Various estrogen analogs were synthesized and tested for binding to human ERα using a fluorescence polarization displacement assay. Binding affinity and orientation were also predicted using docking calculations. Docking was able to accurately predict relative binding affinity and orientation for estradiol, but only if a tightly bound water molecule bridging Arg394/Glu353 is present. Di-hydroxy...

Sex hormones are important for bone growth. However, the mechanism by which sex hormone receptors influence bone growth remains unclear. In orthodontic treatment, there is a need to develop an indicator of bone maturity to accurately predict the beginning and end of growth. This indicator might be developed from the screening of sex hormones. The purpose of this study was to investigate the rol...

Our laboratory has demonstrated that 17β-estradiol (E2) enhances hippocampal memory consolidation via rapid activation of multiple intracellular signaling cascades, including the ERK/MAPK cascade (Fernandez et al., 2008; Fan et al., 2010). However, the receptor mechanisms responsible for these effects of E2 remain unclear. In vitro, estrogen receptor α (ERα) signaling through metabotropic gluta...

Adult male rats were orchidectomized (ORX) and treated with 17β-estradiol or young coconut juice (YCJ) for ten weeks. Their femur L5 vertebra dissected, the percentage of bone volume was measured using a Micro-CT scan. Immunohistochemistry used to detect ERα ERβ determine if osteoporotic protective effects YCJ due attachment active components(s) estrogen receptors. It found that both in osteocy...

Bisphenol A (BPA), an abundant endocrine disruptor, affects stress-responsiveness and related behaviors in children. In rats, perinatal BPA exposure modifies stress response in pubertal offspring via unknown mechanisms. Here we examined possible epigenetic modifications in the glucocorticoid receptor gene and its regulator Fkbp5 in hypothalamus and hippocampus of exposed offspring. We found inc...

The objective of this study was to evaluate the estrogenic effects and mechanisms of three flavonoid components in Xiaoyao powder: quercetin, kaempferol, and isorhamnetin. The drugs were used to treat estrogen receptor (ER)-positive human breast cancer MCF-7 cells, and proliferation was measured using the MTT method. The expression of proteins and mRNA of the ER subtype were measured using west...

The breast cancer resistance protein (BCRP) is abundant in the placenta and protects the fetus by limiting placental drug penetration. We hypothesize that pregnancyspecific hormones regulate BCRP expression. Hence, we examined the effects of progesterone (P4) and 17β-estradiol (E2) on BCRP expression in the human placental BeWo cells. P4 and E2 significantly increased and decreased BCRP protein...

A set of isoflavononid and flavonoid analogs was prepared evaluated for estrogen receptor α (ERα) ERβ transactivation anti-neuroinflammatory activities. Structure–activity relationship (SAR) study naturally occurring phytoestrogens, their metabolites, related isoflavone revealed the importance C-ring isoflavonoids ER activity selectivity. Docking suggested putative binding modes daidzein 2 dehy...

8-Prenylnaringenin (8-PN) is a phytoestrogen with the highest estrogenic activity. The objective of the present study was to confirm the superiority of 8-PN on bone metabolisms and the estrogen receptor (ER) subtype mediating effects of 8-PN. The osteoblast MC3T3-E1 and osteoclast-like cell line RAW264.7 were treated with 17β-estradiol (10(-8) mol/L), genistein (10(-5) mol/L), daidzein (10(-5) ...

Phytoestrogens are estrogen-like compounds of plant origin. The pharmacological activities of phytoestrogens are predominantly due to their antioxidant, anti-inflammatory and lipid-lowering properties, which are mediated via the estrogen receptors (ERs): estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) and possibly G protein-coupled estrogen receptor 1 (GPER). Gypenoside XVII (GP-...