np7b01053_si_001.pdf (14.48 MB)

Isochromophilones A–F, Cytotoxic Chloroazaphilones from the Marine Mangrove Endophytic Fungus Diaporthe sp. SCSIO 41011

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journal contribution
posted on 08.03.2018, 16:13 by Xiaowei Luo, Xiuping Lin, Huaming Tao, Junfeng Wang, Jiayi Li, Bin Yang, Xuefeng Zhou, Yonghong Liu
Six new highly oxygenated chloroazaphilone derivatives, isochromophilones A–F (16), were obtained from the mangrove-derived fungus Diaporthe sp. SCSIO 41011, together with six known analogues (712). The structures of 16 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 μM, and 4 showed activity against 786-O cells with an IC50 of 8.9 μM. Further studies indicated that 4 induced apoptosis in 786-O cells in a dose- and time-dependent manner.