Evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.

Phytoestrogens 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...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Flávia A Resende, Ana Paula S de Oliveira, Mariana S de Camargo, Wagner Vilegas, Eliana A Varanda
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2013
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/7807ad48aef44a6e88f4f313bad7d81b
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:7807ad48aef44a6e88f4f313bad7d81b
record_format	dspace
spelling	oai:doaj.org-article:7807ad48aef44a6e88f4f313bad7d81b2021-11-18T08:52:56ZEvaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.1932-620310.1371/journal.pone.0074881https://doaj.org/article/7807ad48aef44a6e88f4f313bad7d81b2013-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/24098354/?tool=EBIhttps://doaj.org/toc/1932-6203Phytoestrogens 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.Flávia A ResendeAna Paula S de OliveiraMariana S de CamargoWagner VilegasEliana A VarandaPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 8, Iss 10, p e74881 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Flávia A Resende Ana Paula S de Oliveira Mariana S de Camargo Wagner Vilegas Eliana A Varanda Evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.
description	Phytoestrogens 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.
format	article
author	Flávia A Resende Ana Paula S de Oliveira Mariana S de Camargo Wagner Vilegas Eliana A Varanda
author_facet	Flávia A Resende Ana Paula S de Oliveira Mariana S de Camargo Wagner Vilegas Eliana A Varanda
author_sort	Flávia A Resende
title	Evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.
title_short	Evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.
title_full	Evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.
title_fullStr	Evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.
title_full_unstemmed	Evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.
title_sort	evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and mcf7/bus cell proliferation assay.
publisher	Public Library of Science (PLoS)
publishDate	2013
url	https://doaj.org/article/7807ad48aef44a6e88f4f313bad7d81b
work_keys_str_mv	AT flaviaaresende evaluationofestrogenicpotentialofflavonoidsusingarecombinantyeaststrainandmcf7buscellproliferationassay AT anapaulasdeoliveira evaluationofestrogenicpotentialofflavonoidsusingarecombinantyeaststrainandmcf7buscellproliferationassay AT marianasdecamargo evaluationofestrogenicpotentialofflavonoidsusingarecombinantyeaststrainandmcf7buscellproliferationassay AT wagnervilegas evaluationofestrogenicpotentialofflavonoidsusingarecombinantyeaststrainandmcf7buscellproliferationassay AT elianaavaranda evaluationofestrogenicpotentialofflavonoidsusingarecombinantyeaststrainandmcf7buscellproliferationassay
_version_	1718421210155450368

Evaluation of estrogenic potential of flavonoids using a recombinant yeast strain and MCF7/BUS cell proliferation assay.

Ejemplares similares