Horst H J, Dennis M, Kaufmann J, Voigt K D
Acta Endocrinol (Copenh). 1975 Jun;79(2):394-402.
Tritiated 5alpha-androstane-3alpha,17beta-diol (3alpha-diol) and 5alpha-androstane-3beta,17beta-diol (3beta-diol) respectively were administered to patients with benign prostatic hypertrophy (bph) undergoing prostatectomy. In prostate and skeletal muscle homogenates and in plasma the total radioactivity content as well as the formation of metabolites were measured. Histological examination of each ectomized prostate was performed to evaluate the cellular composition of the tissue. After 3alpha-diol injection, a higher uptake of radioactivity in the prostate was obtained than after 3beta-diol. Within 30 min the 3alpha-isomer was very efficiently converted to 5alpha-DHT, while most of the 3beta-isomer remained unchanged. There was, however, also after administration of the 3beta-diol a substantial biconversion to 5alpha-DHT as has been confirmed by recrystallization to constant specific radioactivity. Only after 3beta-diol epiandrosterone was detected in small but significant amounts. 3alpha-diol administration resulted in distinct concentrations of 3beta-diol, whereas the conversion of 3beta-diol to the 3alpha-isomer was insignificant. When comparing the histological composition of the prostatic tissue with the accumulation of radioactivity and the formation of metabolites only a weak correlation between glandular structure and radioactivity uptake after 3alpha-diol administration could be revealed.
分别向接受前列腺切除术的良性前列腺增生（BPH）患者施用氚标记的5α-雄甾烷-3α，17β-二醇（3α-二醇）和5α-雄甾烷-3β，17β-二醇（3β-二醇）。测量前列腺和骨骼肌匀浆以及血浆中的总放射性含量以及代谢产物的形成。对每个切除的前列腺进行组织学检查，以评估组织的细胞组成。注射3α-二醇后，前列腺中放射性的摄取量高于注射3β-二醇后。在30分钟内，3α-异构体非常有效地转化为5α-双氢睾酮（5α-DHT），而大部分3β-异构体保持不变。然而，在施用3β-二醇后，也有大量双向转化为5α-DHT，这已通过重结晶至恒定比放射性得到证实。仅在施用3β-二醇后，才检测到少量但显著量的表雄酮。施用3α-二醇导致3β-二醇的明显浓度，而3β-二醇向3α-异构体的转化不显著。当比较前列腺组织的组织学组成与放射性积累和代谢产物形成时，在施用3α-二醇后，腺结构与放射性摄取之间仅显示出弱相关性。
