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首页> 外文期刊>Life sciences >Characterization of ochratoxin A transport by human organic anion transporters.
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Characterization of ochratoxin A transport by human organic anion transporters.

机译：人类有机阴离子转运蛋白对曲霉毒素A转运的表征。

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摘要

The purpose of this study was to investigate the characteristics of ochratoxin A (OTA) transport by multispecific human organic anion transporters (hOAT1 and hOAT3, respectively) using the second segment of proximal tubule (S2) cells from mice stably expressing hOAT1 and hOAT3 (S2 hOAT1 and S2 hOAT3). S2 hOAT1 and S2 hOAT3 exhibited a time- and dose-dependent, and a saturable increase in uptake of [3H]-OTA, with apparent Km values of 0.42 microM (hOAT1) and 0.75 microM (hOAT3). These OTA uptakes were inhibited by several substrates for the OATs. Para-aminohippuric acid (PAH), probenecid, piroxicam, octanoate and citrinin inhibited [3H]-OTA uptake by hOAT1 and hOAT3 in a competitive manner (Ki = 4.29-3080 microM), with the following order of potency: probenecid > octanoate > PAH > piroxicam > citrinin for hOAT1; probenecid > piroxicam > octanoate> citrinin > PAH for hOAT3. These results indicate that hOAT1, as well as hOAT3, mediates a high-affinity transport of OTA on the basolateral side of the proximal tubule, but hOAT1- and hOAT3-mediated OTA transport are differently influenced by the substrates for the OATs. These pharmacological characteristics of hOAT1 and hOAT3 may be significantly related with the events in the development of OTA-induced nephrotoxicity in the human kidney.
机译：这项研究的目的是使用稳定表达hOAT1和hOAT3（S2）的小鼠近端肾小管（S2）细胞的第二部分，研究多特异性人类有机阴离子转运蛋白（分别为hOAT1和hOAT3）曲毒素A（OTA）的转运特性。 hOAT1和S2 hOAT3）。 S2 hOAT1和S2 hOAT3表现出时间和剂量依赖性，并且对[3H] -OTA的吸收可饱和地增加，表观Km值分别为0.42 microM（hOAT1）和0.75 microM（hOAT3）。这些OTA的吸收受到OAT的几种底物的抑制。对氨基马尿酸（PAH），丙磺舒，吡罗昔康，辛酸酯和柠檬素以竞争方式抑制hOAT1和hOAT3吸收[3H] -OTA（Ki = 4.29-3080 microM），效力顺序如下：丙磺舒>辛酸酯> PAH>吡罗昔康> citrinin用于hOAT1丙磺舒>吡罗昔康>辛酸酯> citrinin> PAH用于hOAT3。这些结果表明，hOAT1和hOAT3在近端小管的基底外侧调节OTA的高亲和力转运，但是hOAT1和hOAT3介导的OTA转运受OAT底物的影响不同。 hOAT1和hOAT3的这些药理特性可能与OTA诱导的人肾肾毒性的发生有关。

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