Document Detail

Basic studies on 5-(7-hydroxy-3-O-phosphonocholyl)aminosalicylic acid for the evaluation of microbial overgrowth.
MedLine Citation:
PMID:  9145212     Owner:  NLM     Status:  MEDLINE    
A newly synthesized conjugate of 7-hydroxy-3-O-phosphonocholic acid (ursodeoxycholic acid monophosphate) with 5-aminosalicylic acid (5-ASA-UDCA monophosphate) was investigated to determine its suitability for the evaluation of enteric bacteria. This compound, 5-ASA-UDCA monophosphate, was efficiently deconjugated by cholylglycine hydrolase to release 5-ASA, whereas it was completely resistant to deconjugation by pancreatic and intestinal mucosal enzymes. In everted gut sac experiments, 5-ASA-UDCA monophosphate was not actively absorbed from any part of the small intestine. In animal experiments, urinary excretions of N-acetyl-5-ASA (Ac-5ASA) were measured for 24 h following the oral administration of 20 mg of 5-ASA-UDCA monophosphate. Control rats excreted 276.3 +/- 89.0 micrograms (mean +/- S.E.) of Ac-5ASA, whereas the rats with intestinal bacterial overgrowth excreted more (1224.1 +/- 231.5 micrograms; p < 0.01). These basic studies indicate that this compound is likely to offer a simple method for the evaluation of microbial overgrowth without the use of radioisotopes or expensive, special apparatus.
T Konishi; M Takahashi; S Ohta
Publication Detail:
Type:  In Vitro; Journal Article    
Journal Detail:
Title:  Biological & pharmaceutical bulletin     Volume:  20     ISSN:  0918-6158     ISO Abbreviation:  Biol. Pharm. Bull.     Publication Date:  1997 Apr 
Date Detail:
Created Date:  1997-07-03     Completed Date:  1997-07-03     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9311984     Medline TA:  Biol Pharm Bull     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  370-5     Citation Subset:  IM    
Department of Hospital Pharmacy, Chugoku Rosai Hospital, Hiroshima, Japan.
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MeSH Terms
Aminosalicylic Acids / chemical synthesis,  diagnostic use*,  pharmacokinetics
Bacteria / growth & development*
Bile / chemistry
Intestines / metabolism,  microbiology*
Liver / enzymology
Pancreatin / metabolism
Rats, Wistar
Ursodeoxycholic Acid / analogs & derivatives*,  chemical synthesis,  diagnostic use,  pharmacokinetics
Reg. No./Substance:
0/5-(7-hydroxy-3-O-phosphonocholyl)aminosalicylic acid; 0/Aminosalicylic Acids; 128-13-2/Ursodeoxycholic Acid; 8049-47-6/Pancreatin

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