Diamond G L, Anders M W, Tremaine L M, Quebbemann A J
Drug Metab Dispos. 1982 Nov-Dec;10(6):573-8.
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.
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。