鬼臼毒素衍生物YB-1EPN对人口腔鳞状上皮癌细胞系增殖的抑制作用研究  

Inhibitory Effect of Podophyllotoxin Derivative (YB-1EPN) Against the Growth of Human Oral Squamous Epithelium Caner Cell

作　　者：毕文超 刘世军 孙克明 刘宪勇 张敏 

机构地区：[1]武警山东省总队医院药剂科,济南250014

出　　处：《中国药房》2012年第47期4422-4424,共3页China Pharmacy

基　　金：国家自然科学基金资助项目(30873363)

摘　　要：目的:研究鬼臼毒素衍生物YB-1EPN对人口腔鳞状上皮癌细胞系(KB)增殖的抑制作用。方法:以KB细胞为研究对象,采用MTT法检测细胞毒作用;荧光染色法观察细胞形态学变化;RT-PCR法检测半胱天冬氨酸蛋白酶(Caspase)-3mRNA的表达;激光共聚焦显微镜观察药物对细胞微管结构的影响。结果:4μmol·L-1YB-1EPN能够直接抑制和杀伤KB细胞;荧光显微镜观察到4μmol·L-1YB-1EPN干预24h后KB细胞出现凋亡小体;RT-PCR法检测到在1、2、4μmol·L-1YB-1EPN干预下KB细胞促凋亡基因Caspase-3表达上调;激光共聚焦显微镜观察到在2、4μmol·L-1YB-1EPN干预24h后KB细胞微管结构被破坏。结论:YB-1EPN能够直接抑制和杀伤KB细胞株,作用机制可能与促凋亡基因的表达上调和抑制微管蛋白聚合有关。OBJECTIVE： To study the inhibitory effect of podophyllotoxin derivative （YB-1EPN） against the growth of human oral squamous epithelium cancer cell（KB）. METHODS： MTT assay was used to detect cytotoxic effect of KB cell; Fluorescent staining method was used to observe the changes of cell morphology; expression of caspase-3 mRNA were measured by RT-PCR assay, and the effect of drugs on microtubules was observed by laser scanning microscope. RESULTS： YB-1EPN（4 μmol·L-1）was demonstrated to exert antiproliferative activity in dose and time dependent manner. Typical apoptotic morphological changes were observed by fluorescence microscope; RT-PCR assay showed that YB-1EPN（1、2、4 μmol·L-1）up-regulated mRNA expression of Caspase-3 dramatically, and the structure of microtubulin was destroyed by laser confocal microscope. CONCLUSION： YB-1EPN show obvious anticancer activity by inducing apoptosis in the dose-dependent manner, which are accompanied by up-regulating Caspase-3 and inhibiting the microtubule polymerization.

关 键 词：鬼臼毒素衍生物 微管蛋白 半胱天冬氨酸蛋白酶-3 增殖 抑制 

分 类 号：R329.24[医药卫生—人体解剖和组织胚胎学]