Journal
MARINE DRUGS
Volume 12, Issue 12, Pages 6003-6013Publisher
MDPI AG
DOI: 10.3390/md12126003
Keywords
Aaptos aaptos; aaptamine; antifungal; anti-HIV-1 activity
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Funding
- National Natural Science Fund for Distinguished Young Scholars of China [81225023]
- National Natural Science Fund of China [41476121, 81072573, 81302691, 81172978, 81373321, 41106127]
- Innovation Program of Shanghai municipal Education Commission [14YZ037]
- National High Technology Research and Development Program of China (863 Projects) [2013AA092902]
- [12XD1400200]
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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 mu g/mL. Compounds 7-8 exhibited anti-HIV-1 activity, with inhibitory rates of 88.0% and 72.3%, respectively, at a concentration of 10 mu M.
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