Tezón J G, Blaquier J A
Endocrinology. 1983 Sep;113(3):1025-30. doi: 10.1210/endo-113-3-1025.
Previous results suggested that the number of androgen-binding sites in rat epididymis was controlled by androgens. Using an exchange technique for receptor determination, we now report that cytoplasmic receptor number decreased to about half the control value after 4 days of castration and reached its lowest level (30% of the control value) after 12 days of castration. The Kd for [3H]methyltrienolone for cytoplasmic receptor varied from 2.8 X 10(-9) M in controls to 0.6 X (10-9) M (P less than 0.001) after 6 or more days of castration. Nuclear binding sites were reduced to 17% of the control value from the second day of castration on, but no change in the affinity for methyltrienolone was noted. The administration of testosterone propionate (400 micrograms/day) to rats castrated for 20 days significantly increased the number of nuclear and cytoplasmic binding sites from the second and third days of treatment, respectively. Labeled thymidine incorporation into DNA rose significantly after a 4-day latency period. The proportion of total binding sites capable of translocation into the nucleus was elevated during the early phase (2-4 days) of androgen treatment. These results also suggest the heterogneity of the cytoplasmic binding site population. Control epididymides were composed of 61.5% receptor-containing epithelial cells, and this proportion was significantly reduced to 53.2% after 20 days of castration. Androgen administration elevated this percentage after an 8-day latency period. Proteolytic activity in cytosol was increased over control values after castration (for 20 days) and until the fourth day after the onset of androgen treatment. However, this activity does not seem to be an important factor in the decrease in binding sites caused by orchidectomy.
先前的研究结果表明,大鼠附睾中雄激素结合位点的数量受雄激素调控。运用一种用于受体测定的交换技术,我们现在报告,去势4天后细胞质受体数量降至对照值的约一半,去势12天后达到最低水平(对照值的30%)。细胞质受体对[3H]甲基三烯olone的解离常数(Kd)在对照中为2.8×10⁻⁹M,去势6天或更长时间后变为0.6×10⁻⁹M(P<0.001)。从去势第二天起,核结合位点降至对照值的17%,但对甲基三烯olone的亲和力未发现变化。对去势20天的大鼠每日给予丙酸睾酮(400微克),分别从治疗的第二天和第三天起,核和细胞质结合位点的数量显著增加。标记的胸苷掺入DNA在4天的潜伏期后显著上升。在雄激素治疗的早期阶段(2 - 4天),能够转运到细胞核中的总结合位点比例升高。这些结果还提示了细胞质结合位点群体的异质性。对照附睾由61.5%含受体的上皮细胞组成,去势20天后这一比例显著降至53.2%。给予雄激素8天潜伏期后,该百分比升高。去势(20天)后直至雄激素治疗开始后的第四天,胞质溶胶中的蛋白水解活性高于对照值。然而,这种活性似乎不是睾丸切除引起结合位点减少的重要因素。