Aaptamine derivatives with antifungal and Anti-HIV-1 activities from the South China Sea sponge Aaptos aaptos

Abstract

Five new alkaloids of aaptamine family, compounds ( 1-5) and three known derivatives (6-8), have been isolated from the South China Sea sponge Aaptos aaptos . The structures of all compounds were unambiguously elucidated by spectroscopic analyses, as well as by comparison with the literature data. Compounds 1-2 are characterized with triazapyrene lactam skeleton, whereas compounds 4-5 share an imidazole-fused aaptamine moiety. These compounds were evaluated in antifungal and anti-HIV-1 assays. Compounds 3, 7, and 8 showed antifungal activity against six fungi, with MIC values in the range of 4 to 64 μg/mL. Compounds 7-8 exhibited anti-HIV-1 activity, with inhibitory rates of 88.0% and 72.3%, respectively, at a concentration of 10 μM.