棘霉素对耐伊马替尼K562细胞SPK及P-gp表达的影响  

Effect of echinomycin on SPK and P-gp expression in K562/Ima cells

作　　者：许严伟 林海红[2] 杜钢军 

机构地区：[1]洛阳市第三人民医院药剂科,河南洛阳471002 [2]河南大学药学院,河南开封475004

出　　处：《河南大学学报（医学版）》2015年第4期240-243,共4页Journal of Henan University:Medical Science

基　　金：国家自然科学基金资助项目(30472082)

摘　　要：目的研究棘霉素对耐伊马替尼K562细胞SPK及P-gp表达的影响。方法 MTT法检测细胞存活率,同位素掺入检测SPK的活性,流式细胞术检测细胞的P-gp表达。结果棘霉素对K562和耐伊马替尼细胞的IC50分别为0.82μg/L和0.87μg/L;棘霉素对耐药细胞中的SPK和P-gp活性有抑制作用;通过抑制SPK的活性可以下调P-gp的表达。结论棘霉素对敏感及耐药K562细胞均有较强的抑制作用,抑制K562/Ima存活的机制可能与影响细胞中SPK的表达,并通过下调SPK进一步影响P-gp的表达,从而增加药物在细胞内的累积浓度有关。Objective This study was aimed to explore the effect of echinomycin on SPK and P-gp in K562/Ima cells.Methods In experiments,thes cell proliferation was detected by MTT assay.SPK and P-gp were examed by TLC and FACS in K562/Ima cells,respectively.Results The results revealed the IC50 of echinomycin in K562 and K562/Ima were 0.82μg/L and 0.87μg/L,respectively.The SPK and P-gp were inhited by echinomycin in K562/Ima.The expression of P-gp was inhibited by down-regulating the activity of SPK.Conclusion Echinomycin can inhibit the proliferation of K562 and K562/Ima cells,and its mechanism of inhibiting K562/Ima may be related to inhibition of SPK,and the expression of P-gp was inhibited by down-regulating the activity of SPK,further increasing cumulative concentration effect of drug in K562/Ima cells.

关 键 词：棘霉素 K562/Ima 鞘氨醇激酶 P糖蛋白 

分 类 号：R966[医药卫生—药理学]