Newly Synthesized Citral Derivatives Serve as Novel Inhibitor in HepG2 Cells

文献类型： 外文期刊

第一作者： Gao, Wei

作者： Gao, Wei;Hua, Xiaoju;Yang, Haikuan;Chi, Yunyang;Liao, Shengliang;Hu, Lifang;Xiahou, Zhikai

作者机构：

关键词： Citral; Derivative; HepG2 liver cancer cell; Cell apoptosis; Anti-cancer

期刊名称：CHEMISTRYOPEN （ 影响因子：3.1； 五年影响因子：2.8 ）

ISSN： 2191-1363

年卷期： 2025 年 14 卷 4 期

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收录情况： SCI

摘要： 2H-pyran compound 1 synthesized from 6-methylpyridine-2,4-diol and citral, has been used for Cu-catalyzed N-arylation with a range of arylboric acids to obtain arylated pyranopyridine core structure derivatives (yield up to 77 %). Among them, compound 3 h exhibited a much better inhibitory effect on HepG2 liver cancer cells compared to citral, and the IC50 value was 5.3 mu M following exposure with the newly synthesized derivatives (herein named 3 h for short in this paper), which was lower than that of the cisplatin (6.5 mu M). Meanwhile, the cell-cycle arrest of HepG2 cells occurred in the S phase, and the apoptosis of HepG2 cells was significantly increased with increasing drug concentration. In addition, real-time fluorescence quantification PCR and Western blotting experiments showed that the expression of apoptotic protein BAX was increased, while the expression of anti-apoptotic protein BCL2 was inhibited in a dose-dependent fashion. The results of these experiments indicated that apoptosis was promoted in HepG2 cells via apoptotic signaling pathway activated by 3 h. Furthermore, 3 h effectively decreased the phosphorylation levels of PI3 K, ATK and ERK, resulting in the inhibitions of MAPK/ERK and PI3 K/ATK signaling pathways. Briefly, 3 h has been found to show inhibitory effects on the survival of HepG2 liver cancer cells and may be used as anti-cancer drug in the future.

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