Document Detail


Sulphation of resveratrol, a natural product present in grapes and wine, in the human liver and duodenum.
MedLine Citation:
PMID:  10923862     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
1. Resveratrol, a polyphenolic compound present in grapes and wine, has beneficial effects against cancer and protective effects on the cardiovascular system. It is present in the diet, and the hepatic and duodenal sulphation might limit the bioavailability of this compound. The aim was to study the sulphation of resveratrol in the human liver and duodenum. 2. A simple and reproducible radiometric assay for resveratrol sulphation was developed. It employed 3'-phosphoadenosine-5'-phosphosulphate-[35S] as the sulphate donor and the rates of resveratrol sulphation (mean +/- SD, pmol/min/mg cytosolic protein) were 90 +/- 21 (liver, n = 10) and 74 +/- 60 (duodenum, n = 10, p = 0.082). 3. Resveratrol sulphotransferase followed Michaelis-Menten kinetics and Km (mean +/- SD; microM) was 0.63 +/- 0.03 (liver, n = 5) and 0.50 +/- 0.26 (duodenum, n = 5, p = 0.39) and Vmax (mean +/- SD, pmol/min/mg cytosolic protein) were 125 +/- 31 (liver, n = 5) and 129 +/- 85 (duodenum, n = 5, p = 0.62). 4. Resveratrol sulphation was inhibited by the flavonoid quercetin, by mefenamic acid and salicylic acid, two commonly used non-steroidal anti-inflammatory drugs. IC50 of resveratrol sulphation for quercetin was 12 +/- 2 pM (liver) and 15 +/- 2 pM (duodenum), those for mefenamic acid were 24 +/- 3 nM (liver) and 11 +/- 0.6 nM (duodenum), and those for salicylic acid were 53 +/- 9 microM (liver) and 66 +/- 4 microM (duodenum). 5. The potent inhibition of resveratrol sulphation by quercetin, a flavonoid present in wine, fruits and vegetables, suggests that compounds present in the diet may inhibit the sulphation of resveratrol, thus improving its bioavailability.
Authors:
C De Santi; A Pietrabissa; R Spisni; F Mosca; G M Pacifici
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Xenobiotica; the fate of foreign compounds in biological systems     Volume:  30     ISSN:  0049-8254     ISO Abbreviation:  Xenobiotica     Publication Date:  2000 Jun 
Date Detail:
Created Date:  2000-12-13     Completed Date:  2000-12-13     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1306665     Medline TA:  Xenobiotica     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  609-17     Citation Subset:  IM    
Affiliation:
Department of Neurosciences, Medical School, Pisa, Italy.
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MeSH Terms
Descriptor/Qualifier:
Adult
Aged
Biological Availability
Duodenum / drug effects,  enzymology,  metabolism*
Humans
Kinetics
Liver / drug effects,  enzymology,  metabolism*
Mefenamic Acid / pharmacology
Middle Aged
Molecular Structure
Phosphoadenosine Phosphosulfate / metabolism
Quercetin / pharmacology
Rosales / chemistry*
Salicylic Acid / pharmacology
Stilbenes / metabolism*,  pharmacokinetics,  pharmacology
Sulfates / metabolism*
Sulfotransferases / antagonists & inhibitors,  metabolism
Wine*
Chemical
Reg. No./Substance:
0/Stilbenes; 0/Sulfates; 117-39-5/Quercetin; 482-67-7/Phosphoadenosine Phosphosulfate; 501-36-0/resveratrol; 61-68-7/Mefenamic Acid; 69-72-7/Salicylic Acid; EC 2.8.2.-/Sulfotransferases

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