阿他美坦对人睾丸中睾酮合成抑制作用的体外研究。

In vitro studies on the inhibition of testosterone synthesis in the human testis by atamestane.

作者信息

Lombardo M E, Hakky S I, Hudson P B

机构信息

Department of Surgery, University of South Florida, College of Medicine.

出版信息

J Steroid Biochem Mol Biol. 1993 Mar;44(3):287-90. doi: 10.1016/0960-0760(93)90089-f.

DOI:10.1016/0960-0760(93)90089-f

PMID:8384873

Abstract

In view of the well established clinical results of the deprivation of androgens through orchiectomy in prostatic cancer and the structural similarities of 4-androsten-3,17-dione and atamestane (1-methyl-ADD), we studied the influence of 1-methyl-ADD on the conversion of 4-androsten-3,17-dione to testosterone by the 17 beta-hydroxysteroid reductase enzyme in human testicular tissue. Our studies, presented in this manuscript, demonstrate that 1-methyl-ADD is a competitive inhibitor of 4-androsten-3,17-dione in its reduction to testosterone by the 17 beta-hydroxysteroid reductase enzyme in the human testis.

摘要

鉴于通过睾丸切除术去除雄激素在前列腺癌治疗中已确立的临床效果，以及4-雄烯-3,17-二酮与阿他美坦（1-甲基-ADD）的结构相似性，我们研究了1-甲基-ADD对人睾丸组织中17β-羟基类固醇还原酶将4-雄烯-3,17-二酮转化为睾酮的影响。我们在本手稿中呈现的研究表明，1-甲基-ADD在人睾丸中是17β-羟基类固醇还原酶将4-雄烯-3,17-二酮还原为睾酮过程中的竞争性抑制剂。