Usui T, Ishibe T, Nakamura K, Mizutani M, Yasukawa A
Department of Urology, Shimane Medical University, Izumo, Japan.
Arch Androl. 1987;19(3):229-35. doi: 10.3109/01485018708986821.
Following the intravenous drip infusion of diethylstilbestrol diphosphate (DES-DP), the diethylstilbestrol (DES) concentrations both in plasma and prostatic tissue obtained from patients with prostatic carcinoma were measured by radioimmunoassay and the effects of DES on the activity of 5 alpha-reductase in the prostate obtained from BPH patients were determined in vitro. Further, the changes in the activity of 5 alpha-reductase in the prostate from the BPH patients who received DES-DP infusion were also determined. The plasma and prostatic tissue concentrations of DES rapidly declined from 2.3 micrograms/ml and 1.6 micrograms/g wet weight 1 h after DES-DP infusion to 0.8 microgram/ml and 0.25 microgram/g wet weight 3 h after DES-DP infusion, respectively, and decreased gradually thereafter until 24 h. In in vitro study progressed by BPH specimens, the 5 alpha-reduction rate was completely inhibited by an addition of 5 x 10(-4) M of DES and the DES concentration on the inhibition rate of 50% was 4 x 10(-5) M. In in vivo study, the mean production rate of 5 alpha-dihydrotestosterone (DHT) in the control specimens of BPH without infusion of DES-DP was 14.0 +/- 3.4 nmol/15 min/mg protein and the production rate of DHT in the DES-DP infused specimens of BPH was 14.7 nmol/15 min/mg protein at 3 h and 15.2 nmol/15 min/mg protein at 12 h after the termination of DES-DP infusion. These results indicated that intravenously administered DES-DP did not act via the inhibition of 5 alpha-reductase in the prostatic cells for producing the clinical effects.
静脉滴注己烯雌酚二磷酸酯（DES-DP）后，通过放射免疫分析法测定前列腺癌患者血浆和前列腺组织中的己烯雌酚（DES）浓度，并在体外测定DES对良性前列腺增生（BPH）患者前列腺中5α-还原酶活性的影响。此外，还测定了接受DES-DP输注的BPH患者前列腺中5α-还原酶活性的变化。DES-DP输注后1小时，血浆和前列腺组织中的DES浓度分别从2.3微克/毫升和1.6微克/克湿重迅速下降至输注后3小时的0.8微克/毫升和0.25微克/克湿重，此后逐渐下降直至24小时。在以BPH标本进行的体外研究中，添加5×10⁻⁴ M的DES可完全抑制5α-还原率，50%抑制率时的DES浓度为4×10⁻⁵ M。在体内研究中，未输注DES-DP的BPH对照标本中5α-双氢睾酮（DHT）的平均生成率为14.0±3.4纳摩尔/15分钟/毫克蛋白，DES-DP输注的BPH标本在DES-DP输注结束后3小时的DHT生成率为14.7纳摩尔/15分钟/毫克蛋白，12小时时为15.2纳摩尔/15分钟/毫克蛋白。这些结果表明，静脉注射DES-DP并非通过抑制前列腺细胞中的5α-还原酶来产生临床效果。
