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Biologic Effects of Delta-8-Estrone Sulfate in Postmenopausal Women

Anthony Cecutti, MD

Mike S. Dey, PhD

Department of Obstetrics and Gynecology and Institute of Medical Sciences and St. Michael's Hospital, University of Toronto, Toronto, Ontario; and Wyeth-Ayerst Research Philadelphia, Pennsylvania

Objective: To determine in postmenopausal women the biological effects of delta-8-estrone sulfate, a novel estrogen component of Premarin (Wyeth-Ayerst, Philadelphia, PA).

Methods: 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 gondotropins (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_c, high-density lipoprotein_c, low-density lipoprotein oxidation, and rate of diene formation) were measured.

Results: 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.

Conclusion: 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.

Key Words: Delta-8—estrone sulfate • oxidized low-density lipoprotein • oxidation lag time • n-telopeptide

Journal of the Society for Gynecologic Investigation, Vol. 5, No. 3, 156-160 (1998)
DOI: 10.1177/107155769800500309


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