Molecular effects of ER alpha- and beta-selective agonists on regulation of energy homeostasis in obese female Wistar rats

Weigt, Carmen; Hertrampf, Torsten; Kluxen, Felix M.; Flenker, Ulrich; Hülsemann, Frank; Fritzemeier, Karl Heinrich; Diel, Patrick

doi:10.1016/j.mce.2013.07.007

Cited by 62 publications

(76 citation statements)

References 73 publications

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“…The ER-β selective agonist and G1, a GPER1 selective agonist, were not as well suited as the E2 and ER-α selective agonist to mediate estrogenic effect in mice uterus1520. Neither tamoxifen nor E2 induced EEC proliferation in ER-αKO mice11.…”

Section: Discussionmentioning

confidence: 95%

“…We then assessed whether anordrin played a role in the classic nuclear pathway of estrogen modulation. Because the ER-β selective agonist was not as well suited as E2 and as an ER-α selective agonist to mediate uterine endometrial proliferation15, we only tested the binding affinity of anordiol to ER-α. ER-α-46 is an effective ligand-regulated transcription isoform of ER-α1617.…”

Section: Resultsmentioning

confidence: 99%

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Anordrin Eliminates Tamoxifen Side Effects without Changing Its Antitumor Activity

Sun

et al. 2017

Sci Rep

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Tamoxifen is administered for estrogen receptor positive (ER+) breast cancers, but it can induce uterine endometrial cancer and non-alcoholic fatty liver disease (NAFLD). Importantly, ten years of tamoxifen treatment has greater protective effect against ER+ breast cancer than five years of such treatment. Tamoxifen was also approved by the FDA as a chemopreventive agent for those deemed at high risk for the development of breast cancer. The side effects are of substantial concern because of these extended methods of tamoxifen administration. In this study, we found that anordrin, marketed as an antifertility medicine in China, inhibited tamoxifen-induced endometrial epithelial cell mitosis and NAFLD in mouse uterus and liver as an anti-estrogenic and estrogenic agent, respectively. Additionally, compared with tamoxifen, anordiol, the active metabolite of anordrin, weakly bound to the ligand binding domain of ER-α. Anordrin did not regulate the classic estrogen nuclear pathway; thus, it did not affect the anti-tumor activity of tamoxifen in nude mice. Taken together, these data suggested that anordrin could eliminate the side effects of tamoxifen without affecting its anti-tumor activity.

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Section: Discussionmentioning

confidence: 95%

Section: Resultsmentioning

confidence: 99%

Anordrin Eliminates Tamoxifen Side Effects without Changing Its Antitumor Activity

Sun

et al. 2017

Sci Rep

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“…In fact, triglyceride accumulation was reduced in liver and muscle, and hepatic glucose uptake was increased, without any significant effect in adipose tissue, probably due to the low concentration of genistein in this tissue. Thus, lipid and glucose metabolism is generally affected positively when ER is activated by genistein [135]. Many clinical studies involving genistein are presently ongoing or completed, some involving, for example, the treatment of neurodegenerative diseases, breast, prostate, bladder and colorectal cancer, metabolic syndrome, etc., to further explore the multifaceted pharmacological profile of this phytoestrogen [73].…”

Section: Update On Chemical Classes Comprising Erα and Erβ Modulatorsmentioning

confidence: 99%

Estrogen receptors alpha (ERα) and beta (ERβ): Subtype-selective ligands and clinical potential

et al. 2014

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Estrogen receptors alpha (ERα) and beta (ERβ) are nuclear transcription factors that are involved in the regulation of many complex physiological processes in humans. Modulation of these receptors by prospective therapeutic agents is currently being considered for prevention and treatment of a wide variety of pathological conditions, such as, cancer, metabolic and cardiovascular diseases, neurodegeneration, inflammation, and osteoporosis. This review provides an overview and update of compounds that have been recently reported as modulators of ERs, with a particular focus on their potential clinical applications.

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“…Paradoxically, 100 nM to 10 µM concentrations of DDT and BPA have the capacity to enhance adipogenesis by estrogen receptor (ER)-mediated signaling, which has classically been shown to inhibit adipogenesis (68, 69, 90–93). Biasiotto and colleagues addressed the issue of multiple endocrine disruptors simultaneously acting on MSCs in the environment (Figure 3).…”

Section: Adipogenesismentioning

confidence: 99%

The Effects of Endocrine Disruptors on Adipogenesis and Osteogenesis in Mesenchymal Stem Cells: A Review

et al. 2017

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Endocrine-disrupting chemicals (EDCs) are prevalent in the environment, and epidemiologic studies have suggested that human exposure is linked to chronic diseases, such as obesity and diabetes. In vitro experiments have further demonstrated that EDCs promote changes in mesenchymal stem cells (MSCs), leading to increases in adipogenic differentiation, decreases in osteogenic differentiation, activation of pro-inflammatory cytokines, increases in oxidative stress, and epigenetic changes. Studies have also shown alteration in trophic factor production, differentiation ability, and immunomodulatory capacity of MSCs, which have significant implications to the current studies exploring MSCs for tissue engineering and regenerative medicine applications and the treatment of inflammatory conditions. Thus, the consideration of the effects of EDCs on MSCs is vital when determining potential therapeutic uses of MSCs, as increased exposure to EDCs may cause MSCs to be less effective therapeutically. This review focuses on the adipogenic and osteogenic differentiation effects of EDCs as these are most relevant to the therapeutic uses of MSCs in tissue engineering, regenerative medicine, and inflammatory conditions. This review will highlight the effects of EDCs, including organophosphates, plasticizers, industrial surfactants, coolants, and lubricants, on MSC biology.

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Molecular effects of ER alpha- and beta-selective agonists on regulation of energy homeostasis in obese female Wistar rats

Cited by 62 publications

References 73 publications

Anordrin Eliminates Tamoxifen Side Effects without Changing Its Antitumor Activity

Anordrin Eliminates Tamoxifen Side Effects without Changing Its Antitumor Activity

Estrogen receptors alpha (ERα) and beta (ERβ): Subtype-selective ligands and clinical potential

The Effects of Endocrine Disruptors on Adipogenesis and Osteogenesis in Mesenchymal Stem Cells: A Review

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