In vitro anti-HIV and cytotoxic effects of pure compounds isolated from Croton macrostachyus Hochst. Ex Delile.
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is an important plant in traditional African medicine, widely utilized to treat a variety of diseases. In Kenya, HIV-infected patients use leaf and root decoctions of the plant as a cure for cough, back pain, bleeding, skin diseases, warts, pneumonia, and wounds. This study aimed to evaluate the anti-HIV activities and cytotoxic effects of extracts and chemical constituents isolated from In our previous study we demonstrated that the hexane, CH Cl , ethyl acetate and methanol soluble fractions of a 1:1 CH Cl /MeOH crude extracts of the leaves and stem bark of exhibited potent anti-HIV activities against HIV-1 with IC values ranging from 0.02–8.1 μg/mL and cytotoxicity effects against MT-4 cells ranging from IC = 0.58–174 μg/mL Hence, hexane soluble extract of 1:1 CH Cl /MeOH crude extract of the leaves of that was more potent against HIV-1 at IC = 0.02 μg/mL was subjected to column chromatography leading to the isolation of 2-methoxy benzyl benzoate (1), lupenone (2), lupeol acetate (3), betulin (4), lupeol (5), sitosterol (6) and stigmasterol (7). Lupenone (2), lupeol acetate (3) and betulin (4) exhibited anti-HIV-1 inhibition at IC = 4.7 nM, 4.3 and 4.5 μg/mL respectively. The results obtained from this study support the potential of as a source of anti-HIV constituents.
