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Inhibitory Effect of Caffeic Acid on Human Organic Anion Transporters hOAT1 and hOAT3: A Novel Candidate for Food-drug Interaction.
MedLine Citation:
PMID:  21697612     Owner:  NLM     Status:  Publisher    
Several kinds of food have been shown to influence the absorption and metabolism of drugs, although there is little information about their effect on renal excretion of drugs. In this study, we performed uptake experiments using Xenopus laevis oocytes to assess the inhibitory effects of chlorogenic acid, caffeic acid and quinic acid, which are contained in coffee, fruits and vegetables, on human organic anion transporters hOAT1 and hOAT3, mediating renal tubular uptake of anionic drugs from blood. Injection of hOAT1 and hOAT3 cRNA stimulated uptake of their typical substrates, p-aminohippurate and estrone sulfate, respectively, into oocytes, and caffeic acid among the three compounds strongly reduced these transports. The apparent 50% inhibitory concentrations of caffeic acid were estimated to be 16.6 µM for hOAT1 and 5.4 µM for hOAT3. Eadie-Hofstee plot analysis showed that caffeic acid inhibited both transporters in a competitive manner. In addition to the transport of p-aminohippurate and estrone sulfate, that of antifolates and antivirals was inhibited by caffeic acid. These findings show that caffeic acid has inhibitory potential for hOAT1 and hOAT3, suggesting that renal excretion of their substrates would be affected in patients consuming a diet including caffeic acid.
Yuichi Uwai; Yukihiro Ozeki; Tomonori Isaka; Hiroaki Honjo; Kikuo Iwamoto
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-6-21
Journal Detail:
Title:  Drug metabolism and pharmacokinetics     Volume:  -     ISSN:  1880-0920     ISO Abbreviation:  -     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-6-23     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101164773     Medline TA:  Drug Metab Pharmacokinet     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Laboratory of Clinical Pharmacodynamics, School of Pharmacy, Aichi Gakuin University.
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