Metabolic and Pharmacological Properties of Rutin, a Dietary Quercetin Glycoside, for Treatment of Inflammatory Bowel Disease

Abstract

Our data suggest that rutin acted as a quercetin deliverer to the large intestine and its anti-inflammatory action in TNBS-induced colitis rats may be through quercetin-mediated inhibition of TNF-alpha-induced NFkappaB activation.

Quercetin Activates an Angiogenic Pathway, Hypoxia Inducible Factor (HIF)-1-Vascular Endothelial Growth Factor, by Inhibiting HIF-Prolyl Hydroxylase: a Structural Analysis of Quercetin for Inhibiting HIF-Prolyl Hydroxylase

“…In our previous report, we suggested that quercetin-mediated amelioration of rat colitis was elicited by inhibiting NFB activity (Kim et al, 2005). Our data demonstrating quercetin activation of HIF-1-VEGF pathway in cells and inflamed colonic tissue suggest that quercetin exerts its clinical effect by not only inhibiting the inflammatory signal but also activating the tissue repair signal.…”

“…We reported previously that quercetin is effective in ameliorating TNBS-induced rat colitis, and the clinical effect is elicited by at least partly inhibiting a major pro-inflammatory NFB pathway (Kim et al, 2005). To explore an additional pharmacological mechanism of the quercetin effect on experimental colitis, we investigated whether quercetin, in addition to suppressing an inflammatory signal, could stimulate a tissue repair signal, which accelerates healing of inflammatory injury.…”

“…However, it is more likely that quercetin exerted a positive effect on angiogenesis in the colitis rat model. This is based on the following reasons: 1) unlike the previous report in which endothelial cells were exposed continually to quercetin for 1 to 3 days, quercetin in the large intestine remained at 200 to 30 M for approximately 6 h after oral administration of a glycoside of quercetin (Kim et al, 2005), which may be enough for quercetin to activate HIF-1-VHL pathway but not to inhibit growth of endothelial cells; 2) because concentration of quercetin diffused to the colonic endothelial cells should be lower than that of quercetin in the gut lumen; and 3) considering the second reason stated above, the tube formation assay, in which the diluted supernatant of quercetin-treated cells was used, may reflect the action of quercetin in the inflamed large intestine and, indeed, VEGF in the diluted supernatant promoted tube formation of HUVEC cells.…”

“…It has numerous biological activities, including anti-inflammatory effect (Nijveldt et al, 2001). In a previous report, we showed that quercetin is effective in ameliorating the experimental colitis of rats and suggested that a molecular mechanism underlying the clinical effect of quercetin is suppression of a major proinflammatory pathway, tumor necrosis factor-dependent NFB activation (Kim et al, 2005). In this study, we investigated an additional molecular mechanism for the clinical effect of quercetin.…”

The role of dietary polyphenols in the moderation of the inflammatory response in early stage colorectal cancer

“…Administration of polyphenols was effective at preventing and treating intestinal inflammation in rodents models of IBD where acute or chronic colitis was induced by intrarectal administration of dinitrobenzene sulphate (Oz et al, 2005, Kim et al, 2005 and addition of dextran sulphate sodium (DSS) to drinking water (Camuesco et al, 2004 (Wang et al, 2008, Elmali et al, 2007, Tang et al, 2007.…”