喜树碱及其衍生物对肝癌细胞HepG2增殖抑制与凋亡的研究  

Research on the effect of camptothecin and its derivatives on proliferation and apoptosis of liver cancer cell HepG2

作　　者：陈琴华[1] 余飞[1] 李鹏[1] 朱军[1] 

机构地区：[1]湖北医药学院附属东风医院药物分析与筛选研究所,湖北十堰442008

出　　处：《实用药物与临床》2016年第3期272-275,共4页Practical Pharmacy and Clinical Remedies

基　　金：湖北省教育厅科学技术研究项目(D20152105);十堰市科学技术研究与开发项目(15Y48);湖北省自然科学基金面上项目(2015CFB615);湖北医药学院优秀中青年科技创新团队计划(2014CXG04)

摘　　要：目的探讨喜树碱(CPT)及其衍生物10-羟基喜树碱(HCPT)、7-乙基喜树碱(SN22)、7-乙基-10-羟基喜树碱(SN38)在体外对肝癌细胞Hep G2增殖抑制与凋亡的影响。方法取对数期生长的HepG2细胞,分为对照组以及实验组,将4种药物配成浓度梯度0.01、0.1、1、10、100μmol/L的药物溶液。将不同浓度的药物溶液作用于肝癌细胞48 h,MTT法测定Hep G2细胞的增殖情况,Anexin V-PI染色,流式细胞仪检测细胞凋亡情况。结果 MTT法显示,4种药物对肝癌细胞Hep G2的增殖具有抑制作用,在一定范围内随着药物浓度的增加,对Hep G2细胞增殖的抑制作用逐渐增强,呈量效依赖关系,其中7-乙基-10-羟基喜树碱抑制效果最好,10-羟基喜树碱、7-乙基喜树碱次之,喜树碱抑制效果最差。不同浓度的喜树碱及衍生物处理肝癌细胞HepG2,与对照组比较差异有统计学意义,随着药物浓度的变化,细胞凋亡也呈现梯度变化,结构修饰后的SN38比SN22、HCPT及CPT作用更强。结论喜树碱及衍生物对肝癌细胞HepG2有抑制作用,并且能够诱导细胞凋亡。Objective To explore the effect of camptothecin（ CPT） and its derivatives 10-hydroxy camptothecin（ HCPT）,7-ethyl camptothecin（ SN22）,7-ethyl-10-hydroxy camptothecin（ SN38） on inhibition of hepatoma cell line Hep G2 and induction of its apoptosis. Methods The vegetative Hep G2 cells of logarithmic phase were assigned as control group and experimental group. Four drugs were made to different concentrations,which were 0. 01,0. 1,1,10,100 μmol / L. Different concentrations of drug solutions were effected on Hep G2 cells in 48 h,then M TT method was used to detect the proliferation of HepG2 cell and cell apoptosis was analyzed by flowcytometry（ FCM） using Anexin V-PI staining. Results The results by M TT method showed four drugs had inhibitory effect on proliferation of HepG2 cells,moreover,the proliferation inhibition of HepG2 cells was enhanced gradually with the increase of drug concentrations in a certain scope drug concentrations,and the proliferation inhibition was dependent on drug concentration. The sequences of proliferation inhibition were SN38,HCPT,SN22,and CPT. With different concentrations of camptothecin and derivatives with HepG2 liver cancer cells,there were significant differences compared with control group,and as drug concentration changed,cell apoptosis also presents gradient change; structure modification of SN38 was stronger than SN22,CPT and HCPT function by FCM using Anexin V-PI staining. Conclusion Camptothecin and its derivatives can inhibit HepG2 cells and induce cell apoptosis.

关 键 词：喜树碱 10-羟基喜树碱 7-乙基喜树碱 7-乙基-10-羟基喜树碱 HEPG2细胞 

分 类 号：R735.7[医药卫生—肿瘤]