通过调节PI3K/AKT和线粒体凋亡通路,从细粒曲霉中提取的emstrin型表多硫代二氧哌嗪具有细胞毒活性

IF 4.8 3区 化学 Q1 CHEMISTRY, MEDICINAL
Pengkun Li, Qin Li, Aimin Fu, Yang Xiao, Chunmei Chen, Hucheng Zhu, Changxing Qi, Wei Wei, Yuan Zhou, Yonghui Zhang
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引用次数: 0

摘要

从细粒曲霉中分离得到5种新型eppolythiiodioxopiperazines (ETPs), preylemestrins C−G(1-5),以及2种已知ETPs, preylemestrin A(6)和preylemestrin B(7)。通过光谱数据、x射线晶体学数据、ECD比较和计算对其结构进行了表征。Prenylemestrins C−G(1−5)是一类罕见的etp,其特征是2,5-二硫代-7,9-重氮杂环[4.2.2]癸烷-8,10-二酮核心包含半萜部分。值得注意的是,化合物6表现出中等的细胞毒性,通过调节PI3K/AKT信号通路和线粒体凋亡机制,诱导L1210细胞G2/M细胞周期阻滞和凋亡。图形抽象
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Emestrin-type epipolythiodioxopiperazines from Aspergillus nidulans with cytotoxic activities by regulating PI3K/AKT and mitochondrial apoptotic pathways

Five novel emestrin-type epipolythiodioxopiperazines (ETPs), prenylemestrins C−G (15), 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.

Graphical Abstract

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来源期刊
Natural Products and Bioprospecting
Natural Products and Bioprospecting CHEMISTRY, MEDICINAL-
CiteScore
8.30
自引率
2.10%
发文量
39
审稿时长
13 weeks
期刊介绍: Natural Products and Bioprospecting serves as an international forum for essential research on natural products and focuses on, but is not limited to, the following aspects: Natural products: isolation and structure elucidation Natural products: synthesis Biological evaluation of biologically active natural products Bioorganic and medicinal chemistry Biosynthesis and microbiological transformation Fermentation and plant tissue cultures Bioprospecting of natural products from natural resources All research articles published in this journal have undergone rigorous peer review. In addition to original research articles, Natural Products and Bioprospecting publishes reviews and short communications, aiming to rapidly disseminate the research results of timely interest, and comprehensive reviews of emerging topics in all the areas of natural products. It is also an open access journal, which provides free access to its articles to anyone, anywhere.
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