Ruh T S, Ruh M F
Endocrinology. 1975 Nov;97(5):1144-50. doi: 10.1210/endo-97-5-1144.
Studies were conducted to determine the ability of androgens in vitro to elicit the induction of a specific uterine protein (IP) normally attributed to estrogens. Both 5alpha-dihydrotestosterone (5alpha-DHT) and testosterone were effective in stimulating IP synthesis in rat uterine tissue in a concentration dependent manner (0.1 muM to 50 muM). 5alpha-DHT was more effective than testosterone and reached approximately 85% of the estradiol stimulated IP response at 10 muM and 50 muM; whereas testosterone was only able to achieve about a 70% IP response at 50 muM. This androgen stimulated IP synthesis was stereospecific since cis-testosterone and 5beta-DHT, inactive androgen isomers, were unable to evoke a detectable IP response at any concentration studied. Antiandrogens were unable to inhibit the 5alpha-DHT stimulated IP synthesis but antiestrogens were able to greatly inhibit the 5alpha-DHT and testosterone stimulated IP responses in a concentration dependent manner. The anti-estrogens, themselves, were very weak inducers of the IP response. The nuclear accumulation of the estrogen receptor by various androgens and inactive androgen isomers was also determined. Approximately 100% nuclear accumulation of receptor was attained with 1 muM 5alpha-DHT, whereas 50 muM testosterone was needed for 100% uptake. 5beta-DHT was unable to translocate the receptor at the lower concentrations tested, but caused a significant nuclear accumulation of 50 muM. Cis-testosterone was unable to cause the nuclear accumulation of the estrogen receptor at all concentrations studied. These studies suggest that some of the estrogen receptors accumulated in the nuclei by androgens, inactive androgen isomers, or antiestrogens may not be capable of eliciting a biological response.
开展了多项研究以确定雄激素在体外引发通常归因于雌激素的特定子宫蛋白(IP)诱导的能力。5α-二氢睾酮(5α-DHT)和睾酮均能以浓度依赖性方式(0.1μM至50μM)有效刺激大鼠子宫组织中的IP合成。5α-DHT比睾酮更有效,在10μM和50μM时达到约85%的雌二醇刺激的IP反应;而睾酮在50μM时仅能达到约70%的IP反应。这种雄激素刺激的IP合成具有立体特异性,因为顺式睾酮和5β-DHT(无活性的雄激素异构体)在任何研究浓度下都无法引发可检测到的IP反应。抗雄激素不能抑制5α-DHT刺激的IP合成,但抗雌激素能够以浓度依赖性方式极大地抑制5α-DHT和睾酮刺激的IP反应。抗雌激素本身是非常弱的IP反应诱导剂。还测定了各种雄激素和无活性雄激素异构体对雌激素受体核内积累的情况。1μM的5α-DHT可使约100%的受体核内积累,而100%摄取则需要50μM的睾酮。5β-DHT在较低测试浓度下无法使受体易位,但在50μM时会导致显著的核内积累。顺式睾酮在所有研究浓度下都无法导致雌激素受体的核内积累。这些研究表明,雄激素、无活性雄激素异构体或抗雌激素在细胞核中积累的一些雌激素受体可能无法引发生物学反应。