Equisetin and a novel opposite stereochemical homolog phomasetin, two fungal metabolites as inhibitors of HIV-1 integrase

Article abstract of DOI:10.1016/S0040-4039(98)00269-X

Integration is an essential step in HIV replication and is catalyzed by an enzyme called integrase. We have isolated equisetin (1a), and a novel opposite stereochemical homolog, phomasetin (2a), from Fusarium heterosporum and a Phoma sp. respectively. They inhibit the invitro recombinant integrase enzyme with IC₅₀ values of 7-20 μM. Unlike known inhibitors, these compounds also inhibit the integration reactions catalyzed by preintegration complexes isolated from HIV-1 infected cells.