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甲基莲心碱抑制K562/A02细胞GSTπ的表达
http://www.100md.com 《西安交通大学学报》 2005年第5期
白血病,,白血病;多药耐药;甲基莲心碱;谷胱甘肽S转移酶π,1材料与方法,2结果,3讨论,参考文献
     摘要:目的 探讨甲基莲心碱(Neferine, Nef)对谷胱甘肽S转移酶π(GSTπ)的影响。 方法 应用MTT法测定甲基莲心碱处理的K562/A02细胞对阿霉素(ADM)敏感性的影响。RTPCR法分析Nef处理后,GSTπmRNA转录的变化。通过Western Blot观察Nef对GSTπ蛋白表达的影响。结果 甲基莲心碱对K562/A02的耐药性具有明显的逆转作用。用Nef处理后,对阿霉素药物敏感性的相对逆转效率第1天、第3天和第5天分别为9.6%、41.4%和10.7%;GSTπmRNA转录水平在用药后第3天下调最大,为(50.7±2.3)%。GSTπ蛋白的表达于用药后第1天、第3天和第5天分别下降25.57%、48.42%和10.68%。结论 甲基莲心碱具有较强的逆转K562/A02细胞多药耐药的作用,其逆转机制可能包括下调K562/A02细胞GSTπmRNA的转录和蛋白的表达。

    关键词:白血病;多药耐药;甲基莲心碱;谷胱甘肽S转移酶π

    Effects of neferine on expression of glutathione

    Stransferasepi in K562/A02 cells in vitroXiao Xibin1, Xie Zhaoxia1, Qin Qun2

    (1. Department of Hematology; 2. Department of Pharmacy, Xiangya Hospital,Central South University, Changsha 410008, China)ABSTRACT: Objective To study the effects of neferine on the expression of glutathione Stransferasepi in vitro and to explore the multidrug resistance reversing mechanism of neferine. Methods 50% inhibition concentration (IC50) of ADM on K562/A02 was determined by MTT method. The transcription of GSTπ gene was detected by semiquantitative RTPCR and the expression level of GSTπ was determined by Western blot after neferine treatment. Results Neferine remarkably enhanced chemosensitivity to ADM of K562/A02 cells. After neferine treatment in day 1, day 3 and day 5, the relative efficiency of K562/A02 to ADM was 9.6%, 41.4% and 10.7%, respectively. Semiquantitative RTPCR showed that mRNA transcription of GSTπ gene was significantly reduced (P<0.01).Neferine was shown to efficiently inhibit the expression of GSTπ according to the results of Western blot (P<0.05). Conclusion Increase of GSTπ expression is one of the MDR mechanisms in K562/A02 cells. Neferine could modulate GSTπ expression in a timedependent manner. Decrease of GSTπ expression may be one of the MDR reversal mechanisms in K562/A02 cells by neferine. ......

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