The choleretic effect of N-acetylglucosamine conjugates of Ursodeoxycholic acid (UDCA) in bile fistura rats

Ursodeoxycholic acid (UDCA) improves clinical and biochemical indices in patients with primary biliary cirrhosis and some other cholestatic liver diseases. Recently, N-acetylglucosamine conjugates have been identified as metabolites of UDCA at high urinary excretion rate both in patients with choles...

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Bibliographic Details
Published in:	Japanese Journal of Pharmacology Vol. 73; no. suppl.1; p. 219
Main Authors:	Iwaki, Tomomichi, Miyazawa, Norio, Hasegawa, Hiromi, Sakakuta, Hirao, Hirabayashi, Norio, Kasai, Hiroshi
Format:	Journal Article
Language:	English
Published:	The Japanese Pharmacological Society 1997
Online Access:	Get full text
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Summary:	Ursodeoxycholic acid (UDCA) improves clinical and biochemical indices in patients with primary biliary cirrhosis and some other cholestatic liver diseases. Recently, N-acetylglucosamine conjugates have been identified as metabolites of UDCA at high urinary excretion rate both in patients with cholestasis and in healthy human beings. In the present investigation, we studied the choleretic effects of N-acetylglucosamine conjugates of UDCA, tauroursodeoxycholic acid (TUDCA) and glycoursodeoxycholic acid (GUDCA) in bile fistura rats, and compared with those of the corresponding unconjugated bile acids. All three N-acetylglucosamine conjugates infused at rates of 0.3 and O.6μmol/min/100g increased significantly bile flow and biliary bile acids excretion as well as the corresponding unconjugated bile acids. N-acetylglucosamine conjugate of UDCA induced maximum increase of bile flow and biliary bile acids excretion after the infusion for 2 hr, on the contrary the other bile acids showed maximum effect within the infusion period. Analysis of bile acids composition indicated that N-acetylglucosamine conjugate of UDCA was excreted into bile without further conjugation, although UDCA is conjugated with taurine or glycine. These results demonstrate that the three N-acetylglucosamine conjugates have choleretic effect, and suggest that delayed effect of N-acetylglucosamine conjugate of UDCA is due to not being conjugated.
ISSN:	0021-5198 1347-3506
DOI:	10.1016/S0021-5198(19)45378-X