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LECTURE 1 Pharmacognosy 2

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LECTURE 1 Pharmacognosy 2

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9s6fgyzyr6
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Pharmacognosy is defined as the study of crude drugs obtained from

plants, animals, & mineral and their constituent. It was derived from
the Greek word, “Gignosco” or “Gignoso”

 Simultaneous application of various scientific disciplines


with the object of acquiring knowledge of drug from every
point of view – Fluckiger
 An applied science that deals with the biologic, biochemical
and economic features of natural drugs and their constituents
– Tyler

1. C.A Seydler (1815) – coined the term from pharmakon and gnosis in
his doctoral thesis Analecta Pharmacognostica.
2. J. A Schmidt (1811) – first person to coined the term or use the
term on his book Lehrbuch der materia medica, which described the
study of medicinal plants and their properties.

HISTORY OF PHARMACOGNOSY

Ancient Podophyllum, Rhubarb, Ginseng, Stramonium. Cinnamon bark


China and Ephedra
Ancient Ebers Papyrus – a collection of 800 prescription and
Egypt mentioning 700 drugs.
Ayurveda – refers to traditional medicine of ancient
Ancient
India. Susrata Samhita - most important writing in
India
Ayurveda
1. Hippocrates – father of medicine and is famous for
his oath now administered doctors.
Ancient 2. Aristotle
Greece and 3. Theoprastus
Rome 4. Dioscorides – describe 600 medicinal plants in his
work, “De materia medica” of which some mention
plants are even used today.
5. Galen – described the method of preparing formula
containing plant and animal drugs.

Pharmakon – Drug
Gignosco or Gignoso – to acquire knowledge of Ayurveda (Ayur – life;
Veda – study )
Crr. Anotheus Seydler
Johann Adam Schmidt – failed to have copyright
Susrata Samhita

1. Pepper
2. Ricinus
3. Castor Oil
4. Valerian
5. Lily

De Materia Medica

1. Belladona
2. Ergot
3. Aloe
4. Hyoscyamus
5. Colchicum
6. Opium

Galen

 Father of Pharmaceutical compounding


 Galenicals (most famous: Cold cream)

Solubility – important factor to consider in extraction

PHARMACY IN ANCIENT BABYLONIANS


 Apothecary (drugstore)
 2600 BC priest, physician and pharmacist (all on one)
 GREEKS – HIPPOCRATES – “Father of Medicine” showed in writing and
practices the fundamental of scientific method of research.
PHARMACY IN ANCIENT CHINA
 Shen Nung (2000 BC) – “Father of Chinese Medicine”
o Pen Ts’ao Kang Mu 365 drugs (herbs, barks and roots)

PAPYRUS EBERS
 EGYPTIAN MEDICINE (300 BC) – George Ebers “Papyrus ebers” (1500
BC) 800 prescriptions, 700 drugs
 German Egyptologist and novelist, discovered the Egyptian medical
papyrus, of ca 1550 BCE
THEOPHRASTUS
 Father of Botany
 Dealing with medicinal qualities and peculiarities of herbs
DIOSCORIDES – MATERIA MEDICA
 Pedanios Dioscorides – recorded the observed promulgated
excellent rules in the collection of drugs, their storage and use
 Greek physician – pharmaco-botanist 78 A.D.
 Author of De Materia Medica – an organized pharmaceutical and
medical knowledge that gives information pertaining to about 600
drugs and their usage.
CLADIUS GALEN – DRUG COMPOUNDER
 Greek physician pharmacist
 Introduced the principles of preparing and compounding medicines
from plants and animals – Galenicals
 Originators – formula of cold cream
 Pharmaceutical preparation “Shotgun prescription”

PARACELSUS – GREAT ALCHEMIST


 Aureolus Phillipus Theoprastus Bombastus von Hohenheim
 Paracelsus – most important advocate of chemically prepared drugs
from crude plant and mineral substances
 Doctrine signature – God had placed the sign on healing
substances indicating their usage against disease
SCHEELE – GREATEST PHYTOCHEMIST
 Carl Wilhelm Scheele – Unicorn apothecary in Gothenburg
 Discovered oxygen, chlorine, prussic acid, tartaric acid,
tungsten, molybdenum, glycerin, nitroglycerin and other organic
compounds.
 Isolated citric acid from lemon juice

SERTURNER – FIRST OF THE ALKALOID CHEMISTS
 Friedrich Wilhelm Adam
Serturner – morphine
(alkaloids)
LEHRBUCH DER MATERIA MEDICA
 Written by Johann Adam Schmidt
(1759 – 1809)
ANALECTA PHARMACOGNOSTICA
 Pharmacognosy appears again in
1815 in a small work by Chr.
Aenostheus Seydler

PHARMACOGNOSY CAN BE DIVIDED INTO:

1. Medical Ethnobotany – the study


of the traditional use of plants for medicinal purposes
2. Ethnopharmacology – the study of the pharmacological qualities of
traditional medicinal substances
3. Phytotherapy – the medicinal use of plant extracts
4. Phytochemistry – the study of chemicals derived from plants

PHYTOCHEMISTRY
 The study of composition of plant principle, their extraction,
biosynthesis and identification
DEFINITION OF TERMS
Natural  Substances found in nature that comprises the
Substance plants or animal parts or secretions.
 Substances that are synthesized in the laboratory
by either of the two methods:  Total synthesis –
complete synthetic process

Example: Total synthesis of Camphor (Vinyl chloride +


Synthetic Cyclopentadiene)
substance
 Semi-synthetic – not entirely a synthetic process
but a chemical modification of a natural product

Example: Semi-synthesis of Camphor (modify a natural


camphor from camphor tree)
 Vegetable or animal drugs that consist of natural
substances that have undergone only the process of
collection and drying.
Crude drugs
 Crude – used in relation to natural products that
has not been in advanced in value or improved in
condition.
Derivatives  Product of extraction process which contains the
(extractives) chief constituent of the drug.
 A process of removing only those substances that
can be dissolved in the liquid or liquid mixture
referred to as solvent (menstruum).

1. Menstruum – liquid or solvent


2. Marc – undissolved portion of the extraction
Extraction
process
3. Extractive - - product of extraction (Solvent +
Dissolved substances)
4. Extract – substance remain after separating or
removing the menstruum from extractives.

 Growing in their native countries or specific


Indigenous plant
locality.
Naturalized  Grown in foreign land other than their native homes
plants or in different locality.

DRUG EXTRACTION PROCESS


 The general accepted method of obtaining the plant principle/s
SOLVENT/MENSTRUA (MENSTRUUM)
 A liquid/s that is employed in the extraction process to
remove/obtain the plant principle/s

GEOGRAPHIC SOURCE/HABITAT
 The region in which the plant or animal yielding the drug
grows
CULTIVATED PLANTS
 These are medicinal plants that have been propagated for many
centuries
DECOCTION
 Is a process of boiling vegetable substances with water to
extract the soluble principles
INFUSION
 Is a process in which vegetable drugs are extracted of their
water-soluble constituents by steeping or drenching them in
water
DIGESTION
 Is a form of maceration in which gentle heat (40-60oC) is
applied to the drug menstruum mixture and maintained
throughout the extraction to increase the solvent powers of
the menstruum

Natural products
 They are chemical compound or substances produced by a living
organism that originate from nature and have pharmacological
and biological activity.
 Natural products are produced as metabolites that are
intermediates or end products in the pathways of primary and
secondary metabolism. Natural Products may include the whole
organism (plant, organism) part of an organism an extract or
crude exudates of an organism isolated pure compound.

Natural products can be divided into broad categories namely:


(i) Microbial: e.g. Cephalosporins – Cephalosporium acremonium.
(ii) Plants: e.g. Paclitaxel – Taxus brevifolia
(iii) Marine: e.g. Discodermolide – Discodermia dissoluta
(iv) Animal: e.g. Epibatidine – African clawed frog.

1. Natural Products from Microbes


 Exploitation of microbes as source of drug candidates began in
earnest after the discovery of Penicillin from the fungus,
Penicillium notatum. Potentially active compounds or drugs
have been discovered such as the macrolide erythromycin from
Saccharopolyspora erythraea is an antibacterial drug that has
broad spectrum activities against gram-positive cocci and
bacilli and is used for mild to moderate, upper and lower
respiratory tract infections. Cephalosporins from
Cephalosporium acremonium is an antibacterial agents.

2. Marine Natural Products


 The first active compounds to be isolated from marine species
were spongouridine and spongothymidine from Carribean sponge
Cryptotheca crypta in 1950s. These compounds are nucleotides
with potent anticancer and antiviral activities.
 Another example is an anti-tumor compound called
discodermolide isolated from marine sponge Discodermia
dissoluta. It has similar activity as Paclitaxol® but with
better water solubility. A combination therapy of the two
drugs is effective in reduction of certain tumor growths.

3. Natural Products from Animal Source


 venoms and toxins from snakes, spiders, scorpions, and insects
are extremely potent because they often have very specific
interactions with a macromolecular target in the body.
 Animals have yielded new natural chemical entities. For
example, a series of antibiotic peptides was extracted from
the skin of the African clawed frog. Epibatidine obtained from
the skin of an Ecuadorian poison frog is ten times more potent
than morphine. Teprotide (pry-trp-pro-arg-glu-ile-pro-pro),
extracted from Brazilian viper, has led to the development of
cilazapril and captopril, which are effective against
hypertension. Cod-liver oil from fresh liver of Gadus morhua
used as oil, or source of vitamins, honey from Apis mellifera
used respiratory problems.

4. Plant Natural Products


During the 19th century a range of drugs was isolated:
 1805 morphine- class of drugs called opiods
(poppy plants Papaver somniferum)
 1817 emetine- alkaloid (Psychotria ipecacuanha)
 1819 strychnine alkaloid (Strychnos nux-vomica
Linn) pesticide
 1820 quinine alkaloids cinchona officinalis
21first century
 ACTM Artemisia annua
Natural products of plant origin used for medicinal purposes are
also called herbal medicines.
Herbal medicine is defined as, use of herbs, herbal materials,
herbal preparations and finished herbal products to treat and manage
diseases. Herbal medicine has been employed by man for centuries as a
remedy for various diseases and is thought to be due to the history of
qualified success, reasonable science, its affordability, its
accessibility and long-standing cultural and spiritual values.
Example of herbal plant with medicinal use include;
1. Thymus serphyllum is commonly used locally for various
purposes such as antiseptic, anti-helminthic, carminative
(flatulence relieve) and expectorant.
2. Crossopteryx febrifuga Benth (family Rubiaceae) preparations
have been used traditionally for treating septic wounds,
respiratory infections, fever, dysentery, pain and malaria.
3. Morphine, from opium poppy (Papaver somniferum), used as an
analgesic.
4. Digoxin and other digitalis glycosides, fromfoxglove
(Digitalis spp.), used to treat heartfailure.
5. Taxol, from the Pacific yew (Taxus brevifolia),
6. vincristine (catharanthus rosea) used as an anticancer
treatment and
7. quinine, from Cinchona bark (Cinchona spp.),used in the
treatment of malaria.

Traditional system of medicine can be classified into three:

1. Traditional scholarly medical systems: have documented knowledge,


pharmacopoeias for doctors and institutions for training doctors
2. Traditional medical knowledge (Folk medicine): orally transmitted
and associated with households, communities and ethnic groups.
3. Shamanistic medicine: have strong spiritual element and is applied
by special practitioners.

Uses of natural products


1. Sold as health foods and food supplements
 Example are:
 Stevia derived from Stevia rebaudiana is 30 times sweeter than
sugar. Since the active ingredient possesses zero calories,
this plant may be useful for people with diabetes,
hypoglycemia.
 Xylitol is also used as a diabetic sweetener and is seen as
beneficial for dental health by reducing caries to a third in
regular use.
 Green, black, and white teas are all derived from Camellia
sinensis, an evergreen shrub of the Theaceae family.
2. Spices are used for flavoring and for preserving foods,
particularly meat products. They also possess antimicrobial
properties.
 Common spices include:
 Cinnamon
 Pepper
 cloves
 nutmeg
 cumin
 ginger

3. Pharmaceutical medicine: Natural products and their derivatives


are an invaluable source not only of lead compounds( a chemical
compound that shows promise as a treatment for a diseases and
may lead to the development of new drug) for pharmaceutical
development but also therapeutic agents themselves.
 Example: morphine from opium poppies (Papaver somniferum) still
provides an important source of opiate analgesics and a starting
material forcodeine synthesis.

4. Cosmetic preparation; there is high demand in use of natural


products as ingredients in cosmetics or use of natural cosmetics
example Aloe vera, roses( rose oil are rich in vitamin C),
lavender, jojoba, chamoline, tea tree, egg oil, avocado, coconut
oil, emu oil, honey, beeswax, rose mary and basil.
5. Production of biofuels as alternative and renewable energy
sources e. g biodiesel derived from vegetable oil (castor oil,
jatropa, palm oil, peanut, soyabean and cotton) and animal fats
(bovine fat and swine fat).

6. Source of income: trade in medicinal plants is a huge. Roughly


half of all approved prescription drugs are natural products,
mostly from plants and microbial sources, their semi-synthetic
derivatives or fully synthetic analogs. Natural products from
both plants and animals are used as fibers, chemicals,
insecticides, fibers and dyes.

Why pharmacognosy
o For the purposes of drug discovery and understanding how dietary
supplements work.
o The development and use of analytical methods for quality control
of natural products in the market place.
o The study of the use of traditional remedies by native cultures.
o The microscopic evaluation and species verification of medicinal
or economically important natural products.
o The use of natural products for specific agricultural purposes,
such as natural pesticides or insect antifeedants.
o Assessing safety and functional properties of compounds found in
novel foods or food ingredients and consumer products.
o The cosmetic application of natural compounds or extracts.
o The study and manipulation of genetic biosynthetic pathways for
the purpose of enhancing the production of natural compounds, or
producing novel compounds.

SCOPE OF PHARMACOGNOSY

1. Medicine
2. Bulk Drugs
3. Food Supplement
4. Pharmaceutical necessities
5. Pesticides
6. Tissue culture biotechnology 7. Engineering

“Simultaneous application of various disciplines with the object of


acquiring knowledge of drugs from every point of view.” – Friedrich
August Fluckiger

CLASSIFICATION OF CRUDE DRUGS

ORGANIZED DRUGS

 Consist of cellular organization in the form of anatomical


features and consist mostly of crude drugs from plant sources.
 Mostly from plant sources
 Example are:
o Cinchona bark
o Sandal wood, Quassia wood
o Senna leaves, Digitalis leaves
o Rauvolfia roots, etc

UNORGANIZED DRUGS

 do not have morphological or anatomical organization as such and


comes directly in the market but their ultimate source remains,
plant, animals or minerals.
 Plant, mineral and animal sources - Examples are:
 Beeswax from Honeycomb of bees
 spermacetti from head cavities of whale
 Plant Exudates such as Gums (Xanthan Gum, tragacanth)
 Plant latex ( opium)

ALPHABETICAL
 Simpliest method; arranged in alphabetical order; employed in
dictionaries, pharmacopoeias, monographs and reference books;
uses Latin, English and Vernacular/Local; Easy and quick to use.
 No repetition of entries
  Avoid confusion
  Location and tracing is easy

 No relationship/correlation among plants.


TAXONOMIC

 Arranged by Kingdoms; based on phylogeny (Natural relationship of


plants among other organism)
 Helpful for studying evolutionary development
 No relationship/correlation among plants*
 Crude drugs are grouped based on the natural relationship or
phylogeny

 Umbellifereae Family – includes cremocard fruits (anise,


fennel, caraway)

 Solanaceae Family – includes plants yielding capsule/berry-


like fruits(belladonna, hyocyamus, stramonium)

 Labiateae Family – include drugs possessing square stems,


opposite leaves (peppermint, spearmint, thyme)

MORPHOLOGICAL

 Crude drugs are grouped according to the part of the plant or


animal represented; such as roots, leaves, organs, glands

 Arranged by morphology or external characteristics of plants;


answers the question “Which part of the plant was used?”
 Helpful in identifying and detecting adulteration
 Convenient for practical study especially if the chemical
structure isn’t understood
 No correlation of chemical constituent with therapeutic action
 Repetition of plants

PHARMACOLOGICAL/THERAPEUTIC

 According to pharmacological/therapeutic effect; most relevant


classification and follow method
 Used for suggesting substitute if drug isn’t available
 Plants with different actions are classified separately in
multiple groups
 Example: Cinchona bark both have antimalarial and antiarrhythmic
effect
 Crude drugs are grouped based on the similarity of therapeutic
effects, regardless of morphology, taxonomy or chemical relation.
Examples are:
 Cascara sagrada, Senna, Podophyllum, Castor oil – affect the
intestinal tract
 Digitalis, Strophantus, Squill – affect the cardiac muscle

PLANT NOMENCLATURE AND TAXONOMY

OLD FAMILY NAME NEW FAMILY NAME

Graminae Poaceae

Palmae Arecaceae

Cruciferae Brassicaceae

Leguminosae Fabaceae

Umbilliferae Apiaceae

Labiatae Lamiaceae

Compositae Asteraceae

Guttiferae Clusiaceae

CHEMICAL/BIOGENETIC

 Depends upon the most important constituent arranged by


carbohydrates, proteins, tannins, saponins etc
 Popular for phytochemical students
 Ambiguous arise when particular drugs possess a lot of
constituents ( must choose the most abundant one as main
classification)

PREPARATION OF CRUDE DRUGS FOR COMMERCIAL MARKET

1. COLLECTION

 Most important step next to Cultivation


 Always ensures a true natural sources & reliable product.
 Drugs should be collected when they contain maximum amount of
constituents in highly scientific manner.
 The most advantageous time for collection is the time when
 The part of the plant constitutes the drug is highest in its
content of active content of active principles
 When the plant material will dry to give the maximum
quantity and appearance
Factors that affects the amount of Constituent present:
1. Season
 Example: Rhubarbs – Best harvested during summer because during
winter, it doesn’t contain anthraquinine(active form; cathartic)
instead, it contains anthranol (inactive form)
2. Age of plant – amount and proportion of constituent are affected
 Example: Young peppermint has pulegone while matured peppermint
has menthol and menthone
3. Time (Day/Night)
 Example: Contained secondary metabolites vary from day and night
due to the plant’s transpiration and expiration. Plants release more
water during the day and release less amount of water during the night
 In general: Leaves are best harvested before flowering season or
when the photosynthesis is active or as the flowers are beginning to
open or when fully expanded. Flowers before it blooms/pollination
process or before they are fully expanded. Underground plants
( rhizomes) when its aerial part dies( after the vegetation process
have ceased) such as carrots, onions and gingers. Roots after the
vegetation process has begun
 Some fruits are collected after full maturity or right after
ripening . Seeds when mature ad fully ripened fruits.
 Most barks are collected at spring season
 Most ideal time in collection of Active constituents is when the
desired constituent is at its highest or the time that could give its
maximum quality.

2. HARVESTING
 Important operation in cultivation technology and the important
point in this process is the type of drug to be harvested
 The mode of harvesting varies with each drug produced and with
the pharmaceutic requirements of each drug
 Manual vs Mechanical labor
 By hand labor – requires “skillful” selection of plant parts
 With the use of mechanical devices
3. DRYING

 Consist of removal of sufficient moisture content of crude drugs,


so as to improve its quality and make it resistant to the growth
of microorganisms.
  Benefits:
1. a) Inhibits partially enzymatic reactions
2. b) Facilitates pulverizing or grinding of crude drugs.
  Types of Drying
1. Natural Drying (Sun Drying)
2. Direct Sun Drying – Contents are stable to high temperature
and sunlight.
3. Shed – Preferred if natural color and volatile principles of
drugs are to be retained
4. Artificial Drying
5. Tray dryers – Suitable for drugs which do not contain
volatile oils and are quite stable to heat or which needs
deactivation of enzymes are dried in this method. Examples:
Belladonna roots, Cinchona bark, Tea and Raspberry leaves,
Gums
6. Vacuum dryers – Suitable for drugs which are sensitive to
higher temperature. Examples: Tannic acid and Digitalis
leaves
7. Spray dryers – Suitable for highly sensitive drugs to
atmospheric conditions and also to temperature of vacuum
drying. Examples: Papaya latex, Pectin and tannins
 Its purpose are
1. Removal of sufficient moisture, to ensure good keeping
qualities
2. To prevent mold growth, enzymatic action; bacterial action,
chemical or other possible changes
3. “Fixes” the constituents
4. Facilitates grinding and milling
5. Converts the drug into a more convenient form for commercial
handling

4. CURING

 special drying process that enhances the properties of the plants


active ingredients
 Examples:
1. a) Vanilla via Sweating Process
2. b) Cascara Sagrada (Cathartic) via maceration with
Magnesium Oxide for 1 year to reduce its active components
into its reduced forms since it’s less irritating

5. GARBLING ( Final step in preparation)

 Consist of removal of foreign organic matter (extraneous matter)


such as other plant parts, dirt, and added adulterants.
 Why remove adulterans? To provide quality .
 This step is carried:
 After the drug has been dried
 Before the drug is labeled or packaged

6. PACKAGING, STORAGE AND PREPARATION


 PACKAGING of drugs depends on their final deposition. It is
customary to choose the type of packaging that provides ample
protection to the drugs and gives economy of space.
 PROPER STORAGE AND PRESERVATION are of important factors in
maintaining a high degree of quality of the drugs.
 All drugs should be preserved in a well-closed and filled
containers, stored in the premises which are water-proof, fire-
proof, and rodent proof. Drugs must also be protected from
insects and molds attacks.
 Factors to be considered:
o For destruction/prevention of insect-contamination: insect
attacks prevention
 Exposure of the drug to a temperature of 65 celsius or
drying the drug thoroughly
 Fumigation of large lots of crude drugs with methyl
bromide, carbon disulfide, hydrocyanic acid
 Addition of few drops of CHCL3 , and CCl4
 For storage, the ideal temperature is just above freezing. The
warehouse or other place of storage should be as cool as possible
(2-8 Celsius)

EVALUATION OF CRUDE DRUGS

 ensures the identity of a drug and determines the quality and


purity of drugs.

1. Organoleptic Evaluation
 refers to the method of analysis like color, odor, taste, size,
shape, and special features  A study that uses organs or senses

2. Microscopic Evaluation
 Identification of small fragments of crude or powdered herbs and
detection of adulterants, as well as identification of plant by
characteristics tissue features

3. Chemical Evaluation
 includes qualitative and quantitative chemical tests, chemical
assays, and instrumental analysis  Titration is applied
 Qualitative: Identification tests for various phytochemicals present
 Quantitative: Acid value,saponification,ester value

4. Physical Evaluation
 often used to determine the physical property of the crude drugs

Solubility,Specificgravity,Opticalrotation,viscosity,refractiveindex,M
Pandwatercontent 5. Biological Evaluation
 plant or extract can be evaluated by various biological methods to
determine pharmacological activity, potency, and toxicity.
 Uses in vivo(using animals)and vitro(using membranes)studies
ASSAY ON LIVING ANIMALS
 Bacteria such as Salmonella typhosa and Micrococcos pyrogenes,
are a means of determining the phenol coefficient or
antiseptic value of certain drugs
 Rats or Mice
o Rat – line test is employed for the assay of vitamin D
preparation, etc.
o Mice – test animal in the safety test for Rabies vaccine
 Guinea pigs
o They are used to test the toxicity and antigenicity of
biological products such as Diphteria toxin and Tetanus
toxoid.
o They are also employed to determine oxytoxic activity of
Vasopressin injection and similar compounds
 Pigeons – utilized in the assay of Digitalis
 Cats – used in drugs with depressor activity, assay of
Glucagon for injection, mydriatic drugs such as atropine
 Rabbits – used in determining the presence of pyrogens in
parenteral solution of the antibiotic, and testing of
ophthalmic preparations
 Dogs – are utilized in assaying Veratrum viride preparation
HUMANS
 Valuable as a means of noting the activity of drugs

BIOASSAY
Glucagon Cat
Atropine Cat
Oxytocin Chicken
Parathyroid hormone Dog
Insulin Rabbit
Tubocurarine Rabbit
Digoxin Pigeon

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