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水杨酸盐对肾脏葡糖醛酸结合作用及酚类肾小管排泄转运的增强作用。

Salicylate enhancement of renal glucuronide conjugation and tubular excretory transfer of phenols.

作者信息

Diamond G L, Anders M W, Tremaine L M, Quebbemann A J

出版信息

Drug Metab Dispos. 1982 Nov-Dec;10(6):573-8.

PMID:6130902
Abstract

Salicylate administration increased glucuronyltransferase activity, with o-aminophenol as the substrate, in chicken kidney homogenates, but did not affect glucuronyltransferase activity in chicken liver homogenates. In addition, salicylate administration increased in vivo renal glucuronidation of catechol and p-nitrophenol without affecting renal sulfate conjugation of these compounds. These results suggest that salicylate administration selectively enhances renal glucuronide conjugation, thereby promoting a more rapid metabolism and elimination of circulating phenols, especially at high plasma phenol concentrations. Isolated human kidney perfusion experiments reveal that glucuronide and sulfate conjugates of phenol, p-nitrophenol, and 1-naphthol are formed in the human kidney, suggesting that the effect of salicylate treatment on renal glucuronidation may apply to humans.

摘要

在鸡肾匀浆中,以邻氨基酚为底物时,水杨酸盐给药可增加葡萄糖醛酸转移酶的活性,但对鸡肝匀浆中的葡萄糖醛酸转移酶活性没有影响。此外,水杨酸盐给药可增加体内儿茶酚和对硝基苯酚的肾脏葡萄糖醛酸化,而不影响这些化合物的肾脏硫酸结合。这些结果表明,水杨酸盐给药可选择性增强肾脏葡萄糖醛酸结合,从而促进循环酚类物质更快地代谢和清除,尤其是在血浆酚浓度较高时。离体人肾灌注实验表明,人肾中可形成苯酚、对硝基苯酚和1-萘酚的葡萄糖醛酸和硫酸结合物,这表明水杨酸盐治疗对肾脏葡萄糖醛酸化的影响可能适用于人类。

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