Activation of EpRE-mediated gene transcription by quercetin glucuronides depends on their deconjugation

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24 Citations (Scopus)

Abstract

Quercetin is a flavonoid reported to have health-promoting properties. Due to its extensive metabolism to glucuronides in vivo, questions were raised if studies conducted with quercetin aglycone, stating its health-promoting activity, are of actual relevance. Here we show that glucuronides of quercetin, and its methylated forms isorhamnetin and tamarixetin, can induce EpRE-mediated gene expression up to 5-fold. Furthermore, evidence is presented that EpRE-mediated gene induction by these glucuronides involves their deglucuronidation. This indicates that although quercetin-derived glucuronides are the major metabolites present in the systemic circulation, deglucuronidated derivatives are the active compounds responsible for their beneficial EpRE-mediated gene expression effects.
Original languageEnglish
Pages (from-to)2128-2134
JournalFood and Chemical Toxicology
Volume46
Issue number6
DOIs
Publication statusPublished - 2008

Keywords

  • dietary polyphenols
  • in-vitro
  • metabolic-fate
  • flavonoids
  • expression
  • absorption
  • glycosides
  • humans
  • cells
  • model

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