Xanthones and benzophenones isolated from the endophytic fungus Penicillium sp. ct-28 of Corydlis tomentella and their cytotoxic activity

Ming, Qianliang ¹Li, Yunong ¹Jiang, Xiuxing ¹Huang, Xiuning ¹He, Yimo ¹Qin, Lingyue ¹Liu, Yanxia ¹Tang, Yu ¹Gao, Ning¹

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作者信息

1. Army Med Univ
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Abstract

One new xanthone, griseophenexanthone A (1), one new benzophenone, digriseophene A (2), and 14 previously reported compounds were isolated from the culture of Penicillium sp. ct-28, an endophytic fungus of Corydlis tomentella. The structures of the isolated compounds were identified by an extensive analysis of HRESIMS, 1D and 2D NMR. MTT assay showed that six xanthones (1 and 3-7) significantly inhibited cell proliferation in four cancer cell lines, with IC50 values ranging from 18.12 +/- 2.42 to 85.55 +/- 7.66 mu M. Our results showed that slight structural changes led to obvious activity differences among these compounds. We also investigated the effects of the six xanthones on cell cycle and apoptosis in human hepatoma HepG2 cells. Compound 7 caused cell cycle arrest at G1 phase, compounds 5 and 6 caused cell cycle arrest at S phase, whereas compounds 1, 3 and 4 had no effects on cell cycle distribution. All six xanthones induced apoptosis in dose-dependent manners in HepG2 cells accompanied by degradation of PARP and activation of caspase 3. The structure-activity relationship analysis revealed that the effects of these xanthones on cell cycle and apoptosis in HepG2 cells were closely related to the substituent groups on their skeleton. Our studies provide novel insights for the structural optimization of xanthones in the development of new anticancer drugs.

Key words

Corydlis tomentella/Penicillium sp./Xanthones/Benzophenones/Cytotoxic activity/METABOLITES/DERIVATIVES/PATHWAY

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出版年

2022

Fitoterapia

SCI

ISSN：0367-326X

被引量4

参考文献量24

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