Document Detail

Synthesis and intestinal metabolism of ursodeoxycholic acid conjugate with an antiinflammatory agent, 5-aminosalicylic acid.
MedLine Citation:
PMID:  9717724     Owner:  NLM     Status:  MEDLINE    
5-Aminosalicylic acid conjugate of ursodeoxycholic acid was synthesized in above 90% yield by adding a basic solution of 5-aminosalicylic acid into the mixed anhydride formed with ursodeoxycholic acid and ethyl chloroformate. The 5-aminosalicylic acid conjugate of ursodeoxycholic acid was poorly secreted into the bile and was deconjugated with cholylglycine hydrolase and Clostridium perfringens, that deconjugate naturally occurring glycine and taurine conjugates of bile acids. However, ursodeoxycholic acid 5-aminosalicylic acid conjugate was not absorbed from the duodenum but was concentrated in the colon where it was partially hydrolyzed by the intestinal bacteria to ursodeoxycholic acid and 5-aminosalicylic acid. We believe that this unique conjugation of ursodeoxycholic acid with 5-aminosalicylic acid may facilitate the transport of both 5-aminosalicylic acid and ursodeoxycholic acid to the colon and may be useful for the treatment of colonic inflammatory bowel diseases, ulcerative colitis and Crohn's disease.
A K Batta; G S Tint; G Xu; S Shefer; G Salen
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Publication Detail:
Type:  Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Journal of lipid research     Volume:  39     ISSN:  0022-2275     ISO Abbreviation:  J. Lipid Res.     Publication Date:  1998 Aug 
Date Detail:
Created Date:  1998-11-16     Completed Date:  1998-11-16     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  0376606     Medline TA:  J Lipid Res     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1641-6     Citation Subset:  IM    
Department of Medicine and Liver Center, University of Medicine and Dentistry-New Jersey Medical School, Newark 07103, USA.
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MeSH Terms
Amidohydrolases / metabolism
Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*,  metabolism*,  therapeutic use
Biological Transport, Active
Clostridium perfringens / metabolism
Colonic Polyps / drug therapy,  metabolism
Inflammatory Bowel Diseases / drug therapy,  metabolism
Intestinal Absorption
Intestines / metabolism*,  microbiology
Mesalamine / chemical synthesis*,  metabolism*,  therapeutic use
Ursodeoxycholic Acid / analogs & derivatives*,  chemical synthesis,  metabolism
Grant Support
Reg. No./Substance:
0/Anti-Inflammatory Agents, Non-Steroidal; 128-13-2/Ursodeoxycholic Acid; 89-57-6/Mesalamine; EC 3.5.-/Amidohydrolases; EC hydrolase

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