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Phytochemistry and Pharmacological Properties of Lychee Litchi Chinensis Sonn

The document summarizes the phytochemistry and pharmacological properties of Lychee (Litchi chinensis Sonn). It discusses the nutritional composition, phytochemicals identified from different parts of lychee including flavonoids, glycosides, amino acids, phenolic compounds and others. It also summarizes the various pharmacological activities exhibited by lychee such as anti-oxidant, anti-cancer, anti-platelet, anti-microbial, anti-pyretic, anti-inflammatory, anti-viral, anti-hyperlipidemic and anti-mutagenic properties.

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0% found this document useful (0 votes)
39 views14 pages

Phytochemistry and Pharmacological Properties of Lychee Litchi Chinensis Sonn

The document summarizes the phytochemistry and pharmacological properties of Lychee (Litchi chinensis Sonn). It discusses the nutritional composition, phytochemicals identified from different parts of lychee including flavonoids, glycosides, amino acids, phenolic compounds and others. It also summarizes the various pharmacological activities exhibited by lychee such as anti-oxidant, anti-cancer, anti-platelet, anti-microbial, anti-pyretic, anti-inflammatory, anti-viral, anti-hyperlipidemic and anti-mutagenic properties.

Uploaded by

Niharika Singh
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© © All Rights Reserved
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com

Journal of Chemical and Pharmaceutical Research, 2016, 8(10):35-48

ISSN : 0975-7384
Review Article
CODEN(USA) : JCPRC5

Phytochemistry and Pharmacological Properties of Lychee (Litchi chinensis


Sonn)
Pooja Taak and Bhupendra Koul*
School of Bioengineering and Biosciences, Lovely Professional University, Jalandhar-Delhi, India

___________________________________________________________________________________

ABSTRACT

Fruits plants are a reservoir of nutrients and natural drugs. At present, researchers recommend the consumption of
fresh fruits to enhance immunity, mental health and physical health. Lychee (Litchi chinensis Sonn.) is one of the
admired genus of the soapberry family (Sapindaceae) which includes 150 genera and 2,000 species. It is one of the
important commercial fruit crop with several pharmaceutical properties. The pericarp, pulp, seeds, fruits, flowers
and leaves are a source of bioactive constituents such as procyanidin A2, procyanidin B2, leucocyanidin,
isolariciresinol, stigmasterol, epicatechin, saponins, rutin etc. The aim of the present review is to summarize the
pharmacological activities represented by the aforementioned bioactive ingredients. Meticulous pharmacological
and phytochemical studies on lychee could yield reliable compounds of pharmacological significance for better
healthcare.

Keywords: Lychee; Anti-oxidant; Pharmacological activities; Fruit crop


___________________________________________________________________________________

INTRODUCTION

Polyphenolic compounds are a rich source of food supplements for better health care [1]. Various medicinal systems
of the world including ‘Ayurveda’ has clearly mentioned the scope of medicinal plants as a cure of various diseases
and to boost the immunity. There are several plant-derived elite drugs which are to be evaluated scientifically for
their mode of action, efficacy and side-effects. If the medicinal plant is a fruit plant, then its demand rises several
folds. Lychee is one among the important fruit plants which possess several bioactive compounds exhibiting
pharmacological activities.

Taxonomical position
Kingdom: Plantae
Order: Sapindales
Family: Sapindaceae
Subfamily: Sapindoideae
Genus: Litchi
Species: chinensis

It is an evergreen plant with a short stout trunk and attains a height upto 30 m. In some varieties, the branches are
twisting and spreading forming a crown like appearance, while some have straight and upright branches forming a
compact and rounded crown. Leaves are alternate and compound with 2-5 leaflets. The flowers are small, yellowish-
white, functionally male or female and apetalous. Fruits are highly variable and depend upon the variety. They can
be ovoid, round and heart shaped. Lychee is native to Guangdong and Fujian regions of China and are an important
commercial fruit crop of many parts of the world. At present, lychee is cultivated as commercial fruit crop in Central

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Pooja Taak and Bhupendra Koul J. Chem. Pharm. Res., 2016, 8(10):35-48
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and South America, some parts of Africa and throughout Asia. China, India, South Africa, Australia, Mauritius,
Madagascar, Thailand are now the major lychee producing countries of the world. India is the second largest
producer of Lychee in the world, after China. The Table 1 enlists the lychee cultivars grown in different countries of
the world. The pharmacological properties of lychee include anti-cancer, anti-platelet, anti-microbial, anti-pyretic,
anti-oxidant, hepato-protective, anti-inflammatory, anti-viral, anti-hyperlipidemic, anti-mutagenic etc. [2-13]. This
review provides explicit information to researchers about the structures of active ingredients of lychee as well as the
pharmacological properties exhibited by them.

Table 1: Major lychee cultivars grown in different countries

Country Cultivars

Kwai May Pink, Tai So, Souey Tung, Fay Zee Siu, Salathiel, Wai
Australia
Chee
Bangladesh Bombai, Muzaffarpur, Bedana, China 3
Brazil Bengal
Early: Sanyuehong, Baitangying

China Mid: Dazao, Heiye, Baila, Feizixiao and Shuidong, Tianyan, Chenzi
Late: Xiangli, Guiwei, Noumici, Huaizhi, Xuehuaizi, Lanzhu,
Bobaitangbo, Yuanhong, Xiafanzhi, Nanmuye
Florida, USA Mauritius and Brewster
Bihar/Jharkhand: Deshi, Purbi, China, Kasba, Bedana, Early Bedana,
Late Bedana, Dehra Rose, Shahi, Manragi, Maclean, Longia, Kaselia
and SwarnaRupa, Ajhauli, Green, Mandraji, Rose Scented
Uttar Pradesh/Uttrakhand/Himachal Pradesh: Early Large Red, Early
Bedana, Late Large Red, Rose Scented, Late Bedana, Calcuttia, Extra
Early, Gulabi, Pickling, Khatti, Dehra Dun, Piyazi
India
West Bengal/Assam:Bombai, Ellaichi Early, China, Deshi, Purbi and
Kasba, Kalyani Selection
Haryana/Punjab: Early Seedless, Late Seedless, Seedless-1 and
Seedless-2, Calcuttia, Muzaffarpur
Chhattisgarh: Sarguja-1, Sarguja-2
Indonesia Local Selections
Israel Mauritius, Floridian
Madagascar Mauritius
Nepal Mujafpuri, Raja Saheb, Dehradun, Calcuttia, China
Philippines Sinco, Tai So, Ulpb Red
South Africa Mauritius, Mclean Red
Thailand Tai So, Chacapat, Wai Chee, Haak Yip, Khom
Vietnam Thieuthauhha
Country Cultivars

Nutritional composition
Lychee fruit is described as a large seeded drupe, with semi-transparent aril (flesh) which is edible and thin corky
pericarp (skin). The fruits are consumed fresh. Moreover, many products like squash, canned lychee, syrup, cordial,
jam, jelly, juice etc. are also available in market. It can be used as dried or dehydrated (lychee nuts) or used in
sorbets and ice-creams [14, 15]. On the basis of variety and climate the fruit contains 60% juice, 8% rag, 19% seed
and 13% skin. Apart from proteins, fats, carbohydrates, minerals, fibrous matter, calcium, phosphorus, iron and
carotene the fruit is also rich in vitamin B1, riboflavin and vitamin C. Lychees have low content of sodium and
saturated fat.

Phytochemistry
Nowadays, HPLC (High performance liquid chromatography) and HPTLC (High performance thin layer
chromatography) has become regular analytical techniques due to their efficiency in quantitation of analytes at

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Pooja Taak and Bhupendra Koul J. Chem. Pharm. Res., 2016, 8(10):35-48
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micro or even nanogram levels and cost effectiveness. Leaf, root, seed, fruit and pericarp extracts of various lychee
have been subjected to HPLC and HPTLC followed by pharmacological analyses. The review of literature reveals a
total of fifty bioactive compounds reported from different parts of the lychee plants (Table 2). These compounds
have been categorized as flavonoids, glycosides, amino acid, phenolic compounds, fatty acids, phenolic aldehyde,
monoterpenes and anthocyanins.

Pharmacological properties
Various biologically active constituents are present in different parts of lychee (leaves, flower, fruit, pericarp, seed).
These compounds are reported to exhibit several pharmacological activities (Figure1).

Leaves
Anti-oxidant activity: The antioxidant potential of organic and aqueous extracts of leaves of the plant was
investigated by using ABTS (2,2’-azinobis 3-ethylbenzothiazoline-6-sulpohonic acid), FRAP (ferric reducing
antioxidant power), DPPH (2.2’-diphenyl-1-picrylhydrazil), TPC (total phenolic content) and the total antioxidant
activity assays. 1-butanol, Methanol, aqueous, and ethyl acetate extract of leaves exhibit strong peroxyl radical
scavenging activity, thus showing its strong anti-oxidant potential [30].

Analgesic and anti-inflammatory activity: Analgesic and anti-inflammatory activity of hydro-alcohol extract of
leaves was evaluated by using acetic acid-induced writhing test, hot plate method in mice and carrageenan-induced
paw edema model in rats respectively. Oral administration of the extract exhibited a strong anti-inflammatory
activity and after 4 hours of administration maximum effect was observed [31].

Hepatoprotective activity: The protective effect of lychee leaf extract on paracetamol-induced liver damage was
demonstrated by observing the effect of extract on various serum biochemical parameters including SGPT (serum
glutamate-pyruvate transaminase), SALP (serum alkaline phosphatase), SGOT (serum glutamate-oxaloacetate
transaminase) and liver biochemical parameters [32].

Flower
Anti-oxidant activity: Acetone extract of lychee flowers exhibited strong DPPH radical scavenging activity and
also inhibit the oxidation of LDL (low density lipoprotein) thus representing their significant anti-oxidant potential.
This was the first attempt to evaluate the anti-oxidant potential of lychee flower [33].

Cardiovascular activity: Aqueous extract of lychee flower is a source of flavonoids, phenols and tannins. Flower
extract elevate the TEAC (trolox equivalent antioxidant capacity) of the serum and thus decreases the peroxidation
of serum lipid in high cholesterol male hamsters. In this way lychee flower extract represents significant
cardiovascular activity [34].

Cyto-toxicity: Cyotoxic effect of acetone extract of lychee flower was evaluated by using lead and cadmium
induced hepatoxicity and TGF-b1 (transforming growth factor b1) mediated activation of hepatic cells. Acetone
extract decreases the peroxidation and lipids and fragmentation of DNA and thus exhibited a significant cytotoxic
activity [35].

Anti-lipase activity: Number of phytochemicals which includes flavonoids, tannins, anthocyanins and
proanthocyanins were reported in aqueous extract of lychee flower. Hypercaloric diet-induced rats were used to
investigate the anti-lipase activity and it was reported that aqueous extract successfully reduced the size of liver,
epididymal and adipose tissues of rat model hence show good anti-lipase activity [36].

Pericarp
Anti-oxidant activity: The antioxidant potential of lychee skin is well defined [12, 13]. Lychee skin contains many
active constituents which represents free radical scavenging activity these are glutathione, ascorbic acid,
polysaccharides, carotenoids [17, 18] flavonoids (flavonols and anthocyanins) and phenolic acids [37]. It has been
reported that procyanidin B2, epicatechin, epigallocatechin and procyanidin B4 are the chief flavonoids in fruit skin
[23]. Two flavonoids that are anthocyanins and procyanidins are the major compounds which contribute maximum
to antioxidant activity [23]. Different types of flavonoids also differ in their antioxidant potential [38]. It has also
been reported that skin of immature fruit has a much stronger antioxidant potential as compare to mature fruit [17].

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Anti-cancer activity: Lychee pericarp is rich source of insoluble fiber (40% dry weight), which inhibit rectum
cancer, diabetes and hemorrhoids [2]. Aqueous extract of lychee skin significantly inhibited the growth of cancer
cells (human hepatoma cells) in vitro and suppressed the development of cancer cells in mice with liver cancer [3].

Table 2: Bioactive compounds reported in lychee

S.
Name of compound Structure Property Reference(s)
No.
Flavonoids

Growth and repair


1 Ascorbic acid of tissues in all
parts of the body

Anti-bacterial;
2 Citric acid anti-fungal; anti-
oxidant

3 Isobutyl acetate Anti-bacterial

[16-19]

4 Isovaleric acid Anti-bacterial

Anti-microbial
5 Guaiacol
activity

Anti-tyrosinase;
6 2-phenyl ethanol
anti-microbial

Anti-oxidant, free
radical
scavenging
7 Epicatechin activity, reduce
blood sugar level,
anti-diabetic, anti-
cancer
[16,19, 20-
26,]

Anti-oxidant
8 Procyanidin B2 activity; prevents
malignancies

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Chemoprevention
9 Epigallocatechin and anti-cancer
activities

Possess anti-
oxidant activity;
inhibition of
proliferation and
induction of
10 Procyanidin B4
apoptosis in
cancer cells
through up and
down-regulation
of multiple genes

Prevents
hyperglycemia
11 Procyanidin A2
and type 2
diabetes

Protects the
12 Leucocyanidin
stomach lining

Free-radical
13 Cyanidin-3-O-glu scavenging
activity

Free-radical
scavenging and
14 Cyanidin-3-O-rut anti-platelet
aggregating
activity

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Malvidin-3-acetyl-O- Anti-oxidant
15
gluoenin properties

(2S)-pinocembrin-7-O-(6′′-
Anti-diabetic
16 O-α-L-arabinosyl-β-D-
property
glucopyranoside

17 Quercetin Supports normal


respiratory health;
supports
cardiovascular
health; promotes
balanced blood
pressure; offers
protection against
stress; offers
nutritional
support for
18 Quercetin 3-O-glucoside overall health

Anti-oxidant;
19 Phlorhizin
anti-diabetic

Anti-oxidant
activity; used to
treat cerebral
ischemia,
20 Pinocembrin-7-O-glucoside neurodegenerative
diseases,
cardiovascular
diseases and
atherosclerosis

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Pooja Taak and Bhupendra Koul J. Chem. Pharm. Res., 2016, 8(10):35-48
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Pinocembrin-7-O-[(6′′-O-β-
21 Dglucopyranoside)-β-D-
glucopyranoside

Pinocembrin-7-O-[(2′′,6′′-di-
22 O-α-L-rhamnopyranosyl)-β-
D-glucopyranoside

23 Kaempferol

Kaempferol-7-O-β-D-
24
glucopyranoside

OH Anti-oxidant;
anti-cancer
HO O

25 Kaempferol 3-O-rutinoside O

OH O O OH
O

OH
HO
OH
OH OH OH

OH

HO O

26 Kaempferol 3-O-glucoside
OH

O O
OH
HO
OH O
OH

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Anti-oxidant;
27 Onychin
anti-cancer

28 Nairutin Anti-oxidant

29 Peonidin 3-O-rutinoside Anti-oxidant

Narcissin (Isorhamnetin-3-O-
30 Anti-oxidant
rutinoside)

31 Catechin Anti-oxidant

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Pooja Taak and Bhupendra Koul J. Chem. Pharm. Res., 2016, 8(10):35-48
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OH

Anti-oxidant;
helps the body to
HO O
OH utilize vitamin c
OH and produce
HO
collagen; heals
32 Rutin O O OH conditions such as
OH O
O
haemorrhoids and
high blood
pressure and
H3C O
reduces
HO cholesterol levels
HO
OH

Fatty acids

O
Blood lipid
33 Palmitic acid
reducing activity
OH

Anti-oxidant;
34 Linoleic acid
anti-carcinogenic

Anti-cancer; anti-
35 Dihydrosterculic acid
tumor

8-methylenehexadecanoic
36 Anti-bacterial
acid

[21, 27]
Cis-5,6-
37 Anti-bacterial
methylenetetradecanoic acid

Cis-3,4-
38 Anti-bacterial
methylenedodecanoic acid

A major
metabolite of anti-
oxidant
39 Protocatechuic acid
polyphenols,
possess anti-
cancer property

Glycoside

Cholesterol
reduction, anti-
oxidant, reduce
40 Saponin cancer risk, [10, 12, 28]
immunity booster,
reduce bone loss,
anti-oxidant

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Amino acid

Possesses
α-
41 hypoglycaemic
methylenecyclopropylglycine
activity

It is capable of
preventing
SH damage to [29]
O important cellular
components
H
-
OOC N COO- caused by reactive
42 Glutathione
oxygen species
N such as free
H
radicals,
NH3 O peroxides, lipid
peroxides and
heavy metals.
Anthocyanin

Anti-oxidant;
43 Cyanidin glycoside [22]
anti-ageing

Phenolic acid

44 Trans-cinnamic acid

Anti-tumor; anti-
45 Gallic acid oxidant; anti-
inflammatory

Anti-oxidant;
blood pressure
46 Chlorogenic acid
lowering effect;
laxative effect

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Anti-oxidant;anti-
hypertension;
Caffeic acid (3,4- anti-
47
dihydroxycinnamic acid) thrombosis;anti-
fibrosis, anti-virus
and anti-tumor

Phenolic aldehyde

O H

Anti-oxidant;
48 Vanillin
Anti-bacterial
CH3
O

OH

Monoterpene

Anti-
49 Cis-rose oxide
inflammatory

Anti-oxidant;
50 Geraniol anti-cancer
properties

In both cases, the anticancer potential of the extract was depended on dose and time. Lychee skin extract effectively
suppress the growth of breast cancer cells [39]. A report indicated that two flavonoids epicatechin and procynidin
B2are highly effective in inhibiting the growth of human breast cancer cells and human lung fibroblast, although
their toxicity to cancer cells was lower than that of paclitaxel (standard anti-cancer drug) [40].

Seed
Dried lychee seed is characterized by traditional Chinese medicine as slightly bitter, warming, cold-driving, pain-
killing, Qi flow promoting and liver- and kidney-tonifying [41]. There is ample information on the health promoting
and medical functions of lychee seed, including antioxidant, anti-cancer, anti-virus, controlling diabetes, and
reducing blood lips.

Anti-oxidant activity: As mentioned above, lychee seed contains flavonoids, which contribute to the antioxidant
activity of the seed. Ethanol and Water extracts of the seed has been reported to reduce the damage caused by free
radicals and promote SOD (superoxide dismutase) activity in ALX (alloxanmo mohydrate) treated mice [42].

Anti-cancer activity: Water extract of the seed significantly suppress the growth of hepatoma tumor cells in mice
[43]. Seed extract of lychee prevents the formation of telomere in hepatoma cells which ultimately stops the division
of cancer cells, which leads to the inhibition of cancer cell growth [44].

Reduces blood sugar and lipid: There are several reports available about the effects of Lychee seed in reducing
blood sugars and lipids and in promoting the function of liver [12, 42, 45, 46].The water extracts of lychee seeds
successfully reduced blood sugar level in ALX induced diabetic rats and that effect was similar to that of
“biguanides” that is anti-diabetic drug, and it was found that the effect of lychee seed extract was long lasted than

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Pooja Taak and Bhupendra Koul J. Chem. Pharm. Res., 2016, 8(10):35-48
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(more than 1 week)biguanides[46]. Seed extract reduced the sugar level in blood because it suppresses the uptake of
glucose by blood capillary but promote glucose uptake in ambient tissues [42]. Guo et al. 2003 also found that
lychee seed extract alleviated sugar metabolism disorder and improved sensitivity to insulin in rat suffering from
insulin resistant Type 2 diabetes (T2DM) induced by streptomycin, and therefore reduced blood sugar [12].Some
authors suggested that α-methylenecyclopropylglycine in lychee seed was the most effective to reduce the level of
blood sugar and glucogen in liver in ALX treated mice[29] while others suggested that anti-diabetes activity was
related to saponins [12, 28].

Figure 1: Pharmacological properties of Litchi chinensis

Anti-virus activity: There are many reports about the anti-virus effects of lychee seed extracts, which were effective
against hepatitis B virus [5-10] respiratory syncytial virus (RSV) [25], influenza virus [24] and SARS coronavirus
[26]. Zheng and Zheng 1992 found that seed extract was the second most effective to control hepatitis B among
1000 tested herbal medicines [5]. It has also been reported that lychee seed extract directly inhibit the expression of
HbsAg (antigen) and HBV-DNA (Hepatitis B virus) [7]. Xu et al. 2004, examined 6 extraction fractions of the seed,
all of them strongly inhibit the expression of HBsAg and HbeAg in Hep G 2.2.15 cell line [8]. Most authors
suggested that anti-virus effect of the seed extracts is due to the presence of flavonoids while some suggested that
saponins in lychee seed is the most effective constituent [10, 25, 26, 43].

Fruit
Anti-inflammatory activity: Ethanol extract of lychee is a mixture of flavanol monomers, dimers and trimers. The
effect of lychee-fruit extract was observed on interleukin treated rat hepatocytes and it was reported that ethanol
extract significantly inhibits the production of interleukin induced Nitric oxide. The flavanols present in ethanol
extract may have been responsible for anti-inflammatory effect and can be used to cure inflammatory diseases [47].

Aldose reductase inhibition activity: Aldose reductase is an enzyme responsible for sugar induced cataract.
Methanol and ethanol extract of lychee fruit was found to inhibit the functioning of aldose reductase enzyme in rat.
In this way fruit-extract can be prove significant so as to cure the diabetic related complications [48].

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Anti-viral activity: An experiment was conducted to find the inhibitory effect of phenolic extract of Lychee on
Betanoda virus (causative agent of viral nervous necrosis in marine fishes). It was reported that oligonol present in
phenol extract inhibited the replication of virus and thus can be used as an anti-viral agent [49].

Hepato-protective activity: Aqueous and alcoholic extract of fruit has significantly shown hepatoprotective activity
at an orally administrated dose of 250 mg/kg body weight and 500 mg/kg body weight. Their hepatoprotective
activity is comparable to LIV-52 (reference drug). Fruit extract decreases the weight of CCl4 induced liver and thus
can be used as a potent heapto-protective agent [50].

Other Functions
Lychee seed extracts are also reported to cure haemorrhoids [51].

CONCLUSIONS

Several investigations have been done to estimate the pharmacological properties of lychee. It can be concluded that
almost all parts of the plant contain bioactive compounds which are responsible for its pharmacological properties.
These results indicate and encourage us for sustainable production of lychee for both pharmaceuticals and dietary
purpose. However, sufficient clinical trials are also required for the evaluation and safety of the aforementioned
natural compounds. There is also a need to develop a robust micro-propagation technique so as to enhance the rate
of multiplication of the quality plants. More researches are required so as to produce seed-less varieties, to increase
the fruit shelf-life, to produce disease-free crop and to reduce the post-harvest loss of the crop.

ACKNOWLEDGEMENTS

The author is thankful to Mrs. Rashmi Mittal, Pro-Chancellor, Lovely Professional University (LPU), Punjab, India
for her valuable suggestions and infrastructural support.

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