Aaptamine Derivatives with Antifungal and Anti-HIV-1 Activities from the South China Sea Sponge Aaptos aaptos |
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| Authors: | Hao-Bing Yu Fan Yang Fan Sun Jing Li Wei-Hua Jiao Jian-Hong Gan Wen-Zhen Hu Hou-Wen Lin |
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| Affiliation: | 1Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China; E-Mails: (H.-B.Y.); (J.-H.G.);2Marine Drugs Research Center, Department of Pharmacy, State Key Laboratory of Oncogenes and Related Genes, Renji Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai 200127, China; E-Mails: (F.Y.); (F.S.); (J.L.); (W.-H.J.); (W.-Z.H.) |
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| 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. |
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| Keywords: | Aaptos aaptos aaptamine antifungal anti-HIV-1 activity |
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