INTRODUCTION:

Herbal medicines are now in great demand in the developing world for primary health care not because they are inexpensive but also for better cultural acceptability, better compatibility with the human body. Calotropis procera (Ait.) R.Br. (giant milkweed) belong to the family Asclepiadaceae, locally known as “aak” is being used as herbal medicine [1] and also found sculptured on Shiva temple symbolizing mythological cum medicinal value enjoyed by the plant in ancient India [2]. In the traditional Indian Medicinal system, this plant has been used for a variety of disease conditions including asthma, cold, cough, piles, ulcers, diarrhoea, heart diseases, leprosy, rheumatism and diseases of skin, spleen, liver and abdomen [3-5].

Calotropis procera Linn. possesses a wide range of biological activities such as anti-diabetic, analgesic, anti-flammatory, anti-arthritic, anti-oxidant, anthelmintic, anti-candidial, wound healing, anti-convulsant, anti-tumor, anti-asthmatic, hepatoprotective and cytotoxic. It is commonly referred to as Ark, Dead sea apple, Sodom apple, Swallow-wart or Milkweed and it found frequently in Indonesia, Malaysia, China and the Indian subcontinent as waste land weed. The Ark plant with white lowers is a superior variety and is referred to as Calotropis procera. In India, it is found from the Punjab and Rajasthan to Assam and Kanyakumari up to an altitude of 1050 meters. It grows abundantly in Rajasthan. It is found in waste lands and grows as a weed in cultivated areas. It also grows well on rubbish heaps, waste and fallow land, by the roadside and in sand dunes [6]. The inner bark of Calotropis is used to make strong fibres called madar which are used in the manufacture of weave carpets, ropes, sewing thread and fishing nets.

Vernacular Name:

Sanskrit : Swetarka, Arka, Ravi

English : Madar

Hindi : Ak, Akada, Safed-ak, Akvan, Madar

Bengali : Akanda, Akone.

Gujarati : Akado, Nani rui

Kannada : Ekka, Ekkagida.

Malayalam: Erikku.

Marathi : Aakmadara.

Punjabi : Ak, Madar

Tamil : Vellaerukku

Telugu : Nallajelledu, Mandaramu

Odiya : Arkha

Rajasthani: Aak, Akaro

Botanical Description:

The plant is a small shrub. The bark is soft, corky and light grey. The leaves are opposite, sessile, oblong-obviate, short pointed to blunt at the apex and are about 7 to 18 cm long and 5 to 13 cm broad, slightly leathery and have a fine coat of soft hair. The flowers are white in colour. The fruit are inflated, 8-12 cm long, grey-green in colour and having flat, brown seeds with a toft of white hair at one end. The roots are simple, whitish grey in colour with wrinkles, curved woody appearance. The aerial parts of the plant contain milky sap called latex.[8]

Ayurvedic Uses:

The parts of the plant used in Ayurvedic medicine are the leaf, roots, root bark, flower and latex in different formulation. It is thermogenic, laxative, anthelmintic, anticarcinogenic, expectorant, depurative and good tonic. It is used in worms and ulcer. The root bark has been used for cutaneous disease, intestinal worm, cough, ascites and anasarca. The root powder is useful in bronchitis, dyspepsia, gastroenteritis, dysentery, piles, boils, scrotal enlargement, filariasis, and cancer. The latex is thermogenic and used as blistering agent. In large dose it is purgative and emetic [9]. The powdered leaves are used for the fast healing of wounds, as a purgative and to treat indigestion. They are also used to treat skin disorders and liver problems. The dried leaves are used to promote sexual health including penile dysfunction and are reputed to be an aphrodisiac. Hot poultices are made from the leaves and to the stomach to relieve pain, and stop headaches and also applied to sprains to ease the swelling and pain. The flowers are used as a milk drink to treat a variety of complaints including coughs and catarrh, asthma and indigestion, as well as cholera. They are collected from September to February and are also used to treat piles when prepared in the form of a paste. [10]

Pharmacological Activities:

Analgesic Activity:

A single oral dose of dry latex ranging from 165 to 830 mg/kg produces a significant dose-dependent analgesic effect against acetic acid-induced writhing. The effect of dry latex at a dose of 415 mg/kg is more pronounced tan a 100 mg/kg oral dose of aspirin. In addition, dry latex (830 mg/kg) produces marginal analgesia in a tail-flick model which is similar to that of aspirin. The analgesic effect of dry latex is delayed 1 h by naloxone at a dose of 0.5 mg/kg, which completely blocks the analgesic effect of morphine (10 mg/kg). However, the effect of aspirin was not blocked by naloxone. An 830 mg/kg oral dose of dry latex did not produce any toxic effects in mice and the LD50 was found to be 3000 mg/kg [11].

Antifertility Activity:

The effect of an ethanolic extract of the roots of Calotropis procera Linn. has been studied in albino rats to explore its anti-fertility and hormonal activities. Strong anti-implantation (inhibition 100 %) and uterotropic activity was observed at a dose of 250 mg∕kg (1∕4 of LD50). No anti-estrogenic activity was detected [12].

Anti-Tumor Studies:

The anti-tumor potential of the root extracts of Calotropis procera Linn., was investigated using the methanolic (CM), hexane (CH), aqueous (CW) and ethyl acetate extract (CE) and its possible mechanism against Hep2 cancer cells was studied. Cellula proliferation activities were assayed by tetrazolium bromide (MTT) colorimetry. Morphological changes in cancer cells were observed under an inverted microscope and the cell cycle parameters were determined by flow cytometry following propidium iodide staining. Treatment with the extracts at different doses of 1, 5, 10 and 25 μg/ml revealed that CM, CH and CE possessed cytotoxicity, whereas CW had no cytotoxic effect. CE (10 μg/ml) showed strongest cytotoxic effect (96.3 %) on Hep2 at 48 hr following treatment, whereas CM and CH exhibited cytotoxicity of 72.7 and 60.5 %, respectively. The extract-treated cells exhibited typical morphological changes of apoptosis. The results of flow cytometric analysis clearly demonstrated that the root extracts produced apoptosis of Hep2 cells through cell cycle arrest at the S phase, thus preventing cells from entering the G2/M phase. The results of this study indicate that the root extracts of C. procera inhibit the proliferation of Hep2 cells via mechanisms based on apoptosis and cell cycle disruption [13].

Anthelmintic activity:

The anthelmintic activity of Calotropis procera Linn. Flowers, in comparison with levamisole, was evaluated in a series of in vitro and in vivo studies. The in vitro studies demonstrated the anthelmintic effects (P<0.05) of crude aqueous (CAE) and crude methanolic extracts (CME) of Calotropis procera flowers on live Haemonchus (H.) contortus as shown by mortality or temporary paralysis. For the in vivo studies, Calotropis procera flowers were administered as a crude powder (CP), CAE and CME to sheep naturally infected with a mixed sample of gastrointestinal nematodes. It was found that Calotropis procera flowers possess good anthelmintic activity against nematodes, although this was less than that exhibited by levamisole (97.8 %–100 %). It is suggested that further research be carried out on a larger scale involving a greater number of animals, doses higher than those used in the current study, together with identification of active principles, and standardization of the dose and toxicity studies for drug development [14].

Anti-Malarial Activity:

The ethanolic extracts of the different parts of Calotropis procera showed IC50 values ranging from 0.11 to 0.47 mg/ml against P. falciparum MRC20_CQ-sensitive and from 0.52 to 1.22 mg/ ml against MRC76_CQ-resistant strains, flower and bud extracts being the most active. Although 220-440 times less effective than CQ, these extracts deserve further study aimed at identification of the active constituents. The results obtained support the ethnobotanical use of this plant [15].

Toxicity:

The plant is toxic and is one of the few plants not eaten by grazing animals. Due to its toxicity, the latex extracted from the stem has traditionally been used to make poison arrows. The latex is highly toxic to human eyes and produces sudden painless dimness of vision with photophobia [16].

Anti-Convulsant Effects:

The anticonvulsant activity of different extracts of Calotropis procera roots was studied using seizures induced by maximal electroshock seizures (MES), pentylenetetrazol (PTZ), lithium-pilocarpine and electrical kindling seizures. In the MES test, the chloroform extract of Calotropis procera roots showed the most significant (P<0.01) anticonvulsant effect by decreasing the duration of hind limb extension (extensor phase), clonus and also the duration of the stupor phase, compared with the controls. In the PTZ test, the chloroform extract exhibited a highly significant (P<0.001) effect, and the aqueous extract had the most significant (P<0.01) effect compared with the controls by delaying the onset of convulsions. The extracts also inhibited convulsions induced by lithium-pilocarpine and electrical kindling. The results of this study indicate that the chloroform extract and aqueous extract of Calotropis procera roots may be beneficial in absence (petit mal) and tonic clonic (grand mal) types of seizures [17].

Anti-Bacterial Activity:

Antibacterial effects of these extracts on Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa showed that the flowers can be used in the treatment of gastrointestinal infection and diarrhoea and skin diseases.[18] and they can also be used in the treatment of urinary tract infection associated with Proteus sp.[19]. The extracts of these plants can be used in the treatment of boils, sores and wounds, since Staphylococcus aurous and Pseudomonas aeruginosa have been implicated as causative agents of these diseases[20]. The analysis of antimicrobial activity of aqueous and ethanolic extract of root and leaves of Calotropis procera Linn, against Staphylococcus aureus, Streptococcus pyogen, Escherichia coli and Pseudomona aeruginosa reveals that in disc method, the zone of inhibition produced by the crude ethanol and aqueous extracts against sensitive bacteria showed both, ethanolic and aqueous extracts of Calotropis procera Linn and it had inhibitory effect on the growth of isolates. The effect exhibited by ethanolic extract of leaves and roots was significantly greater than the aqueous extract of leaves and roots. The results provide a support for the use of Calotropis procera Linn, in traditional medicine and suggest its further advance investigation.[21]

Adverse Effects:

The adverse effects of Calotropis procera Linn. consumption are reported to cause blisters, lesions and eruptions when taken by patients for the treatment of joint pains and gastrointestinal problems. The preparations of Calotropis procera Linn. need to be used under the careful surveillance of a trained medical practitioner. Although Calotropis procera Linn. is associated with variety of medicinal virtues, but has been observed to be potentially injurious after prolong or continuous use. In one study, the flower extract was caused wide spread testicular necrosis.[22]

CONCLUSION:

The World Health Organization has estimated more than 80 % of the world’s population in Developing countries depends primarily on herbal medicines for their basic healthcare needs. In recent years, ethno-botanical and traditional uses of natural compounds, especially those of plant origin, have received much attention as they are well known for their efficacy and are generally believed to be safe for human use. It is best to use the classical approach in the search for new molecules to manage a variety of diseases. A thorough review of the published literature on Calotropis procera Linn. 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. Researchers are exploring the therapeutic potential of this plant as it is likely to have more therapeutic properties than are currently known.

ACKNOWLEDGEMENT:

The authors are very grateful to the Director General and Deputy Director (Tech), CCRAS, New Delhi, for their encouragement and support.

REFERENCES:

1. Calotropis R. Br., in The wealth of India-a dictionary of Indian raw materials and industrial products (Publications and Information Directorate, CSIR, New Delhi), 3rd Volume, 1992, p.78.

2. Gupta S M, Plants in Indian temple art (BR Publishing Corp., New Delhi) 1996, p.56.

3. Razzak H M A, Unani System of Medicine in India (Central Council for Research in Unani Medicine, New Delhi), 1991, p. 29.

4. Kartikar K R and Basu N, Indian Medicinal Plants (Lolit Mohan Basu, Allahabad), 1935, p. 1606.

5. Verma R, Satsangi G P and Shrivastava J N, Ethno-medicinal profile of different plant parts of Calotropis procera (Ait.) R. Br., Ethnobotanical Leaflets, 2010, 14, 721-742.

6. Yelne MB, Sharma PC, Dennis TJ. Database on Medicinal Plants used in Ayurveda, Central Council for Research in Ayurveda and Siddha, New-Delhi, 2000, 2(1): 69- 73.

7. Sharma.P.C, Yelne M.B. and Dennis T.J.- Database on Medicinal Plants used in Ayurveda, Vol-3, Published by CCRAS, Reprint-2005,p-69.

8. Gupta Sudesh et al. Ethnopharmacological potential of Calotropis procera: An overview. IRJP 2012,3(12) p-19-22

9. Sharma.P.C, Yelne M.B. and Dennis T.J.- Database on Medicinal Plants used in Ayurveda, Vol-3, Published by CCRAS, Reprint-2005,p-70

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11. Kumar VL, Sangraula H, Dewan S. Preliminary studies on the analgesic activity of latex of Calotropis procera. Journal of Ethnopharmacology, 2000, 73(1-2): 307-311.

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14. Iqbal Zafar, Lateef Muhammad, Jabbar Abdul. Anthelmintic activity of Calotropis procera (Ait.), flowers in sheep. Journal of Ethnopharmacology, 2005,102 (2): 256-261.

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21. G. A. Mako, A. H. Memon, U. R. Mughal, A. J. Pirzado and S. A. Bhatti, antibacterial effects of leaves and root extract of calotropis procera linn. Pak. J. Agri., Agril. Engg., Vet. Sci., 2012, 28 (2): 141-149.

22. Perkins K.D. and Payne W.W. Guide to poisonous and Irritant Plants of Florida. Fla. Coop. Ext. Servo University of Florida, Gainesville, pp.217-218 (1978).

Received on 07.11.2014 Modified on 20.12.2014

Res. J. Pharmacology & P’dynamics. 7(1): Jan.-Mar. 2015; Page 46-49

DOI: 10.5958/2321-5836.2015.00011.7