Document Detail


Effects of YJA20379-4 on gastric secretion, Helicobacter pylori growth and various gastric and duodenal lesions in rats.
MedLine Citation:
PMID:  9635498     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Effects of a newly synthesized antiulcer agent, YJA20379-4, on gastric proton pump (H+/K+-ATPase) activity, Helicobacter pylori (H. pylori) growth, gastric acid secretion, and gastro-duodenal lesions, were examined in comparison with those of omeprazole. YJA20379-4 markedly inhibited the H+/K+-ATPase activity in a concentration-dependent manner and the inhibitory effect was increased under a weak acidic condition; the IC50 values were 32 and 81 microM at pH 6.4 and 7.4, respectively. The inhibition was completely antagonized by 0.5 mM dithiothreitol (DTT). In addition, YJA20379-4 showed a significant anti-H. pylori activity determined by the agar dilution method. The value of minimum inhibitory concentration (MIC, 3.9-11.7 microg/ml) was at least 3 times more potent than that of omeprazole. In pylorus ligated rats, YJA20379-4 inhibited basal gastric acid secretion when administered by the intraduodenal route (ED50: 23.6 mg/kg). In experimental ulcer models, YJA20379-4 administered by the oral route dose-dependently prevented the development of gastro-duodenal lesions in rats. Moreover, repeated administration of YJA20379-4 promoted the healing of gastric ulcers induced by acetic acid. On the basis of the data obtained, it is suggested that YJA20379-4 has a wide spectrum of antiulcer activities, and its mode of antiulcer actions is dependent on the inhibition of H+/K+-ATPase activity and H. pylori growth and the enhancement of a mucosal defense. Thus, YJA20379-4 might prove to be a beneficial therapy for gastritis and peptic ulcer diseases.
Authors:
T W Woo; M S Chang; Y K Chung; K B Kim; S K Sohn; S G Kim; W S Choi
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Biological & pharmaceutical bulletin     Volume:  21     ISSN:  0918-6158     ISO Abbreviation:  Biol. Pharm. Bull.     Publication Date:  1998 May 
Date Detail:
Created Date:  1998-08-24     Completed Date:  1998-08-24     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9311984     Medline TA:  Biol Pharm Bull     Country:  JAPAN    
Other Details:
Languages:  eng     Pagination:  449-55     Citation Subset:  IM    
Affiliation:
Pharmacology and Toxicology Laboratory, Research and Development Center, Yung-Jin Pharmaceutical Co., Ltd., Kyunggi-Do, Korea.
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MeSH Terms
Descriptor/Qualifier:
Animals
Anti-Ulcer Agents / pharmacology*
Benzimidazoles / pharmacology*
Dithiothreitol / pharmacology
Duodenal Ulcer / etiology,  prevention & control*
Female
Gastric Acid / secretion*
Gastric Mucosa / cytology,  drug effects,  secretion*
H(+)-K(+)-Exchanging ATPase / antagonists & inhibitors
Helicobacter pylori / drug effects,  growth & development*
Immersion
Male
Microbial Sensitivity Tests
Omeprazole / pharmacology
Proton Pumps / antagonists & inhibitors
Rabbits
Rats
Rats, Sprague-Dawley
Stomach Ulcer / etiology,  prevention & control*
Stress, Psychological / complications
Sulfhydryl Reagents / pharmacology
Chemical
Reg. No./Substance:
0/Anti-Ulcer Agents; 0/Benzimidazoles; 0/Proton Pumps; 0/Sulfhydryl Reagents; 0/YJA 20379-4; 3483-12-3/Dithiothreitol; 73590-58-6/Omeprazole; EC 3.6.1.10/H(+)-K(+)-Exchanging ATPase

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