| Metabolism and effects on cholestasis of isoursodeoxycholic and ursodeoxycholic acids in bile duct ligated rats. | |
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MedLine Citation:
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PMID: 11287121 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Isoursodeoxycholic acid (isoUDCA), the 3 beta-epimer of ursodeoxycholic acid (UDCA), may have pharmaceutical potential because of its similar hydrophilicity and in vitro cytoprotection as compared with UDCA. We compared metabolism and effects on cholestasis of UDCA and isoUDCA in experimental cholestasis in rats. Cholestasis was induced by bile duct ligation. For bile flow and biliary bile acid analysis, UDCA or isoUDCA were infused intraduodenally. For the study of chronic effects, chow was supplemented with 2.5 g/kg UDCA or isoUDCA for 3 weeks. Sham-operated animals served as controls. IsoUDCA became completely converted to UDCA in the liver. Choleresis and biliary bile acids were the same after the intraduodenal administration of either compound. Oral administration of UDCA or isoUDCA significantly improved liver biochemistry but not clinical and histological parameters in chronic cholestasis. The decrease of serum cholic acid in control animals was more pronounced after isoUDCA (-93%) than after UDCA (-76%). Only after UDCA, this decrease was compensated by increases of UDCA, beta-muricholic acid (MCA), and Delta(22)-beta-MCA. Our results show that isoUDCA has the same effect on choleresis and liver biochemistry as UDCA. IsoUDCA features pro-drug characteristics of UDCA and causes compared to the latter lower serum bile acid concentrations in non-cholestatic animals. |
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Authors:
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E Purucker; H U Marschall; R Winograd; S Matern |
Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Biochimica et biophysica acta Volume: 1526 ISSN: 0006-3002 ISO Abbreviation: Biochim. Biophys. Acta Publication Date: 2001 Apr |
Date Detail:
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Created Date: 2001-04-05 Completed Date: 2001-05-10 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 0217513 Medline TA: Biochim Biophys Acta Country: Netherlands |
Other Details:
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Languages: eng Pagination: 44-52 Citation Subset: IM |
Affiliation:
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Department of Internal Medicine III, Medical Faculty, Aachen University of Technology, Germany. epurucker@post.klinikum.rwth-aachen.de |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Bile / metabolism Bile Acids and Salts / blood, urine Bile Ducts / physiology*, surgery Body Weight Cholestasis / metabolism* Cholic Acids / analysis Eating Ligation Liver / drug effects, metabolism Liver Function Tests Male Rats Rats, Sprague-Dawley Ursodeoxycholic Acid / analogs & derivatives*, metabolism, pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Bile Acids and Salts; 0/Cholic Acids; 128-13-2/Ursodeoxycholic Acid; 39016-49-4/muricholic acid; 78919-26-3/isoursodeoxycholic acid |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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