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Anti-Plasmodial Activity of Some Zulu Medicinal Plants and of Some Triterpenes Isolated from Them
Department of Biochemistry & Microbiology, University of Zululand, Private Bag X1001, KwaDlangezwa 3886, South Africa
Department of Chemistry, University of Zululand, Private Bag X1001, KwaDlangezwa 3886, South Africa
Division of Pharmacology, University of Cape Town, Private Bag X3, Rondebosch 7701, South Africa
Discipline of Biochemistry, University of KwaZulu-Natal, Private Bag X54001, Durban 4000, South Africa
* Author to whom correspondence should be addressed.
Received: 6 August 2013; in revised form: 16 September 2013 / Accepted: 24 September 2013 / Published: 8 October 2013
Abstract: Mimusops caffra E. Mey. ex A.DC and Mimusops obtusifolia Lam (both members of the Sapotaceae family), and Hypoxis colchicifolia Bak (family Hypoxidaceae) are used by traditional healers in Zululand to manage malaria. Anti-plasmodial investigation of the crude extracts and some triterpenes isolated from the plants showed activity against a chloroquine sensitive (CQS) strain of Plasmodium falciparum (D10). Among the crude extracts the leaves of M. caffra exhibited the highest activity, with an IC50 of 2.14 μg/mL. The pentacyclic tritepenoid ursolic acid (1), isolated from the leaves of M. caffra was the most active compound (IC50 6.8 μg/mL) as compared to taraxerol (2) and sawamilletin (3) isolated from the stem bark of M. obtusifolia (IC50 > 100). Chemical modification of the ursolic acid (1) to 3β-acetylursolic acid (4) greatly enhanced its anti-plasmodial activity. Compound 4 reduced parasitaemia against Plasmodium berghei by 94.01% in in vivo studies in mice. The cytotoxicity of 3β-acetylursolic acid (IC50) to two human cell lines (HEK293 and HepG2) was 366.00 μg/mL and 566.09 μg/mL, respectively. The results validate the use of these plants in folk medicine.
Keywords: Plasmodium falciparum; Mimusops caffra; Mimusops obtusifolia; Hypoxis colchicifolia; ursolic acid
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Simelane, M.B.C.; Shonhai, A.; Shode, F.O.; Smith, P.; Singh, M.; Opoku, A.R. Anti-Plasmodial Activity of Some Zulu Medicinal Plants and of Some Triterpenes Isolated from Them. Molecules 2013, 18, 12313-12323.
Simelane MBC, Shonhai A, Shode FO, Smith P, Singh M, Opoku AR. Anti-Plasmodial Activity of Some Zulu Medicinal Plants and of Some Triterpenes Isolated from Them. Molecules. 2013; 18(10):12313-12323.
Simelane, Mthokozisi B.C.; Shonhai, Addmore; Shode, Francis O.; Smith, Peter; Singh, Mogie; Opoku, Andy R. 2013. "Anti-Plasmodial Activity of Some Zulu Medicinal Plants and of Some Triterpenes Isolated from Them." Molecules 18, no. 10: 12313-12323.