Publicação:
Evaluation of Estrogenic Potential of Flavonoids Using a Recombinant Yeast Strain and MCF7/BUS Cell Proliferation Assay

dc.contributor.authorResende, Flávia A. [UNESP]
dc.contributor.authorde Oliveira, Ana Paula S. [UNESP]
dc.contributor.authorde Camargo, Mariana S. [UNESP]
dc.contributor.authorVilegas, Wagner [UNESP]
dc.contributor.authorVaranda, Eliana Aparecida [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.date.accessioned2014-05-27T11:30:49Z
dc.date.available2014-05-27T11:30:49Z
dc.date.issued2013-10-01
dc.description.abstractPhytoestrogens are of interest because of their reported beneficial effects on many human maladies including cancer, neurodegeneration, cardiovascular disease and diabetes. Furthermore, there is a search for compounds with estrogenic activity that can replace estrogen in hormone replacement therapy during menopause, without the undesirable effects of estrogen, such as the elevation of breast cancer occurrence. Thus, the principal objective of this study was to assess the estrogenic activity of flavonoids with different hydroxylation patterns: quercetin, kaempferol, luteolin, fisetin, chrysin, galangin, flavone, 3-hydroxyflavone, 5-hydroxyflavone and 7-hydroxyflavone via two different in vitro assays, the recombinant yeast assay (RYA) and the MCF-7 proliferation assay (E-screen), since the most potent phytoestrogens are members of the flavonoid family. In these assays, kaempferol was the only compound that showed ERα-dependent transcriptional activation activity by RYA, showing 6.74±1.7 nM EEQ, besides acting as a full agonist for the stimulation of proliferation of MCF-7/BUS cells. The other compounds did not show detectable levels of interaction with ER under the conditions used in the RYA. However, in the E-screen assay, compounds such as galangin, luteolin and fisetin also stimulated the proliferation of MCF-7/BUS cells, acting as partial agonists. In the evaluation of antiestrogenicity, the compounds quercetin, chrysin and 3-hydroxyflavone significantly inhibited the cell proliferation induced by 17-β-estradiol in the E-screen assay, indicating that these compounds may act as estrogen receptor antagonists. Overall, it became clear in the assay results that the estrogenic activity of flavonoids was affected by small structural differences such as the number of hydroxyl groups, especially those on the B ring of the flavonoid. © 2013 Resende et al.en
dc.description.affiliationDepartment of Biological Sciences Univ Estadual Paulista, Araraquara, São Paulo
dc.description.affiliationCampus do Litoral Paulista-Unidade São Vicente Univ Estadual Paulista, São Vicente, São Paulo
dc.description.affiliationUnespDepartment of Biological Sciences Univ Estadual Paulista, Araraquara, São Paulo
dc.description.affiliationUnespCampus do Litoral Paulista-Unidade São Vicente Univ Estadual Paulista, São Vicente, São Paulo
dc.identifierhttp://dx.doi.org/10.1371/journal.pone.0074881
dc.identifier.citationPLoS ONE, v. 8, n. 10, 2013.
dc.identifier.doi10.1371/journal.pone.0074881
dc.identifier.file2-s2.0-84885068685.pdf
dc.identifier.issn1932-6203
dc.identifier.lattes7927877224326837
dc.identifier.orcid0000-0003-3032-2556
dc.identifier.scopus2-s2.0-84885068685
dc.identifier.urihttp://hdl.handle.net/11449/76758
dc.identifier.wosWOS:000325427100012
dc.language.isoeng
dc.relation.ispartofPLOS ONE
dc.relation.ispartofjcr2.766
dc.relation.ispartofsjr1,164
dc.rights.accessRightsAcesso aberto
dc.sourceScopus
dc.titleEvaluation of Estrogenic Potential of Flavonoids Using a Recombinant Yeast Strain and MCF7/BUS Cell Proliferation Assayen
dc.typeArtigo
dcterms.licensehttp://www.plos.org/open-access/
dspace.entity.typePublication
unesp.author.lattes7927877224326837
unesp.author.orcid0000-0003-3032-2556[4]
unesp.campusUniversidade Estadual Paulista (UNESP), Instituto de Biociências, São Vicentept
unesp.campusUniversidade Estadual Paulista (UNESP), Faculdade de Ciências Farmacêuticas, Araraquarapt
unesp.departmentCiências Biológicas - FCFpt
unesp.departmentCiências Biológicas - IBCLPpt

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