title: Intestinal uptake of quercetin-3-glucoside in rats involves hydrolysis by lactase phlorizin hydrolase.
abstract: Quercetin has antioxidant, anti-inflammatory, antiproliferative and anticarcinogenic properties. In plant foods, quercetin occurs mainly bound to various sugars via a beta-glycosidic link. We hypothesized that lactase phlorizin hydrolase (LPH), an enzyme at the brush border membrane of intestinal cells, is involved in the in vivo intestinal uptake of quercetin-sugars. To study this, we measured the appearance of quercetin metabolites in plasma and perfusate after perfusing the jejunum and ileum with 50 micro mol/L quercetin-3-glucoside in an in situ rat perfusion model. LPH was inhibited by the selective LPH inhibitor N-butyldeoxygalactonojirimycin (0, 0.5, 2 or 10 mmol/L) (n = 5 rats/group). Quercetin in plasma and perfusion buffer was determined by HPLC with CoulArray detection. Results are given as means +/- SEM. In the perfusion buffer, 13.8 +/- 0.7 micro mol/L quercetin-3-glucoside was hydrolyzed during intestinal passage. Co-perfusion with 0.5, 2 and 10 mmol/L N-butyldeoxygalactonojirimycin resulted in 38% (P < 0.05), 50% (P < 0.01) and 67% (P < 0.01) less hydrolysis, respectively. Plasma concentrations of quercetin in the corresponding groups were 36% (P = 0.12), 55% (P < 0.01) and 75% (P < 0.01) lower than in controls (1.23 +/- 0.22 micro mol/L). These data suggest that LPH is a major determinant of intestinal absorption of quercetin-3-glucoside in rats.
authors.affiliation: Department of Pharmacology and Toxicology, Nijmegen Center for Molecular Life Sciences, The Netherlands. a.sesink@ncmls.kun.nl
authors.forename: Aloys L A
authors.initials: AL
authors.lastname: Sesink
authors.forename: Ilja C W
authors.initials: IC
authors.lastname: Arts
authors.forename: Maria
authors.initials: M
authors.lastname: Faassen-Peters
authors.forename: Peter C H
authors.initials: PC
authors.lastname: Hollman
mesh_terms: D017485:1-Deoxynojirimycin / Q000031:analogs & derivatives* / Q000494:pharmacology; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004791:Enzyme Inhibitors / Q000494:pharmacology; D044948:Flavonols; D006868:Hydrolysis; D007082:Ileum / Q000201:enzymology; D007422:Intestines / Q000201:enzymology* / Q000648:ultrastructure; D007583:Jejunum / Q000201:enzymology; D010694:Lactase-Phlorizin Hydrolase / Q000037:antagonists & inhibitors / Q000378:metabolism*; D008297:Male; D008871:Microvilli / Q000201:enzymology; D011794:Quercetin / Q000031:analogs & derivatives* / Q000097:blood / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar
chemical_list: D004791:Enzyme Inhibitors; D044948:Flavonols; C047368:3-methylquercetin; C016527:isoquercitrin; D017485:1-Deoxynojirimycin; D011794:Quercetin; C090092:migalastat; D010694:Lactase-Phlorizin Hydrolase