Phytochemical and Pharmacological activity of Wonder Shrub: Calotropis gigantia

 

Dilip Kumar Tiwari, Dr. Neeraj Upmanyu

School of Pharmacy & Research, People’s University, Bhopal-462039

*Corresponding Author E-mail: dilip21k@gmail.com

 

ABSTRACT:

Calotropis gigantia is a valuable medicinal plant also known as arka and it is native to india. It is widely found in wasteland having enormous amount of benefit. C. gigantea contain chemical constituents are cardenolides, flavonoids, triterpenes, steroids pregnanes and a nonprotein amino acid. Calotropis gigantia has been used in unani, ayurvedic and siddha system of medicine. A scrutiny of literature revealed some notable pharmacological activities of the plant such as Analgesic, hepatoprotective, anti-diarrhoeal, antidiabetic, anti-inflammatory, anticonvulsant, antimicrobial, anticancer, antifertility and antioxidant activity. The purpose of this review was to assess the published scientific journal suggestion on various uses of Calotropis gigantia.

 

KEYWORDS: Calotropis gigantia, Pregnanes, Ayurvedic, Pharmacological activity.

 

 


INTRODUCTION:

Plant-based natural products, animal derived natural products and minerals have been the foundation of treatment of different human diseases. Many people around the world, especially in the developing countries, are increasingly relying on plant-derived traditional medicines. The world health organization defined medicinal plants as any plant that possess bioactive compounds in one or more of its organs that can be used for healing purposes.1

 

Calotropis gigantea Linn belongs to the family Asclepiadaceae which includes more than 280 genera and approximately 2,000 species. Calotropis gigantea (Linn) R.Br. and Calotropis procera (Ait) R.Br. are the two common and closely related species. Calotropis gigantea is a well known medicinal herb commonly known as Madar has been used in Unani, Ayurveda, and Siddha system of medicine for years. The drug Calotropis gigantea.2

 

 
 

Figure: 1 Morphological view of Calotropis gigantia leaf and flower

 

Geographical Distribution:

It is a native of India, China and Malaysia and distributed in almost all over the world. In India found chiefly in lower Bengal, Himalya, Punjab, Assam, Madras and South India. Common in waste land, road sides, railway embankments, ascending to about 1000m in the Himalayas from Punjab to Assam.3

 

Botanical Description

Classification of Calotropis gigantia

Kingdom - Plantae

Division - Magnoliophyta

Class - Magnoliopsida

Subclass - Asteridae

Order - Gentianales

Family - Asclipiadaceae

Subfamily - Caesalpinioideae

Genus - Calotropis

Species – Gigantia.4

 

Ethanobotany of Plant:

A small erect and compact shrub covered, found growing wild throughout India in comparatively drier and warmer areas, up to an altitude 1200m. Calotropis gigantia has been observed to grow mainly on coarse, sandy and alkaline soils. They are good soils binder and recommended for deserts. The life span of Calotropis is 15-20 years. It will be seen that root-bark from older plants has a higher percentage of acrid and bitter resinous matter than that from younger plants. In the supplement to the pharmacopoeia of India, he reports that he found that the older the plant, the more active is the bark in its effects.5,6

 

Morphological Characteristics of Plant:

The morphological studies revealed the plant is erect, tall, much branched succulent, xerophytic small laticiferous tree up to 2.5m, commonly known as “milkweed” or “Crown flower” Calotropis gigantia have large bushy shrub, leaves decussate, inflorescence extra axillary umbellate panicale, corolla white, lobes erect. The leaves are sub- sessile, 6-15 cm by 4.5-8cm, broadly ovate, ovate-oblong, elliptic or obovate acute, pubescent; when young and glabrous on both sides when mature.7

 

Phytochemistry:

Different parts of Calotropis gigantea is reported to have abundant phytochemical constituent as mentioned in table

 

Stem Bark

Giganteol, α and β calotropeol, β amyrin.8

Root

Calotrop naphthalene [naphthalene derivative], calotropisesquiterpenol, calotropisesterterpenol [terpene derivatives], calotropbenzofuranone [aromatic product] and sucros.9

Seed    

Oil extracted from seeds contains palmitic, oleic, linoleic and linolenic acid. The unsaponifiable fraction contains phytosterol, stigmasterol, melissyl alcohol and laurane.10

Flower

Ester of α-and β-calotropeols.10

Leaves

Sapogenins, holarrhetine; cyanidin-3-rhamnoglucoside; taraxasterol isovalerate. mudarine and three glycosides calotropin uscharin, calotoxin along with phenol

Latex

Water and water soluble substance (86-95.5%) and caoutchouc (0.6-1.9%). The coagulam consist of caoutchouc (5.1-18.6), resin (73.6-87.8) and insoluble matter (4.5-13.8%).11

α- and β-calotropeols (also in latex); latex-protease, calotropains FI and FII, flower β-amyrin, stigmasterol.12 Calotoxin, uscharin, and calactin.13

Two new Triterpine ester-3’-methyl butanoates of α-amyrin and Ψ taraxasterol–isolated from latex.14

Root Bark

Root bark contains β-amyrin, two isomeric crystalline alcohols, giganteol and isogiganteol.8

 

Pharmacological Aspects:

Anti-Solar activity of Calotropis gigantea L. (leaf) methonolic extract has more flavonoid content based on this chemical substance photo protective activity was evaluated using UV visible spectrophotometry, where the method is diffused transmittance and the range of UV-visible about 200-400nm. Absorption of UV radiation is a main characteristic for identification of flavonoids in natural sources. The results showed strong-tomoderate absorption of UV radiation along the whole range and this ability may be due to the presence of flavonoids.15

 

Antibacterial studies:

In vitro antibacterial potential of the chloroform, ethyl acetate, hexane, methanol and aqueous extracts ofCalotropis gigantia (L.) R. Br. was evaluated by using five cariogenic bacteria, Actinomyces viscosus, Lactobacillus acidophilus, Lactobacillus casei, Streptococcus mitis and Streptococcus mutans. Agar well diffusion method and minimum inhibitory concentration (MIC) were used for this purpose. The chloroform extracted fraction of latex showed inhibitory effect against S. mutans and L. acidophilus with MIC value of 0.032 and 0.52mg/mL, respectively. Qualitative investigation on structure elucidation of bioactive compound using IR, NMR and GC–MS techniques revealed the presence of methyl nonanoate, a saturated fatty acid.

 

A study to evaluate in-vitro antibacterial activity of methanol extract of the leaves against gram negative bacteria such as Salmonella typhi, Pseudomonas fluorescens, Pseudomonas aeruginosa and Escherichia coli was carried out. The pathogens were tested by disc diffusion assay method and minimum inhibitory concentration was evaluated. An attempt has been made to compare the activity of extract with standard ciprofloxin. Maximum activity was seen in case of Pseudomonas fluorescens where the zone diameter was 32 mm (300μg/ml). The antibacterial activity therefore shows clearly that the resistance to the pathogens may be minimized by these natural products of the plant            origins. 16

 

Hepatoprotective Activity:

Suspension of alcoholic extract of root bark of the plant calotropis gigantia 0.6% carboxy methyl cellulose (cmc were evaluated for hepatoprotective activity in wistar albino rats by inducing hepatic injury with D-galactosamine (400mg/kg).alcohlic extract of root bark of the plant Calotropis gigantea at an oral dose of 200 mg/kg and 400mg/kg Alcoholic extract of root bark of the plant Calotropis gigantea at an oral dose of 200 mg/kg and 400mg/kg exhibited a significant (P<0.001, P<0.01 and P<0.05) protection effect by normalizing the levels of aspartate amino transferase (ASAT/GOT), alanine amino transferase (ALAT/GPT), alkaline phosphatase (ALP), total bilirubin (TB), lactate dehydrogenase (LDH), which were significantly (P<0.001) increased in rats by treatment with 400mg/kg i.p. of D-galactosamine. Silymarin (25mg/kg), a known hepatoprotective drug used for comparison exhibited significant activity (P<0.001).17

 

Ethanolic extract (50%) of stems of Calotropis gigantea R. Br. (Asclepiadaceae) at doses of 250 and 500mg kg–1 were studied for hepatoprotective activity in male Wistar rats with liver damage induced using carbon tetrachloride, 2mL kg–1 twice a week. The protective effect of C. gigantea extract was compared with the standard drug silymarin. Various biochemical parameters such as aspartate amino transferase (AST), alanine amino transferase (ALT), glutathione (GSH), lipid peroxide (LPO), superoxidedismutase (SOD), glutathione peroxidase (GPx) and catalase (CAT) were evaluated. The results revealed that the C. gigantea extract significantly decreased AST, ALT (p < 0.001) and lipid peroxide (p < 0.01) levels. The antioxidant parameters GSH, GPx, SOD and catalase levels were increased considerably compared to their levels in groups not treated with C. gigantea extract.18.

 

Cytotoxicity activity:

A new lignan, 9′-methoxypinoresinol (1), and two new glycosylated 5-hydroxymethylfurfurals, calofurfuralside A (2), and calofurfuralside B (3), together with nine known compounds (412) have been isolated from the active fractions, CHCl3 (IC50, 0.32μg mL−1) and EtOAc (IC50, 0.55μg mL−1) fractions of the leaves of Calotropis gigantea. Among the isolated compounds, compounds 1 and 9 exhibited potent cytotoxicity against PANC-1 human pancreatic cancer cell line under the normoglycemic condition with IC50 values of 3.7 and 3.3 μM, respectively. 9′-Methoxypinoresinol (1) significantly inhibited the colony formation of PANC-1 cells in a concentration-dependent manner.19

 

Analgesic Activity:

The alcoholic extract of the flowers of Calotropis gigantea was administered orally and explored for its analgesic activity in chemical and thermal models in mice. In acetic acid induced writhing test, an inhibition of 20.97% and 43.0% in the number of writhes was observed at the doses of 250 and 500mg/kg, respectively. In the hot plate method the paw licking time was delayed. The analgesic effect was observed after 30 min of dose administration which reached its maximum after 90 min.20.

 

Wound healing activity:

Root bark extract of calotropis gigantea were topically treated by using simple ointment BP as base. 5% (w/w) Topical application of in excision wound model increased the percentage of wound contraction. Scar area and epithelization time were decreased. In incision wound and dead space wound breaking strength of wounds and hydroxyproline was increased.21.

 

Latex of Calotropis gigantean (200mg/kg/day) was evaluated for its wound healing activity in albino rats using excision and incision wound models. Latex treated animal sex exhibit 83.42% reduction in wound area when compared to controls which was 76.22%. The extract treated wounds are found to epithelize faster as compared to controls. Significant (p<0.001) increase in granuloma breaking strength (485±34.64) was observed. The Framycetin sulphate cream (FSC) 1 % w/w was used as standard.22

 

Antiinflamatory Activivity:

Ethanolic extract of leaves Calotropis gigantia was evaluated for in vitro anti–inflammatory activity by using inhibition of albumin denaturation technique. Ethanolic extract studied according to Muzushima and Kabayashi7 with slight modification. Ibuprofen (100mg/kg) was used as standard reference drug. The % inhibition of denaturation produced by ethanolic extract of Calotropis gigantea leaves was comparable with that produced by Ibuprofen (85.71%) which shows that Calotropis gigantea leaves extract possess significant anti – inflammatory activity.23

 

Anti-Diabetic Activity:

Anti-Diabetic Activity of proteases extracted from specific protein antigen, bovine serum albumin (BSA) using Calotropis gigantea, flowers dissolved in phosphate buffered saline (PBS, acidic pH 5) was determinine. In this study, treatment of acidic proteases of different concentration on diabetic human whole blood samples in order to cross-examine its blood counts (lymphocytes, monocytes and granulocytes count) and also analyzed forward scatter (shape and size) and side scatter (granularity of the cell) using flow cytometry. The results showed that acidic protease enhanced the granulocytes count which is generally useful aspect in order to prevent the cardiovascular infections and also retained the monocytes count in normal range and also showed that there is enhancement in the count of forward and side scatter in case of diabetic human blood samples.24

 

Hypoglycemic Activity:

In normal rats was carried out by treatment using chloroform extract of Calotropis gigantea leaf and flower 10, 20 and 50mg/kg, orally. The oral glucose tolerance test was carried out by administering glucose (2g/kg, p.o), to non-diabetic rats treated with leaf and flowers extracts at oral doses 10, 20 and 50mg/kg, p.o and glibenclamide 10mg/kg. The administration of leaf and flower extracts to streptozotocin-induced diabetic rats showed a significant reduction in serum glucose             levels. 25

 

Nootropic Activity:

Methanolic extract of Calotropis gigantea (Linn.) roots was examined for nootropic activity on in scopolamine (SCO) induced cognitive deficit rats. Seven days of treatment animals were at once scarified the estimation of markers of oxidative stress in the brain was measured. The protective and cognitive enhancing effects of MCGE on cognitive shortfall rats induced by scopolamine were investigated by assessing the elevated plus maze, the passive avoidance test and the Morris water maze test. Pretreatment of scopolamine memory deficit rats with MCGE 200mg/kg and piracetam 200 mg/kg resulted in a significant decrease in MDA level as compared to scopolamine group. MCGE 200mg/kg and piracetam 200mg/kg significantly increased the level of GSH as compared with scopolamine group and it is also inhibited AChE, thereby elevating acetylcholine concentration in the brain and ultimately improved memory in rats.26

 

Antidiarrheal Activity:

The anti-diarrheal effect of hydroalcoholic (50:50) extract of aerial part of Calotropis gigantea was studied against castor oil-induced-diarrhea model in rats. The gastrointestinal transit rate was expressed as the percentage of the longest distance traversed by the charcoal divided by the total length of the small intestine. The weight and volume of intestinal content induced by castor oil were studied by enteropooling method and it was found that all doses of the plant extracts significantly retarded the castor-oil induced enteropooling and intestinal transit. The dose 100 (P<0.01), 200 and 400mg/kg significantly inhibited (P<0.001) weight and volume of intestinal content.27

 

Procoagulant Activity:

Latex of Calotropis gigantea was studied against controlling bleeding. The crude extract hydrolysis crude fibrin clot strongly compared to trypsin and papain. Pharmacologically the crude extract is hemorrhagic and induces skin hemorrhage at >75μg and reduces the coagulation time of citrated plasma from 150 to 47 s and promotes blood coagulation28.

 

Antiarthritic activity:

Antiarthritic activity of various extract of calotropis gigantia was examined on freund’s adjuvant arthritis in albino rats. The extracts were administered orally for 21 days and the mean changes in diameter of paw were noted at regular intervals. The changes in body weight were recorded daily. The Calotropis gigantea leaves extracts reduced the hind paw oedema. In biochemical study Calotropis gigantea extracts showed increase in haemoglobin content as compared to adjuvant positive control group. The increased WBC count was significantly suppressed by extracts.29

 

Anticancer Activity:

Anticancer Activity of the glycosides from Calotropis gigantea on breast cancer MCF-7 cells through analysis of modulation of gene expression. Cardiac glycosides were isolated from the leaves of C. gigantea, and the compounds were identified through LC-MS. Influence of the glycoside sample on the expression of p53 and Bcl-2 genes in MCF-7 cells was assessed by comparative RT-PCR of MCF-7 cells treated with the test sample, standard drug, and control followed by validation through colony formation assay. Influence of the glycosides on the modulation of the expression of tumor suppressor gene p53 indicated a weak down-regulation of its expression, whereas on the modulation of Bcl-2 was found to be drastic with almost absolute inhibition of its expression. Results of the study suggest that cardiac glycosides cast a dual influence on MCF-7 cells, namely cytotoxic effect through down-regulation of p53 gene expression and antiproliferative effect through down-regulation of Bcl-2 gene expression of which latter is more effective.30

 

Antimicrobial activity:

Leaves of Calotropis gigantia were investigated for its morphological, microscopical and phytochemical constituents to check the authenticity of the plant. Column fractionation was done. A study to evaluate in-vitro antibacterial activity of methanol extract of the leaves against gram negative bacteria such as Salmonella typhi, Pseudomonas fluorescens, Pseudomonas aeruginosa and Escherichia coli was carried out. The pathogens were tested by disc diffusion assay method and minimum inhibitory concentration was evaluated. An attempt has been made to compare the activity of extract with standard ciprofloxin. Maximum activity was seen in case of Pseudomonas fluorescens where the zone diameter was 32 mm (300μg/ml).31

 

CONFLICTS OF INTEREST:

Authors have no conflicts to declare.

 

ACKNOWLEDGEMENT:

Authors are thankful to Vindhya Herbal (A unit of MP state minor forest produce) for providing valuable help. Authors are also thankful to Dr. Shushma Mishra for providing necessary guidance and support.

 

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Received on18.01.2020          Modified on 12.02.2020

Accepted on 20.03.2020 ©AandV Publications All right reserved

Res. J. Pharmacognosy and Phytochem. 2020; 12(2): 106-110.

DOI: 10.5958/0975-4385.2020.00018.7