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. 2014 Dec 16;12(12):6003-13.
doi: 10.3390/md12126003.

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

Hao-Bing Yu  1 , Fan Yang  2 , Fan Sun  3 , Jing Li  4 , Wei-Hua Jiao  5 , Jian-Hong Gan  6 , Wen-Zhen Hu  7 , Hou-Wen Lin  8
Affiliations

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

Hao-Bing Yu et al. Mar Drugs. .

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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Figures

Figure 1
Figure 1
COSY, HMBC and selected NOESY correlations of compounds 1, 3, and 4.
Figure 2
Figure 2
Structures of compounds 1–8.
See this image and copyright information in PMC

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