Quercetin, quercetin glycosides and taxifolin differ in their ability to induce AhR activation and CYP1A1 expression in HepG2 cells.

摘要: The natural flavonoid quercetin is a low affinity ligand of the aryl hydrocarbon receptor (AhR), transcription factor regulating expression cytochrome P450 (CYP) 1A enzymes. This study examined ability quercetin, isoquercitrin (quercetin-3-O-glucoside), rutin (quercetin-3-O-rutinoside) and taxifolin (dihydroquercetin) to activate AhR induce CYP1A1 in human hepatoma HepG2 cells. Gene reporter assays showed that significantly activated triggered after 24 h exposure. These effects were, however, much lower than those 2,3,7,8-tetrachlorodibenzo-p-dioxin, prototypical ligand. Quercetin also induced significant increase mRNA levels together with moderate level activity. In contrast, had negligible on activity expression. Taxifolin at highest concentration tested (50 µm) produced mild non-significant transcription. increased expression, but this effect was approximately 15 times weaker not accompanied by induction It concluded its 3-O-glycosides rutin, induces activation cells CYP1A1-inducing has toxicological potential. Copyright © 2012 John Wiley & Sons, Ltd.