Medicinal Uses, Phytochemistry and Pharmacological Activities of Antigonon leptopus Hook. and Arn. (Polygonaceae): A Review

Abstract

Antigonon leptopus Hook. & Arn., belonging to the family Polygonaceae, is an invasive evergreen, woody liana. It is native to Mexico and is distributed in various parts of the world including India. In the present review, an extensive literature survey was carried out to update information available on the medicinal uses, phytochemistry and pharmacological activities of A. leptopus. The plant is shown to possess a wide range of phytochemicals. Alkaloids, phenolic compounds, saponins, triterpenoids and glycosides are detected in different parts of the plant. Compounds such as trihydroxy benzaldehyde, ferulic acid, quercetin-3-rhamnoside, anthraquinones, b-sitosterol and kaempherol-3-glucoside have been identified in the plant. The plant is used ethnomedicinally in various parts of the world for treating various ailments such as pain, cough, diabetes, dermatological problems, flu and stomachache. Different parts of the plant are investigated for pharmacological properties. The plant is reported to possess various bioactivities such as antimicrobial, antioxidant, hepatoprotective, analgesic, anti-inflammatory, cytotoxic and antidiabetic activities. Nanoparticles synthesized using A. leptopus were shown to exhibit bioactivities such as antimicrobial, antioxidant and cytotoxic activity. Information gathered from this extensive literature survey indicates the potential ethnomedicinal applications of A. leptopus and the possible utilization of the plant to develop pharmaceutical agents for disease therapy.

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Journal of Chemical and Pharmaceutical Research, 2018, 10(2):103-110
Review Article
ISSN : 0975-7384
CODEN(USA) : JCPRC5
103
Medicinal Uses, Phytochemistry and Pharmacological Activities of Antigonon
leptopus Hook. and Arn. (Polygonaceae): A Review
Prashith Kekuda TR1 and Raghavendra HL2*
1Department of Microbiology, S.R.N.M.N College of Applied Sciences, N.E.S Campus, Balraj Urs Road,
Shivamogga, Karnataka, India
2Department of Biochemistry, School of Medicine, Wollega University, Nekemte, Ethiopia
_____________________________________________________________________________
ABSTRACT
Antigonon leptopus Hook. & Arn., belonging to the family Polygonaceae, is an invasive evergreen, woody liana. It is
native to Mexico and is distributed in various parts of the world including India. In the present review, an extensive
literature survey was carried out to update information available on the medicinal uses, phytochemistry and
pharmacological activities of A. leptopus. The plant is shown to possess a wide range of phytochemicals. Alkaloids,
phenolic compounds, saponins, triterpenoids and glycosides are detected in different parts of the plant. Compounds
such as trihydroxy benzaldehyde, ferulic acid, quercetin-3-rhamnoside, anthraquinones, b-sitosterol and
kaempherol-3-glucoside have been identified in the plant. The plant is used ethnomedicinally in various parts of the
world for treating various ailments such as pain, cough, diabetes, dermatological problems, flu and stomachache.
Different parts of the plant are investigated for pharmacological properties. The plant is reported to possess various
bioactivities such as antimicrobial, antioxidant, hepatoprotective, analgesic, anti-inflammatory, cytotoxic and
antidiabetic activities. Nanoparticles synthesized using A. leptopus were shown to exhibit bioactivities such as
antimicrobial, antioxidant and cytotoxic activity. Information gathered from this extensive literature survey
indicates the potential ethnomedicinal applications of A. leptopus and the possible utilization of the plant to develop
pharmaceutical agents for disease therapy.
Keywords: Antigonon leptopus hook & Arn.; Polygonaceae; Phytochemicals; Ethnomedicine; Pharmacological
activities _____________________________________________________________________________
INTRODUCTION
The genera belonging to the family Polygonaceae includes herbs, shrubs, trees and lianas of which majority are
herbaceous plants. Antigonon leptopus Hook. & Arn., (Corallita, Honolulu creeper, coral vine, coral creeper,
queen’s wreath, Mexican creeper, railway creeper, bee bush) belonging to the botanical family Polygonaceae
(buckwheat family), is an invasive, fast growing, evergreen, perennial woody liana native to Mexico. The plant is
naturalized in India. Like many other members of Polygonaceae, A. leptopus is considered as an invasive species of
natural areas. The plant grows commonly along roadsides and hedges. The plant flourishes at lowlands, beside
streams and gullies as well as on dry and sandy heaps along the coast. It is often cultivated as an ornamental plant
due to beautiful flowers. The flowers of A. leptopus are visited by a tremendous variety of insects (flies, butterflies,
honey bees etc.) and birds like humming bird which facilitates its sexual reproduction outside of its natural range. It
is a climber and it climbs on supporting materials with the help of tendrils. The plant grows in any type of soil and
persists vegetatively by means of production of numerous tubers. The plant prefers full sunlight but can grow in
partial sunlight also. Propagation is mainly by seeds. Caterpillars seem to be pests for the plant. In several parts of
the world, the tubers (looks like small sized eggs) and flowers are consumed as food. The fried flour-coated leaves

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and flowers of are served with noodles in Thailand. The flowers are used in the preparation of omelets and the hot
tea prepared from the aerial portion is used as a treatment for cough and throat constriction in Jamaica [1-6]. In the
present review, an extensive literature survey is carried out to compile data available on the medicinal uses,
chemical compounds/groups present and pharmacological activities of A. leptopus by referring standard flora,
journals, and search engines such as Google scholar, ScienceDirect and Pubmed.
Plant Description
A. leptopus (Figure 1) is an extensive, rapidly growing climber reaching up to 40 feet or higher and climbs with the
help of slender tendril. Leaves are light to dark green, alternate, up to 12 × 8 cm, ovate or triangular, cordate or
hastate at base and acute to acuminate at apex. Petiole is up to 3.5 cm long and stipular sheaths are inconspicuous.
Flowers are monoecious, pink or white in color, showy, and occur in terminal or axillary racemes that end in
branched tendrils. Perianth segments are 5 in number, petaloid, 2 or 3 outer ones cordate or ovate, inner ones
oblong. Stamens are 8 in number. Flowering occurs more or less throughout the year. Fruit is brown, 3-angled at
least above and is loosely covered in the enlarged papery perianth-segments [7].
Figure 1: Antigonon leptopus Hook. & Arn.
Phytochemistry of A. Leptopus
Plants produce several kinds of primary and secondary metabolites. The chemical compounds that are present in
plants are known as phytochemicals. Plants produce diverse primary and secondary metabolites. Many of the plant
metabolites exert beneficial effects such as avoiding herbivores and controlling pathogenic organisms. Besides,
some plant constituents are responsible for contributing color and aroma to plants. Many of these metabolites are
responsible for therapeutic potential of plants. The diverse chemical nature of plant metabolites provides leads to
develop novel drugs with potential applications. Drugs such as taxol, quinine, vincristine, vinblastine, digoxin,
codeine, berberine and nicotine are from plant origin [8-13]. A range of phytochemicals are found in the plant A.
leptopus. Some studies have detected several groups of phytochemicals in different parts of the plant while few
studies have revealed a detailed note on the isolation of purified compounds from the plant. Several bioanalytical
techniques have been employed to isolate compounds in pure form from A. leptopus and to identify them. Tables 1
and 2 depict the phytochemical groups/chemical compounds identified in different parts of A. leptopus. Structures of
some of the compounds identified in A. leptopus are shown in Figure 2.
Table 1: Phytochemical groups detected in different parts of A. leptopus
Part
Phytochemicals detected
References
Flower
Phenol, saponins, tannins, coumarins, steroids
Antonisamy et al. [14]
Leaf
Phenols, hydrocarbons, quinazolines, coumarins, steroids, cadinene, juniper camphor and
others
Priya et al. [15]
Root
Steroids, alkaloids, flavonoids, tannins and glycosides
Mamidipalli et al. [16]
Flower
Volatile oils, glycosides, terpenes
Bolla and Bhogavalli [17]
Leaf
Alkaloids, flavonoids, glycosides, tannins, saponins and steroids
Licayan et al. [18]
Flower
Phenol, flavonoids, saponins, steroids, tannins, coumarins
Jeeva et al. [19]
Leaf
Sterol, triterpenes, alkaloids, flavonoids, tannins, saponins, glycosides, coumarins
Elhaj et al. [20]
Leaf
Tannins, cardiac glycosides, steroids, triterpenes, flavonoids
Rashmi and Rajkumar [21]
Leaf
Tannins, alkaloids, flavonoids, phenols, terpenoids
Sravanthi et al. [22]
Whole plant
Alkaloids, glycosides, flavonoids, tannins, saponins, steroids, volatile oils.
Kanthal et al. [23]
Leaf
Alkaloids, flavonoids, tannins, glycosides, terpenoids, saponins
Pradhan and Bhatnagar [24]
Leaf
Saponin, phenolic compounds, tannins, flavonoids, alkaloids, fixed oils and amino acids
Balasubramani et al. [25]
Roots and rhizomes
Triterpenoids, flavonoids and tannins
Battu and Raju [26]

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Table 2: Chemical compounds identified in A. leptopus
Part
Phytochemicals detected
References
Flower
Gallic acid, protocatechuic acid, p-hydroxy benzoic acid, chlorogenic acid, vanilic acid, caffeic acid, syringic
acid, p-coumaric acid, ferulic acid, sinapic acid
Kaisoon et al. [27]
Aerial parts
2,3,4-trihydroxy benzaldehyde
Mulabagal et al. [28]
Aerial parts
quercetin-3-O-a-rhamnopyranoside, 1,8-dihydroxy-6-(hydroxymethyl)-3-methoxy-2-pyrrolidinium
anthraquinone, 1,8-dihydroxy-6-(methyl)-3-methoxy-2-pyrrolidinium anthraquinone, 1,8-dihydroxy-6-
(hydroxymethyl)-3-methoxy-2-piperidinium anthraquinone, 1,8-dihydroxy-6-(methyl)-3-methoxy-2-
piperidinium anthraquinone.
Olaoluwa et al. [29]
Arial parts
n-hentriacontane, ferulic acid, 4-hydroxycinnamic acid, quercetin-3-rhamnoside, and kaempherol-3-glucoside,
b-sitosterol, b-sitosterol-glucoside and d-mannitol
Vanisree et al. [2]
Ethnomedicinal Uses of A. Leptopus
Ethnobotany is the relationship between man and plants. Worldwide, plants have been used as medicine. Traditional
medicinal practitioners use many plants in certain formulations for treating several diseases or disorders. An
estimate by WHO highlights that around 80% of population rely on medicinal plants for primary healthcare needs.
Plants are known to be essential component of indigenous systems of medicine viz. Ayurveda, Unani and Siddha
[12,30-35]. The plant A. leptopus is one among several plants that have been used traditionally for treating various
ailments. Different parts such as roots, aerial parts, leaves and seeds of the plant are used ethnomedicinally
worldwide. A brief description of ethnomedicinal uses of A. leptopus is presented in Table 3.
Table 3: Ethnomedicinal uses of A. leptopus
Geographical area
Uses
Reference
Iloilo, Philippines
Gastrointestinal disorders
Tantiado [36]
Amarkantak region, M.P., India
Paste made from fresh leaves is applied externally in skin
problems.
Srivastava et al. [37]
Pratapgarh tehsil, Rajasthan, India
Seeds are used as famine food; leaves are used to treat blisters.
Meena et al. [38]
Malayali tribals, Eastern Ghats, Tamil Nadu,
India
Seeds are used in diabetes.
Vaidyanathan et al. [39]
Fatehpur, UP, India
Decoction of aerial parts used for prevention of cough and flu
related pains.
Agarwal [40]
Trinidad and Tabago
Diabetes
Lans [41]
Nigeria
Antimicrobial
El-Ghani [42]
Sonora, Mexico
Leaves and roots used in stomachache.
Salazar et al. [43]
Himalayan region, India
Medicinal
Sekar [44]
Irula tribes, Walayar valley, Southern Western
Ghats, India
Decoction made from roots orally to treat dermatological
infections/diseases
Venkatachalapathi et al. [45]
Burhanpur district, M.P., India
Leaves are used in skin diseases.
Siddiqui and Sainkhediya [46]
Bhil tribe of Alirajpur district, M.P., India
Flower is used in pain and cold; leaf is used in blood pressure
and as heart tonic.
Bhargav and Patel [47]
Eastern Nicaragua
Root is used as food and medicine
Coe and Andersen [48]
Pharmacological Activities of A. Leptopus
Plants have been extensively used as therapeutic agents for treatment of various disorders throughout world. Such
medicinal uses of plants can be identified by subjecting the plants and their formulations to in vitro as well as in vivo
pharmacological studies. The findings of such pharmacological studies can possibly highlight the potential
utilization of plants in the treatment of diseases or disorders by traditional systems of medicine. The plant A.
leptopus is investigated for various pharmacological properties. Studies have shown a tremendous range of
biological activities such as antimicrobial, antioxidant, anti-inflammatory, analgesic, hepatoprotective and
antidiabetic activities exhibited by the plant A. leptopus and are discussed below.
Antimicrobial Activity
Battu and Raju [26] evaluated antimicrobial activity of methanol, hexane and ethyl acetate extracts of root and
rhizomes of A. leptopus. Among extracts, methanol extract was shown to display stronger antimicrobial property.
Bolla and Bhogavalli [17] determined antibacterial activity of flower extract of A. leptopus by disc diffusion
method. It was observed that ethanol extract displayed marked inhibition of test bacteria when compared to
chloroform extract. In a study, Udayaprakash et al. [49] evaluated antibacterial activity of various solvent extracts of
leaves of A. leptopus by disc diffusion method. Among extracts, acetone and methanol extracts exhibited dose
dependent inhibitory activity while chloroform and hexane extracts were ineffective. In the study carried out by
Gupta et al. [50], ethanolic extract of A. leptopus flower exhibited higher inhibitory activity against Gram positive

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and Gram negative bacteria when compared to chloroform extract. Jeeva et al. [19] determined antibacterial activity
of methanolic extract of flowers of A. leptopus against a panel of bacteria. The extract was found to exhibit
inhibitory activity against 9 out of 12 test bacteria with maximum antibacterial activity against Bacillus cereus. The
study of Rashmi and Rajkumar [21] showed marked antifungal activity of leaf extract against Macrophomina
phaseolina isolated from diseased maize. Sravanthi et al. [22] found antimicrobial activity in hexane, ethyl acetate
and aqueous extracts of leaves of A. leptopus. Ethyl acetate extract exhibited stronger antimicrobial activity. The
study carried out by Balasubramani et al. [25] revealed the marked potential of methanolic leaf extract of A. leptopus
to inhibit fish pathogens viz. Providencia and Aeromonas when compared to clinical pathogens. Pushpavathi et al.
[51] showed potent antifungal activity of methanolic leaf extract of A. leptopus against seed-borne fungi isolated
from sorghum seeds. Curvularia sp. and Aspergillus flavus were inhibited to highest and least extent respectively by
the extract.
Anthelmintic Activity
Chloroform fraction of methanol extract of leaves of A. leptopus was shown to exhibit anthelmintic activity against
earthworm model in a dose dependent manner [15]. Raju and Rao [52] evaluated anthelmintic activity of ethyl
acetate and methanolic extract of roots and rhizomes of A. leptopus in earthworm model. Both extracts exhibited
significant anthelmintic activity and the methanolic extract was more active. The study of Kanthal et al. [23]
revealed dose dependent anthelmintic activity of chloroform extract of A. leptopus whole plant.
Analgesic Activity
Mamidipalli et al. [16] evaluated analgesic activity of methanol extract of leaves of A. leptopus (200 and 400mg/kg
body weight) by hot plate and acetic acid writhing response in mice. The extract was shown to exhibit dose
dependent analgesic potential which was related to peripheral and central mechanisms. In another study, Ranjan et
al. [53] determined analgesic activity of methanol and chloroform extracts of leaves in albino rats by tail immersion
method. A significant dose dependent analgesic activity was observed.
Anti-inflammatory Activity
Anti-inflammatory activity of two concentrations, viz. 200 and 400 mg/kg body weight, of methanol extract of
leaves of A. leptopus was determined by Carrageenan induced paw edema in rats [16]. The extract was shown to
display inhibition of paw edema in a dose dependent manner. In a similar study carried out by Carey et al. [54], the
methanolic extract of roots of A. leptopus was shown to produce a significant inhibition of peritoneal and cutaneous
vascular permeability induced by acetic acid, granuloma induced by cotton-pellet and migration of leucocytes and
neutrophils induced by carrageenan in animals at the doses of 100, 200 and 400 mg/kg. The tea as a dried extract
prepared from aerial parts of A. leptopus was shown to inhibit cyclooxygenases COX-1 and COX-2 by 38% and
89%, respectively at 100 μg/ml [28].
Hepatoprotective Activity
Raju and Rao [55] screened hepatoprotective activity of ethyl acetate and methanol extracts of roots of A. leptopus
against carbon tetrachloride induced liver damage in Wistar albino rats. The extracts showed significant
hepatoprotective activity as evidenced by significant reduction in serum enzymes and total bilirubin. Methanol
extract was more effective than ethyl acetate extract. The study carried out by Babu et al. [56] revealed a significant
hepatoprotective activity of aqueous extract obtained from root of A. leptopus against hepatotoxicity induced by
paracetamol in albino rats.
Antidiabetic Activity
Angothu et al. [57] determined antidiabetic activity of methanolic extract of aerial parts of A. leptopus (200 and 400
mg/kg body weight) in alloxan induced diabetic rats. The extract displayed a dose-dependent fall in fasting blood
glucose levels. The results of biochemical parameters and histopathological studies also suggested that the extract
possesses significant antidiabetic property. In a similar study, Rani et al. [58] showed antidiabetic effect of toluene,
ethyl acetate and butanone fractions of methanol extract of leaves of A. leptopus on streptozotocin - induced diabetic
rats. Oral administration of toluene, ethyl acetate, and butanone fractions at 50 and 100 mg/kg body weight
significantly reduced the fasting blood glucose level in diabetic rats. Among the fractions tested, ethyl acetate
fraction was shown to be more effective. In another study by Sujatha et al. [59], the methanolic extract of flower of
A. leptopus was shown to exhibit antihyperglycemic activity in alloxan induced diabetic rats.

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Cytotoxic Activity
Elhaj et al. [20] determined cytotoxicity of ethanol extract of leaves of A. leptopus against Vero cell line by MTT
assay. The extract was shown to exhibit dose dependent cytotoxicity with an IC50 value of 289.60 µg/ml. The study
by Kanthal et al. [23] showed a dose dependent cytotoxic effect of chloroform extract of whole plant (by MTT
assay) against two cell lines viz., A-549 and CHOK 1. The study of Pradhan and Bhatnagar [24] revealed dose
dependent cytotoxicity of various solvent extracts viz. hexane, ethyl acetate, methanol and chloroform extract of
leaves of A. leptopus against brine shrimp larvae.
Antithrombin Activity
The antithrombin activity of methylene chloride and methanol extracts prepared from A. leptopus was investigated
by a chromogenic bioassay. The extract was found to demonstrate a significant activity [60].
Juvenoid Activity
The study of Neraliya and Gaur [61] revealed potent juvenoid activity of extract of A. leptopus against filarial
mosquito Culex quinquefasciatus.
Antioxidant Activity
The tea as a dried extract prepared from aerial parts of A. leptopus was shown to inhibit lipid peroxidation [28]. In a
study, Udayaprakash et al. [62] screened free radical scavenging potential of methanolic leaf extract of A. leptopus
by DPPH assay. The extract was shown to scavenge radicals dose dependently with an EC50 value of 38.33 µg/ml.
The study of Elhaj et al. [20] revealed scavenging of DPPH radicals by ethanolic extract of leaves of A. leptopus.
Licayan et al. [18] observed antioxidant potential of methanolic extract from leaves of A. leptopus by DPPH, ABTS
and FRAP assays. The content of total phenolics and total flavonoids was found to be mg 37.29 mg Gallic acid
equivalents/g and 111.47 mg Quercetin equivalents/g of extract respectively. Tea prepared by brewing dried flowers
at 90, 95 and 100°C for 3, 5 and 10 minutes were evaluated for antioxidant activity FRAPS method [63]. Total
phenolic content was higher in tea that was brewed for 10 minutes. The tea samples exhibited ferric reducing
potential. The study carried out by Pradhan and Bhatnagar [24] revealed dose dependent antioxidant activity of
various solvent extracts of A. leptopus leaf (evaluated by DPPH and nitric oxide radical scavenging activity and
FRAP assay). Ethyl acetate and methanol extracts showed marked antioxidant potential while chloroform and
hexane extracts displayed lower activity.
Biological Activities of Purified Compounds from A. Leptopus
A wide range of compounds have been purified from different parts of A. leptopus and investigated for some
bioactivities. 4-hydroxycinnamic acid, quercetin-3-rhamnoside, and kaempherol-3-glucoside (Figure 2) isolated
from aerial parts of A. leptopus were shown to inhibit lipid peroxidation by 19.5%, 41.0% and 60.5%, respectively,
at 5 µg/ml concentration. These compounds were also effective in inhibiting COX-1 and COX-2 enzymes indicating
their potential antioxidant and anti-inflammatory potential [2]. A compound 2,3,4-trihydroxyl benzaldehyde (Figure
2), isolated from the tea (as a dried extract) prepared from aerial parts of A. leptopus, was shown to exhibit
inhibitory activity against COX-2 while COX-1 enzyme was not inhibited [28]. Novel anthraquinones isolated from
aerial parts of A. leptopus were shown to exhibit antibacterial activity [29]. A new steroidal saponin (Figure 2),
isolated from crude methanolic extract of leaves of A. leptopus was shown to be a noncompetitive inhibitor of
xanthine oxidase [64].
Bioactivities of Nanoparticles Synthesized using A. Leptopus
Studies have shown the green synthesis of nanoparticles using A. leptopus. Nanoparticles produced from A. leptopus
were shown to exhibit some bioactivities. The study of Gunaie et al. [65] revealed a simple, single pot approach for
synthesizing bimetallic Ag/Au nanoparticles using aqueous extract prepared from different parts of A. leptopus.
Balasubramani et al. [66] screened antioxidant and cytotoxic potential of gold nanoparticles synthesized using
decoction of leaves of A. leptopus. The nanoparticles exhibited stronger antioxidant effect when compared to leaf
extract. The nanoparticles also exhibited marked cytotoxicity against human adenocarcinoma breast cancer (MCF-7)
cells with a growth inhibitory concentration (GI50) of 257.8 μg/ml. Sravanthi et al. [67] described the synthesis of
copper oxide nanoparticles from copper sulfate solution using leaf extract of A. leptopus. The synthesized copper
oxide nanoparticles were shown to exhibit potent and moderate antibacterial activity against gram positive gram
negative bacterial strains respectively. The gold nanoparticles produced from aqueous extract of A. leptopus were
found to catalyze the degradation of organic pollutants viz. Congo red and Ramazol brilliant blue [68].

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Figure 2: Structures of some compounds identified in A. leptopus
CONCLUSION
An extensive literature survey indicated that the plant A. leptopus is widely used in ethnomedicine for treatment of
several ailments such as skin problems, cough, pain and diabetes. Several pharmacological studies have been carried
out using A. leptopus and indicated potent bioactivities such as antimicrobial, antioxidant, hepatoprotective,
antidiabetic, analgesic, anti-inflammatory and cytotoxic activity. Besides, isolated chemicals from A. leptopus have
been shown to exhibit antibacterial, enzyme inhibitory and lipid peroxidation inhibition activity. The presence of
various phytochemicals in different parts of the plants can be attributed to potential medicinal properties of the plant
A. leptopus. The plant can be utilized as a remedy for various ailments and to develop drugs with potent
pharmacological activities that can benefit human beings.
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