Disposition and metabolism of [2-C-14]quercetin-4 '-glucoside in rats

B A Graf, W Mullen, S T Caldwell, R C Hartley, G G Duthie, M E J Lean, A Crozier, C A Edwards

Research output: Contribution to journalArticle

58 Citations (Scopus)

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-C-14] 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-C-14] quercetin-4'-glucoside had been metabolized. More than 85% of the ingested radioactivity was present in the gastrointestinal tract at all time points with similar to 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.

Original languageEnglish
Pages (from-to)1036-1043
Number of pages8
JournalDrug Metabolism and Disposition
Volume33
Issue number7
DOIs
Publication statusPublished - Jul 2005

Keywords

  • small intestine
  • in vitro
  • quercetin glycosides
  • flavonoid quercetin
  • heart disease
  • bioavailability
  • absorption
  • rutin
  • derivatives
  • volunteers

Cite this

Graf, B. A., Mullen, W., Caldwell, S. T., Hartley, R. C., Duthie, G. G., Lean, M. E. J., ... Edwards, C. A. (2005). Disposition and metabolism of [2-C-14]quercetin-4 '-glucoside in rats. Drug Metabolism and Disposition, 33(7), 1036-1043. https://doi.org/10.1124/dmd.104.002691

Disposition and metabolism of [2-C-14]quercetin-4 '-glucoside in rats. / Graf, B A ; Mullen, W ; Caldwell, S T ; Hartley, R C ; Duthie, G G; Lean, M E J ; Crozier, A ; Edwards, C A .

In: Drug Metabolism and Disposition, Vol. 33, No. 7, 07.2005, p. 1036-1043.

Research output: Contribution to journalArticle

Graf, BA, Mullen, W, Caldwell, ST, Hartley, RC, Duthie, GG, Lean, MEJ, Crozier, A & Edwards, CA 2005, 'Disposition and metabolism of [2-C-14]quercetin-4 '-glucoside in rats', Drug Metabolism and Disposition, vol. 33, no. 7, pp. 1036-1043. https://doi.org/10.1124/dmd.104.002691
Graf, B A ; Mullen, W ; Caldwell, S T ; Hartley, R C ; Duthie, G G ; Lean, M E J ; Crozier, A ; Edwards, C A . / Disposition and metabolism of [2-C-14]quercetin-4 '-glucoside in rats. In: Drug Metabolism and Disposition. 2005 ; Vol. 33, No. 7. pp. 1036-1043.
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AB - 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-C-14] 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-C-14] quercetin-4'-glucoside had been metabolized. More than 85% of the ingested radioactivity was present in the gastrointestinal tract at all time points with similar to 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.

KW - small intestine

KW - in vitro

KW - quercetin glycosides

KW - flavonoid quercetin

KW - heart disease

KW - bioavailability

KW - absorption

KW - rutin

KW - derivatives

KW - volunteers

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