达那唑在体外对人胎盘孕酮合成的抑制作用。

Inhibition of human placental progesterone synthesis by danazol in vitro.

作者信息

Rabe T, Kiesel L, Runnebaum B

出版信息

Fertil Steril. 1983 Sep;40(3):330-3. doi: 10.1016/s0015-0282(16)47295-x.

Abstract

In vitro, danazol showed a slight dose-dependent inhibition of the mitochondrial cholesterol side chain cleavage enzyme isolated from early gestational (8th to 12th week of gestation) placenta. In the presence of 100 microM danazol, the enzyme activity was 65% of controls. Danazol inhibits dose-dependently the mitochondrial 3 beta-hydroxysteroid dehydrogenase (I50 = 3.1 microM; Ki = 1 microM) (noncompetitive inhibition) and the cytoplasmic 20 alpha-hydroxysteroid dehydrogenase (I50 = 1.4 microM; Ki = 2.6 microM) (competitive inhibition). The inhibition of human placental progesterone synthesis by danazol in vitro is a further example for the direct interference of danazol with steroidogenesis.

摘要

在体外，达那唑对从妊娠早期（妊娠第8至12周）胎盘分离出的线粒体胆固醇侧链裂解酶表现出轻微的剂量依赖性抑制作用。在存在100微摩尔达那唑的情况下，酶活性为对照组的65%。达那唑剂量依赖性地抑制线粒体3β-羟基类固醇脱氢酶（半数抑制浓度I50 = 3.1微摩尔；抑制常数Ki = 1微摩尔）（非竞争性抑制）和细胞质20α-羟基类固醇脱氢酶（I50 = 1.4微摩尔；Ki = 2.6微摩尔）（竞争性抑制）。达那唑在体外对人胎盘孕酮合成的抑制是达那唑直接干扰类固醇生成的又一实例。