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<p>Five novel emestrin-type epipolythiodioxopiperazines (ETPs), prenylemestrins C−G (<b>1</b>–<b>5</b>), along with two known ETPs, prenylemestrin A (<b>6</b>) and prenylemestrin B (<b>7</b>), were obtained from <i>Aspergillus nidulans</i>. Their structures were characterized by spectroscopic data, X-ray crystallographic data, ECD comparisons and calculations. Prenylemestrins C−G (<b>1</b> − <b>5</b>) represent a&#xa0;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 <b>6</b> 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.</p> Graphical Abstract <p></p>

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Emestrin-type epipolythiodioxopiperazines from Aspergillus nidulans with cytotoxic activities by regulating PI3K/AKT and mitochondrial apoptotic pathways

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年3月10日

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  • Pengkun Li,
  • Qin Li,
  • Aimin Fu,
  • Yang Xiao,
  • Chunmei Chen,
  • Hucheng Zhu,
  • Changxing Qi,
  • Wei Wei,
  • Yuan Zhou,
  • Yonghui Zhang

摘要

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.

Graphical Abstract