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Indian Journal of Drugs, 2013, 1(2), 63-69
ISSN: 2348-1684
CALOTROPIS PROCERA: AN OVERVIEW OF ITS PHYTOCHEMISTRY AND
PHARMACOLOGY
Shoaib Quazi*, Kumkum Mathur, Sandeep Arora
Pharmacy Wing, Lachoo Memorial Col ege of Science and Technology, Shastri Nagar, Jodhpur, Rajasthan.
*For Correspondence:
ABSTRACT
Herbal medicines have been used from the earliest times to the Pharmacy Wing, Lachoo Memorial College of present day. The ethno pharmacology is as old as man himself.
Science and Technology, Shastri Nagar, Herbal medicines exhibit a remarkable therapeutic diversity.
Calotropis procera Linn. is an Ayurvedic plant which is used in several traditional medicines to treat a variety of diseases. The extracts from different parts of the plant have significant therapeutic value. The whole plant when dried exhibits good tonic, antihelmintic and expectorant activities. The roots also Received: 11.11.2013
have similar activities and also act as an effective laxative.
Accepted: 27.12.2013
Traditionally, the powdered root is used to treat bronchitis, Access this article online
asthma, leprosy, eczema, elephantiasis while the latex s used to, Website:
treat vertigo, baldness, hair loss, toothache, intermittent fevers, rheumatoid/joint swellings, and paralysis, The leaves are used Quick Response Code:
to treat joint pain, and reduce swelling. Besides its Ayurvedic use, Calotropis procera Linn. is also used as a homeopathic medicine. In ancient Ayurvedic medicine the plant Calotropis procera Linn. was known as “Rakta arka”. The pungent latex extracted from the leaves and flowers of Calotropis procera is processed and used in the commercial preparation of eye tonics.
phytochemistry; Calotropis procera Linn INTRODUCTION
properties. It is commonly referred to as ark, frequently in Indonesia, Malaysia, China, and Cwith important medicinal properties. It the Indian subcontinent as wasteland weed.
is known by various vernacular names like The ark plant with white flowers is a superior Swallow wort in English, madar in Hindi and variety and is referred to as Calotropis procera.
Alarka in Sanskrit. It is found in most parts of In India, it is found from the Punjab and the world with a warm climate in dry, sandy Rajasthan to Assam and Kanyakumari up to an and alkaline soils. Calotropis is primarily altitude of 1050 m. It grows abundantly in harvested because of its distinctive medicinal Rajasthan. It is found in waste lands and grows as a weed in cultivated areas. It also grows well ester. Chemical investigation of this plant has on rubbish heaps, waste and fallow land, by the roadside and in sand dunes. The inner bark calotropursenyl acetate and calopfriedelenyl, of Calotropis is used to make strong fibers a norditerpenyl ester, calotropternyl ester oleanene triterpenes like calotropoleanyl manufacture of weave carpets, ropes, sewing thread and fishing nets. Calotropis procera Linn is an erect, tall, large, highly branched and uscharin, calotoxin and calactin The plant also perennial shrub or small tree that grows to a has been investigated for the presence of height of 5.4 m, with milky latex throughout .Phytochemical investigation of the roots of MORPHOLOGY OF PLANT
phytoconstituents, procerursenyl acetate and Flower : Flowers consist of 5 small triangular
dirty white sepals, 5 thick ovate petals (1cm x 1cm) which are white at the base and purple at mono-oleolyl-2- phosphate, methyl myrisate, the tips and 5 purple tipped stamens, which methyl behenate and glyceryl-1, 2-dicapriate- Fruit: Fruits consist of green, spongy ovoid
fruits (follicles), up to 15 cm long by 10 cm alpha-I -12, 20 (30)-diene-3 beta-yl acetate and n-triacontan-10 beta-ol on the basis of spectral papery light brown seeds with a pappus of data analysis and chemical reactions. The root white filaments up to 6 cm long on one side.
bark has also been found to possess α-amyrin, Root: The root occurs in the entire condition.
β-amyrin , lupeol, β-sitosterol [9] and flavanols The bark is separated from the wood 0.5-2.0 like quercetin-3-rutinoside.In the leaves, cm. in diameter bearing rootlets with diameter mudarine is the principal active constituent as varying from 0.2 to 0.5 cm. externally whitish well as a bitter yellow acid, resin and 3 toxic grey in colour, wrinkled in the fresh condition, glycosides calotropin, uscharin and calotoxin.
plenty of whitish latex exudes from cuts or The latex contains a powerful bacteriolytic wounds in the bark. Fracture is incomplete.
enzyme, a very toxic glycoside calactin (the Leaf: Simple, opposite, sub-sessile, slightly
concentration of which is increased following thick, fleshy, coriacious, 10-15 cm. long and 4.5 insect or grasshopper attack as a defense to 6.5 cm. broad, broadly cuneate, obovate or mechanism), calotropin D I, calotropin D I , obovate oblong, slightly cordate and auricled calotropin-F I, calotropin F I and a non-toxic at base with tuff of short simple hairs on the protealytic enzyme calotropin (2 %-3 %). This upper side near place of the attachment to the calotropin is more proteolytic than papain, and gelatin and casein. The whole plant contains PHYTOCHEMISTRY
teraxasterol, gigantin, giganteol, isogiganteol, proceragenin, while the root bark contains benzoylinesolone and benzoylisolinelone. The PHARMACOLOGICAL ACTIVITIES
calotropenyl acetate, and multiflavenol and The plant has attracted much attention due to the latex contains uzarigenin, and terpenol following biological activities: The previous pharmacological studies include reports of mg/kg). In the hot plate test, an increase in anticancer, antifungal and insecticidal activity the reaction time was observed only at 60 min of C. procera (Ahmed et al., 2006). The flowers after treatment with latex at doses of 25 (79.5 of the plant exhibit hepatoprotective activity, anti-inflammatory, antipyretic, analgesic, and controls and naloxone was unable to reverse antimicrobial effects and larvicidal activity. The this effect. It was concluded that the protein latex of the plant is reported to possess analgesic and wound healing activity as well as Calotropis procera possesses antinociceptive anti-inflammatory and antimicrobial acivity activity, which is independent of the opioid while the roots are reported to have anti- Antifertility activity
The effect of an ethanolic extract of the roots Analgesic Activity
of Calotropis procera has been studied in A single oral dose of dry latex ranging from albino rats to explore its antifertility and 165 to 830 mg/kg produces a significant dose- hormonal activities. Strong anti-implantation dependent analgesic effect against acetic acid- (inhibition 100 %) and uterotropic activity was induced writhing. The effect of dry latex at a observed at a dose of 250 mg∕kg (1∕4 of LD50).
dose of 415 mg/kg is more pronounced than a 100 mg/kg oral dose of aspirin. In addition, dry latex (830 mg/kg) produces marginal analgesia Anti-tumor studies
in a tail-flick model which is similar to that of The anti-tumor potential of the root extracts of aspirin. The analgesic effect of dry latex is Calotropis procera Linn., was investigated mg/kg, which completely blocks the analgesic aqueous (CW) and ethyl acetate extract (CE) effect of morphine (10 mg/kg). However, the effect of aspirin was not blocked by naloxone.
cancer cells was studied. Cellular proliferation An 830 mg/kg oral dose of dry latex did not activities were assayed by tetrazolium bromide produce any toxic effects in mice and the LD50 (MTT) colorimetry. Morphological changes in was found to be 3000 mg/kg (Ahmed et al., cancer cells were observed under an inverted 2005). Antinociceptive effect of proteins from microscope and the cell cycle parameters were Calotropis procera (Asclepiadaceae) latex using propidium iodide staining. Treatment with the nociception in mice. The latex protein fraction extracts at different doses of 1, 5, 10 and 25 administered intraperitoneally to male mice at μg/ml revealed that CM, CH and CE possessed cytotoxicity, whereas CW had no cytotoxic compared with the respective controls in all cytotoxic effect (96.3 %) on Hep2 at 48 hr assays. Inhibition of the acetic acid induced abdominal constrictions was observed at doses exhibited cytotoxicity of 72.7 and 60.5 %, of 12.5 (67.9 %), 25 (85 %) and 50 (99.5 %) mg/kg compared with controls. Latex protein exhibited typical morphological changes of at doses of 25 (39.8 %; 42 %) and 50 mg/kg apoptosis. The results of flow cytometric analysis clearly demonstrated that the root extracts produced apoptosis of Hep2 cells phases, respectively, and this effect was not through cell cycle arrest at the S phase, thus reversed by pretreatment with naloxone (1 phase. The results of this study indicate that prevented the body weight loss in diabetic rats the root extracts of C. procera inhibit the and reduced the daily water consumption to proliferation of Hep2 cells via mechanisms values comparable with those of normal rats.
based on apoptosis and cell cycle disruption Dry latex also produced an increase in the (Rajani and Gupta, 2009; Lal et al., 1985).
hepatic levels of endogenous antioxidants, Anthelmintic activity
namely superoxide dismutase (SOD), catalase The anthelmintic activity of Calotropis procera and glutathione, while it reduced the levels of Linn. Flowers, in comparison with levamisole, thiobarbituric acid-reactive substances (TBARS) was evaluated in a series of in vitro and in vivo in alloxan-induced diabetic rats. The efficacy of studies. The in vitro studies demonstrated the dry latex as an antioxidant and as an anti- anthelmintic effects (P<0.05) of crude diabetic agent was comparable with that of aqueous (CAE) and crude methanolic extracts the standard antidiabetic drug, glibenclamide (CME) of Calotropis procera flowers on live Hepatoprotective activity
mortality or temporary paralysis. For the in The plant is a rich source of phytoconstituents vivo studies, Calotropis procera flowers were but there is no scientific basis or reports in administered as a crude powder (CP), CAE and recent literature regarding the usefulness of CME to sheep naturally infected with a mixed the root bark as a hepatoprotective agent and sample of gastrointestinal nematodes. The this prompted us to evaluate the root bark of percentage reduction in egg count (ECR) was recorded as 88.4 and 77.8 % in sheep treated activity. An aqueous ethanolic extract (70 %) of with CAE and CP at 3000 mg/kg body weight Calotropis procera flowers was prepared and tested for its hepatoprotective effect against respectively. CME was the least effective paracetamol-induced hepatitis in rats.
producing only a 20.9 % reduction in ECR on Changes in the levels of biochemical markers day 7 PT. It was found that Calotropis procera flowers possess good anthelmintic activity bilirubin, cholesterol, HDL and tissue GSH, against nematodes, although this was lessthan that exhibited by levamisole (97.8 %–100 %).
untreated groups. Paracetamol (2000 mg/kg) It is suggested that further research be carried out on a larger scale involving a greater ALP, bilirubin and cholesterol levels and reduce number of animals, doses higher than those serum levels of HDL and the tissue level of GSH while treatment with an aqueous ethanolic extract of C. procera flowers (200 mg/kg and 400 mg/kg) restored the altered levels of studies for drug development (Larhsini et al., biochemical markers to almost normal levels in a dose-dependent manner (Ranab et al., 2002).
Anti-hyperglycemic effect
Inflammatory activity
Latex of Calotropis procera was studied for its possessing potent anti-inflammatory activity inflammatory reactions using pedal oedema and air pouch models of inflammation in rats.
antihyperglycemic effects in rats with alloxan- Subcutaneous injection of aqueous solution induced diabetes. Daily oral administration of (0.1 ml of 1%) of dry latex (DL) into the plantar dry latex at 100 and 400 mg/kg produced a dose-dependent decrease in blood glucose and an increase in hepatic glycogen. Dry latex also response was obtained 1 h after the injection and was maintained for a further 1 h. The alter the electrolyte concentration in the intestinal fluid compared with castor oil- an increase in vascular permeability that Anti-convulsant effects
Inflammation was also induced in the 6-day- The anticonvulsant activity of different root old rat air pouch by injecting a 2.5 % solution extracts of Calotropis procera was studied in of DL. The latter model was characterized for rats in order to evaluate the traditional use of this plant. The anticonvulsant activity of concentration, and wet and dry weights of different extracts of Calotropis procera roots granuloma. A time-course study indicated that was studied using seizures induced by maximal both the exudates volume and the weight of electroshock seizures (MES), pentylenetetrazol granuloma were at maximum on day 5 after DL (PTZ), lithium-pilocarpine and electrical injection while the protein concentration peaked on the third day. Further, the two chloroform extract of Calotropis procera roots showed the most significant (P<0.01) inflammatory effect of various drugs. It was duration of hind limb extension (extensor phase), clonus and also the duration of the prednisolone while almost complete inhibition stupor phase, compared with the controls. In the PTZ test, the chloroform extract exhibited cyproheptadine. On the other hand, in the air a highly significant (P<0.001) effect, and the pouch model, prednisolone was more effective (P<0.01) effect compared with the controls by delaying the onset of convulsions. The extracts inflammation in different models could be also inhibited convulsions induced by lithium- pilocarpine and electrical kindling. The results of this study indicate that the chloroform Anti-diarrhoeal activity
extract and aqueous extract of Calotropis The dry latex (DL) of Calotropis procera, a procera roots may be beneficial in absence potent anti-inflammatory agent, was evaluated (petit mal) and tonic clonic (grand mal) types for its anti-diarrhoeal activity. Like atropine and phenylbutazone (PBZ), a single oral dose Anti-microbial activity
We studied the antimicrobial activities of decrease in the frequency of defecation and chloroform and methanol extracts of seeds of the severity of diarrhea as well as protecting from diarrhoea in 80 % rats treated with castor located in the forest area of Ghaziabad, India.
oil. To understand the mechanism of its anti- The chloroform extract of Calotropis procera diarrhoeal activity, we evaluated its effect on seeds exhibited better antimicrobial activity intestinal transit, castor oil-induced intestinal while the extracts obtained from Calotropis procera seeds were evaluated for their electrolyte concentration in intestinal fluid.
possible in vitro antibacterial activities using Dry latex produced a decrease in intestinal Oestrogenic functionality
normal and castor oil-treated animals. Unlike The effects of ethanolic and aqueous extracts atropine, dry latex significantly inhibited castor of Calotropis procera roots were studied on oil induced enteropooling. However, it did not the oestrous cycle and on some parameters of oestrogenic functionality in rats. Both extracts were found to interrupt the normal oestrous inflammation in different models could be cycle in 60 % and 80 % of rats treated. The rats exhibited a prolonged dioestrous stage of the Productivity of Calotropis procera and its use
inhibition of ovulation. The contemporary in renewable energy
India has over 180 million of wasteland out of progestinic preparation exhibited the same effects in 100 % of rats treated. However, the degraded and denuded lands arise due to soil extracts had no oestrogenic activity when erosions as well as secondary salinizations.
However Calotropis procera is a potential plant ovariectomized rats (Zafar et al., 2005).
for bioenergy and biofuel production in semi- Anti-malarial activity
arid regions of the country because it is able to The ethanolic extracts of the different parts of grow on such lands. The plant has a growth Calotropis procera showed IC50 values ranging potential of 2 dry tons to 40 dry tons per ha from 0.11 to 0.47 mg/ml against P. falciparum depending on the agro climatic conditions of MRC20-CQ-sensitive. And from 0.52 to 1.22 mg/ml against MRC76_CQ-resistant strains, regeneration potential and could be harvested flower and bud extracts being the most active.
up to 4 times a year. The plant yields valuable Although 220-440 times less effective than CQ, hydrocarbons which could be converted into these extracts deserve further study aimed at diesel substitutes. The bio-diesel derived from identification of the active constituents. The Calotropis procera is free from NOx gases, S02 results obtained support the ethnobotanical and Suspended Particulate Matter (SPM) and has high cetane value. Due to its enormous potential for growth under adverse climatic TOXICITY STUDIES
conditions Calotropis procera is suggested as The plant is toxic and is one of the few plants potential plant for bio-diesel production under toxicity, the latex extracted from the stem has traditionally been used to make poison arrows.
The latex is highly toxic to human eyes and CONCLUSION
produces sudden painless dimness of vision The World Health Organization has estimated with photophobia. Latex of Calotropis procera more than 80 % of the world’s population in was studied for its inflammatory effects using developing countries depends primarily on herbal medicines for their basic healthcare inflammation in rats. Subcutaneous injection needs In recent years, ethno-botanical and of an aqueous solution (0.1 ml of 1 %) of dry latex (DL) into the plantar surface of the paw especially those of plant origin, have received produced significant inflammation. It was much attention as they are well known for observed that, in the pedal oedema model, their efficacy and are generally believed to be safe for human use. It is best to use the prednisolone while almost complete inhibition molecules to manage a variety of diseases. A cyproheptadine. On the other hand, in the air thorough review of the published literature on pouch model, prednisolone was more effective Calotropis procera shows that it is a popular remedy in a variety of ethnic groups, as well as Ayurvedic and traditional practitioners for the treatment of a range of ailments. Calotropis procera is suggested as potential plant for bio- of Calotropis procer roots. Indian diesel production under semi-arid and arid conditions. Researchers are exploring the therapeutic potential of this plant as it is likely 9. Rajani, M. and Gupta, S.K. (2009).
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