Evaluation and comparison of MRP1 activity with three fluorescent dyes and three modulators in leukemic cell lines
Evaluation and comparison of MRP1 activity with three fluorescent dyes and three modulators in leukemic cell lines
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DOI：
10.1016/j.leukres.2003.10.015
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发表时间：
2004-06-01
影响因子：
2.7
通讯作者：
Marie, JP
中科院分区：
文献类型：
--
作者：
Dogan, AL;Legrand, O;Marie, JP
应用钙黄绿素乙酰氧甲酯(Calcein-AM)、二乙酸羧基荧光素(CFDA)和罗丹明123(Rh123)与调节剂环孢素A(CsA)、丙磺舒(Probenecid)和MK571相结合的功能分析方法，对11种不同MRP1表达水平的细胞株的MRP1活性进行评估和比较。MRP1的表达与MK571对钙黄素-AM摄取的调节作用(P=0.01)和丙磺舒对CFDA摄取的调节作用(P=0.02)具有良好的相关性。此外，MK571和丙磺舒对CFDA摄取(P<；0.0001)和钙黄素-AM摄取(P=0.0001)的联合调节作用非常显著。未发现MRP1的表达与三种调节剂对Rh123摄取或外排的影响之间存在相关性。综上所述，Calcein-AM和CFDA摄取试验是检测MRP1活性的最佳选择，两种调节剂的联合使用可能会提高这两种方法的效率。(C)2003爱思唯尔有限公司。保留所有权利。
MRP1 activity was evaluated and compared in 11 cell lines with different levels of MRP1 expression using functional assays of calcein acetoxymethyl ester (calcein-AM), carboxyfluorescein diacetate (CFDA) and Rhodamine 123 (Rh123) in combination with the modulators cyclosporin A (CsA), probenecid and MK571. A good correlation was found between MRP1 expression and the modulatory effect of MK571 on calcein-AM uptake (P = 0.01) and probenecid effect on CFDA uptake (P = 0.02). Additionally, the combined modulatory effect of MK571 and probenecid on CFDA uptake (P < 0.0001) and on calcein-AM uptake (P = 0.0001) were highly significant. No correlation was found between MRP1 expression and the effects of three modulators on Rh123 uptake or efflux. In conclusion, calcein-AM and CFDA uptake assays are the best choices to probe MRP1 activity and combination of two modulators may improve the efficiency of these assays. (C) 2003 Elsevier Ltd. All rights reserved.