11β-羟类固醇脱氢酶 1 对类固醇、毒素和药物的代谢。

The metabolism of steroids, toxins and drugs by 11β-hydroxysteroid dehydrogenase 1.

机构信息

Department of Pharmacology, School of Pharmacy, Wenzhou Medical College, Wenzhou, Zhejiang 325000, China.

出版信息

Toxicology. 2012 Feb 6;292(1):1-12. doi: 10.1016/j.tox.2011.11.012. Epub 2011 Nov 28.

DOI:10.1016/j.tox.2011.11.012

Abstract

11β-Hydroxysteroid dehydrogenase isoform 1 (11β-HSD1) is a member of the alcohol short-chain family enzyme, and catalyzes the interconversion between active glucocorticoid cortisol (in human) and inactive cortisone. The redox ratio of NADP+/NADPH determines its direction with NADPH favoring its reductase activity and NADP+ favoring its oxidase activity. In many tissues such as the liver and lung, 11β-HSD1 behaves primarily as a reductase because of the intracellular enzyme coupling with hexose-6-phosphate dehydrogenase, which uses the NADP+ as cofactor to supply NADPH driving 11β-HSD1 to function as a reductase. 11β-HSD1 catalyzes the metabolism of 7- or 11-keto steroids as well as many toxins and drugs. Some steroids, drugs and toxins are metabolically activated. The present review discusses the steroid, drug and toxin metabolism by 11β-HSD1.

摘要

11β-羟类固醇脱氢酶同工酶 1（11β-HSD1）是醇短链家族酶的成员，催化活性糖皮质激素皮质醇（在人类中）和非活性可的松之间的相互转化。NADP+/NADPH 的氧化还原比决定了其方向，NADPH 有利于其还原酶活性，而 NADP+ 有利于其氧化酶活性。在许多组织中，如肝脏和肺部，由于 11β-HSD1 与己糖-6-磷酸脱氢酶的细胞内酶偶联，主要表现为还原酶，该酶利用 NADP+作为辅助因子提供 NADPH，促使 11β-HSD1 作为还原酶发挥作用。11β-HSD1 催化 7-或 11-酮甾体以及许多毒素和药物的代谢。一些甾体、药物和毒素被代谢激活。本综述讨论了 11β-HSD1 对甾体、药物和毒素的代谢。