文章基本信息

标题：Helicobacter pylori Urease Inhibition by Rabeprazole, a Proton Pump Inhibitor
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作者：Mamiko TSUCHIYA ; Lisa IMAMURA ; JongBeak PARK 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1995
卷号：18
期号：8
页码：1053-1056
DOI：10.1248/bpb.18.1053
出版社：The Pharmaceutical Society of Japan
摘要：We investigated the inhibitory effects of four gastric proton pump inhibitors (PPIs) : rabeprazole, a novel benzimidazole PPI, omeprazole, lansoprazole and AG-2000, on the urease activity of Helicobacter pylori (H. pylori). Their 50% inhibitory concentrations (I₅₀s) were found to be 0.29, 5.4, 9.3 and 0.3 μM respectively. Rabeprazole and omeprazole were also potent inhibitors of Jack bean and Proteus mirabilis cellular ureases. The thioether derivative of rabeprazole, one of its metabolites, had no inhibitory effect on H.pylori urease, despite being reported as a more potent inhibitor of H. pylori growth than rabeprazole. The inhibitory effect of rabeprazole was prevented completely and reversed considerably by the addition of sulfhydryl compounds, such as β-mercaptoethanol, glutathione and dithiothreitol. Moreover, the addition of β-mercaptoethanol recovered the urease activity inhibited by rabeprazole. From these results, we expected that rabeprazole inhibited H. pyloriurease activity by forming disulfide bonds between it and the active site of the enzyme.
关键词：Helicobacter pylori;lansoprazole;omeprazole;proton pump inhibitor;rabeprazole;urease