Dietary polyphenols (-)-epicatechin and chrysin inhibit intestinal glucuronidation metabolism to increase drug absorption

Journal of Pharmaceutical Sciences

Volumn 93, Issue 9, 2004, Pages 2407-2410

  Mizuma, Takashi ^a   Awazu, Shoji ^a  

^a TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES   (Japan)

Author keywords

Absorption clearance; Bioavailability; Clearance; First pass metabolism; Food effects; Food interactions; Glucuronidation; Glucuronosyltransferases (UGT); Intestinal absorption; Kinetics; Metabolic clearance; Polyphenol

Indexed keywords

1 NAPHTHOL; BAICALIN; CHRYSIN; DRUG; EPICATECHIN; EPIGALLOCATECHIN GALLATE; GLUCURONOSYLTRANSFERASE; POLYPHENOL; QUERCETIN;

ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; DIET; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG METABOLISM; FIRST PASS EFFECT; FOOD DRUG INTERACTION; GLUCURONIDATION; INTESTINE ABSORPTION; MALE; METABOLIC CLEARANCE RATE; METABOLIC INHIBITION; NONHUMAN; RAT; SMALL INTESTINE;

EID: 4344717895     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1002/jps.20146     Document Type: Article

References (11)

1. Mizuma T, Awazu S. 1998. Inhibitory effect of phloridzin and phloretin on glucuronidation of p-nitrophenol, acetaminophen and 1-naphthol: Kinetic demonstration of the influence of glucuronidation metabolism on intestinal absorption in rats. Biochim Biophys Acta 1425:398-404.
2. Mizuma T, Ohta K, Koyanagi A, Awazu S. 1996. Improvement of intestinal absorption of leucine enkephalin by sugar coupling and peptidase inhibitors. J Pharm Sci 85:854-857.
3. Hollman PCH, Arts ICW. 2000. Flavonols, flavones and flavanols-Nature, occurrence and dietary burden. J Sci Food Agric 80:1081-1093.
4. Siess MH, Le Bon AM, Canivenc-Lavier MC, Amiot MJ, Sabatier S, Aubert SY, Suschetet M. 1996. Flavonoids of honey and propolis: Characterization and effects on hepatic drug-metabolizing enzymes and benzo[a]pyrene-DNA binding in rats. J Agric Food Chem 44:2297-2301.
5. Mizuma T, Koyanagi A, Awazu S. 2000. Intestinal transport and metabolism of glucose-conjugated kyotorphin and cyclic kyotorphin: Metabolic degradation is crucial to intestinal absorption of peptide drugs. Biochim Biophys Acta 1475:90-98.
6. Piskula M, Terao J. 1998. Accumulation of (-)-epicatechim metabolites in rat plasma after oral administration and disposition of conjugation enzymes in rat tissues. J Nutr 128:1172-1178.
7. Crespy V, Morand C, Manach C, Besson C, Demigne C, Remesy C. 1999. Part of quercetin absorbed in the small intestine is conjugated and further secreted in the intestinal lumen. Am J Physiol 277:G120-G126.
8. Spencer JPE, Chowrimootoo G, Choudhury R, Debnam ES, Srai SK, Rice-Evans C. 1999. The small intestine can both absorb and glucuronidate luminal flavonoids. FEBS Lett 458:224-230.
9. Walle UK, Galijatovic A, Walle T. 1999. Transport of the flavonoid chrysin and its conjugated metabolites by the human intestinal cell line Caco-2. Biochem Pharmacol 58:431-438.
10. Walle UK, Walle T. 2002. Induction of human UDP-glucuronosyltransferase UGT1A1 by flavonoids-structural requirements. Drug Metab Dispos 30:564-569.
11. Gray PA, Park GR, Cockshott ID, Douglas EJ, Shunker B. 1992. Propofol metabolism in man during the anhepatic and reperfusion phases of liver transplantation. Xenobiotica 22:105-114.