期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 31, 期 1, 页码 152-157出版社
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756366.2015.1014476
关键词
Acetylcholine esterase; affinity chromatography carbonic anhydrase; enzyme inhibition; enzyme purification; trimethoxyindane derivatives
资金
- Deanship of Research Chairs Program at King Saud University [RGP-VPP-254]
Carbonic anhydrases (CAs, EC 4.2.1.1) had six genetically distinct families described to date in various organisms. There are 16 known CA isoforms in humans. Human CA isoenzymes I and II (hCA I and hCA II) are ubiquitous cytosolic isoforms. Acetylcholine esterase (AChE. EC 3.1.1.7) is a hydrolase that hydrolyzes the neurotransmitter acetylcholine relaying the signal from the nerve. In this study, some trimethoxyindane derivatives were investigated as inhibitors against the cytosolic hCA I and II isoenzymes, and AChE enzyme. Both hCA isozymes were inhibited by trimethoxyindane derivatives in the low nanomolar range. These compounds were good hCA I inhibitors (Kis in the range of 1.66-4.14nM) and hCA II inhibitors (Kis of 1.37-3.12nM) and perfect AChE inhibitors (Kis in the range of 1.87-7.53nM) compared to acetazolamide as CA inhibitor (Ki: 6.76nM for hCA I and Ki: 5.85nM for hCA II) and Tacrine as AChE inhibitor (Ki: 7.64nM).
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