天然产物研究与开发 ›› 2014, Vol. 26 ›› Issue (8): 1193-1197.

• 研究论文 • 上一篇    下一篇

甘草次酸-顺铂复合物的制备及其对人肝癌Bel-7402细胞的抗癌活性研究

木合布力·阿布力孜1,王永波1,高苗苗1,徐方野1,盛 磊2,热娜·卡斯木1*   

  1. 1 新疆医科大学药学院药物化学有机教研室;2 新疆医科大学 新疆地方病分子生物学重点实验室,乌鲁木齐 830011
  • 出版日期:2014-08-30 发布日期:2014-11-06

Preparation and Anticancer Property of Glycyrrhetinic acid-Cisplatin Against Human Bel-7402 cancer cells

Mourboul ABLISE1, WANG Yong-bo1, GAO Miao-miao1, XU Fang-ye1, SHENG Lei2, Rena KASIM1*   

  1. 1 Department of Medicinal and Organic chemistry,College of Pharmacy; 2 Xinjiang Key Laboratory of Molecular Biology  and Endemic Diseases,Xinjiang Medical University,Urumqi 830011, China
  • Online:2014-08-30 Published:2014-11-06

摘要: 以天然活性成分18β-甘草次酸和抗癌药顺铂为原料,经缩合制备甘草次酸-顺铂(GA-Pt)复合物;利用人肝癌细胞株Bel-7402做体外模型,用MTT法观察GA-Pt对癌细胞增殖的抑制活性。发现目标化合物对肝癌Bel-7402细胞的增殖显明显的抑制活性,浓度在5~400 μg/mL范围内,对肿瘤细胞增殖的抑制率可达29.31%~92.25%。此结果显示,肝癌Bel-7402细胞对甘草次酸顺铂类复合物具有较好的敏感性;甘草次酸与顺铂的偶合可提高顺铂的抗癌活性,这可能是产生抗癌协同及化疗增敏作用的结果。此结果对新型肝靶向抗癌候选药物的筛选奠定了一定的基础。

关键词: 甘草次酸-顺铂复合物, 制备, 抗癌活性

Abstract: Glycyrrhetinic acid-cisplatin complex (GA-Pt) was prepared by the combination of natural compound 18β-glycyrrhetinic acid and anticancer drug cis-Platin within a three-step reaction.The in vitro anticancer activity of the synthesized complex was studied using human Bel-7402 hepatocarcinoma cell lines.Cell viability was determined by MTT method.Statistical analysis showed that GA-Pt inhibited Bel-7402 cell proliferation significantly.The inhibitory rate was 29.31%-92.25% at the concentration range of 5-400 μg/mL.The experimental results suggested that the human Bel-7402 hepatocarcinoma cells have a relatively high sensitivity to GA-Pt.The combination of glycyrrhetinic acid with cis-Platin increased their anticancer activity.This may be related to the synergistic anti-cancer property and chemotherapy sensitizing effect of GA to Cis-platin.This work provided an initial basis for pharmacological screening of new liver-targeting anticancer agents from glycyrrhetinic acid-cisplatin complex.

Key words: Glycyrrhetinic acid-cisplatin complex, preparation, anticancer activity

中图分类号: 

R943