Ijeoma Solomon Okoro
Federal University of Agriculture, Nigeria
Title: Screening of Anthocleista djalonesis Fractions and Compounds against HIV-1 Integrase and HIV-1 Protease
Biography
Biography: Ijeoma Solomon Okoro
Abstract
HIV, the virus that causes AIDS, is one of the world’s deadliest diseases today. Drug resistance and narrow spectrum of available therapeutics is a main problem during HIV treatment. Therefore, new drugs effective against drug-resistant HIV strains are needed. The aim of this study was to screen Anthocleista djalonensis extracts, fractions and isolated compounds for in vitro anti-HIV-1 Integrase (HIV-1 IN) and HIV-1 Protease (HIV -1PR) activities. The ethyl acetate and acetone extracts of the roots of Anthocleista djalonensis and fractions and compounds obtained from column chromatography of acetone extract were screened for their inhibitory activity against HIV -1 Integrase using a non-radioactive ELISA-based HIV-1 integrase assay. The screening was carried out at concentration range of 10-5-102 ug/ml. The screening for anti-protease activity was performed using a fluorogenic octapeptide substrate, HIV-FRET (1) and a recombinant HIV-1 Protease solution. The ethyl acetate and acetone extracts showed inhibitoryeffects on HIV -1 Integrase with IC50 of 1.3001 ± 0.217 μg/mL and 0.7216 ± 0.0028 μg/mL respectively. IC50 values of 0.0077 ± 0.009 μg/mL, 5.0001± 0.1719 μg/mL, 3.5113 ± 0.3613 μg/mL and 0.0736 ± 0.0005 μg/ml were obtained for chromatographic fractions F-1, F-2, F-3 and F-4 respectively. The compounds Bauerenone, Bauerenol and a mixture of Stigmasterol and β-Sitosterol isolated from A. djalonensis had IC50 values of 5.6112 ± 0.8767 μg/mL, 4.8075 ± 0.0732 μg/mL and 0.8916 ± 0.0327 respectively. Bauerenone, Bauerenol and a mixture of Stigmasterol and β-Sitosterol isolated from A. djalonensis showed significant (P< 0.05) inhibitory activities against HIV-1 Integrase. However, there was no activity against HIV-1 protease at 50 μg/mL by the extracts, fractions and isolated compounds.