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Intestinal disposition of quercetin and its phase‐II metabolites after oral administration in healthy volunteers
Ist Teil von
Journal of pharmacy and pharmacology, 2018-08, Vol.70 (8), p.1002-1008
Ort / Verlag
England: Wiley Subscription Services, Inc
Erscheinungsjahr
2018
Quelle
Wiley Online Library - AutoHoldings Journals
Beschreibungen/Notizen
Objectives
Quercetin is one of the main dietary flavonoids and undergoes a substantial intestinal phase‐II metabolism. Quercetin conjugates have been detected in plasma and in urine, but their presence in the small intestine has not been assessed. This study aimed to investigate the intestinal metabolism and metabolite excretion of quercetin by the human small intestinal wall after oral dosing.
Methods
Six healthy volunteers were given a capsule of 500 mg of quercetin with 240 ml of water. Duodenal fluids were collected using the intraluminal sampling technique for 4 h and analysed by LC‐MS/MS.
Key findings
Phase‐II metabolites of quercetin were detected and quantified in aspirated intestinal fluids. Metabolites appeared almost immediately after administration, indicating an intestinal metabolism and apical excretion into the lumen. Quercetin‐3′‐O‐glucuronide was found to be the main intestinal metabolite. Our results could not conclude on the enterohepatic recycling of quercetin or its metabolites, although several individual profiles showed distinctive peaks.
Conclusions
This study highlights the intestinal metabolism and excretion of quercetin and its conjugates in humans and gives insights into the relevant concentrations which should be used to investigate potential food–drug interactions in vitro.