.
These is one of the challenges to treatment of pharmacological and
therapeutic plant medicines for this we should development our natural and
plant resource and our technology to the issue of forthcoming self-dependent
and implemented our techno friendly policy. Glycyrrhizin and Glycyrrhetinic
acid the bioactive constituents of licorice (Glycyrrhiza glabra) can induce
nitrous oxide synthetase which in turn blocks viral replication.
Various authors give good idea through the review about recent disease
susceptibility and their therapeutic drug discovery through the plants.
CADD- Computer-added drug design, RDD-Rational drug design, CAMD-
Computer assisted molecular modelling, SBDD-Structure Based Drug
Design MTDs-Multi Target Drugs, QSAR-Quantitative Structure Activity
Relationship LBDD-Ligand based Drug Design. Another example is that
deep learning methods will become a major computer, added drug design
discovery approach in the near future. A new paradigm in drug discovery of
the poly pharmacology, which is the process off in ding new uses for
existing approached drug which focuses on multi targets drugs (MTDs). To

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drug design approach many novel technologies and methodologies will be
develop to implement the drug discovery process and should effort drug
discovery related program those dependent on computational methodologies
these are future prediction and checked experimental results. Many advances
discussed above are supported by computational tools including data bases
such as genomic chemical spectral analysis data for a recent review on
natural product tools that enable the analysis of genetic information the
prediction of chemical structures and pharmacological activities.
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