Potential Estrogenic Properties of 17β-Hydroxy-ethylimine Estradiol Derivative Targeted to Menopause Stage.

Biol Pharm Bull

Departament of Pharmacology, National Autonomous University of Mexico. Av. Universidad No. 3000, Ciudad Universitaria, Colonia Copilco Universidad.

Published: August 2021

Background/aim: Hormone replacement therapy during menopause increases the risk of thromboembolic diseases and cancer, so safety alternative therapeutic strategies are needed. 17β-Aminoestrogens are a synthetic estrogens group that possess mild anticoagulant activity that contrasts with the pro-coagulant effects showed by estradiol's (E) in rodents. Being considered an alternative to conventional hormone replacement therapy during menopause without thrombogenic risks producing. The present study aimed to determine the estrogenic profile and anxiolytic activity of 17β-[hydroxy-ethylimine]-1,3,5(10)-estratrien-3-ol (IE), a related compound unknown until now.

Methods: IE was assessed in immature rats by uterotrophic assay administering IE E or vehicle. In ovariectomized adult Wistar rats (Ovx) to facilitating the lordotic behavior compared with E estradiol benzoate, or vehicle. The effect of IE on anxiety was estimated in Ovx animals treated with IE, E, or vehicle group and evaluated in the elevated plus-maze model.

Results And Conclusion: IE produced an uterotrophic effect, lordotic behavior, and anxiolytic effect in a dose-dependent manner, similar to E. IE depicted estrogenicity, indicating potential clinical use as hormone replacement therapy during menopause.

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http://dx.doi.org/10.1248/bpb.b20-00596DOI Listing

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