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<datestamp>2017-12-21</datestamp>
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<title lang=en>Assessment of the potential activity of major dietary compounds as selective estrogen receptor modulators in two distinct cell models for proliferation and differentiation</title>
<creator>Lecomte, Sylvain</creator>
<creator>Lelong, Marie</creator>
<creator>Bourgine, Gaëlle</creator>
<creator>Efstathiou, Théo</creator>
<creator>Saligaut, Christian</creator>
<creator>Pakdel, Farzad</creator>
<contributor>Institut de recherche, santé, environnement et travail [Rennes] (Irset) ; Université d'Angers (UA) - Université des Antilles et de la Guyane (UAG) - Université de Rennes 1 (UR1) - École des Hautes Études en Santé Publique [EHESP] (EHESP) - Institut National de la Santé et de la Recherche Médicale (INSERM) - Structure Fédérative de Recherche en Biologie et Santé de Rennes ( Biosit : Biologie - Santé - Innovation Technologique )</contributor>
<contributor>Analyses et Recherche ; Nutrinov</contributor>
<contributor>This work was funded by Fonds Unique Interministériel (FUI, mVolio project), Région Bretagne and Rennes Métropole. This research was also supported by Inserm and CNRS.</contributor>
<description>International audience</description>
<source>ISSN: 0041-008X</source>
<source>EISSN: 1096-0333</source>
<source>Toxicology and Applied Pharmacology</source>
<publisher>Elsevier</publisher>
<identifier>hal-01558816</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01558816</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01558816/document</identifier>
<identifier>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01558816/file/Lecomte%20et%20al.%20-%20Assessment%20of%20the%20potential%20activity%20of%20major%20diet.pdf</identifier>
<source>https://hal-univ-rennes1.archives-ouvertes.fr/hal-01558816</source>
<source>Toxicology and Applied Pharmacology, Elsevier, 2017, 325, pp.61-70. 〈10.1016/j.taap.2017.04.005〉</source>
<identifier>DOI : 10.1016/j.taap.2017.04.005</identifier>
<relation>info:eu-repo/semantics/altIdentifier/doi/10.1016/j.taap.2017.04.005</relation>
<identifier>PUBMED : 28396216</identifier>
<relation>info:eu-repo/semantics/altIdentifier/pmid/28396216</relation>
<language>en</language>
<subject lang=en> Cell Proliferation</subject>
<subject lang=en> Zearalenone</subject>
<subject lang=en> Transfection</subject>
<subject lang=en> Genetic</subject>
<subject lang=en> Transcription</subject>
<subject lang=en> Stilbenes</subject>
<subject lang=en> Nerve Tissue Proteins</subject>
<subject lang=en> MCF-7 Cells</subject>
<subject lang=en> Isoflavones</subject>
<subject lang=en> Humans</subject>
<subject lang=en> Neoplastic</subject>
<subject lang=en> Gene Expression Regulation</subject>
<subject lang=en> Female</subject>
<subject lang=en> Estrogen Receptor alpha</subject>
<subject lang=en> Drug</subject>
<subject lang=en> Dose-Response Relationship</subject>
<subject lang=en> Differentiation</subject>
<subject lang=en> Diet</subject>
<subject lang=en> Chemokine CXCL12</subject>
<subject lang=en> SERM</subject>
<subject lang=en> Selective Estrogen Receptor Modulators</subject>
<subject lang=en> Response Elements</subject>
<subject lang=en> Rats</subject>
<subject lang=en> PROLIFERATION</subject>
<subject lang=en> Phytoestrogens</subject>
<subject lang=en> Pheochromocytoma</subject>
<subject lang=en> PC12 Cells</subject>
<subject lang=en> Neurites</subject>
<subject lang=en> Neurogenesis</subject>
<subject lang=en> PC12</subject>
<subject lang=en>Adrenal Gland Neoplasms</subject>
<subject lang=en> Animals</subject>
<subject lang=en> Antineoplastic Agents</subject>
<subject lang=en> Phytogenic</subject>
<subject lang=en> Apigenin</subject>
<subject lang=en> Breast cancer cell lines</subject>
<subject lang=en> Breast Neoplasms</subject>
<subject>[SDV.TOX] Life Sciences [q-bio]/Toxicology</subject>
<subject>[SDV.SP.PHARMA] Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology</subject>
<type>info:eu-repo/semantics/article</type>
<type>Journal articles</type>
<description lang=en>Estrogen receptors (ERs) α and β are distributed in most tissues of women and men. ERs are bound by estradiol (E2), a natural hormone, and mediate the pleiotropic and tissue-specific effects of E2, such as proliferation of breast epithelial cells or protection and differentiation of neuronal cells. Numerous environmental molecules, called endocrine disrupting compounds, also interact with ERs. Phytoestrogens belong to this large family and are considered potent therapeutic molecules that act through their selective estrogen receptor modulator (SERM) activity. Using breast cancer cell lines as a model of estrogen-dependent proliferation and a stably ER-expressing PC12 cell line as a model of neuronal differentiating cells, we studied the SERM activity of major dietary compounds, such as apigenin, liquiritigenin, daidzein, genistein, coumestrol, resveratrol and zearalenone. The ability of these compounds to induce ER-transactivation and breast cancer cell proliferation and enhance Nerve Growth Factor (NGF) -induced neuritogenesis was assessed. Surprisingly, although all compounds were able to activate the ER through an estrogen responsive element reporter gene, they showed differential activity toward proliferation or differentiation. Apigenin and resveratrol showed a partial or no proliferative effect on breast cancer cells but fully contributed to the neuritogenesis effect of NGF. However, daidzein and zearalenone showed full effects on cellular proliferation but did not induce cellular differentiation. In summary, our results suggest that the therapeutic potential of phytoestrogens can diverge depending on the molecule and the phenotype considered. Hence, apigenin and resveratrol might be used in the development of therapeutics for breast cancer and brain diseases.</description>
<date>2017</date>
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