A Comprehensive Review on Calotropis Procera on Its Analgesic Activity

Calotropis procera, a widely distributed medicinal plant, has long been used in traditional medicine for pain and inflammation. Its diverse phytoconstituents—including cardenolides, flavonoids, alkaloids, triterpenoids, and proteolytic enzymes such as calotropin and uscharin—contribute significantly to its analgesic activity. Preclinical studies confirm both central and peripheral analgesic effects through modulation of nociceptive pathways, inhibition of inflammatory mediators, and interactions with opioid receptors. Extracts from the latex, leaves, and roots demonstrate promising results in experimental pain models. Despite these findings, challenges remain concerning toxicity and dosage standardization, which limit clinical translation. Overall, Calotropis procera represents a promising natural source for novel analgesic drug development. Further pharmacological and well-designed clinical studies are warranted to establish its efficacy, safety, and mechanisms in humans. Calotropis procera exhibits significant analgesic activity, primarily attributed to its bioactive compounds such as lupeol, n-hexadecanoic acid, and cyclopentane. Studies have demonstrated that ethanolic extracts of Calotropis procera flowers possess pain-ameliorative effects in various animal models, including the tail-flick test, hot plate method, and acetic acid-induced writhing test.

Calotropis procera, Analgesic activity, Triterpenoids, Cardenolides, Pain management, Anti-inflammatory, Phytopharmaceutical development.

1. Abdel-Hameed ESS, Bazaid SA, Sabra AN, Salman MS. Antimicrobial activities of the methanol extract of Calotropis procera flowers and leaves against some pathogenic microorganisms. Life Sci J. 2012;9(4):1781–8. [Google Scholar] [Crossref]

2. Al-Dhabi NA, Balachandran C, Raj MK, Duraipandiyan V, Muthukumar C, Ignacimuthu S. Antimicrobial, antioxidant and cytotoxic properties of Calotropis gigantea and Calotropis procera from Saudi Arabia. J King Saud Univ Sci. 2015;27(2):105–12. [Google Scholar] [Crossref]

3. Al-Rowaily SL, Abd-ElGawad AM, Assaeed AM, Dar BA, Mohamed TA, Elshamy AI, El-Amier YA. Essential oil, phenolic profile, and biological activities of Calotropis procera (Aiton). Sci Rep. 2019;9:19963. [Google Scholar] [Crossref]

4. Al-Taweel AM, Perveen S, Fawzy GA, Khan SI, El-Feraly FS. Antibacterial diterpenes from the latex of Calotropis procera. Fitoterapia. 2006;77(6):531–6. [Google Scholar] [Crossref]

5. Ali AA, El-Baz FK, Aly HF, Mahmoud K, Mohamed AA. Antioxidant and hepatoprotective activities of Calotropis procera extract. Egypt J Biol. 2012;14:1–13. [Google Scholar] [Crossref]

6. Ali M, Ravinder E, Ramachandram R, Ahmed F, Shuaib M. Phytochemical investigation of the roots of Calotropis procera (Ait.) R. Br. Indian J Chem. 2001;40B:895–9. [Google Scholar] [Crossref]

7. Anwar F, Ahmad B, Ashraf M. Antibacterial activities of Calotropis procera root extract. Pak J Biol Sci. 2005;8(3):470–5. [Google Scholar] [Crossref]

8. Akinmoladun FO, Komolafe TR, Farombi EO. Neuroprotective potential of Calotropis procera in experimental models: A review. J Ethnopharmacol. 2019;244:112138. [Google Scholar] [Crossref]

9. Badria FA, El-Badry AA, Ameen M. Biologically active secondary metabolites from Calotropis procera. Nat Prod Res. 2012;26(19):1745–53. [Google Scholar] [Crossref]

10. Basu A, Chaudhuri P. Preliminary studies on the anti-inflammatory and analgesic activities of Calotropis procera root extract. J Ethnopharmacol. 1991;31(3):319–24. [Google Scholar] [Crossref]

11. Bawaskar PH, Bawaskar HS. Clinical profile of Calotropis procera poisoning. J Assoc Physicians India. 2012;60:52–4. [Google Scholar] [Crossref]

12. Chaturvedi A, Shukla S. Analgesic and antipyretic activities of ethanolic extract of Calotropis procera roots. Int J Pharm Sci Res. 2010;1(11):123–7. [Google Scholar] [Crossref]

13. Chundattu SJ, Joy JM, Paul B. Phytochemical screening and antimicrobial activity of Calotropis procera. Int J Pharm Pharm Sci. 2012;4(1):334–7. [Google Scholar] [Crossref]

14. Dey P, Chaudhuri TK. Pharmacological aspects of Calotropis procera (Ait.) R. Br. J Nat Remedies. 2014;14(2):81–97. [Google Scholar] [Crossref]

15. Dhankhar S, Kaur R, Ruhil S, Balhara M, Dhankhar S, Chhillar AK. A review on Calotropis procera Linn and its ethnobotanical relevance. Res J Med Plant. 2012;6(6):493–502. [Google Scholar] [Crossref]

16. El-Badry AA, Mohamed HM, Mahmoud K, Aly HF. Biochemical studies on anti-inflammatory and analgesic activity of Calotropis procera extract. J Appl Sci Res. 2013;9(8):5074–82. [Google Scholar] [Crossref]

17. El-Kamali HH. Therapeutic potential of Calotropis procera latex: A review. J Med Plants Res. 2010;4(16):1771–6. [Google Scholar] [Crossref]

18. Farahna M, Elkhidir IM. The antibacterial activity of latex of Calotropis procera. Sudan J Med Sci. 2008;3(3):205–8. [Google Scholar] [Crossref]

19. Gajalakshmi S, Vijayalakshmi S, Rajeswari R. Pharmacological activities of Calotropis procera: A review. Int J Pharm Pharm Sci. 2013;5(2):32–6. [Google Scholar] [Crossref]

20. Gupta R, Sharma V, Sharma R. Hepatoprotective activity of Calotropis procera root extract against paracetamol-induced liver damage in rats. Asian Pac J Trop Med. 2012;5(6):442–5. [Google Scholar] [Crossref]

21. Hassan A, Ahmed S, Al-Hazimi A. In vitro antioxidant activity of extracts of Calotropis procera flowers. Saudi J Biol Sci. 2015;22(5):502–7. [Google Scholar] [Crossref]

22. Iqbal Z, Lateef M, Jabbar A, Ghayur MN, Gilani AH. In vivo anthelmintic activity of Calotropis procera flowers against gastrointestinal nematodes of sheep. Vet Parasitol. 2005;127(3–4):237–44. [Google Scholar] [Crossref]

23. Kaur A, Kaur R, Kataria H. Wound healing activity of Calotropis procera root bark in rats. J Ethnopharmacol. 2011;133(3):751–4. [Google Scholar] [Crossref]

24. Kumar VL, Arya S. Medicinal uses and pharmacological properties of Calotropis procera. Int J Green Pharm. 2006;2(3):129–31. [Google Scholar] [Crossref]

25. Mahmoud K, El-Baz FK, Aly HF, Ali AA. Anti-inflammatory and analgesic activities of Calotropis procera extract. J Appl Sci Res. 2013;9(8):5074–82. [Google Scholar] [Crossref]

26. Mueen Ahmed KK, Rana AC, Dixit VK. Calotropis species (Asclepiadaceae) – A comprehensive review. Pharmacogn Mag. 2005;1(2):48–52. [Google Scholar] [Crossref]

27. Nenaah G. Antimicrobial activity of Calotropis procera and synergistic effect with antibiotics. Afr J Tradit Complement Altern Med. 2013;10(2):230–9. [Google Scholar] [Crossref]

28. Parihar G, Sharma A, Ghule S, Sharma P. Evaluation of analgesic activity of latex of Calotropis procera in albino mice. J Ethnopharmacol. 2012;139(2):563–7. [Google Scholar] [Crossref]

29. Raj V, Rai A, Varma A. Anti-inflammatory potential of Calotropis procera latex. Pharm Biol. 2011;49(12):1216–23. [Google Scholar] [Crossref]

30. Rathore K, Shekhawat N. Antimicrobial activity of root bark of Calotropis procera. J Med Plants Res. 2008;2(6):177–80. [Google Scholar] [Crossref]

31. Saadabi AM, Ayoub SM. Comparative antibacterial activity of Calotropis procera latex and extract. Res J Med Med Sci. 2009;4(2):170–4. [Google Scholar] [Crossref]

32. Saleem R, Ahmad M, Hussain SA, Qazi AM, Ahmad SI, Shamim A. Analgesic and anti-inflammatory effects of Calotropis procera extract in animal models. Phytother Res. 1999;13(4):275–7. [Google Scholar] [Crossref]

33. Santhosh Kumar M, Uma Maheswari TN, Ravichandran V. Wound healing and antimicrobial activities of Calotropis procera root bark extract. J Nat Med. 2010;64(3):406–12. [Google Scholar] [Crossref]

34. Senthilkumar M, Gurumoorthi P, Janardhanan K. Some medicinal plants used by Irular, the tribal people of Marudhamalai hills, Coimbatore, Tamil Nadu. Nat Prod Radiance. 2006;5(5):382–8. [Google Scholar] [Crossref]

35. Sharma P, Parmar J, Verma P, Goyal PK. Antitumor activity of Calotropis procera latex extract. Asian Pac J Cancer Prev. 2012;13(8):3809–14. [Google Scholar] [Crossref]

36. Shivkar YM, Kumar VL. Histamine mediates the proinflammatory effect of latex of Calotropis procera. Inflamm Res. 2003;52(3):154–9. [Google Scholar] [Crossref]

37. Singh B, Bani S, Gupta DK, Chandan BK, Kaul A. Anti-inflammatory activity of Calotropis procera latex. Phytother Res. 2000;14(6):452–4. [Google Scholar] [Crossref]

38. Tripathi AK, Shukla SK, Tripathi R, Singh RH. Wound healing activity of extracts of Calotropis procera root bark. Int J Pharm Pharm Sci. 2013;5(2):320–3. [Google Scholar] [Crossref]

39. Vetrivel U, Subramanian V. Molecular docking studies of bioactive compounds from Calotropis procera. Bioinformation. 2010;5(3):108–13. [Google Scholar] [Crossref]

40. Yelne MB, Sharma PC, Dennis TJ. Database on medicinal plants used in Ayurveda. Vol. 2. New Delhi: CCRAS; 2000. p. 70–3. [Google Scholar] [Crossref]

41. https://www.google.com/imgres?imgurl=https%3A%2F%2Fwww.cabidigitallibrary.org%2Fcms%2F10.1079%2Fcabicompendium.16847%2Fasset%2Fafb89db1-d3a8-4720-b90b-2c4ef0cf0bf5%2Fassets%2Fgraphic%2F16847_01.jpg&tbnid=Mi7s8gMFaeC1OM&vet=1&imgrefurl=https%3A%2F%2Fwww.cabidigitallibrary.org%2Fdoi%2Ffull%2F10.1079%2Fcabicompendium.16847&docid=Sbdul4g3H-yx-M&w=840&h=600&hl=en-US&source=sh%2Fx%2Fim%2Fm6%2F4&kgs=841947aaf92a672a&shem=isst [Google Scholar] [Crossref]

42. https://share.google/images/NuV1OjyEZjqPBT6t1 [Google Scholar] [Crossref]

• QbD Approach to Hplc Method Development and Validation of the Simultaneous Estimation of Sulbactum and Durlobactum in Pharmaceutical Dosage Form
• A Review on an Evaluation of a Liposomal Hydrogel for Combined Minoxidil and Tretinoin Delivery in Androgenetic Alopecia
• Qualitative Screening and Analysis of Lunasia amara Blanco (Tawal-ulad) Ethanolic Leaves Extract as Potential Anti-Angiogenic Inhibitors Using the Chorioallantoic Membrane Assay on Mallard Duck Embryo
• Formulation, Characterization and In-Vitro Evaluation of Curcumin Loaded Liposome for Colon Drug delivery
• Assessment of Phytochemical Constituents and Toxicity Profile of Trema Orientalis Leaves Extract.