18-取代甾体。第18部分。2α-和2β-羟基醛固酮的化学合成及盐皮质激素活性

18-Substituted steroids. Part 18. Chemical synthesis and mineralocorticoid activity of 2 alpha- and 2 beta-hydroxyaldosterone.

作者信息

Kirk D N, Schröder M H, Latif S A, Souness G W, Morris D J

机构信息

Department of Chemistry, Queen Mary and Westfield College, London, UK.

出版信息

Steroids. 1993 Feb;58(2):59-63. doi: 10.1016/0039-128x(93)90053-p.

DOI:10.1016/0039-128x(93)90053-p

PMID:8484185

Abstract

The 2 alpha-hydroxy and 2 beta-hydroxy derivatives of aldosterone have been synthesized chemically from aldosterone, after the earlier identification of 2 alpha-hydroxylated metabolites formed in liver. Both 2 alpha- and 2 beta-hydroxyaldosterone are potent mineralocorticoids, with activities on the order of 1/10 that of aldosterone on the basis of a rat bioassay.

摘要

在先前鉴定出肝脏中形成的2α-羟基化代谢产物后，已从醛固酮化学合成了醛固酮的2α-羟基和2β-羟基衍生物。基于大鼠生物测定法，2α-羟基醛固酮和2β-羟基醛固酮都是有效的盐皮质激素，其活性约为醛固酮的1/10。