Ecabet sodium, a locally acting antiulcer drug, inhibits urease activity of Helicobacter pylori

被引:46
作者
Ito, Y
Shibata, K
Hongo, A
Kinoshita, M
机构
[1] Tanabe Seiyaku Co Ltd, Lead Optimizat Res Lab, Toda, Saitama 335, Japan
[2] Tanabe Seiyaku Co Ltd, Pharmaceut Dev Res Lab, Toda, Saitama 335, Japan
[3] Tanabe Seiyaku Co Ltd, Lead Generat Res Lab, Toda, Saitama 335, Japan
关键词
Helicobacter pylori; urease; ecabet sodium; antiulcer drug;
D O I
10.1016/S0014-2999(97)01622-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In order to clarify the mechanism of the anti-Helicobacter-pylori action of ecabet sodium (ecabet), a locally acting antiulcer drug, we evaluated the effects of ecabet on H. pylori urease activity in vitro. H. pylori was cultured and a crude preparation of urease was made. Urea-dependent survival of H. pylori at acid pH was significantly inhibited by ecabet. The urease activity of intact cells and a crude enzyme preparation from H. pylori had two pH optima: pH 1.5-5.0 and 8.0. Ecabet (1-4 mg/ml) concentration dependently inhibited the urease activity of both preparations at pH 5.0, but there was no inhibition at pH 8.0. The enzyme activity was inhibited by ecabet gradually and was not restored by dilution, in contrast to the inhibition elicited by benzohydroxamic acid, a specific and reversible urease inhibitor. These results suggest that irreversible inhibition of H. pylori urease activity contributes to the anti-H. pylori action of ecabet. (C) 1998 Elsevier Science B.V.
引用
收藏
页码:193 / 198
页数:6
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