Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
Helicobacter pylori Urease Inhibition by Rabeprazole, a Proton Pump Inhibitor
Mamiko TSUCHIYALisa IMAMURAJongBeak PARKKyoichi KOBASHI
Author information
JOURNALS FREE ACCESS

1995 Volume 18 Issue 8 Pages 1053-1056

Details
Abstract

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.

Information related to the author
© The Pharmaceutical Society of Japan
Previous article Next article
feedback
Top