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      Anti- Helicobacter pylori activity of ethoxzolamide

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          Abstract

          Ethoxzolamide (EZA), acetazolamide, and methazolamide are clinically used sulphonamide drugs designed to treat non-bacteria-related illnesses (e.g. glaucoma), but they also show antimicrobial activity against the gastric pathogen Helicobacter pylori. EZA showed the highest activity, and was effective against clinical isolates resistant to metronidazole, clarithromycin, and/or amoxicillin, suggesting that EZA kills H. pylori via mechanisms different from that of these antibiotics. The frequency of single-step spontaneous resistance acquisition by H. pylori was less than 5 × 10 −9, showing that resistance to EZA does not develop easily. Resistance was associated with mutations in three genes, including the one that encodes undecaprenyl pyrophosphate synthase, a known target of sulphonamides. The data indicate that EZA impacts multiple targets in killing H. pylori. Our findings suggest that developing the approved anti-glaucoma drug EZA into a more effective anti- H. pylori agent may offer a faster and cost-effective route towards new antimicrobials with a novel mechanism of action.

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          Helicobacter pylori update: gastric cancer, reliable therapy, and possible benefits.

          David Graham (2015)
          Helicobacter pylori infection contributes to the development of diverse gastric and extragastric diseases. The infection is necessary but not sufficient for the development of gastric adenocarcinoma. Its eradication would eliminate a major worldwide cause of cancer death, therefore there is much interest in identifying how, if, and when this can be accomplished. There are several mechanisms by which H pylori contributes to the development of gastric cancer. Gastric adenocarcinoma is one of many cancers associated with inflammation, which is induced by H pylori infection, yet the bacteria also cause genetic and epigenetic changes that lead to genetic instability in gastric epithelial cells. H pylori eradication reduces both. However, many factors must be considered in determining whether treating this bacterial infection will prevent cancer or only reduce its risk-these must be considered in designing reliable and effective eradication therapies. Furthermore, H pylori infection has been proposed to provide some benefits, such as reducing the risks of obesity or childhood asthma. When tested, these hypotheses have not been confirmed and are therefore most likely false. Copyright © 2015 AGA Institute. Published by Elsevier Inc. All rights reserved.
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            A standardized mouse model of Helicobacter pylori infection: introducing the Sydney strain.

            A. Lee, J. O'Rourke, MC De Ungria … (1997)
            Currently available Helicobacter pylori models show variable and, in some instances, poor colonization. There is a need for a strain with high colonizing ability to act as a standard for animal studies. After screening a range of fresh clinical isolates and long-term adaptation in mice, a strain of H. pylon has been isolated with a very good colonizing ability. This strain, named the Sydney strain of H. pylori (strain SS1), is cagA and vacA positive. High levels of colonization (10(6)-10(7) colony-forming units/g tissue) were achieved consistently in C57BL/6 mice. Colonization levels varied depending on the mouse strain used with BALB/c, DBA/2, and C3H/He, all being colonized but in lower numbers. In all strains of mice, bacteria were clearly visible at the junctional zone between the antrum and the body. The phenotype was stable with colonizing ability remaining after 20 subcultures in vitro. The bacterium attached firmly to gastric epithelium. During 8 months, a chronic active gastritis slowly developed, progressing to severe atrophy in both C57BL/6 and BALB/c mice. The Sydney strain of H. pylori is available to all and will provide a standardized mouse model for vaccine development, compound screening, and studies in pathogenesis.
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              Essential role of urease in pathogenesis of gastritis induced by Helicobacter pylori in gnotobiotic piglets.

              Danice K. Eaton, S Krakowka, D Morgan … (1991)
              A mutant strain of Helicobacter pylori with weak urease activity was created by using N-methyl-N'-nitro-N-nitrosoguanidine. The urease activity of the mutant (0.036 +/- 0.009 nmol of urea per micrograms of bacterial protein per min) was 0.4% of that of the parental strain (8.20 +/- 2.30 nmol of urea per micrograms of bacterial protein per min). The mutant was otherwise indistinguishable from the parental strain. Both demonstrated prominent catalase and oxidase activities, and both produced vacuolating cytotoxin. Restriction endonuclease and sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) patterns and ultrastructure were identical for the two strains. The mutant was fully motile, as evaluated by spreading in soft agar and by direct microscopic examination. Growth rate and colony size and morphology were identical for the mutant and parental strains. Seventeen gnotobiotic piglets were challenged with either the mutant or the parental strain and sacrificed 3 or 21 days after challenge. Gastric tissue was examined histologically and cultured for H. pylori. Of seven piglets challenged with the parental strain, all became infected. H. pylori was not recovered from any of 10 piglets challenged with the urease-negative strain. Lymphofollicular gastritis was present in all seven piglets challenged with the parental strain but in none of the piglets challenged with the urease-negative strain. These results suggest that prominent urease activity is essential for colonization by H. pylori.
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                Author and article information

                Journal
                Journal ID (nlm-ta): J Enzyme Inhib Med Chem
                Journal ID (iso-abbrev): J Enzyme Inhib Med Chem
                Journal ID (publisher-id): IENZ
                Journal ID (publisher-id): ienz20
                Title: Journal of Enzyme Inhibition and Medicinal Chemistry
                Publisher: Taylor & Francis
                ISSN (Print): 1475-6366
                ISSN (Electronic): 1475-6374
                Publication date Collection: 2019
                Publication date (Electronic): 17 September 2019
                Volume: 34
                Issue: 1
                Pages: 1660-1667
                Affiliations
                [a ]Department of Microbiology, Monash University , Clayton, Australia;
                [b ]Infection and Immunity Program, Monash Biomedicine Discovery Institute, Monash University , Clayton, Australia;
                [c ]Department of Biochemistry and Molecular Biology, Monash University , Clayton, Australia;
                [d ]Monash Infectious Diseases, Monash University, Monash Health , Australia;
                [e ]Centre for Innate Immunity and Infectious Diseases, Hudson Institute of Medical Research , Clayton, Australia;
                [f ]Laboratorio di Chimica Bioinorganica, Polo Scientifico, Università degli Studi di Firenze , Sesto Fiorentino, Italy;
                [g ]Neurofarba Department, Sezione di Scienze Farmaceutiche, Università degli Studi di Firenze , Sesto Fiorentino, Italy
                Author notes
                [*]

                These authors contributed equally to this work.

                Supplemental data for this article can be accessed here .

                CONTACT Anna Roujeinikova anna.roujeinikova@ 123456monash.edu 19 Innovation Walk, Monash University , Clayton, Victoria 3800, Australia
                Author information
                http://orcid.org/0000-0003-4262-0323
                Article
                Publisher ID: 1663416
                DOI: 10.1080/14756366.2019.1663416
                PMC ID: 6759998
                PubMed ID: 31530039
                SO-VID: 01964898-bb5b-4229-9dd3-ab5f913d9773
                Copyright © & 2019 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group
                License:

                This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial License ( http://creativecommons.org/licenses/by-nc/4.0/), which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                Date received : 24 July 2019
                Date revision received : 16 August 2019
                Date accepted : 23 August 2019
                Page count
                Figures: 5, Tables: 3, Pages: 8, Words: 5449
                Categories
                Subject: Research Paper

                ScienceOpen disciplines: Pharmaceutical chemistry
                Keywords: mutation frequency,mic/mbc,ethoxzolamide,genome sequencing
                Data availability:
                ScienceOpen disciplines: Pharmaceutical chemistry
                Keywords: mutation frequency, mic/mbc, ethoxzolamide, genome sequencing

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