Document Detail

The choleretic effects of N-acetylglucosaminides, major urinary metabolites of ursodeoxycholic acid, in bile fistula rats.
MedLine Citation:
PMID:  9877080     Owner:  NLM     Status:  MEDLINE    
We investigated the effects of three bile acids conjugated with N-acetylglucosamine, ursodeoxycholate N-acetylglucosaminide, tauroursodeoxycholate N-acetylglucosaminide and glycoursodeoxycholate N-acetylglucosaminide, on bile flow and biliary excretion of various markers in comparison with ursodeoxycholic acid, tauroursodeoxycholic acid and glycoursodeoxycholic acid in bile fistula rats. These bile acids were infused intravenously at a constant rate of 0.3 or 0.6 micromol/min/100 g b.w. for 2 h. All bile acids examined increased bile flow in a dose-dependent manner. In particular, ursodeoxycholate N-acetylglucosaminide has a longer-lasting effect after its infusion on bile flow than the other bile acids. Furthermore, these bile acids markedly increased biliary total bile acid excretion. At a higher dose level, the coefficient of determination (r2) between the biliary total bile acid excretion and bile flow for ursodeoxycholate N-acetylglucosaminide (r2 = 0.39) was lower than that for the other bile acids (r2 = 0.75-0.92). The ursodeoxycholate N-acetylglucosaminide, as well as tauroursodeoxycholic acid, glycoursodeoxycholic acid, tauroursodeoxycholate N-acetylglucosaminide and glycoursodeoxycholate N-acetylglucosaminide, was mostly excreted in an unchanged form in bile, whereas ursodeoxycholic acid was excreted as a conjugate with taurine. The three N-acetylglucosaminides as well as ursodeoxycholic acid, tauroursodeoxycholic acid and glycoursodeoxycholic acid significantly increased the biliary excretion of cholesterol, phospholipid, bilirubin and total Ca2+. In contrast, the N-acetylglucosaminides significantly decreased in biliary bicarbonate concentration, whereas ursodeoxycholic acid significantly increased biliary bicarbonate concentration. However, tauroursodeoxycholic acid and glycoursodeoxycholic acid did not significantly change the biliary bicarbonate concentration. The results indicate that N-acetylglucosaminides have a choleretic effect in bile fistula rats. Our present study also demonstrates that N-acetylglucosaminides, but not ursodeoxycholic acid, tauroursodeoxycholic acid or glycoursodeoxycholic acid, can significantly reduce the biliary bicarbonate concentration. Furthermore, our findings suggest that ursodeoxycholate N-acetylglucosaminide may partly exert a choleretic effect via mechanisms different from those of the other bile acids.
T Iwaki; N Hirabayashi; N Miyazawa; Y Takeuchi; K Ishizaki; H Sakakura; H Kasai; M Maeda; T Araki
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  European journal of pharmacology     Volume:  363     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1998 Dec 
Date Detail:
Created Date:  1999-04-16     Completed Date:  1999-04-16     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  41-8     Citation Subset:  IM    
Medicinal Research Group II, Kazusa Research Laboratories, Tokyo Tanabe, Chiba, Japan.
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MeSH Terms
Bicarbonates / analysis*
Bile / chemistry,  drug effects,  secretion*
Bile Acids and Salts / analysis,  pharmacology*
Biliary Fistula
Biological Markers
Cholagogues and Choleretics / pharmacology*
Dose-Response Relationship, Drug
Injections, Intravenous
Rats, Wistar
Time Factors
Ursodeoxycholic Acid / metabolism*
Reg. No./Substance:
0/Bicarbonates; 0/Bile Acids and Salts; 0/Biological Markers; 0/Cholagogues and Choleretics; 128-13-2/Ursodeoxycholic Acid

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