Physiological Relevance of the Antiproliferative and Estrogenic Effects of Dietary Polyphenol Aglycones versus Their Phase-II Metabolites on Breast Cancer Cells: A Call of Caution

Journal of Agricultural and Food Chemistry
María Ángeles Ávila-GálvezAntonio González-Sarrías

Abstract

While preclinical studies suggest the breast cancer (BC) chemopreventive effects of dietary polyphenols, the human evidence is still very weak. The huge existing in vitro-in vivo gap is mainly due to the plethora of potential effects reported by in vitro studies that usually assay polyphenols as occurring in the food (beverages, extracts, foods) and/or derived aglycone metabolites with doubtful physiological relevance. Since phase-II metabolites can reach systemic tissues such as malignant breast tumors, we aimed here to compare for the first time the antiproliferative and estrogenic/antiestrogenic effects of dietary polyphenols and microbiota-derived metabolites (i.e., resveratrol, dihydroresveratrol, urolithins (A, B, and Isourolithin A), and the flavanone hesperetin), with those effects exerted by their physiologically relevant glucuronides and sulfates on human BC cell lines (MDA-MB-231 and MCF-7). Results showed that aglycones exerted dose-dependent antiproliferative and estrogenic/antiestrogenic activities, but both their glucuronide and sulfate conjugates lacked these activities. In addition, aglycones underwent phase-II metabolism in BC cells, mainly via sulfation, which determined the cell-dependent differences in the ...Continue Reading

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Citations

Jan 29, 2019·Molecular Nutrition & Food Research·María Ángeles Ávila-GálvezJuan Carlos Espín
Aug 24, 2019·Molecular Nutrition & Food Research·Juan Antonio Giménez-BastidaAntonio González-Sarrías
Oct 30, 2019·Food & Function·Gabriele Serreli, Monica Deiana
Apr 20, 2020·Molecular Nutrition & Food Research·Juan Antonio Giménez-BastidaClaus Schneider
Sep 23, 2020·European Journal of Nutrition·Aneta BobowskaJakub P Piwowarski
Nov 18, 2018·Toxins·Elena CatanzaroCarmela Fimognari
Aug 14, 2020·International Journal of Molecular Sciences·María Ángeles Ávila-GálvezAntonio González-Sarrías
Aug 11, 2020·Oxidative Medicine and Cellular Longevity·Jasmina DjedjibegovicLuciano Saso
May 4, 2021·Molecular Nutrition & Food Research·María Ángeles Ávila-GálvezJuan Carlos Espín
Jun 25, 2021·Frontiers in Nutrition·Sami A Al-HarbiMohammad Imran Khan
Mar 13, 2019·Journal of Agricultural and Food Chemistry·Joe A Vinson

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