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

Abstract

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 2 ) 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 2 ), a related compound unknown until now. Methods: IE 2 was assessed in immature rats by uterotrophic assay administering IE 2, E 2, or vehicle. In ovariectomized adult Wistar rats (Ovx) to facilitating the lordotic behavior compared with E 2, estradiol benzoate, or vehicle. The effect of IE 2 on anxiety was estimated in Ovx animals treated with IE 2 , E 2 , or vehicle group and evaluated in the elevated plus-maze model. Results and conclusion: IE 2 produced an uterotrophic effect, lordotic behavior, and anxiolytic effect in a dose-dependent manner, similar to E 2 . IE 2 depicted estrogenicity, indicating potential clinical use as hormone replacement therapy during menopause.