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

• DOI: 10.1021/acs.jafc.8b03100
• Publication Date: 2018-07-20T02:47:35Z
• Authors: María Ángeles Ávi...; Juan Carlos Espín; Antonio González-...
• Keywords: Aglycone; Glucuronide; Flavanone; Hesperetin

While preclinical studies suggest the breast cancer (BC) chemopreventive effects of dietary polyphenols, human evidence is still very weak. The huge existing in vitro–in vivo gap mainly due to plethora potential reported by vitro that usually assay polyphenols as occurring food (beverages, extracts, foods) and/or derived aglycone metabolites with doubtful physiological relevance. Since phase-II can reach systemic tissues such malignant tumors, we aimed here compare for first time antiproliferative and estrogenic/antiestrogenic microbiota-derived (i.e., resveratrol, dihydroresveratrol, urolithins (A, B, Isourolithin A), flavanone hesperetin), those exerted their physiologically relevant glucuronides sulfates on BC cell lines (MDA-MB-231 MCF-7). Results showed aglycones dose-dependent activities, but both glucuronide sulfate conjugates lacked these activities. In addition, underwent metabolism cells, via sulfation, which determined cell-dependent differences observed. Therefore, limits antiproliferative, estrogenic, antiestrogenic activities cells. Likewise, a call caution, enthusiasm should be limited publishing are not relevant.