To explore the uterine effects of administration of compounds that exert their bone-sparing functions through estrogen receptors, we administered 17beta-E2, raloxifene, or genistein to ovariectomized mice and analyzed the uterus weight and histology 4 weeks after beginning the treatments. Results indicated that raloxifene and genistein have partial agonistic properties on the uterus in estrogen-depleted mice, and that genistein induced apoptosis and several atypias in the glandular epithelium of endometrium, as demonstrated in hematoxylin-eosin-stained histological sections.
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http://dx.doi.org/10.1016/j.fertnstert.2006.03.029 | DOI Listing |
Pharmacol Res
June 2024
Key Laboratory of Adolescent Health Assessment and Exercise Intervention of Ministry of Education, East China Normal University, Shanghai 200241, China; College of Physical Education and Health, East China Normal University, Shanghai 200241,China. Electronic address:
Neuropsychiatric disorders shorten human life spans through multiple ways and become major threats to human health. Exercise can regulate the estrogen signaling, which may be involved in depression, Alzheimer's disease (AD) and Parkinson's disease (PD), and other neuropsychiatric disorders as well in their sex differences. In nervous system, estrogen is an important regulator of cell development, synaptic development, and brain connectivity.
View Article and Find Full Text PDFRev Bras Ortop (Sao Paulo)
April 2024
Laboratório de Ginecologia Estrutural e Molecular (LIM 58), Disciplina de Ginecologia, Departamento de Obstetrícia e Ginecologia, Hospital das Clínicas, Faculdade de Medicina, Universidade de São Paulo (HCFMUSP), São Paulo, SP, Brasil.
Drug Res (Stuttg)
February 2023
Assistant Professor, Amity University, Somathne, Mumbai, Maharashtra, India.
A series of 7 compounds with isoxazole - indole - γ-resorcylic acid scaffold, segregated into B2 & A2 series, wherein, B2 comprises Compounds: 13, 14, 15 & 16 and A2 comprises Compounds: 10, 11 & 12, on the basis of the variable substituents at the indole, resorcinol and isoxazole end of the scaffold as in Figure: 1, were designed and docked with human estrogen receptor: 1ERRα. The Binding affinity (BA) and the interacting amino acids compared with reference selective estrogen receptor modulators (SERM's) such as Raloxifene, Estradiol, Bazedoxifene, Bisphenol, Genistein, Daidzein, Ormiloxifene, Tamoxifen, 6-hydroxy-naphthalen-2yl-benzo(D)-isoxazol-6-ol(1) using PyRx software and their ADME properties predicted with SWISS ADME online tool. Significant similarities and minor differences in the binding pattern between the key interacting aminoacids such as Arg 394, Glu 353, Asp 351, Leu 346, Leu 525, Trp 383, Phe 404, Ala 350, Leu 387, Met 421 responsible for ER agonist/antagonist affinity found in the binding cavity of a 1 Errα -Bazedoxifene/1 Errα -raloxifene/1 Errα -estradiol docked complex AND 1 Errα -isoxazole-indole- resorcinol docked complex indicate their promising potential to serve as potent ER agonists in bone or ER antagonists against breast cancer and other cancer diseases.
View Article and Find Full Text PDFDrug Res (Stuttg)
November 2022
Assistant Professor, Amity University, Lucknow, Uttar Pradesh, India.
A series of 9 compounds with isoxazole-indole-γ-resorcylic acid scaffold, segregated into B1 & A1 series, wherein, B1 comprises compounds:1,3,4,5, & 9 and A1comprises compounds: 2,6,7, & 8 , on the basis of variable substituents at the indole , resorcinol and isoxazole end of the scaffold as in Fig. 1, were designed and docked with human estrogen receptor:1ERRα. The binding affinity (BA) and the interacting amino acids compared with reference selective estrogen receptor modulators (SERMs) such as Raloxifene, Estradiol, Bazedoxifene, Bisphenol, Genistein, Daidzein, Ormiloxifene,Tamoxifen,6-hydroxy-naphthalen-2yl-benzo(D)-isoxazol-6-ol(1)(WAY-397) using PyRx software and their ADME properties predicted with SWISS ADME online tool.
View Article and Find Full Text PDFGene
March 2022
Department of Kampo Medicine, Yokohama University of Pharmacy, Yokohama 245-0066, Japan. Electronic address:
20(S)-Protopanaxadiol (PPD) and 20(S)-Protopanaxatriol (PPT) are major metabolites of ginseng in humans and are considered to have estrogenic activity in cellular bioassays. In this study, we conducted in silico analyses to determine whether PPD and PPT interact with estrogen receptor alpha (ERα) and compared them with ERα agonists, partial agonists, and antagonists to identify their ERα activity. The transcriptome profile of 17β-estradiol (E2), PPD, and PPT in MCF-7 cells expressing ERα was further compared to understand the ERα activity of ginsenoside metabolites.
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