Nondigestible Saccharides Suppress the Bacterial Degradation of Quercetin Aglycone in the Large Intestine and Enhance the Bioavailability of Quercetin Glucoside in Rats

Abstract

Contribution of intestinal bacterial degradation of quercetin aglycone to the promotive effects of fructooligosaccharides and di-D-fructose anhydride III (DFAIII) on quercetin-3-O-beta-glucoside (Q3G) bioavailability was examined. Male Sprague-Dawley rats were fed 0.68% Q3G diets with or without 1.5% or 3% oligosaccharides for 2 weeks. Blood levels and urinary excretion of quercetin and methylquercetin conjugates, measured by methanol extraction and LC-MS analyses, were dose-dependently and adaptively increased by the oligosaccharide supplementation with increasing cecal fermentation (Experiment 1). Degradation of Q3G and quercetin aglycone by cecal bacteria in oligosaccharide-fed rats was much lower than that in the control rats using an anaerobic culture system (Experiment 2). Using the ligated intestinal sacs of anesthetized rats, we found that the cecum possessed high absorptive capacity for quercetin derivatives (Experiment 3). These results demonstrate that feeding of the oligosaccharides strongly suppresses the bacterial degradation of quercetin aglycone in the cecum, thus largely contributing to the increased bioavailability of Q3G.

Non-digestible stachyose promotes bioavailability of genistein through inhibiting intestinal degradation and first-pass metabolism of genistein in mice

“…It is widely acknowledged that the degradation of flavonoid in the gut is the important factor influencing its bioavailability [10]. Herein, we employed UPLC-qTOF/MS to determinate genistein aglycone and its gut microorganism-based characteristic metabolite (DH-GEN) in feces in order to indirectly evaluate the stability of genistein in the gut.…”

“…It was suggested that the possible potential mechanism was associated with the inhibition of non-digestible oligosaccharides against the bacterial degradation of quercetin aglycone in the intestine [10], but this effect has not yet been confirmed by analysis of the microbial characteristic metabolites of flavonoids. In the present study, the DH-GEN was found to be a characteristic metabolite of genistein degraded by intestinal microflora, and its feces excretion of the tested mice in the co-treatment groups was also decreased with the increased doses of simultaneous ingested stachyose (Figure 3).…”

“…Matsukawa et al have shown that the large intestine is one of the crucial target organs for non-digestible oligosaccharides to promote bioavailability of flavonoid glycosides [10]. Some other studies have also reported that the large intestine is a main position to absorb genistein [20].…”

“…Similarly, our previous studies also indicated that soy stachyose as raffinose family oligosaccharide could increase absorption of tea polyphenols or soy genistein and hepatic protective effects in mice [8,9]. Interestingly, some oligosaccharides were approved to strongly suppress the bacterial degradation of quercetin aglycone, thus contributing to the increased bioavailability of quercetin glycoside [10]. It is worth noting that stachyose is a kind of natural prebiotic and its consumption was able to favorably modulate the composition of the intestinal microbiota in humans and animals [11].…”

Quercetin increases claudin-4 expression through multiple transcription factors in intestinal Caco-2 cells

“…It is reported that plasma polyphenol concentrations are no more than~5 μM following oral consumption, but the luminal concentrations are known to reach a much higher level. Matsukawa et al have reported that the quercetin concentration reached 300 μM in the cecum of rats fed a diet containing 0.68% quercetin glucoside (Matsukawa et al, 2009). This evidence suggests that the transcriptional regulation of claudin-4 by quercetin, leading to the promotion of barrier integrity, could be translated to in vivo applications.…”