Document Detail

Gallic acid and gallic acid derivatives: effects on drug metabolizing enzymes.
MedLine Citation:
PMID:  12769668     Owner:  NLM     Status:  MEDLINE    
Gallic acid and its structurally related compounds are found widely distributed in fruits and plants. Gallic acid, and its catechin derivatives are also present as one of the main phenolic components of both black and green tea. Esters of gallic acid have a diverse range of industrial uses, as antioxidants in food, in cosmetics and in the pharmaceutical industry. In addition, gallic acid is employed as a source material for inks, paints and colour developers. Studies utilising these compounds have found them to possess many potential therapeutic properties including anti-cancer and antimicrobial properties. In this review, studies of the effects of gallic acid, its esters, and gallic acid catechin derivatives on Phase I and Phase II enzymes are examined. Many published reports of the effects of the in vitro effects of gallic acid and its derivatives on drug metabolising enzymes concern effects directly on substrate (generally drug or mutagen) metabolism or indirectly through observed effects in Ames tests. In the case of the Ames test an antimutagenic effect may be observed through inhibition of CYP activation of indirectly acting mutagens and/or by scavenging of metabolically generated mutagenic electrophiles. There has been considerable interest in the in vivo effects of the gallate esters because of their incorporation into foodstuffs as antioxidants and in the catechin gallates with their potential role as chemoprotective agents. Principally an induction of Phase II enzymes has been observed however more recent studies using HepG2 cells and primary cultures of human hepatocytes provide evidence for the overall complexity of actions of individual components versus complex mixtures, such as those in food. Further systematic studies of mechanisms of induction and inhibition of drug metabolising enzymes by this group of compounds are warranted in the light of their distribution and consequent ingestion, current uses and suggested therapeutic potential. However, it must be noted that numerous constituents of foodstuffs have been found to be potent modulators of xenobiotic metabolism and the net human health effects may depend on concentrations of individual components and individual genetic makeup.
Yin-Yin Ow; Ieva Stupans
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Current drug metabolism     Volume:  4     ISSN:  1389-2002     ISO Abbreviation:  Curr. Drug Metab.     Publication Date:  2003 Jun 
Date Detail:
Created Date:  2003-05-28     Completed Date:  2003-06-30     Revised Date:  2005-11-16    
Medline Journal Info:
Nlm Unique ID:  100960533     Medline TA:  Curr Drug Metab     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  241-8     Citation Subset:  IM    
Center for Pharmaceutical Research, School of Pharmaceutical, Molecular and Biomedical Sciences, University of South Australia, SA, 5000, Australia.
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MeSH Terms
Catechin / pharmacology
Enzymes / metabolism*
Food-Drug Interactions
Gallic Acid / analogs & derivatives*,  pharmacology*
Mixed Function Oxygenases / metabolism
Pharmaceutical Preparations / metabolism*
Reg. No./Substance:
0/Enzymes; 0/Pharmaceutical Preparations; 149-91-7/Gallic Acid; 154-23-4/Catechin; EC 1.-/Mixed Function Oxygenases

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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