Evaluation of HIV1 GP 120-CD4 Binding Inhibition Potentials of the Stem Bark Extracts of Diospyros mespiliformis

Abstract

The study was conducted to evaluate the HIV-1 gp120-CD4 binding inhibitory potential of crude aqueous, methanol, and petroleum ether extracts of Diospyros mespiliformis. The extracts were obtained by Soxhlet extraction. Phytochemical screening, gp120-CD4 binding inhibitory potential, and sub-acute toxicity tests were carried out using standard techniques. A total of six phyto-constituents were identified in the extracts: flavonoids, alkaloids, and balsams in the aqueous extract; flavonoids, alkaloids, tannins, balsams, steroids, and cardiac glycosides in the methanol extract; and flavonoids, alkaloids in the petroleum ether extract. Mean percentage inhibitions of the extracts of Diospyros mespiliformis against HIV-1 gp120-CD4 binding were recorded at various concentrations of the extracts, with 10% inhibition recorded at 125 µg/ml in the aqueous extract, 13% and 18% inhibitions recorded at 250 µg/ml and 125 µg/ml in the methanol extract respectively, while 3% inhibition was found in 125 µg/ml of the petroleum ether extract. Physical signs of toxicity such as weight changes, hair loss, diarrhea, and body weakness were observed in laboratory animals treated with 250 mg/kg and 125 mg/kg. There was no significant difference (P>0.05) in serum Aspartate Aminotransferase (AST) and Alkaline Phosphatase (ALP). No signs of inflammation were observed in the tissues of animals treated with any of the extracts. It can be concluded that the methanol extract possessed higher anti-gp120-CD4 binding activity and that the extracts were non-toxic to the animals.