Bioavailabilities of Quercetin-3-Glucoside and Quercetin-4′-Glucoside Do Not Differ in Humans

• Published in: The Journal of nutrition Vol. 130; no. 5; pp. 1200 - 1203
• Main Authors: Olthof, Margreet R., Hollman, Peter C.H., Vree, Tom B., Katan, Martijn B.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.05.2000; American Institute of Nutrition
• Subjects: Administration, Oral; Adult; Afdeling Humane voeding; ALIMENTOS; analogs & derivatives; ANTIOXIDANTES; ANTIOXIDANTS; ANTIOXYDANT; Area Under Curve; AVAILABILITY; bioavailability; blood plasma; chemistry; Chromatography, High Pressure Liquid; dietary supplements; duration; Female; FLAVONOIDE; FLAVONOIDES; FLAVONOIDS; flavonols; FOODS; GLICOSIDOS; GLUCOSIDE; GLUCOSIDES; GLUCOSIDOS; GLYCOSIDE; GLYCOSIDES; Half-Life; Human Nutrition; Human Nutrition & Health; Human Nutrition (HNE); Humane Voeding; Humane Voeding & Gezondheid; Humans; kinetics; Male; MAN; men; Metabolism; Middle Aged; molecular conformation; Nutrition; Parasympatholytics; Parasympatholytics - chemistry; Parasympatholytics - metabolism; Parasympatholytics - pharmacokinetics; pharmacokinetics; Plant Extracts; Plant Extracts - chemistry; Plant Extracts - metabolism; Plant Extracts - pharmacokinetics; PRODUIT ALIMENTAIRE; QUERCETIN; Quercetin - analogs & derivatives; Quercetin - chemistry; Quercetin - metabolism; Quercetin - pharmacokinetics; quercetin glucosides; QUERCETINA; QUERCETINE; RIKILT; Structure-Activity Relationship; Sugar; urine; VLAG; Wageningen Food Safety Research; women; metabolism; quercetin glucosides; bioavailability; humans; AUC0→72h; flavonols
• ISSN: 0022-3166; 1541-6100
• DOI: 10.1093/jn/130.5.1200

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 μmol of pure quercetin-3-glucoside and a single dose of 331 μmol 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 μmol/L (±se) after subjects had ingested quercetin-3-glucoside and 4.5 ± 0.7 μmol/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.