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Open AccessArticle

Aaptamine Derivatives with Antifungal and Anti-HIV-1 Activities from the South China Sea Sponge Aaptos aaptos

Laboratory of Marine Drugs, Department of Pharmacy, Changzheng Hospital, Second Military Medical University, Shanghai 200003, China
Marine 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
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Mar. Drugs 2014, 12(12), 6003-6013;
Received: 15 October 2014 / Revised: 3 November 2014 / Accepted: 2 December 2014 / Published: 16 December 2014
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Five new alkaloids of aaptamine family, compounds (15) and three known derivatives (68), 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 12 are characterized with triazapyrene lactam skeleton, whereas compounds 45 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 78 exhibited anti-HIV-1 activity, with inhibitory rates of 88.0% and 72.3%, respectively, at a concentration of 10 μM. View Full-Text
Keywords: Aaptos aaptos; aaptamine; antifungal; anti-HIV-1 activity Aaptos aaptos; aaptamine; antifungal; anti-HIV-1 activity

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Yu, H.-B.; Yang, F.; Sun, F.; Li, J.; Jiao, W.-H.; Gan, J.-H.; Hu, W.-Z.; Lin, H.-W. Aaptamine Derivatives with Antifungal and Anti-HIV-1 Activities from the South China Sea Sponge Aaptos aaptos. Mar. Drugs 2014, 12, 6003-6013.

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