| ORIGINAL ARTICLES |
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Emestrin-type epipolythiodioxopiperazines from Aspergillus nidulans with cytotoxic activities by regulating PI3K/AKT and mitochondrial apoptotic pathways |
| Pengkun Li1, Qin Li1, Aimin Fu1, Yang Xiao1, Chunmei Chen1, Hucheng Zhu1, Changxing Qi1, Wei Wei2, Yuan Zhou1, Yonghui Zhang1 |
1. 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;
2. China National Center for Biotechnology Development, Beijing, 100039, People's Republic of China |
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Abstract 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.
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| Keywords
Aspergillus nidulans
Epipolythiodioxopiperazines
Thioethanothio bridge
Structural elucidation
Cytotoxicity
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| Fund:National Natural Science Foundation of China (U22A20380, 82173706, 82104028) and Fundamental Research Funds for the Central Universities (2024BRA018) financially supported this project. |
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Corresponding Authors:
Wei Wei, E-mail:weiwei@cncbd.org.cn;Yuan Zhou, E-mail:zhouyuan@hust.edu.cn;Yonghui Zhang, E-mail:zhangyh@mails.tjmu.edu.cn
E-mail: weiwei@cncbd.org.cn;zhouyuan@hust.edu.cn;zhangyh@mails.tjmu.edu.cn
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Issue Date: 17 May 2025
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