Ruh T S, Wassilak S G, Ruh M F
Steroids. 1975 Feb;25(2):257-73. doi: 10.1016/s0039-128x(75)90169-5.
The effect of androgens on the nuclear uptake of both tritiated estradiol (3H-E2) and the estrogen receptor was studied in immature rat uteri. It was demonstrated that in vitro preincubation of immature rat uteri with various androgens (1 muM to 50 muM) followed by incubation with 3H-E2 (20 nM) resulted in a greatly decreased specific nuclear uptake of 3H-E2. Non-androgenic steroids had no effect. It was also confirmed that 5alpha-dihydrotestosterone (DHT) causes the accumulation of the estrogen receptor in the nuclei of uterine tissue. In vitro incubations of rat uteri with DHT (1muM and 50muM) were found to cause maximal nuclear estrogen receptor accumulation to the same degree as caused by estradiol, i.e. the nuclear uptake of approximately 100% of the estrogen receptor. Antiandrogens, which block the binding of androgens to the testosterone receptor in various tissues, did not inhibit the DHT - induced decrease in the 3H-E2 uptake by the uterine nuclei or the DHT - caused accumulation of the estrogen receptor in nuclei. These results seem to indicate that the uterine testosterone receptor has no role in the androgen - induced nuclear uptake of the estrogen receptor. However, the non-steroidal antiestrogens inhibited the DHT - induced nuclear accumulation of the estrogen receptor. This would seem to indicate that the estrogen - and androgen - induced nuclear accumulation of the estrogen receptor share a common mechanism.
研究了雄激素对未成熟大鼠子宫中氚标记雌二醇（3H-E2）和雌激素受体核摄取的影响。结果表明，用不同浓度雄激素（1μM至50μM）对未成熟大鼠子宫进行体外预孵育，随后与3H-E2（20 nM）孵育，会导致3H-E2的特异性核摄取大幅降低。非雄激素类甾体没有这种作用。还证实了5α-二氢睾酮（DHT）会导致子宫组织细胞核中雌激素受体的积累。发现用DHT（1μM和50μM）对大鼠子宫进行体外孵育，会引起最大程度的核雌激素受体积累，其程度与雌二醇引起的相同，即约100%的雌激素受体的核摄取。抗雄激素药物可阻断雄激素与各种组织中睾酮受体的结合，但并不抑制DHT诱导的子宫细胞核对3H-E2摄取的减少，也不抑制DHT引起的细胞核中雌激素受体的积累。这些结果似乎表明，子宫睾酮受体在雄激素诱导的雌激素受体核摄取中不起作用。然而，非甾体类抗雌激素药物可抑制DHT诱导的雌激素受体核积累。这似乎表明，雌激素和雄激素诱导的雌激素受体核积累具有共同机制。
