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四氧嘧啶糖尿病大鼠中尿苷二磷酸葡萄糖醛酸基转移酶的抑制与激活

Inhibition and activation of UDP-glucuronyltransferase in alloxanic-diabetic rats.

作者信息

Vega P, Gaule C, Sanchez E, del Villar E

出版信息

Gen Pharmacol. 1986;17(6):641-5. doi: 10.1016/0306-3623(86)90293-4.

Abstract

Short or long term alloxan diabetes produced activation of oestrone and morphine glucuronidation and inhibition of p-nitrophenol glucuronidation in rat liver microsomes. Insulin treatment restored decreased glucuronyltransferase (GT) activity for p-nitrophenol and it did not abolish diabetes activation on oestrone glucuronidation. Triton X-100 detergent activation reduced differences between normal, diabetic and insulin treated rats in the glucuronidation rates of the substrates assayed. 1,4-Benzodiazepines inhibited morphine GT activity and stimulated oestrone GT activity in normal, diabetic and insulin treated diabetic rats. Activation and inhibition of GT activities for oestrone and xenobiotics in diabetes mellitus appears to be related with membrane perturbations of liver microsomes.

摘要

短期或长期的四氧嘧啶糖尿病会使大鼠肝微粒体中雌酮和吗啡葡糖醛酸化作用激活,并抑制对硝基苯酚葡糖醛酸化作用。胰岛素治疗可恢复对硝基苯酚葡糖醛酸转移酶(GT)降低的活性,且不会消除糖尿病对雌酮葡糖醛酸化作用的激活。Triton X-100去污剂激活可减少正常、糖尿病和胰岛素治疗大鼠在所检测底物葡糖醛酸化速率上的差异。1,4-苯二氮䓬类药物在正常、糖尿病和胰岛素治疗的糖尿病大鼠中均抑制吗啡GT活性并刺激雌酮GT活性。糖尿病中雌酮和外源性物质的GT活性激活与抑制似乎与肝微粒体的膜扰动有关。

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