ABSTRACT
OBJECTIVE: To investigate the HIV-1 integrase inhibitory activity of endophytic fungi from medicinal plant Aquilaria sinensis (Lour.) Gilg. METHODS: HIV-1 integrase inhibitory activity of the isolated endophytic fungi was determined by HIV-1 integrase strand transfer inhibitory activity assay, and the active metabolites of the endophytic fungi with the greatest potential were studied by activity tracking. RESULTS: Among 78 strains of endophytic fungi isolated from A. sinensis, nine strains (11.54%) showed strong inhibitory activity against HIV-1 integrase. Three compounds were obtained from the fermentation of strain HN-AS-8 which was identified to be Chaetomium globosum by HIV-1 integrase strand reaction. Compound 1 inhibited HIV-1 integrase with IC50 value of 35.4 μmol · L-1, and compounds 1 and 3 were for the first time isolated from Chaetomium sp. CONCLUSION: Potential anti-HIV-1 metabolites exist in the endophytic fungi from A. sinensis, which can be new resources for new anti-AIDS drugs.