%0 Journal Article
%T 阿帕替尼逆转P-gp转运体介导的乳腺癌化疗多药耐药性的作用及其机制
%A 张圣村
%A 徐丽丽
%A 马敏
%J 肿瘤防治研究
%D 2018
%R 10.3971/j.issn.1000-8578.2018.17.1112
%X 摘要 目的 探讨阿帕替尼对人乳腺癌化疗多药耐药性的逆转作用及其机制。方法 不同浓度的阿帕替尼作用于体外培养的人乳腺癌MCF-7及MCF-7/ADR细胞48 h，MTT法检测阿帕替尼对两种细胞的细胞毒性；低毒浓度的阿帕替尼与化疗药物紫杉醇及阿霉素联用，探讨阿帕替尼对两种细胞化疗耐药性的影响；采用流式细胞术检测阿帕替尼对罗丹明123在MCF-7及MCF-7/ADR细胞内蓄积的影响；采用Pgp-Glo? Assay Systems试剂盒观察阿帕替尼对多药耐药相关蛋白P-gp的ATPase活性的影响；采用Western blot法检测阿帕替尼对P-gp表达及AKT磷酸化的影响。结果 阿帕替尼可浓度依赖性地逆转乳腺癌MCF-7/ADR细胞对紫杉醇及阿霉素的多药耐药性（P<0.05）、增加罗丹明123在MCF-7/ADR细胞内的蓄积（P<0.05）及激活P-gp转运体的ATPase活性（P<0.05），而对P-gp的表达没有影响；此外，阿帕替尼不改变AKT的磷酸化水平。结论 阿帕替尼可能通过抑制P-gp转运体的外排功能逆转P-gp转运体介导的乳腺癌化疗多药耐药性
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%U http://www.zlfzyj.com/CN/abstract/abstract9135.shtml