Schröder H, Ziegler M, el Etreby M F
Research Laboratories of Schering AG, Berlin, F.R.G.
J Steroid Biochem. 1988 Oct;31(4B):685-90. doi: 10.1016/0022-4731(88)90019-2.
In an in vitro rat testis cell suspension model, the metabolism of tritiated testosterone, dihydrotestosterone and androstenedione was investigated. In the presence of aromatase inhibitors like 1-methyl-androsta-1,4-dien-3,17-dione (SH 489) and 4-hydroxy-androstenedione, the metabolism was shifted towards 17-keto forms. The same effect was observed in the presence of androstenedione, the parent compound of the two aromatase inhibitors. The consequent consideration of the whole labelled steroidal spectrum in each experiment leads to the conclusion that androstenedione and the derived aromatase inhibitors activate the 17 beta-hydroxysteroid-dehydrogenase in a product activating manner. Our results imply that aromatase inhibitors may regulate the intratissular levels not only of estrogens but also of other hormonally active steroids like dihydrotestosterone and 5-androstenedione.
在体外大鼠睾丸细胞悬浮模型中,研究了氚标记的睾酮、双氢睾酮和雄烯二酮的代谢。在存在1-甲基-雄甾-1,4-二烯-3,17-二酮(SH 489)和4-羟基雄烯二酮等芳香化酶抑制剂的情况下,代谢向17-酮形式转变。在两种芳香化酶抑制剂的母体化合物雄烯二酮存在的情况下也观察到了相同的效果。在每个实验中对整个标记甾体谱的后续考虑得出结论,雄烯二酮和衍生的芳香化酶抑制剂以产物激活的方式激活17β-羟基类固醇脱氢酶。我们的结果表明,芳香化酶抑制剂不仅可以调节组织内雌激素的水平,还可以调节双氢睾酮和5-雄烯二酮等其他具有激素活性的类固醇的水平。