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

• Published in: Journal of enzyme inhibition and medicinal chemistry Vol. 35; no. 1; pp. 1359 - 1362
• Main Authors: Argan, Onur, Çıkrıkçı, Kübra, Baltacı, Aybike, Gencer, Nahit
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 01-01-2020; Taylor & Francis Ltd; Taylor & Francis Group
• Subjects: Acetazolamide - pharmacology; Arteriosclerosis; Atherosclerosis; Atorvastatin; carbonic anhydrase; Carbonic anhydrase I; Carbonic Anhydrase I - antagonists & inhibitors; Carbonic anhydrase II; Carbonic Anhydrase II - antagonists & inhibitors; Carbonic Anhydrase Inhibitors - pharmacology; Cardiac drugs; Cardiovascular diseases; Chromatography, Affinity - methods; Coronary artery disease; Drugs; enzyme inhibition; Erythrocytes - enzymology; Esterase; Furosemide; Heart diseases; Humans; Isoenzymes; Propranolol; Research Paper; enzyme inhibition; carbonic anhydrase; Cardiac drugs
• ISSN: 1475-6366; 1475-6374
• DOI: 10.1080/14756366.2020.1781844

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.