Cell proliferation and modulation of interaction of estrogen receptors with coregulators induced by ERα and ERβ agonists

Evers, Nynke M.; Berg, J.H.J. van den; Wang, Si; Melchers, Diana; Houtman, René; Haan, L.H.J. de; Ederveen, A. G. H.; Groten, J.P.; Rietjens, Ivonne M. C. M.

doi:10.1016/j.jsbmb.2014.06.002

Cited by 19 publications

(8 citation statements)

References 44 publications

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“…Luciferase activity was induced by E2 in a concentration-dependent manner in SKBR3 cells cotransfected with the ER-responsive luciferase reporter plasmid and either ERa or ERb expression vectors ( Figure 1A) with half-maximal induction of 8.5 AE 2.2 pM and 75 AE 29 pM E2, respectively ( Figure 1A; Table 1). These EC50 values are comparable to previously published results in human osteosarcoma cells transfected with ERa or ERb [30]. Concentration-dependent analysis showed that the ERb-selective ligands genistein or Br-ERb-041 were more potent activators of ERb-dependent luciferase reporter gene expression than that observed with ERa ( Figures 1B and C), with EC50 induction values in ERb-and ERa-transfected SKBR3 cells for genistein of 44 AE 19 nM and 260 AE 79 nM, and for Br-ERb-041 54 AE 8.5 nM and 970 AE 130 nM, respectively (Table 1).…”

Section: Subtype Selectivity Of Ligandssupporting

confidence: 90%

Development of a recombinant human ovarian (BG1) cell line containing estrogen receptor α and β for improved detection of estrogenic/antiestrogenic chemicals

Brennan

Bassal

et al. 2015

Enviro Toxic and Chemistry

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Estrogenic endocrine disrupting chemicals are found in environmental and biological samples, commercial and consumer products, food, and numerous other sources. Given their ubiquitous nature and potential for adverse effects, there is a critical need for rapidly detecting these chemicals. We developed an estrogen-responsive recombinant human ovarian (BG1Luc4E2) cell line recently accepted by the USEPA and OECD as a bioanalytical method to detect estrogen receptor (ER) agonists/antagonists. Unfortunately, these cells appear to contain only one of the two known ER isoforms, ERα but not ERβ, and the differential ligand selectivity of these ERs indicates that the currently accepted screening method only detects a subset of total estrogenic chemicals. To improve the estrogen screening bioassay, BG1Luc4E2 cells were stably transfected with an ERβ expression plasmid and positive clones identified using ERβ-selective ligands (genistein and Br-ERβ-041). A highly responsive clone (BG1LucERβc9) was identified that exhibited greater sensitivity and responsiveness to ERβ-selective ligands than BG1Luc4E2 cells and qRT-PCR confirmed the presence of ERβ expression in these cells. Screening of pesticides and industrial chemicals identified chemicals that preferentially stimulated ERβ-dependent reporter gene expression. Together, these results not only demonstrate the utility of this dual ER recombinant cell line for detecting a broader range of estrogenic chemicals than the current BG1Luc4E2 cell line, but screening with both cell lines allows identification of ERα and ERβ-selective chemicals.

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Section: Subtype Selectivity Of Ligandssupporting

confidence: 90%

Development of a recombinant human ovarian (BG1) cell line containing estrogen receptor α and β for improved detection of estrogenic/antiestrogenic chemicals

Brennan

Bassal

et al. 2015

Enviro Toxic and Chemistry

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“…Our present results indicate that E 2 , by activating the intracellular ERα, shortens the time spent by macrophages in the inflammatory status and facilitates the onset of the AD phenotype. Our findings are in line with and provide mechanistic insights to the reports of an estrogen positive effect on angiogenesis and proliferation 41 42 43 or in wound healing of chronic wounds 44 45 .…”

Section: Discussionsupporting

confidence: 87%

Estrogen accelerates the resolution of inflammation in macrophagic cells

Villa

Rizzi

Vegeto

et al. 2015

Sci Rep

200

139

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Although 17β-estradiol (E2) anti-inflammatory activity has been well described, very little is known about the effects of this hormone on the resolution phase of the inflammatory process. Here, we identified a previously unreported ERα-mediated effect of E2 on the inflammatory machinery. The study showed that the activation of the intracellular estrogen receptor shortens the LPS-induced pro-inflammatory phase and, by influencing the intrinsic and extrinsic programs, triggers the resolution of inflammation in RAW 264.7 cells. Through the regulation of the SOCS3 and STAT3 signaling pathways, E2 facilitates the progression of the inflammatory process toward the IL10-dependent “acquired deactivation” phenotype, which is responsible for tissue remodeling and the restoration of homeostatic conditions. The present study may provide an explanation for increased susceptibility to chronic inflammatory diseases in women after menopause, and it suggests novel anti-inflammatory treatments for such disorders.

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“…As a result, a certain phytoestrogen may have different effects in, for example, the uterus, in which ERα is the major isoform (Pearce and Jordan, ), than in the prostate, in which ERβ is dominant (Enmark et al , ; Pearce and Jordan, ). These tissue‐specific effects may also result from differences in coactivators and corepressors activated upon activation of the two ERs in different tissues and/or the possible crosstalk of the ERs with other nuclear receptors (Wilson et al , ; Chang et al , ; Vanden Berghe and Haegeman, ; Evers et al , ; Evers et al , ). Furthermore, the actual mode of action of a phytoestrogen, either as an agonist or an antagonist, may also depend on the level of endogenous estrogens present (Barnes et al , ).…”

Section: Introductionmentioning

confidence: 99%

The potential health effects of dietary phytoestrogens

Rietjens

Louisse

Beekmann

2016

British J Pharmacology

410

246

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Phytoestrogens are plant‐derived dietary compounds with structural similarity to 17‐β‐oestradiol (E2), the primary female sex hormone. This structural similarity to E2 enables phytoestrogens to cause (anti)oestrogenic effects by binding to the oestrogen receptors. The aim of the present review is to present a state‐of‐the‐art overview of the potential health effects of dietary phytoestrogens. Various beneficial health effects have been ascribed to phytoestrogens, such as a lowered risk of menopausal symptoms like hot flushes and osteoporosis, lowered risks of cardiovascular disease, obesity, metabolic syndrome and type 2 diabetes, brain function disorders, breast cancer, prostate cancer, bowel cancer and other cancers. In contrast to these beneficial health claims, the (anti)oestrogenic properties of phytoestrogens have also raised concerns since they might act as endocrine disruptors, indicating a potential to cause adverse health effects. The literature overview presented in this paper illustrates that several potential health benefits of phytoestrogens have been reported but that, given the data on potential adverse health effects, the current evidence on these beneficial health effects is not so obvious that they clearly outweigh the possible health risks. Furthermore, the data currently available are not sufficient to support a more refined (semi) quantitative risk–benefit analysis. This implies that a definite conclusion on possible beneficial health effects of phytoestrogens cannot be made.Linked ArticlesThis article is part of a themed section on Principles of Pharmacological Research of Nutraceuticals. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v174.11/issuetoc

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Cell proliferation and modulation of interaction of estrogen receptors with coregulators induced by ERα and ERβ agonists

Cited by 19 publications

References 44 publications

Development of a recombinant human ovarian (BG1) cell line containing estrogen receptor α and β for improved detection of estrogenic/antiestrogenic chemicals

Development of a recombinant human ovarian (BG1) cell line containing estrogen receptor α and β for improved detection of estrogenic/antiestrogenic chemicals

Estrogen accelerates the resolution of inflammation in macrophagic cells

The potential health effects of dietary phytoestrogens

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