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Effect of P-glycoprotein modulators on alkaline phosphatase activity in cultured rat hepatocytes

机译：P-糖蛋白调节剂对培养大鼠肝细胞碱性磷酸酶活性的影响

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摘要

Alkaline phosphatases (orthophosphoric-monoester phosphohydrolase, E.C. 3.1.3.1) are a group of nonspecific phosphomonoesterases located primarily in the plasma membrane of the cells in which they occur [1]. It was recently demonstrated that alkaline phosphatase (ALP) concentration in different tissues is positively correlated with the extent of exchange surface per unit volume of the tissue, suggesting an association between ALP and transport systems [2]. Moreover, several groups [3,4,5] obtained evidence of an involvement of ALP in the modulation of P-glycoprotein activity in hepatocytes. The aim of the present study was to determine the putative influence of compounds known to modulate P-glycoprotein-mediated transport on hepatic ALP activity, by using primary cultured rat hepatocytes. The K-m and V-max values of ALP were determined (657.2 muM (306.8-933.1) and 32.0+/-1.5 nmol mg protein(-1) min-respectively). Vanadate and corticosterone concentration-dependently reduced ALP activity, producing maximal reductions of 79% (100 muM) and 71% (100 muM), respectively. The IC50's were found to be 7.9 muM (2.1-29.5 muM) and 2.4 muM (0.2-35.2 muM), respectively. Cyclosporin A, verapamil, octreotide, kaempferol, daunomycin and genistein produced a concentration-dependent increase in ALP activity. ALP activity was maximally increased to 253%, 390%, 180%, 487%, 449% and 193% of control in the presence of 100 muM cyclosporin A, 50 muM verapamil, 10 muM octreotide, 100 muM kaempferol, 100 muM daunomycin and 1 muM genistein, respectively. The results show that all P-glycoprotein modulators tested were able to significantly affect the activity of hepatic-ALP. These effects on ALP activity may contribute to the modulation of P-glycoprotein activity by these drugs. Copyright (C) 2000 S. Karger AG, Basel. [References: 46]
机译：碱性磷酸酶（正磷酸单酯磷酸水解酶，E.C。3.1.3.1）是一组非特异性磷酸单酯酶，主要位于发生它们的细胞的质膜中[1]。最近发现，不同组织中碱性磷酸酶（ALP）的浓度与单位体积组织交换表面的程度呈正相关，表明ALP与运输系统之间存在关联[2]。此外，几组[3,4,5]获得了ALP参与肝细胞P糖蛋白活性调节的证据。本研究的目的是通过使用原代培养的大鼠肝细胞来确定已知的调节P-糖蛋白介导的转运的化合物对肝ALP活性的假定影响。确定ALP的K-m和V-max值（分别为657.2μM（306.8-933.1）和32.0 +/- 1.5 nmol mg蛋白（-1）min）。钒酸盐和皮质酮的浓度依赖性降低ALP活性，分别最大降低79％（100μM）和71％（100μM）。发现IC50分别为7.9μM（2.1-29.5μM）和2.4μM（0.2-35.2μM）。环孢菌素A，维拉帕米，奥曲肽，山奈酚，道诺霉素和金雀异黄素产生了ALP活性浓度依赖性的增加。在100μM环孢菌素A，50μM维拉帕米，10μM奥曲肽，100μM山萘酚，100μM道诺霉素和1μM染料木黄酮分别。结果显示，所有测试的P-糖蛋白调节剂均能够显着影响肝ALP的活性。这些对ALP活性的影响可能有助于这些药物对P-糖蛋白活性的调节。版权所有（C）2000 S.Karger AG，巴塞尔。 [参考：46]

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