Potential Estrogenic Properties of 17β-Hydroxy-ethylimine Estradiol Derivative Targeted to Menopause Stage
| Autor: | Guadalupe Luisa Jimenez-Sánchez, Mariana Segovia-Mendoza, Cristina Lemini, Alejandra Figueroa |
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| Rok vydání: | 2021 |
| Předmět: |
Male
0301 basic medicine medicine.medical_specialty medicine.drug_class viruses Pharmaceutical Science Anxiolytic 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Internal medicine medicine Animals Hormone replacement therapy Rats Wistar Stage (cooking) Pharmacology Dose-Response Relationship Drug Estradiol business.industry Uterus Cancer Estrogens General Medicine Lordosis behavior medicine.disease Rats Menopause 030104 developmental biology Endocrinology Anti-Anxiety Agents chemistry 030220 oncology & carcinogenesis Ovariectomized rat Estradiol benzoate Female business |
| Zdroj: | Biological and Pharmaceutical Bulletin. 44:63-68 |
| ISSN: | 1347-5215 0918-6158 |
| DOI: | 10.1248/bpb.b20-00596 |
| Popis: | 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 (E2) 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 (IE2), a related compound unknown until now. METHODS IE2 was assessed in immature rats by uterotrophic assay administering IE2, E2, or vehicle. In ovariectomized adult Wistar rats (Ovx) to facilitating the lordotic behavior compared with E2, estradiol benzoate, or vehicle. The effect of IE2 on anxiety was estimated in Ovx animals treated with IE2, E2, or vehicle group and evaluated in the elevated plus-maze model. RESULTS AND CONCLUSION IE2 produced an uterotrophic effect, lordotic behavior, and anxiolytic effect in a dose-dependent manner, similar to E2. IE2 depicted estrogenicity, indicating potential clinical use as hormone replacement therapy during menopause. |
| Databáze: | OpenAIRE |
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