Baker H W, Bailey D J, Feil P D, Jefferson L S, Santen R J, Bardin C W
Department of Medicine, Milton S. Hershey Medical Center, Pennsylvania State University, Hershey 17033.
Endocrinology. 1977 Mar;100(3):709-21. doi: 10.1210/endo-100-3-709.
The uptake of androgens into the nuclei of caput epididymis, ventral prostate, seminal vesicle and testis was studied by recirculating physiological and pharmacological concentrations of [3H]testosterone in an artificial medium through the lower half (hemicorpus) of castrated or hypophysectomized rats. The accumulation of dihydrotestosterone in accessory sex organ nuclei was saturable, inhibited by perfusion of excess testosterone or cyproterone acetate, and associated with binding to 3S salt-extractable molecules. In castrated preparations the mean saturation levels (pmol/mg DNA) were different in the three organs: seminal vesicle, 2.8; ventral prostate, 1.8; caput epididymis, 0.9. The saturation level was significantly lower in ventral prostate of hypophysectomized rats (1.2) treated with testosterone to regenerate the accessory sex organs. Testosterone was the major nuclear androgen in the testes of mature hypophysectomized preparations perfused with testosterone. Although there was a large amount of nonspecific accumulation, testosterone binding to 3S molecules was shown by sucrose gradient centrifugation. Binding of dihydrotestosterone to 3S molecules in testicular nuclei was also demonstrated. The ratio of dihydrotestosterone to testosterone was different in immature and mature testicular nuclei and was altered by treatments known to affect testicular 5 alpha-reductase activity. The results suggest that in rat accessory sex organs and immature testis the major active androgen is dihydrotestosterone, whereas in mature testis it is testosterone. The shift in the predominant nuclear androgen in the testis from dihydrotestosterone to testosterone is most simply explained by the maturational change in 5 alpha-reductase activity.
通过在人工培养基中使生理浓度和药理浓度的[3H]睾酮在去势或垂体切除大鼠的下半部分(半体)循环,研究雄激素进入附睾头、腹侧前列腺、精囊和睾丸细胞核的情况。双氢睾酮在附属生殖器官细胞核中的积累是可饱和的,可被过量睾酮或醋酸环丙孕酮灌注所抑制,并且与3S盐可提取分子的结合有关。在去势制剂中,三个器官的平均饱和水平(pmol/mg DNA)不同:精囊为2.8;腹侧前列腺为1.8;附睾头为0.9。用睾酮处理以再生附属生殖器官的垂体切除大鼠的腹侧前列腺中的饱和水平显著较低(1.2)。睾酮是灌注睾酮的成熟垂体切除制剂睾丸中的主要核雄激素。尽管存在大量非特异性积累,但通过蔗糖梯度离心显示睾酮与3S分子结合。还证明了双氢睾酮与睾丸细胞核中3S分子的结合。未成熟和成熟睾丸细胞核中双氢睾酮与睾酮的比例不同,并且已知会影响睾丸5α-还原酶活性的处理会改变该比例。结果表明,在大鼠附属生殖器官和未成熟睾丸中,主要的活性雄激素是双氢睾酮,而在成熟睾丸中是睾酮。睾丸中主要核雄激素从双氢睾酮向睾酮的转变最容易通过5α-还原酶活性的成熟变化来解释。