Yamamoto T, Yoshiji S, Urabe M, Shiroshita K, Fujii M, Honjo H, Okada H
Nihon Sanka Fujinka Gakkai Zasshi. 1987 May;39(5):849-52.
The inhibitory effects of androstenedione aromatase activity in human placenta using fluoroethindrone (10 beta-fluoro-17 alpha-ethynyl-19-nortestosterone), which is a derivative of norethindrone (17 alpha-ethynyl-19-nortestosterone, ENT) and, unlike ENT, is considered to be refractory to aromatization, was investigated in this study. When fluoroethindrone was added to the placental microsomes in the presence of NADPH, androstenedione aromatase activity in the placental microsomes was decreased time dependently and dose-dependently by fluoroethindrone compared with the samples without NADPH. This finding suggests that fluoroethindrone acts as a suicide substrate for androstenedione aromatase in human placenta.
本研究考察了炔诺酮（17α-乙炔基-19-去甲睾酮，ENT）的衍生物氟炔诺酮（10β-氟-17α-乙炔基-19-去甲睾酮）对人胎盘雄烯二酮芳香化酶活性的抑制作用，与ENT不同，氟炔诺酮被认为不易发生芳香化。当在存在NADPH的情况下将氟炔诺酮添加到胎盘微粒体中时，与没有NADPH的样品相比，氟炔诺酮使胎盘微粒体中的雄烯二酮芳香化酶活性呈时间依赖性和剂量依赖性降低。这一发现表明，氟炔诺酮在人胎盘中可作为雄烯二酮芳香化酶的自杀底物。
