Further screening of Venda medicinal plants for activity against HIV type 1 reverse transcriptase and integrase

Abstract

The use of medicinal plants for AIDS-related conditions is common in South Africa. In order to establish an antiviral rationale for the use of these plants we screened fractions of the methanol extracts of medicinal plants for activity against HIV-1 reverse transcriptase (RT) and integrase (IN). The n-butanol fraction obtained from the crude methanol extracts of the roots of Bridelia micrantha (Hochst) Baill. (Euphorbiaceae) was observed to be as the most active inhibiting the RNA-dependent-DNA polymerization (RDDP) activity of HIV-1 RT with an IC50 of 7.3 g/ml. However, it had no activity on the 3’-end processing activity of HIV integrase. Bioassay-guided fractionation of the n-butanol fraction yielded friedelin and -sistosterol, which did not inhibit the RDDP of RT or 3’-end processing functions of IN even at a concentration of 500 M. An uncharacterized fraction obtained in the bioassay-guided fractionating process inhibited the RDDP with an IC50 of 9.6 g/ml, but had no inhibition on IN. Phytochemical screening indicated the presence of flavonoids and tannins in the uncharacterized fraction.

Key words: HIV-1; reverse transcriptase; integrase; medicinal plants; inhibition; Venda; South Africa