【摘要】 目的探讨蛋白激酶抑制剂LY294002对多药耐药细胞KB/VCR的耐药逆转作用及逆转机制。方法采用MTT法检测LY294002对VCR和ADR的耐药逆转作用,流式细胞仪检测Rh123在KB和KB/VCR细胞内的蓄积,Western blot法检测LY294002对P-gp蛋白表达的影响,DAPI染色检测细胞凋亡。结果 LY294002对化疗药物具有协同增效作用,可以显著逆转KB/VCR的耐药性,能明显减少Rh123的外排,同时降低P-gp的表达。结论LY294002能够逆转KB/VCR细胞的多药耐药性,不仅能够抑制P-gp功能,而且能够降低P-gp蛋白表达,使肿瘤细胞内化疗药物的浓度增加,提高化疗药物的杀伤作用。更多还原

【Abstract】 Objective To explore the reversal effect and potential mechanism of protein kinase inhibitor LY294002 on multidrug resistance of KB / VCR cells. Methods MTT assay was used to investigate reversal effect of LY294002 on multidrug resistance of VCR and ADR. Flow cytometry was used to measure Rh123 accumulation in KB and KB / VCR cells.Western blotting was used to detect the effect of LY294002 on protein expression of P-gp. DAPI staining was used to analyze the apoptosis of KB / VCR cells. Results LY294002 obviously reversed the multidrug resistant phenotype of KB / VCR cells. Further study showed that it significantly increased the accumulation of Rh123 in KB / VCR cells,and LY294002 also down-regulated the expression of P-gp. Conclusion LY294002 may reverse the multidrug resistance of KB / VCR cells,not only can inhibit P-gp function,but also can down-regulate the expression of P-gp protein,increase the concentration of chemotherapy drugs in tumor cells,and improve the killing effect of chemotherapy.更多还原