当前位置: X-MOL 学术J. Enzyme Inhib. Med. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
The effects of cardiac drugs on human erythrocyte carbonic anhydrase I and II isozymes.
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2020-06-22 , DOI: 10.1080/14756366.2020.1781844
Onur Argan 1 , Kübra Çıkrıkçı 2 , Aybike Baltacı 2 , Nahit Gencer 2
Affiliation  

Abstract

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, Ki, 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.



中文翻译:

心脏药物对人红细胞碳酸酐酶I和II同工酶的影响。

摘要

心血管疾病是全球死亡的主要原因。近年来,碳酸酐酶抑制剂与动脉粥样硬化之间的关系已引起关注。在这项研究中,我们旨在确定35种常用的心脏药物对人碳酸酐酶I(hCA I)和II(hCA II)的体外作用。用水合酶法和酯酶法测定了药物对hCA I和hCA II的抑制作用。观察到的最有效的抑制剂是普罗帕酮(hCA I:2.8 µM和hCA II:3.02 µM)和卡托普利(hCA I:1.58 µM和hCA II:6.25 µM)。单硝酸异山梨酯,普萘洛尔,速尿和阿托伐他汀也是有效的抑制剂。抑制剂常数K i根据Lineweaver-Burk图,普罗帕酮的hCA I值为2.38 µM,hCA II为2.97 µM。测试的心脏药物显示出对hCA I和II同功酶的有效体外抑制作用。特别地,在患有动脉粥样硬化性心脏病的患者中,这些药物可能是优选的,这主要是由于抑制碳酸酐酶对动脉粥样硬化的有益作用。

更新日期:2020-06-22
down
wechat
bug