Isochromophilones A-F, Cytotoxic Chloroazaphilones from the Marine Mangrove Endophytic Fungus Diaporthe sp SCSIO 41011
Isochromophilones A-F, Cytotoxic Chloroazaphilones from the Marine Mangrove Endophytic Fungus Diaporthe sp SCSIO 41011
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DOI：
10.1021/acs.jnatprod.7b01053
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发表时间：
2018-04-01
影响因子：
5.1
通讯作者：
Liu, Yonghong
中科院分区：
文献类型：
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作者：
Luo, Xiaowei;Lin, Xiuping;Liu, Yonghong
从红树林衍生真菌Diaporthe sp. SCSIO 41011中获得了六种新的高度氧化的氯氮杂菲酮衍生物，异色素A-F（1-6），以及六种已知的类似物（7-12）。化合物1-6的结构（包括绝对构型）通过详细的NMR、MS光谱分析和电子圆二色谱确定。化合物1和2代表了首次报道的在C-6处缺少羰基的azaphilones。化合物8显示出对三种肾癌细胞系ACHN、OS-RC-2和786-O细胞的细胞毒活性，IC 50值为3.0 - 4.4 μ M，化合物4显示出对786-O细胞的活性，IC 50为8.9 μ M。进一步的研究表明，4以剂量和时间依赖的方式诱导786-O细胞凋亡。
Six new highly oxygenated chloroazaphilone derivatives, isochromophilones A-F (1-6), were obtained from the mangrove-derived fungus Diaporthe sp. SCSIO 41011, together with six known analogues (7-12). The structures of 1-6 including absolute configurations were determined by detailed NMR, MS spectroscopic analyses, and electronic circular dichroism spectra. Compounds 1 and 2 represent the first reported azaphilones lacking a carbonyl group at C-6. Compound 8 exhibited cytotoxic activities against three renal carcinoma cell lines, ACHN, OS-RC-2, and 786-O cells, with IC50 values ranging from 3.0 to 4.4 mu M, and 4 showed activity against 786-O cells with an ICso of 8.9 mu M. Further studies indicated that 4 induced apoptosis in 786-O cells in a dose- and time-dependent manner.