Document Detail

Inhibition of human liver and duodenum sulfotransferases by drugs and dietary chemicals: a review of the literature.
MedLine Citation:
PMID:  15487807     Owner:  NLM     Status:  MEDLINE    
Sulfotransferase catalyzes the transfer of sulfate, donated by 3'-phosphoadenosine-5'-phosphosulfate, to an acceptor substrate that may be a hydroxy group or an amine group. Man is exposed daily to drugs and dietary chemicals that can inhibit sulfotransferase activity. The aim of this study was to review the literature concerning the inhibition of sulfotransferases by drugs and dietary chemicals in the human liver and duodenum. The IC50 value of mefenamic acid for human liver phenol sulfotransferase (SULT 1A1) was 0.02 microM and for human liver catechol sulfotransferase (SULT1A3) 76 microM with a SULT 1A3/SULT1A1 ratio for the IC50 of 3,800. Mefenamic acid is therefore a potent and selective inhibitor of human liver SULT1A1. The IC50 values of mefenamic acid for the sulfation rates of (-)-salbutamol and (-)-apomorphine were 4 orders of magnitude greater in the human duodenum than in the liver. Salicylic acid inhibited the sulfation of (-)-apomorphine in human liver with an IC50 of 54 gM but did not inhibit the sulfation of (-)-apomorphine in human duodenum. Quercetin, a flavonoid present in edible fruit, vegetable and wine, was a potent inhibitor of human liver SULT1A1 and estrogen sulfotransferase (EST) activities and the sulfation of resveratrol. Quercetin inhibited the sulfation of dopamine, (-)-salbutamol, minoxidil and paracetamol and the IC50 values were 1 - 2 orders of magnitude greater in human duodenum than in the liver. In conclusion, mefenamic acid, salicylic acid and quercetin inhibit SULT1A1 whereas SULT1A3 is relatively resistant to the inhibition by these compounds. Under particular circumstances, human duodenum sulfotransferase is more resistant than liver sulfotransferase to the inhibition by mefenamic acid, salicylic acid and quercetin.
G M Pacifici
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  International journal of clinical pharmacology and therapeutics     Volume:  42     ISSN:  0946-1965     ISO Abbreviation:  Int J Clin Pharmacol Ther     Publication Date:  2004 Sep 
Date Detail:
Created Date:  2004-10-18     Completed Date:  2004-12-09     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9423309     Medline TA:  Int J Clin Pharmacol Ther     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  488-95     Citation Subset:  IM    
Department of Neurosciences, Section of Pharmacology, Medical School, Pisa, Italy.
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MeSH Terms
Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
Duodenum / drug effects*,  enzymology
Inhibitory Concentration 50
Liver / drug effects*,  enzymology
Mefenamic Acid / pharmacology
Quercetin / pharmacology
Salicylic Acid / pharmacology
Sulfotransferases / antagonists & inhibitors,  biosynthesis*
Reg. No./Substance:
0/Anti-Inflammatory Agents, Non-Steroidal; 117-39-5/Quercetin; 61-68-7/Mefenamic Acid; 69-72-7/Salicylic Acid; EC 2.8.2.-/Sulfotransferases

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