Anti-Plasmodial Activity of Some Zulu Medicinal Plants and of Some Triterpenes Isolated from Them

作者：Simelane Mthokozisi B C^*; Shonhai Addmore; Shode Francis O; Smith Peter; Singh Moganavelli; Opoku Andy R

来源：Molecules, 2013, 18(10): 12313-12323.

DOI：10.3390/molecules181012313

• Plasmodium falciparum
• Mimusops caffra
• Mimusops obtusifolia
• Hypoxis colchicifolia
• ursolic acid

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 mu g/mL. The pentacyclic tritepenoid ursolic acid (1), isolated from the leaves of M. caffra was the most active compound (IC50 6.8 mu g/mL) as compared to taraxerol (2) and sawamilletin (3) isolated from the stem bark of M. obtusifolia (IC50 %26gt; 100). Chemical modification of the ursolic acid (1) to 3 beta-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 3 beta-acetylursolic acid (IC50) to two human cell lines (HEK293 and HepG2) was 366.00 mu g/mL and 566.09 mu g/mL, respectively. The results validate the use of these plants in folk medicine.

• 出版日期2013-10