木犀草素抑制白血病耐药株K562/A02的GST-π表达  

Luteolin Inhibiting Expression of Glutathione S-transferase-pi in K562/A02 Cells

作　　者：许静[1] 李瑞明[2] 肖希斌[3] 罗子玲[1] 官碧琼[1] 陈杰[2] 

机构地区：[1]南方医科大学附属第三医院药剂科,广东广州510630 [2]中山大学附属第一医院药学部,广东广州510008 [3]浙江大学医学院附属第二医院血液科,浙江杭州310009

出　　处：《今日药学》2012年第1期7-9,29,共4页Pharmacy Today

基　　金：广东省医院药学基金(编号:2010A13);广东省自然科学基金(编号:8451008901000788);广东省医学科研基金(编号:A2009163)

摘　　要：目的探讨木犀草素(luteolin)对白血病耐药株K562/A02细胞谷胱甘肽S转移酶π(GST-π)的影响。方法木犀草素30 mmol/L预处理K562/A02细胞第1、35、d后,MTT法测定阿霉素IC50,采用722分光光度计测定细胞内GSH含量及Western Blot法测定木犀草素处理后GST-π蛋白表达。结果木犀草素对K562/A02的耐药性具有明显的逆转作用,用木犀草素处理后,对阿霉素药物敏感性的相对逆转效率第1、3、5 d分别为10.7%4、2.7%和15.8%;木犀草素显著降低K562/A02细胞内GSH含量,GST-π蛋白的表达于用药后第1、35、d分别下降22%5、6%和34%。结论木犀草素具有较强的逆转K562/A02细胞多药耐药的作用,其逆转机制可能与降低细胞内GSH含量,下调K562/A02细胞GST-π蛋白的表达相关。Objective To investigate the effects of luteolin on the expression of glutathione S-transferase pi （GST-π） in vitro and to explore the multi-drug resistance reversing mechanism of luteolin. Methods The half maximal inhibitory concentration （IC50） of ADM in K562/A02 was determined by MTT method. The protein expression level of GST-π was determined by Western blot after luteolin treatment. Results Luteolin remarkably enhanced chemo-sensitivity to ADM of K562/A02 cells. After luteoliu treatment in day 1, day 3 and day 5, the relative efficiency of K562/A02 to ADM was 10. 7%, 42.7% and 15.8%, respectively. According to the results of Western blot, luteolin was shown to efficiently inhibit the expression of GST-π （ P 〈 0.05 ）. Conclusion Luteolin can modulate GST-π expression in a time-dependent manner, GST-π expression down regulation may be one of the MDR reversal mechanisms in K562/A02 cells by luteolin.

关 键 词：白血病 木犀草素 多药耐药 谷胱甘肽S转移酶Π 

分 类 号：R733.7[医药卫生—肿瘤]