Source:http://linkedlifedata.com/resource/pubmed/id/16455235
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1-2
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| pubmed:dateCreated |
2006-3-14
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| pubmed:abstractText |
We previously reported that 5-aminosalicyltaurine (taurine-conjugated 5-ASA, 5-ASA-Tau) showed a potential as a colon-specific prodrug of 5-aminosalicylic acid (5-ASA) by in vitro evaluation. In this report, we in vivo-evaluated 5-ASA-Tau as a colon-specific prodrug for treatment of experimental colitis. Taurine conjugation of 5-ASA greatly reduced absorption of 5-ASA from the intestine. Oral administration of taurine-conjugated 5-ASA not only increased the colonic delivery efficiency of 5-ASA but also decreased the systemic absorption of free 5-ASA as compared with that of 5-ASA and, moreover, taurine is similarly effective to known colon-specific carriers for 5-ASA, glycine and aspartic acid, suggesting that taurine conjugation is an efficient way to increase the therapeutic effect and to reduce the adverse effects of 5-ASA. Intracolonic treatment with combined 5-ASA/taurine additively ameliorated TNBS-induced colitis rats indicating that taurine acted as not only a promoiety but also a therapeutically active agent. Furthermore, 5-ASA-Tau is slightly more effective than sulfasalazine in alleviating the colonic inflammation induced by TNBS. Taken together, our data suggest that 5-ASA-Tau is a potential colon-specific prodrug of 5-aminosalicylic acid with improved therapeutic activity against inflammatory bowel disease.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/5-aminosalicyltaurine,
http://linkedlifedata.com/resource/pubmed/chemical/Aminosalicylic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Inflammatory Agents...,
http://linkedlifedata.com/resource/pubmed/chemical/Gastrointestinal Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Mesalamine,
http://linkedlifedata.com/resource/pubmed/chemical/Prodrugs,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfasalazine,
http://linkedlifedata.com/resource/pubmed/chemical/Taurine,
http://linkedlifedata.com/resource/pubmed/chemical/Trinitrobenzenesulfonic Acid
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| pubmed:status |
MEDLINE
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| pubmed:month |
May
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| pubmed:issn |
0928-0987
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| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
28
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
26-33
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| pubmed:dateRevised |
2006-11-15
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| pubmed:meshHeading |
pubmed-meshheading:16455235-Aminosalicylic Acids,
pubmed-meshheading:16455235-Animals,
pubmed-meshheading:16455235-Anti-Inflammatory Agents, Non-Steroidal,
pubmed-meshheading:16455235-Chromatography, High Pressure Liquid,
pubmed-meshheading:16455235-Colitis,
pubmed-meshheading:16455235-Colon,
pubmed-meshheading:16455235-Drug Delivery Systems,
pubmed-meshheading:16455235-Feces,
pubmed-meshheading:16455235-Gastrointestinal Agents,
pubmed-meshheading:16455235-Intestinal Absorption,
pubmed-meshheading:16455235-Male,
pubmed-meshheading:16455235-Mesalamine,
pubmed-meshheading:16455235-Prodrugs,
pubmed-meshheading:16455235-Rats,
pubmed-meshheading:16455235-Rats, Sprague-Dawley,
pubmed-meshheading:16455235-Sulfasalazine,
pubmed-meshheading:16455235-Taurine,
pubmed-meshheading:16455235-Trinitrobenzenesulfonic Acid
|
| pubmed:year |
2006
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| pubmed:articleTitle |
Evaluation of 5-aminosalicyltaurine as a colon-specific prodrug of 5-aminosalicylic acid for treatment of experimental colitis.
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| pubmed:affiliation |
Lab of Biomedicinal Chemistry, College of Pharmacy, Pusan National University, Busan 609-735, Republic of Korea.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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