The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth
Carbonic anhydrases, catalysing the reversible CO2 hydration reaction, contribute in all living organisms to the maintenance of stable metabolic functions depending on intracellular concentrations of carbon dioxide, bicarbonate, and protons. Recent studies have examined how CAs affect bacterial life...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2022-12-01
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| Series: | Journal of Enzyme Inhibition and Medicinal Chemistry |
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| Online Access: | https://www.tandfonline.com/doi/10.1080/14756366.2022.2101644 |
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| author | Viviana De Luca Vincenzo Carginale Claudiu T. Supuran Clemente Capasso |
| author_facet | Viviana De Luca Vincenzo Carginale Claudiu T. Supuran Clemente Capasso |
| author_sort | Viviana De Luca |
| collection | DOAJ |
| description | Carbonic anhydrases, catalysing the reversible CO2 hydration reaction, contribute in all living organisms to the maintenance of stable metabolic functions depending on intracellular concentrations of carbon dioxide, bicarbonate, and protons. Recent studies have examined how CAs affect bacterial lifecycle, considering these enzymes druggable targets due to interference with their activities by using inhibitors or activators. Here, we propose Escherichia coli cells as a model for testing the effect of acetazolamide (AZA), a potent CA inhibitor, on bacterial survival by evaluating E. coli growth through its glucose consumption. AZA, at concentrations higher than 31.2 µg/mL, was able to impair E. coli growth and glucose uptake. AZA is a good inhibitor of the two recombinant E. coli CAs, the β-CA CynT2, and the γ-CA EcoCAγ, with KIs of 227 and 248 nM, respectively. This study provides a proof-of-concept, low-cost method for identifying effective CA inhibitors capable of impairing bacterial metabolism. |
| format | Article |
| id | doaj-art-c24a82beb06d4e3fbdd07d88c98bb8a8 |
| institution | OA Journals |
| issn | 1475-6366 1475-6374 |
| language | English |
| publishDate | 2022-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Journal of Enzyme Inhibition and Medicinal Chemistry |
| spelling | doaj-art-c24a82beb06d4e3fbdd07d88c98bb8a82025-08-20T02:36:30ZengTaylor & Francis GroupJournal of Enzyme Inhibition and Medicinal Chemistry1475-63661475-63742022-12-013712092209810.1080/14756366.2022.2101644The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growthViviana De Luca0Vincenzo Carginale1Claudiu T. Supuran2Clemente Capasso3Institute of Biosciences and Bioresources, National Research Council, Napoli, ItalyInstitute of Biosciences and Bioresources, National Research Council, Napoli, ItalySection of Pharmaceutical and Nutraceutical Sciences, Department of Neurofarba, University of Florence, Florence, ItalyInstitute of Biosciences and Bioresources, National Research Council, Napoli, ItalyCarbonic anhydrases, catalysing the reversible CO2 hydration reaction, contribute in all living organisms to the maintenance of stable metabolic functions depending on intracellular concentrations of carbon dioxide, bicarbonate, and protons. Recent studies have examined how CAs affect bacterial lifecycle, considering these enzymes druggable targets due to interference with their activities by using inhibitors or activators. Here, we propose Escherichia coli cells as a model for testing the effect of acetazolamide (AZA), a potent CA inhibitor, on bacterial survival by evaluating E. coli growth through its glucose consumption. AZA, at concentrations higher than 31.2 µg/mL, was able to impair E. coli growth and glucose uptake. AZA is a good inhibitor of the two recombinant E. coli CAs, the β-CA CynT2, and the γ-CA EcoCAγ, with KIs of 227 and 248 nM, respectively. This study provides a proof-of-concept, low-cost method for identifying effective CA inhibitors capable of impairing bacterial metabolism.https://www.tandfonline.com/doi/10.1080/14756366.2022.2101644Carbonic anhydrasessulphonamideinhibitorphenol-sulphuric acid assayglucose consumptionbacterial growth |
| spellingShingle | Viviana De Luca Vincenzo Carginale Claudiu T. Supuran Clemente Capasso The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth Journal of Enzyme Inhibition and Medicinal Chemistry Carbonic anhydrases sulphonamide inhibitor phenol-sulphuric acid assay glucose consumption bacterial growth |
| title | The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth |
| title_full | The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth |
| title_fullStr | The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth |
| title_full_unstemmed | The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth |
| title_short | The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth |
| title_sort | gram negative bacterium escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth |
| topic | Carbonic anhydrases sulphonamide inhibitor phenol-sulphuric acid assay glucose consumption bacterial growth |
| url | https://www.tandfonline.com/doi/10.1080/14756366.2022.2101644 |
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