Azaphilones with anti-colon cancer activities from the plant endophytic fungus Talaromyces primulinus WZ-883

被引:4
作者
Gong, Yuan-Xiang [1 ]
Li, Xin [1 ]
Shi, Li-Yuan [1 ]
Feng, Li [1 ]
Wang, Jing-Wen
Tan, Ning-Hua [1 ]
Wang, Zhe [1 ]
机构
[1] China Pharmaceut Univ, Sch Tradit Chinese Pharm, State Key Lab Nat Med, Nanjing 211198, Peoples R China
基金
中国国家自然科学基金;
关键词
Pseudostellaria heterophylla; Caryophyllaceae; Talaromyces primulinus; Trichocomaceae; Azaphilones; Anti-colon cancer activities; COLORECTAL-CANCER; PSEUDOSTELLARIA-HETEROPHYLLA; 5-FLUOROURACIL TOXICITY; NATURAL-PRODUCT; A-D; CHEMISTRY; CYCLOPEPTIDES; METABOLITES; APOPTOSIS;
D O I
10.1016/j.phytol.2023.08.006
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Two new bulgarialactones of azaphilones named talaroilones A and B (1 and 2), together with four known azaphilones (3-6), were isolated and characterized from the endophytic fungus Talaromyces primulinus WZ-883. Their structures were elucidated by extensive spectroscopic analysis and computational methods. All isolated compounds were evaluated for their cytotoxicities, and the results showed that 6 possessed the most potent inhibitory effect against colorectal cancer cells with an IC50 value of 4.17 & mu;M (HCT116). Compound 6 also strikingly induced apoptosis and autophagic cell death in HCT116 cells. Moreover, the transcriptome analysis of 6-treated HCT116 cells were performed, and differentially expressed genes were identified. Besides, the MAPK and mTOR signaling pathways were regulated by 6. This work obtained six azaphilones containing two new ones, and clarified the anti-tumor activity and mechanism of 6 against CRC (Colorectal cancer) cells for the first time, which will contribute to the future development of 6 as a novel therapeutic leading compound for CRC.
引用
收藏
页码:115 / 125
页数:11
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