Bioavailabilities of quercetin-3-glucoside and quercetin-4'-glucoside do not differ in humans

J Nutr. 2000 May;130(5):1200-3. doi: 10.1093/jn/130.5.1200.

Abstract

The flavonoid quercetin is an antioxidant which occurs in foods mainly as glycosides. The sugar moiety in quercetin glycosides affects their bioavailability in humans. Quercetin-3-rutinoside is an important form of quercetin in foods, but its bioavailability in humans is only 20% of that of quercetin-4'-glucoside. Quercetin-3-rutinoside can be transformed into quercetin-3-glucoside by splitting off a rhamnose molecule. We studied whether this 3-glucoside has the same high bioavailability as the quercetin-4'-glucoside. To that end we fed five healthy men and four healthy women (19-57 y) a single dose of 325 micromol of pure quercetin-3-glucoside and a single dose of 331 micromol of pure quercetin-4'-glucoside and followed the plasma quercetin concentrations. The bioavailability was the same for both quercetin glucosides. The mean peak plasma concentration of quercetin was 5.0+/-1.0 micromol/L (+/-SE) after subjects had ingested quercetin-3-glucoside and 4.5+/-0.7 micromol/L after quercetin-4'-glucoside consumption. Peak concentration was reached 37 +/-12 min after ingestion of quercetin-3-glucoside and 27+/-5 min after quercetin-4'-glucoside. Half-life of elimination of quercetin from blood was 18.5+/-0.8 h after ingestion of quercetin-3-glucoside and 17.7+/-0.9 h after quercetin-4'-glucoside. We conclude that quercetin glucosides are rapidly absorbed in humans, irrespective of the position of the glucose moiety. Conversion of quercetin glycosides into glucosides is a promising strategy to enhance bioavailability of quercetin from foods.

Publication types

  • Clinical Trial
  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adult
  • Area Under Curve
  • Chromatography, High Pressure Liquid
  • Female
  • Half-Life
  • Humans
  • Male
  • Middle Aged
  • Parasympatholytics / chemistry
  • Parasympatholytics / metabolism
  • Parasympatholytics / pharmacokinetics*
  • Plant Extracts / chemistry
  • Plant Extracts / metabolism
  • Plant Extracts / pharmacokinetics
  • Quercetin / analogs & derivatives*
  • Quercetin / chemistry
  • Quercetin / metabolism
  • Quercetin / pharmacokinetics
  • Structure-Activity Relationship

Substances

  • Parasympatholytics
  • Plant Extracts
  • isoquercitrin
  • Quercetin
  • spiraeoside