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  

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

作　　者：木合布力.阿布力孜 王永波[1] 高苗苗[1] 徐方野[1] 盛磊[2] 热娜.卡斯木[1] 

机构地区：[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　　处：《天然产物研究与开发》2014年第8期1193-1197,共5页Natural Product Research and Development

基　　金：国家自然科学基金项目(81260379);新疆医科大学博士后创新基金项目(2012-02)

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∽400μg/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。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 MTr 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 hepatocareinoma cells have a relatively high sensitivity to GA-Pt. The combination of glyeyrrbetinic acid with eisPlatin 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-targe- ting anticancer agents from glycyrrhetinic acid-cisplatin complex.

关 键 词：甘草次酸-顺铂复合物 制备 抗癌活性 

分 类 号：R943[医药卫生—药剂学]