Smals A G, Dony J M, Smals A E, Pieters G F, Hermus A R, Boers G H, Benraad T J, Kloppenborg P W
J Clin Endocrinol Metab. 1985 Jun;60(6):1127-31. doi: 10.1210/jcem-60-6-1127.
Aromatase inhibition by delta 1-testolactone [(17 oxa-D-homo 1,4 androstanediene-3,17 dione) 500 mg twice daily for 10 days] in nine normal men lowered circulating estradiol (E2) levels by about 25%, enhanced the secretion of FSH, 17-hydroxyprogesterone (17-OHP), and to a lesser degree testosterone (T), but did not affect serum LH levels. Despite E2 lowering there was greater accumulation of 17-OHP than of T after 7 days of treatment, suggesting 17,20-lyase inhibition. Unexpectedly, administration of delta 1-testolactone almost halved the T response to hCG (Pregnyl, 1500 IU), but did not affect the 17-OHP response. Thus, E2 lowering by testolactone aggravated the hCG-induced 17,20-lyase block present before testolactone administration. Although the present data might suggest that estrogens do not play a role in the genesis of the hCG-induced late steroidogenic block, the results suggest that testolactone per se, in addition to its reported antiestrogenic action, inhibits 17,20 lyase.
在九名正常男性中,使用δ1-睾酮内酯([17-氧杂-D-高-1,4-雄甾二烯-3,17-二酮],每日两次,每次500毫克,共10天)抑制芳香化酶,可使循环雌二醇(E2)水平降低约25%,增强促卵泡生成素(FSH)、17-羟孕酮(17-OHP)的分泌,并在较小程度上增强睾酮(T)的分泌,但不影响血清促黄体生成素(LH)水平。尽管E2水平降低,但治疗7天后,17-OHP的积累量比T更多,提示存在17,20-裂解酶抑制。出乎意料的是,给予δ1-睾酮内酯后,T对人绒毛膜促性腺激素(Pregnyl,1500国际单位)的反应几乎减半,但不影响17-OHP的反应。因此,睾酮内酯降低E2水平加重了在给予睾酮内酯之前就已存在的人绒毛膜促性腺激素诱导的17,20-裂解酶阻滞。尽管目前的数据可能表明雌激素在人绒毛膜促性腺激素诱导的晚期类固醇生成阻滞的发生中不起作用,但结果表明,睾酮内酯本身除了其已报道的抗雌激素作用外,还抑制17,20-裂解酶。