Research on the anti-hepatocellular carcinoma activity and mechanisms of glycyrrhetinic acid derivatives
10.12360/CPB202503064
- VernacularTitle:甘草次酸衍生物的合成及其抗肝癌活性
- Author:
Xu-xin CUI
1
;
Wen-ping CUI
;
Yan-xing BI
;
Fan CHENG
;
Yu-ning LI
;
Bao-lai ZHANG
;
Quan-yi ZHAO
;
Xiao-lai YANG
Author Information
1. 甘肃中医药大学药学院;甘肃省人民医院药剂科
- Publication Type:Journal Article
- Keywords:
glycyrrhetinic acid;
synthesis;
deriva-tives;
antitumor activity;
hepatocellular carcinoma;
cell apoptosis
- From:
Chinese Pharmacological Bulletin
2025;41(11):2150-2157
- CountryChina
- Language:Chinese
-
Abstract:
Aim To design and synthesize a series of glycyrrhetinic acid derivatives by using glycyrrhetinic acid as the parent nucleus,screen their antitumor activ-ities,and investigate the in vitro and in vivo antitumor effects and mechanisms of the most active compound.Methods MTT assay was used to screen for the com-pound with the most potent antitumor activity.MTT as-say,wound healing assay,colony formation assay and Transwell migration assay were used to evaluate the effects of the compound on tumor cell viability and mi-gration.Flow cytometry was employed to assess the im-pact of the compound on tumor cell cycle progression and apoptosis.Western blot was conducted to verify the effects on the expression of pro-apoptotic proteins Bax,caspase-3 and cleaved caspase-3.A mouse model of hepatocellular carcinoma ascites tumor was estab-lished to examine the antitumor effects of the compound in vivo.Results Compound C22 was identified as having the most significant inhibitory effect on hepato-cellular carcinoma cells.C22 inhibited the viability and migration of hepatocellular carcinoma cells in a time and concentration-dependent manner.C22 upreg-ulated the expression of pro-apoptotic proteins Bax,caspase-3 and cleaved caspase-3 in hepatocellular car-cinoma cells,induced apoptosis,and arrested the cell cycle in the G0/G1 and S phases.C22 significantly re-duced the growth of mouse hepatocellular carcinoma as-cites tumors and prolonged survival.Conclusion Glycyrrhetinic acid derivative C22 significantly inhibits the viability and migration of hepatocellular carcinoma cells in vitro and in vivo,and induces cell cycle arrest and apoptosis.
