Kubli-Garfias C, López-Fiesco A, Pacheco-Cano M T, Ponce-Monter H, Bondani A
Steroids. 1980 Jun;35(6):633-41. doi: 10.1016/0039-128x(80)90088-4.
The effectiveness of ring A reduced (5 alpha and 5 beta) testosterone (T) derivatives upon the rat uterus spontaneous contractility was tested in vitro. Compounds with the 3 alpha-hydroxy-5 alpha reduced configuration, such as androsterone and androstanediol, and one 5 beta reduced (5 beta-dihydrotestosterone) elicited a remarkable inhibitory effect upon the myometrial activity. Although steroids with 5 beta reduction were less potent than 3 alpha-hydroxy-5 alpha reduced compounds for depressing the myometrial activity, they were somewhat more potent than T, DHEA, androstenedione and the remaining 5 alpha reduced compounds tested. Therefore, T could act as a "prehormone", accounting for the maintenance of the physiological myometrial activity through its 5-reduced derivatives.
在体外测试了A环还原(5α和5β)睾酮(T)衍生物对大鼠子宫自发收缩性的有效性。具有3α-羟基-5α还原构型的化合物,如雄酮和雄烷二醇,以及一种5β还原产物(5β-双氢睾酮)对子宫肌层活性产生了显著的抑制作用。尽管5β还原的甾体在抑制子宫肌层活性方面比3α-羟基-5α还原的化合物效力稍弱,但它们比T、脱氢表雄酮、雄烯二酮以及所测试的其余5α还原化合物效力略强。因此,T可作为一种“前激素”,通过其5-还原衍生物维持子宫肌层的生理活性。