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

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. Com...

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Bibliographic Details
Published in:Marine drugs 2014-12, Vol.12 (12), p.6003-6013
Main Authors: Yu, Hao-Bing, Yang, Fan, Sun, Fan, Li, Jing, Jiao, Wei-Hua, Gan, Jian-Hong, Hu, Wen-Zhen, Lin, Hou-Wen
Format: Article
Language:English
Subjects:
aaptamine
Aaptos aaptos
Alkaloids - chemistry
Alkaloids - pharmacology
Animals
Anti-HIV Agents - chemistry
Anti-HIV Agents - pharmacology
anti-HIV-1 activity
antifungal
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
China
Fungi - drug effects
HIV-1 - drug effects
Marine
Naphthyridines - chemistry
Naphthyridines - pharmacology
Porifera - chemistry
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Summary: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.
ISSN:1660-3397
1660-3397
DOI:10.3390/md12126003