Effect of rabeprazole on MDRI-mediated transport of rhodamine 123 in Caco-2 and Hvr100-6 cells
Effect of rabeprazole on MDRI-mediated transport of rhodamine 123 in Caco-2 and Hvr100-6 cells
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DOI：
10.1248/bpb.27.1694
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发表时间：
2004-10-01
影响因子：
2
通讯作者：
Kohda, Y
中科院分区：
文献类型：
--
作者：
Itagaki, F;Homma, M;Kohda, Y
我们研究的目的是研究雷贝拉唑（一种质子泵抑制剂）对人结肠癌细胞系 Caco-2 和 MDR1 过表达人宫颈癌细胞系（通过暴露于 100 nm 长春花碱选择的 HeLa 细胞（Hvr100-6 细胞））上表达的 MDRI 的影响。在这些细胞中检查了雷贝拉唑对 MDR1 介导的罗丹明转运的抑制作用][23。千微摩尔雷贝拉唑使 Caco-2 和 Hvr100-6 细胞中罗丹明 123 的摄取分别增加 68% 和 185%。雷贝拉唑在1-100μm的浓度下没有观察到明显的作用。由于雷贝拉唑在血浆水平（约 1 mum）对通过 MDRI 的罗丹明 123 转运没有任何影响，因此认为药物与 MDR1 底物的相互作用将是最小的，即使相互作用发生在接受雷贝拉唑治疗的患者中。
The aim of our study was to investigate the effects of rabeprazole, a proton pump inhibitor, on MDRI expressed on human colon carcinoma cell line, Caco-2, and MDR1-overexpressing human cervical carcinoma cell line, HeLa cells selected by exposure to 100 nm vinblastine (Hvr100-6 cells). Inhibitory effects of rabeprazole on MDR1-mediated transport of Rhodamine][23 were examined in these cells. A thousand micro molar rabeprazole increased Rhodamine 123 uptakes in Caco-2 and Hvr100-6 cells by 68% and 185%, respectively. No significant effects of rabeprazole were observed at the concentration of 1-100 mum. Since rabeprazole did not show any effects on Rhodamine 123 transport via MDRI at the plasma levels (approximately 1 mum), it was considered that the drug interaction with MDR1 substrates would be minimal even though the interaction occurred in the patients with rabeprazole treatment.