双酰基单环β-内酰胺衍生物的体外抗肿瘤活性研究  

Biacyl Substituted Monocycle β-LactamDerivative for Evaluation as Anticancer Agents

作　　者：高海涛 曾小华[1,2] 

机构地区：[1]湖北医药学院药学院,湖北十堰 [2]湖北省武当特色中药研究重点实验室及湖北医药学院医学化学研究所,湖北十堰

出　　处：《世界肿瘤研究》2019年第1期27-31,共5页World Journal of Cancer Research

摘　　要：目的:研究双酰基取代单环β-内酰胺类化合物对脑胶质瘤细胞(U87)、宫颈癌细胞(HeLa)、肝癌细胞(HepG2)3种肿瘤细胞和1种正常细胞间充质干细胞(MSC)的体外抗肿瘤活性。方法:采用MTT法测定了不同药物浓度对细胞的抑制作用,以半数抑制浓度(IC50)评价目标化合物的抗肿瘤活性。结果:实验结果表明双酰基取代单环β-内酰胺对U87、HeLa、HepG2和MSC正常细胞都具有一定的抑制作用,其中,化合物5a对HepG2细胞增殖的抑制活性最强,其IC50值为8.15 μmol/L。结论:初步的体外抗肿瘤活性测试显示双酰基取代单环β-内酰胺类化合物具有抑制肿瘤细胞的生长,表现出潜在的抗肿瘤活性。Objective: To study antitumor activities of diacyl substituted monocyclic β-Lactam derivatives against U87, HeLa and HepG2 human tumor cell lines and MSC human normal cell lines. Method: The antitumor activities of diacyl substituted monocyclic β-Lactam derivatives were screened using cis-platinum as positive contron by MTT method. Results: Among them 5a stood out as the most po-tent showing an IC50 of 8.15 μmol/L against human tumor cell lines (HepG2). Conclusion: Bioassay of the compounds indicated that diacyl substituted monocyclic β-Lactam derivatives showed potential antitumor activities, which these compounds can be established as lead molecules for developing novel antitumor drugs.

关 键 词：双酰基取代单环β-内酰胺 体外抗肿瘤活性研究 

分 类 号：R28[医药卫生—中药学]