Key Laboratory of Marine Biogenetic Resources, Third Institute of Oceanography, Ministry of Natural Resources, 184 Daxue Road, Xiamen 361005, People's Republic of China.
College of Pharmaceutical Sciences, Zhejiang Chinese Medical University, 548 Binwen Road, Hangzhou 310053, People's Republic of China.
J Nat Prod. 2020 Apr 24;83(4):1157-1166. doi: 10.1021/acs.jnatprod.9b01165. Epub 2020 Mar 20.
Eight new nitrogenated azaphilones (-) and two known compounds (chaetoviridin A and chaetoviridin E, , ) were isolated from the culture of the deep-sea-derived fungus MP4-S01-7. The absolute configurations of new compounds were elucidated by HSQC-HECADE NMR data, -based configuration analysis, and modified Mosher's method and finally verified by comparison of recorded and computed NMR chemical shifts from quantum chemical calculations coupled with a statistical procedure (DP4+). All of the compounds were evaluated for their cytotoxicities against the gastric cancer cell lines MGC803 and AGS, and most of them showed significant inhibition on cancer cell viability at 10 μM. Among them, compounds , , and exerted the most potent cytotoxic activities, with IC values less than 1 μM. Further studies showed that compound inhibited cell cycle progression, and both compounds and induced apoptosis of gastric cancer cells in a concentration-dependent manner.
从深海来源真菌 MP4-S01-7 的培养物中分离得到了 8 个新的氮杂菲酮(-)和 2 个已知化合物(chaetoviridin A 和 chaetoviridin E,,)。新化合物的绝对构型通过 HSQC-HECADE NMR 数据、基于的构型分析以及改进的 Mosher 法确定,并最终通过量子化学计算与统计程序(DP4+)结合比较记录和计算的 NMR 化学位移来验证。所有化合物均评估了其对胃癌细胞系 MGC803 和 AGS 的细胞毒性,大多数化合物在 10 μM 时对癌细胞活力表现出显著的抑制作用。其中,化合物、和表现出最强的细胞毒活性,IC 值小于 1 μM。进一步的研究表明,化合物抑制细胞周期进程,化合物和均以浓度依赖的方式诱导胃癌细胞凋亡。