Intestinal uptake of quercetin-3-glucoside in rats involves hydrolysis by lactase phlorizin hydrolase

J Nutr. 2003 Mar;133(3):773-6. doi: 10.1093/jn/133.3.773.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Deoxynojirimycin / analogs & derivatives*
  • 1-Deoxynojirimycin / pharmacology
  • Animals
  • Chromatography, High Pressure Liquid
  • Enzyme Inhibitors / pharmacology
  • Flavonols*
  • Hydrolysis
  • Ileum / enzymology
  • Intestines / enzymology*
  • Intestines / ultrastructure
  • Jejunum / enzymology
  • Lactase-Phlorizin Hydrolase / antagonists & inhibitors
  • Lactase-Phlorizin Hydrolase / metabolism*
  • Male
  • Microvilli / enzymology
  • Quercetin / analogs & derivatives*
  • Quercetin / blood
  • Quercetin / metabolism*
  • Rats
  • Rats, Wistar

Substances

  • Enzyme Inhibitors
  • Flavonols
  • 3-methylquercetin
  • isoquercitrin
  • 1-Deoxynojirimycin
  • Quercetin
  • migalastat
  • Lactase-Phlorizin Hydrolase