Eckstein B, Shani J, Ravid R, Goldhaber G
Endocrinology. 1981 Feb;108(2):500-5. doi: 10.1210/endo-108-2-500.
Androstanediols are the major products of the immature rat ovary and are present in peripheral circulation mainly as sulfate conjugates. In this paper we identified 5 alpha-androstane-3 beta, 17 beta-diol-3-monosulfate (3 beta-A-MS) as one of the forms found in blood and subsequently synthesized and administered it to ovariectomized rats at a dose of 100 microgram/100 g BW . day from 21-45 days of age. This dose effectively inhibits postcastrational LH elevation. Other androstanediols examined, like 5 alpha-A-3 alpha, 17 beta-diol-disulfate, 5 alpha-A-3 beta, 17 beta-diol-disulfate, and the free 5 alpha-A-3 beta, 17 beta-diol do not exert such an effect on LH release. The MCR of 3 beta-A-MS was 441 +/- 64 ml/h, independent of the infusion rate between 0.15-15.0 microgram/h, and its production rate was calculated to be 37 microgram/day at the age of 30 days. The quantitative relations of the steroid level in serum to its capacity to inhibit LH release was studied using Silastic capsules. A steady concentration of 1.1 ng 3 beta-A-MS/ml serum inhibits postcastrational LH release in the immature female rat. Since a similar or higher concentration of the steroid is present in the intact rat, it is assumed that 3 beta-A-MS controls pituitary LH release in the intact immature female rat. (Endocrinology 108: 500, 1981)
雄甾二醇是未成熟大鼠卵巢的主要产物,主要以硫酸酯结合物的形式存在于外周循环中。在本文中,我们鉴定出5α-雄甾烷-3β,17β-二醇-3-单硫酸酯(3β-A-MS)是血液中发现的一种形式,随后合成并以100微克/100克体重·天的剂量给去卵巢大鼠从21至45日龄开始给药。该剂量可有效抑制去势后LH升高。所检测的其他雄甾二醇,如5α-A-3α,17β-二醇-二硫酸酯、5α-A-3β,17β-二醇-二硫酸酯以及游离的5α-A-3β,17β-二醇对LH释放均无此作用。3β-A-MS的代谢清除率为441±64毫升/小时,与0.15至15.0微克/小时之间的输注速率无关,其生成速率在30日龄时计算为37微克/天。使用硅橡胶胶囊研究了血清中甾体水平与其抑制LH释放能力的定量关系。血清中1.1纳克3β-A-MS/毫升的稳定浓度可抑制未成熟雌性大鼠去势后的LH释放。由于完整大鼠体内存在相似或更高浓度的该甾体,因此推测3β-A-MS在完整的未成熟雌性大鼠中控制垂体LH释放。(《内分泌学》108:500,1981)