消癌平对非小细胞肺癌厄洛替尼耐药的逆转作用  

The Experimental Studies of Xiaoaiping Injection on the Reversal of Erlotinib Resistance in non-small cell lung cancer

作　　者：顾晓燕[1] 肖瑶[2] 汪洋[1] 陈建[1] 

机构地区：[1]浙江大学医学院附属第一医院药剂科,浙江杭州310003 [2]浙江中医药大学,浙江杭州310003

出　　处：《药品评价》2014年第6期30-34,共5页Drug Evaluation

基　　金："ERCC1;RRM1和BRCA1表达水平与晚期NSCLC化疗反应的相关性研究"。浙江省医药卫生科技计划项目;编号:2010KYA07

摘　　要：目的：研究消癌平对厄洛替尼非小细胞肺癌（NSCLC）耐药细胞株PC9/G2的逆转作用机制。方法：MTT法考察消癌平对PC9/G2非毒性剂量，以及对厄洛替尼NSCLC耐药的逆转效应；RT-PCR法测定消癌平对EGFR下游通路PI3K mRNA表达水平的影响，Western blot法测定PI3K蛋白水平变化，分光光度法测定凋亡蛋白Caspase-3活性的变化。结果：消癌平对PC9/G2的非毒性剂量为10mg/mL；消癌平联合厄洛替尼组有明显的逆转耐药作用，细胞存活率比对照组（单用厄洛替尼）降低15%～23%；消癌平使PI3K mRNA和蛋白表达水平显著下降，Caspase-3凋亡蛋白活性提高。结论：消癌平对厄洛替尼NSCLC耐药有逆转作用，可能通过抑制PI3K表达，进而激活凋亡蛋白Caspase-3的机制实现。Objective： To investigate the effect and its mechanism of Xiaoaiping injection on the reversal of Erlotinib resistance in non-small lung cancer cell line PC9/G2. Methods： The non-toxic dosage of PC9/G2 to Xiaoaiping injection and the reversal of drug resistance were determined with MTT method. The expression of PI3K mRNA was tested with RT-PCR. The level of PI3K protein was tested with Western blot. The activity of apoptosis proteins Caspase-3 was determined with spectrophotometry. Results：The non-toxic dosage of PC9/G2 to Xiaoaiping injection was 10mg/mL. The cell survival rate decreased 15%~23%in Xiaoaipin injection combining Erlotinib group compared with Erlotinib group. The expression of PI3K mRNA and protein dropped significantly, and Caspase-3 apoptosis proteins activity increased significantly. Conclusion： Xiaoaiping injection could reverse the Erlotinib resistance cell line PC9/G2 in a certain extent,which may be attributed to down regulating of PI3K expression and inducing more apoptosis proteins Caspase-3.

关 键 词：消癌平 厄洛替尼耐药 逆转 机制 

分 类 号：R734.2[医药卫生—肿瘤]