Pro-oxidant activity of flavonoids induces EpRE-mediated gene expression

Chem Res Toxicol. 2006 Nov;19(11):1499-505. doi: 10.1021/tx060157q.

Abstract

Flavonoids are important bioactive dietary compounds. They induce electrophile-responsive element (EpRE)-mediated expression of enzymes, such as NAD(P)H-quinone oxidoreductase (NQO1) and glutathione S-transferases (GSTs), which are major defense enzymes against electrophilic toxicants and oxidative stress. The induction of EpRE-mediated gene transcription involves the release of the transcription factor Nrf2 from a complex with Keap1, either by a direct interaction of the inducer with Keap1 or by protein kinase C (PKC)-mediated phosphorylation of Nrf2. The inhibition of PKC in Hepa1c1c7 cells, stably transfected with human NQO1-EpRE-controlled luciferase revealed that PKC is not involved in flavonoid-induced EpRE-mediated gene transcription. However, the ability of flavonoids to activate an EpRE-mediated response correlates with their redox properties characterized by quantum mechanical calculations. Flavonoids with a higher intrinsic potential to generate oxidative stress and redox cycling are the most potent inducers of EpRE-mediated gene expression. Modulation of the intracellular glutathione (GSH) level showed that the EpRE-activation by flavonoids increased with decreasing GSH and vice versa, supporting an oxidative mechanism. In conclusion, the pro-oxidant activity of flavonoids can contribute to their health-promoting activity by inducing important detoxifying enzymes, pointing to a beneficial effect of a supposed toxic chemical reaction.

MeSH terms

  • Animals
  • Cell Line
  • Flavonoids / pharmacology*
  • Gene Expression Regulation / drug effects*
  • Humans
  • Liver Neoplasms, Experimental / drug therapy
  • Liver Neoplasms, Experimental / enzymology
  • Liver Neoplasms, Experimental / genetics
  • Mice
  • Molecular Structure
  • Oxidation-Reduction
  • Protein Kinase C / metabolism
  • Response Elements / drug effects*
  • Response Elements / genetics

Substances

  • Flavonoids
  • Protein Kinase C