Abstract
Quercetin-4′-glucoside is a major flavonol in onions, and this study investigated the absorption and fate of radiolabeled quercetin-4′-glucoside in rats. Rats ingested [2-14C]quercetin-4′-glucoside and the distribution of radioactivity throughout the body was determined after 0.5, 1, 2, and 5 h. The gastrointestinal tract, liver, kidney, and plasma were extracted, and radiolabeled components were identified and quantified using high-performance liquid chromatography with on-line radioactivity detection and tandem mass spectrometry. Two hours after dosing, all the [2-14C]quercetin-4′-glucoside had been metabolized. More than 85% of the ingested radioactivity was present in the gastrointestinal tract at all time points with ∼6% being absorbed and present in blood and internal organs, primarily the liver and kidneys. More than 95% of the absorbed radioactivity was in the form of >20 different methylated glucuronated and/or sulfated quercetin conjugates. Five hours after ingestion, the main radiolabeled metabolites were quercetin diglucuronides in the gut, liver, and kidneys and glucuronyl sulfates of methylated quercetin in plasma. The main site of quercetin metabolism seemed to be the gastrointestinal tract. Quercetin metabolites may have a major influence on the gut mucosal epithelium and on colonic disease.
Footnotes
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This study was supported by a University of Glasgow Fleck Postgraduate Fellowship (to S.T.C.) and the New Zealand Crop Research Institute, Christchurch. G.G.D. received financial support from the Scottish Executive Environmental and Rural Affairs Department. The HPLC-MS-MS used in the study was purchased with a Biotechnology and Biological Sciences Research Council grant (to A.C. and J. R. Coggins).
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Article, publication date, and citation information can be found at http://dmd.aspetjournals.org.
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doi:10.1124/dmd.104.002691.
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ABBREVIATIONS: GI, gastrointestinal tract; HPLC, high-performance liquid chromatography; RC, radiocounting; MS-MS, tandem mass spectrometry.
- Received November 2, 2004.
- Accepted April 12, 2005.
- The American Society for Pharmacology and Experimental Therapeutics
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