来自构巢曲霉的具有细胞毒性活性的埃默菌素型环多硫代二氧哌嗪，通过调节PI3K/AKT和线粒体凋亡途径发挥作用。
Emestrin-type epipolythiodioxopiperazines from Aspergillus nidulans with cytotoxic activities by regulating PI3K/AKT and mitochondrial apoptotic pathways.
作者信息
Li Pengkun, Li Qin, Fu Aimin, Xiao Yang, Chen Chunmei, Zhu Hucheng, Qi Changxing, Wei Wei, Zhou Yuan, Zhang Yonghui
机构信息
Hubei Key Laboratory of Natural Medicinal Chemistry and Resource Evaluation, School of Pharmacy, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430030, People's Republic of China.
China National Center for Biotechnology Development, Beijing, 100039, People's Republic of China.
出版信息
Nat Prod Bioprospect. 2025 Mar 10;15(1):17. doi: 10.1007/s13659-025-00498-8.
Five novel emestrin-type epipolythiodioxopiperazines (ETPs), prenylemestrins C-G (1-5), along with two known ETPs, prenylemestrin A (6) and prenylemestrin B (7), were obtained from Aspergillus nidulans. Their structures were characterized by spectroscopic data, X-ray crystallographic data, ECD comparisons and calculations. Prenylemestrins C-G (1 - 5) represent a rare class of ETPs, characterized by a 2,5-dithia-7,9-diazabicyclo[4.2.2]decane-8,10-dione core involving a hemiterpene moiety. Notably, compound 6 exhibited moderate cytotoxicity, inducing G2/M cell cycle arrest and apoptosis of L1210 cells by regulating the PI3K/AKT signaling pathway and mitochondrial apoptotic mechanisms.
从构巢曲霉中获得了5种新型孕甾烯型环多硫代二氧哌嗪（ETP），即异戊烯基孕甾烯C-G（1-5），以及2种已知的ETP，异戊烯基孕甾烯A（6）和异戊烯基孕甾烯B（7）。通过光谱数据、X射线晶体学数据、电子圆二色光谱（ECD）比较和计算对它们的结构进行了表征。异戊烯基孕甾烯C-G（1-5）代表一类罕见的ETP，其特征是具有一个包含半萜部分的2,5-二硫代-7,9-二氮杂双环[4.2.2]癸烷-8,10-二酮核心。值得注意的是，化合物6表现出中等细胞毒性，通过调节PI3K/AKT信号通路和线粒体凋亡机制诱导L1210细胞的G2/M期细胞周期阻滞和凋亡。
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