Aspernigrins with anti-HIV-1 activities from the marine-derived fungus Aspergillus niger SCSIO Jcsw6F30

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• 作者：Xuefeng Zhou^a ; ^&dagger ; ; Wei Fang^b ; ^&dagger ; ; Suiyi Tan^c ; ^&dagger ; ; Xiuping Lin^a ; Tianrong Xun^c ; Bingjie Yang^a ; ^c ; Shuwen Liu^c ; ^{liusw@smu.edu.cn" class="auth_mail" title="E-mail the corresponding author} ; Yonghong Liu^a ; ^{yonghongliu@scsio.ac.cn" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Aspergillus niger ; Aspernigrins ; Malformin C ; HIV-1 SF162
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 January 2016
• 年：2016
• 卷：26
• 期：2
• 页码：361-365
• 全文大小：712 K

文摘

Two new 2-benzylpyridin-4-one containing metabolites, aspernigrins C (3) and D (4), together with six known compounds (1, 2, and 5–8), were isolated from the marine-derived fungus Aspergillus niger SCSIO Jcsw6F30. The structures of the new compounds were determined by NMR, MS, and optical rotation analyses. All the isolated compounds were evaluated for their inhibitory activities against infection with HIV-1 SF162 in TZM-bl cells. Malformin C (5) showed the strongest anti-HIV-1 activity with IC₅₀ of 1.4 ± 0.06 μM (selectivity index, 11.4), meanwhile aspernigrin C (3) also exhibited potent activity with IC₅₀ of 4.7 ± 0.4 μM (selectivity index, 7.5).