广西师范大学学报（自然科学版） ›› 2025, Vol. 43 ›› Issue (6): 162-173.doi: 10.16088/j.issn.1001-6600.2024121301

• 生态环境科学研究 • 上一篇    下一篇

草酰胺衍生物Z21对人肝癌细胞株Hep G2的体外抗肿瘤活性研究

谢文彬1,2, 喻宇慧1,2, 禹海双1,2, 邬慧贤1,2, 金俊飞1,2, 陈振锋3, 卢幸1,2*   

  1. 1.广西肝脏损伤与修复分子医学重点实验室(桂林医学院附属医院),广西 桂林 541001;
    2.广西神经鞘脂代谢相关疾病基础研究重点实验室(桂林医学院附属医院),广西 桂林 541001;
    3.省部共建药用资源化学与药物分子工程国家重点实验室(广西师范大学),广西 桂林 541004
  • 收稿日期:2024-12-13 修回日期:2025-01-18 发布日期:2025-11-19
  • 通讯作者: 卢幸(1989—),男,安徽芜湖人,桂林医学院附属医院副研究员,博士。E-mail: xinglu@glmc.edu.cn
  • 基金资助:
    国家自然科学基金(82304305);广西自然科学基金(2025GXNSFHA069051,2024GXNSFAA010286);广西科技厅中央引导地方科技发展资金项目(桂科ZY21195024)

Anti-Tumor Activity of Oxalamide Derivative Z21 in Human Hepatoma Cell Line Hep G2

XIE Wenbin1,2, YU Yuhui1,2, YU Haishuang1,2, WU Huixian1,2, JIN Junfei1,2, CHEN Zhenfeng3, LU Xing1,2*   

  1. 1. Guangxi Key Laboratory of Molecular Medicine in Liver Injury and Repair (Affiliated Hospital of Guilin Medical University), Guilin Guangxi 541001, China;
    2. Guangxi Health Commission Key Laboratory of Basic Research in Sphingolipid Metabolism Related Diseases (Affiliated Hospital of Guilin Medical University), Guilin Guangxi 541001, China;
    3. State Key Laboratory for Chemistry and Molecular Engineering of Medicinal Resources (Guangxi Normal University), Guilin Guangxi 541004, China
  • Received:2024-12-13 Revised:2025-01-18 Published:2025-11-19

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摘要： 本文对一种新型抗肿瘤化合物草酰胺衍生物Z21的活性和作用机制进行研究。活性筛选显示Z21能有效抑制多种肿瘤细胞株的生长,尤其对人肝癌细胞株Hep G2的抑制效应最为显著。将Hep G2细胞作为实验对象,通过显微镜观察细胞形态学、MTT法与ATP含量测定法检测细胞活力、EdU掺入法与克隆形成实验检测细胞增殖能力、PI染色检测细胞周期、Annexin V/PI染色法检测细胞凋亡、Western blot检测凋亡相关蛋白的表达。结果显示:Z21以剂量依赖性的方式抑制Hep G2细胞增殖,降低Bcl-2的表达,提高Bax的表达,并通过Caspase依赖性凋亡途径诱导细胞发生凋亡,而对细胞周期无明显阻滞作用。研究结果说明Z21具有良好的抗肿瘤活性,其作用机制与诱导细胞凋亡相关。

关键词: 草酰胺衍生物, 肝癌, 抗肿瘤, Hep G2, 细胞凋亡

Abstract: In this study, the activity and mechanism of a novel anti-tumor compound oxalamide derivative Z21 were studied. Activity screening showed that Z21 could effectively inhibit the growth of various tumor cell lines, especially human hepatoma cell line Hep G2 cells. With Hep G2 cells as experimental subjects, we observed cell morphology by microscope, detected cell viability by MTT assay and ATP assay, detected cell proliferation capacity by EdU incorporation assay and clonal formation assay, detected cell cycle by PI staining, detected cell apoptosis by Annexin V/PI staining, and detected the expressions of apoptosis-related proteins by Western blot. Mechanism studies showed that Z21 suppressed the proliferation of Hep G2 cells in a dose-dependent manner, reduced the expression of Bcl-2, promoted the expression of Bax and significantly induced cell apoptosis by caspase-dependent apoptosis pathway, but no significant cell cycle arrest was observed. These results indicate that Z21 contains great anti-tumor activity, and its ability to suppresses the proliferation of Hep G2 cells may be related to inducing cell apoptosis.

Key words: oxalamide derivative, hepatoma, anti-tumor, Hep G2, cell apoptosis

中图分类号:  R735.7

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