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The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes

Cardiovascular diseases are the leading cause of mortality worldwide. In recent years, the relationship between carbonic anhydrase inhibitors and atherosclerosis has attracted attention. In this study, we aimed to determine the in vitro effects of 35 frequently used cardiac drugs on human carbonic a...

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Autores principales: Argan, Onur, Çıkrıkçı, Kübra, Baltacı, Aybike, Gencer, Nahit
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7717712/
https://www.ncbi.nlm.nih.gov/pubmed/32567385
http://dx.doi.org/10.1080/14756366.2020.1781844
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author Argan, Onur
Çıkrıkçı, Kübra
Baltacı, Aybike
Gencer, Nahit
author_facet Argan, Onur
Çıkrıkçı, Kübra
Baltacı, Aybike
Gencer, Nahit
author_sort Argan, Onur
collection PubMed
description Cardiovascular diseases are the leading cause of mortality worldwide. In recent years, the relationship between carbonic anhydrase inhibitors and atherosclerosis has attracted attention. In this study, we aimed to determine the in vitro effects of 35 frequently used cardiac drugs on human carbonic anhydrase I (hCA I) and II (hCA II). The inhibitory effects of the drugs on hCA I and hCA II were determined with both the hydratase and esterase methods. The most potent inhibitors observed were propafenone (hCA I: 2.8 µM and hCA II: 3.02 µM) and captopril (hCA I: 1.58 µM and hCA II: 6.25 µM). Isosorbide mononitrate, propranolol, furosemide, and atorvastatin were also potent inhibitors. The inhibitor constant, K(i), value from the Lineweaver–Burk plot for propafenone was 2.38 µM for hCA I and 2.97 µM for hCA II. The tested cardiac drugs showed potent in vitro inhibition of the hCA I and II isozymes. Especially, in patients with atherosclerotic heart disease, these drugs may be preferred primarily due to the beneficial effects of carbonic anhydrase inhibition on atherosclerosis.
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spelling pubmed-77177122020-12-10 The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes Argan, Onur Çıkrıkçı, Kübra Baltacı, Aybike Gencer, Nahit J Enzyme Inhib Med Chem Research Paper Cardiovascular diseases are the leading cause of mortality worldwide. In recent years, the relationship between carbonic anhydrase inhibitors and atherosclerosis has attracted attention. In this study, we aimed to determine the in vitro effects of 35 frequently used cardiac drugs on human carbonic anhydrase I (hCA I) and II (hCA II). The inhibitory effects of the drugs on hCA I and hCA II were determined with both the hydratase and esterase methods. The most potent inhibitors observed were propafenone (hCA I: 2.8 µM and hCA II: 3.02 µM) and captopril (hCA I: 1.58 µM and hCA II: 6.25 µM). Isosorbide mononitrate, propranolol, furosemide, and atorvastatin were also potent inhibitors. The inhibitor constant, K(i), value from the Lineweaver–Burk plot for propafenone was 2.38 µM for hCA I and 2.97 µM for hCA II. The tested cardiac drugs showed potent in vitro inhibition of the hCA I and II isozymes. Especially, in patients with atherosclerotic heart disease, these drugs may be preferred primarily due to the beneficial effects of carbonic anhydrase inhibition on atherosclerosis. Taylor & Francis 2020-06-22 /pmc/articles/PMC7717712/ /pubmed/32567385 http://dx.doi.org/10.1080/14756366.2020.1781844 Text en © 2020 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Paper
Argan, Onur
Çıkrıkçı, Kübra
Baltacı, Aybike
Gencer, Nahit
The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes
title The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes
title_full The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes
title_fullStr The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes
title_full_unstemmed The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes
title_short The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes
title_sort effects of cardiac drugs on human erythrocyte carbonic anhydrase i and ii isozymes
topic Research Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7717712/
https://www.ncbi.nlm.nih.gov/pubmed/32567385
http://dx.doi.org/10.1080/14756366.2020.1781844
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