[11]-chaetoglobosins with cytotoxic activities from Pseudeurotium bakeri

Authors：Duan, Fangfang; Gao, Ying; Peng, Xiaogang; Meng, Xianggao; Chang, Jinling; Gan, Yutian; Ouyang, Qianxi; Ruan, Hanli^*

Source：Bioorganic Chemistry, 2022, 127: 106011.

DOI：10.1016/j.bioorg.2022.106011

• [11]-chaetoglobosins
• Pseudeurotium bakeri P1-1-1
• G2
• M cell cycle arrest
• apoptosis
• cyclin B1
• Cdk1
• Bcl-2
• caspase-3
• PARP pathway

Fourteen new [11]-chaetoglobosins (1-14), along with two known congeners, cytochalasins X and Y (15 and 16), were isolated from the cultures of an endophytic fungus Pseudeurotium bakeri P1-1-1. Their structures incorporating absolute configurations were elucidated based on the comprehensive analyses of one- and twodimensional NMR data, HRESIMS spectrometry, chemical methods, and single-crystal X-ray diffraction analysis (Cu K alpha). All isolates were evaluated for their cytotoxic activities and chaetopseudeurin M (1) displayed significant cytotoxic effects against seven human cancer cell lines, with IC50 values ranging from 5.1 +/- 0.9 to 10.8 +/- 0.1 mu M. Western blot experiments exhibited that compound 1 exerted its cytotoxic effect in MCF-7 cells by inducing G2/M cell cycle arrest and apoptosis via downregulating the expression of cyclin B1 and Cdk1, and activating Bcl-2/caspase-3/PARP pathway, respectively.

• Institution
  华中科技大学