Wilcox J G, Stanczyk F Z, Morris R S, Gentzschein E, Lobo R A
University of Southern California School of Medicine, Los Angeles, USA.
Fertil Steril. 1996 Nov;66(5):748-52. doi: 10.1016/s0015-0282(16)58629-4.
To determine the independent biologic effects of 17 alpha-dihydroequilin sulfate.
Prospective randomized study.
University of Southern California Medical Center.
PATIENTS(S): Twenty-one postmenopausal women, mean age 50 +/- 2 (+/-SEM) years, and mean body mass index 27 +/- 2.
INTERVENTION(S): Women were randomized to receive daily oral doses of either 1.25 mg of estrone sulfate (E1S), 0.2 mg of 17 alpha-dihydroequilin sulfate, or a combination. Three blood and urine samples were obtained before and after 30 and 90 days of treatment.
RESULT(S): After 30 and 90 days of treatment, E1S alone increased sex hormone-binding globulin (SHBG) levels significantly, 19.7% +/- 6.0% and 61.3% +/- 13.0%, whereas 17 alpha-dihydroequilin sulfate reduced SHBG levels, 20.8% +/- 68% and 12.4% +/- 7.5%, respectively. Nevertheless, the combination of E1S and 17 alpha-dihydroequilin sulfate significantly increased SHBG levels, 103% +/- 27.9% and 98.2% +/- 19.1%, compared with baseline at 30 and 90 days. Fewer changes were evident with corticosteroid-binding globulin (CBG). After 90 days of treatment, CBG levels significantly increased 30.9% +/- 5.5% with E1S, decreased by 7.2% +/- 5.0% with 17 alpha-dihydroequilin sulfate, and, with the combination, significantly increased by 10.5% +/- 2.4% compared with baseline. Changes in lipids and lipoproteins were more variable. However, high-density-lipoprotein cholesterol increased significantly with E1S at 30 and 90 days compared with baseline, 96.5% +/- 39% and 91.5% +/- 22.6%, and with the combination increased 66.4% +/- 13.3% and 79.2% +/- 24.4%, respectively. Fewer changes were evident with 17 alpha-dihydroequilin sulfate alone, decreasing 4.4% +/- 22% and 2.6% +/- 21.3%. Urinary ratios of bone collagen equivalents-creatinine and calcium-creatinine decreased in all three groups. However, the combination group resulted in a significantly greater percentage decrease in bone collagen equivalents-creatinine than with E1S alone.
CONCLUSIONS(S): 17 alpha-Dihydroequilin sulfate could modify some of the first-pass effects of conjugated equine estrogens and act synergistically with other conjugated equine estrogens to reduce bone resorption.
确定硫酸17α - 双氢马萘雌酮的独立生物学效应。
前瞻性随机研究。
南加州大学医学中心。
21名绝经后女性，平均年龄50±2（±标准误）岁，平均体重指数27±2。
女性被随机分配，每日口服剂量分别为1.25毫克硫酸雌酮（E1S）、0.2毫克硫酸17α - 双氢马萘雌酮或两者组合。在治疗30天和90天前后采集三份血液和尿液样本。
治疗30天和90天后，单独使用E1S可显著提高性激素结合球蛋白（SHBG）水平，分别提高19.7%±6.0%和61.3%±13.0%，而硫酸17α - 双氢马萘雌酮则降低SHBG水平，分别降低20.8%±6.8%和12.4%±7.5%。然而，E1S与硫酸17α - 双氢马萘雌酮组合在30天和90天时与基线相比显著提高SHBG水平，分别提高103%±27.9%和98.2%±19.1%。皮质类固醇结合球蛋白（CBG）变化不明显。治疗90天后，E1S使CBG水平显著升高30.9%±5.5%，硫酸17α - 双氢马萘雌酮使其降低7.2%±5.0%，组合使用时与基线相比显著升高10.5%±2.4%。脂质和脂蛋白的变化更具变异性。然而，与基线相比，E1S在30天和90天时使高密度脂蛋白胆固醇显著升高，分别升高96.5%±39%和91.5%±22.6%，组合使用时分别升高66.4%±13.3%和79.2%±24.4%。单独使用硫酸17α - 双氢马萘雌酮变化不明显，分别降低4.4%±22%和2.6%±21.3%。三组的骨胶原当量 - 肌酐和钙 - 肌酐尿比值均下降。然而，组合组骨胶原当量 - 肌酐的下降百分比显著大于单独使用E1S组。
硫酸17α - 双氢马萘雌酮可改变结合马雌激素的一些首过效应，并与其他结合马雌激素协同作用以减少骨吸收。
