摘要
目的探讨苦参碱对人膀胱癌BIU-87/ADM细胞多药耐药逆转作用的机制。方法 MTT法检测细胞生长抑制率;荧光分光光度计检测阿霉素(ADM)的蓄积和外排;免疫印迹法检测P-糖蛋白(P-gp)表达;P-gp-GloTMAssay System试剂盒检测P-gp ATP酶活性。结果经ADM作用后,与敏感细胞株BIU-87存活率比较,耐药细胞株BIU-87/ADM存活率明显增加(P<0.001),苦参碱呈剂量依赖地降低BIU-87/ADM细胞存活率(P<0.01),而对敏感细胞株BIU-87细胞存活率无显著影响。苦参碱呈剂量依赖地增加ADM在BIU-87/ADM细胞中蓄积水平,抑制ADM细胞内外排。苦参碱明显抑制P-gp蛋白表达,降低P-gp ATP酶活性。结论苦参碱通过抑制BIU-87/ADM细胞P-gp蛋白和ATP酶活性,减弱P-gp外排功能,增加细胞内ADM蓄积,从而发挥对人膀胱癌BIU-87/ADM细胞多药耐药的逆转作用。
Objective To investigate the reversal mechanism of matrine on multidrug resistance(MDR) in BIU-87/ADM cells. Methods The cell proliferation inhibition rate was detected by MTT assay; the accumulation and efflux of ADM was detected by fluorescence spectrophotometer; the expression of P-gp protein was tested by Western blot; the activity of P-gp ATPase was measured by P-gp-GloTM Assay System kit. Results Compared with the sensitive cell line BIU-87, the survival rate of multidrug resistant cell line BIU-87/ADM was significantly increased after treated with ADM(P<0.001); matrine reduced the survival rate of BIU-87/ADM cells with a manner of dose-dependently(P<0.01), without significant effect on the BIU-87 cell. Matrine increased accumulation of ADM and inhibited P-gp-mediated efflux of ADM. Matrine decreased the expression of P-gp and inhibited the activity of P-gp ATPase significantly. Conclusion Matrine can reverse multidrug resistance in BIU-87/ADM cells by inhibiting the expression of P-gp and ATPase activity, reducing P-gp-mediated efflux of ADM, and increasing accumulation of ADM to play the role in reversal effects on multidrug resistance of human bladder cancer BIU-87/ADM cells.
出处
《中国中医药信息杂志》
CAS
CSCD
2016年第2期73-75,共3页
Chinese Journal of Information on Traditional Chinese Medicine
基金
甘肃省自然科学研究基金计划(145RJYA256)
