苯基乙炔磺酰胺与荜拨酰胺抗肺癌A549细胞增殖作用研究  

The anti-proliferative effect of PFT-μ and piplartine on human lung cancer cell line A549

作　　者：王继双[1] 何焱[1] 张文静[1] 张鹏[1] 黄启来[1] 华子春[1,2] 

机构地区：[1]澳门科技大学中医药学院澳门药物与健康应用研究所中药质量研究国家重点实验室,澳门999078 [2]南京大学医药生物技术国家重点实验室,江苏南京210093

出　　处：《中国生化药物杂志》2012年第6期754-758,共5页Chinese Journal of Biochemical Pharmaceutics

基　　金：澳门科技发展基金(071/2009/A3;091/2009/A)

摘　　要：目的探讨HSP70抑制剂PFT-μ(苯基乙炔磺酰胺)及荜拨酰胺单独使用及合用时,对非小细胞肺癌A549细胞增殖活性的影响。方法 MTT法检测荜拨酰胺、PFT-μ单用及合用对A549细胞增殖的影响;DAPI染色观察A549细胞凋亡形态改变;Western blot法检测相关凋亡蛋白PARP、Bid的变化。结果荜拨酰胺剂量依赖性抑制A549细胞增殖,两药合用显著降低细胞增殖活性,与各单独给药组存在统计学差异(P<0.01);两药合用后细胞核数目明显减少,但是凋亡现象没有荜拨酰胺组明显;PFT-μ不引起相关凋亡蛋白变化。荜拨酰胺降低Bid表达,增加PARP剪切体表达。与荜拨酰胺组相比,合用增加Bid表达,减少PARP剪切体表达。结论 PFT-μ与荜拨酰胺合用,能增加对A549细胞的细胞毒性,但二者可能通过不同的方式促进细胞死亡。Purpose To determine the anti-proliferative activity of PFT-μor piplartine and their com- bination on human lung cancer cell line （A549）. Methods The cell viability was analyzed by MTT assay. The apoptotic morphology was examined by DAPI staining. The PARP, Bid protein expression was deter- mined by Western blot analysis. Results The anti-proliferation of piplartine had a dose-effect relation- ship. The combinational treatment significantly reduced the proliferation of the cells and the anti-prolifera- tive effect of the combination group was significantly different from both the PFT-p, group and the piplar- tine group（P 〈 0.01 ）. Compared with the piplartine group, the apoptotic morphological changed in the combination group was decreased. PFT-μ treatment had no influence on PARP and Bid protein expression. Piplartine significantly reduced Bid protein expression,and induced more PARP cleavage than the control group. Compared with the piplartine group,combination treatment decreased Bid protein expression and in- duced less PARP cleavage. Conclusion Combination treatment of PFT-μ and piplartine exhibited more po- tent anti-proliferative effect and this may be attributed to other cell death mechanism than apoptosis.

关 键 词：苯基乙炔磺酰胺 荜拨酰胺 联合用药 PARP BID 

分 类 号：R961[医药卫生—药理学]