Bhavnani B R, Cecutti A, Dey M S
Department of Obstetrics and Gynecology, University of Toronto, Ontario.
J Soc Gynecol Investig. 1998 May-Jun;5(3):156-60. doi: 10.1016/s1071-5576(98)00003-3.
To determine in postmenopausal women the biological effects of delta-8-estrone sulfate, a novel estrogen component of Premarin (Wyeth-Ayerst, Philadelphia, PA).
An open-label, nonrandomized study of six healthy postmenopausal women was conducted. Each subject took 0.125 mg of delta-8-estrone sulfate daily for 8 weeks. Blood samples were collected at day 0 (baseline) and once a week for 8 weeks. Urine was collected on day 0 and at weeks 2, 3, 5, 6, 7, and 8. Serum gonadotropins (follicle-stimulating hormone/luteinizing hormone), plasma binding proteins (corticosteroid-binding globulin/sex hormone-binding globulin), a marker for bone turnover (urinary n-telopeptide), and markers for cardiovascular effects (cholesterol, low-density lipoprotein, high-density lipoprotein(c), low-density lipoprotein oxidation, and rate of diene formation) were measured.
Follicle-stimulating hormone levels decreased from 84.0 +/- 8.5 to 67.0 +/- 8.5 mlU/mL (P = .02), whereas luteinizing hormone levels did not change. Corticosteroid-binding globulin levels increased from 3.30 +/- 0.16 to 4.10 +/- 0.16 mg/dL (P = .02), and no change in sex hormone-binding globulin was noted. The n-telopeptide levels decreased an average of 31% from 40.7 +/- 4.9 to 28 +/- 7.0 nmol/L bone collagen equivalents/mmol/L creatinine (P = .03). Plasma diene concentration and diene production rate decreased by 34% and 40%, respectively; these changes were not significantly different from baseline values. In contrast, a significant (P = .03) 68% increase in the lag time for low-density lipoprotein(c) oxidation (38.5 +/- 5.5 minutes versus 64.8 +/- 8.5 minutes) was observed. No significant change occurred in total cholesterol, high-density lipoprotein(c), and low-density lipoprotein(c).
Small doses (0.125 mg) of delta-8-estrone sulfate have profound estrogenic effects in postmenopausal women. The changes observed in n-telopeptide levels and the lag-time delay in oxidation of low-density lipoprotein(c) indicate that this estrogen contributes toward the overall beneficial effects on bone and cardiovascular system associated with Premarin therapy.
确定硫酸δ-8-雌酮（倍美力（惠氏-艾尔斯特，宾夕法尼亚州费城）的一种新型雌激素成分）对绝经后女性的生物学效应。
对6名健康绝经后女性进行了一项开放标签、非随机研究。每位受试者每天服用0.125mg硫酸δ-8-雌酮，持续8周。在第0天（基线）和之后的8周内每周采集一次血样。在第0天以及第2、3、5、6、7和8周收集尿液。检测血清促性腺激素（促卵泡激素/促黄体生成素）、血浆结合蛋白（皮质类固醇结合球蛋白/性激素结合球蛋白）、骨转换标志物（尿N-端肽）以及心血管效应标志物（胆固醇、低密度脂蛋白、高密度脂蛋白（c）、低密度脂蛋白氧化和二烯生成速率）。
促卵泡激素水平从84.0±8.5降至67.0±8.5mIU/mL（P = 0.02），而促黄体生成素水平未发生变化。皮质类固醇结合球蛋白水平从3.30±0.16升至4.10±0.16mg/dL（P = 0.02），性激素结合球蛋白未见变化。N-端肽水平平均下降31%，从40.7±4.9降至28±7.0nmol/L骨胶原当量/mmol/L肌酐（P = 0.03）。血浆二烯浓度和二烯生成速率分别下降34%和40%；这些变化与基线值无显著差异。相比之下，观察到低密度脂蛋白（c）氧化的延迟时间显著增加（P = 0.03）68%（从38.5±5.5分钟增至64.8±8.5分钟）。总胆固醇、高密度脂蛋白（c）和低密度脂蛋白（c）无显著变化。
小剂量（0.125mg）硫酸δ-8-雌酮对绝经后女性具有显著的雌激素效应。观察到的N-端肽水平变化以及低密度脂蛋白（c）氧化延迟时间表明，这种雌激素有助于产生与倍美力治疗相关的对骨骼和心血管系统的总体有益作用。
