三甲氧基茚满衍生物对人碳酸酐酶同工酶I和II（hCA I和II）的抑制作用。
The human carbonic anhydrase isoenzymes I and II (hCA I and II) inhibition effects of trimethoxyindane derivatives.
作者信息
Taslimi Parham, Gulcin Ilhami, Ozgeris Bunyamin, Goksu Suleyman, Tumer Ferhan, Alwasel Saleh H, Supuran Claudiu T
机构信息
a Department of Chemistry, Faculty of Sciences , Atatürk University , Erzurum , Turkey .
b Department of Zoology, College of Science , King Saud University , Riyadh , Saudi Arabia .
出版信息
J Enzyme Inhib Med Chem. 2016;31(1):152-7. doi: 10.3109/14756366.2015.1014476. Epub 2015 Feb 20.
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 1.66-4.14 nM) and hCA II inhibitors (Kis of 1.37-3.12 nM) and perfect AChE inhibitors (Kis in the range of 1.87-7.53 nM) compared to acetazolamide as CA inhibitor (Ki: 6.76 nM for hCA I and Ki: 5.85 nM for hCA II) and Tacrine as AChE inhibitor (Ki: 7.64 nM).
碳酸酐酶（CAs，EC 4.2.1.1）在各种生物体中迄今已被描述有六个基因上不同的家族。人类中有16种已知的CA同工型。人类CA同工酶I和II（hCA I和hCA II）是普遍存在的胞质同工型。乙酰胆碱酯酶（AChE，EC 3.1.1.7）是一种水解酶，可水解传递神经信号的神经递质乙酰胆碱。在本研究中，研究了一些三甲氧基茚满衍生物作为针对胞质hCA I和II同工酶以及AChE酶的抑制剂。两种hCA同工酶均被三甲氧基茚满衍生物在低纳摩尔范围内抑制。与作为CA抑制剂的乙酰唑胺（hCA I的Ki：6.76 nM，hCA II的Ki：5.85 nM）和作为AChE抑制剂的他克林（Ki：7.64 nM）相比，这些化合物是良好的hCA I抑制剂（Ki在1.66 - 4.14 nM范围内）和hCA II抑制剂（Ki为1.37 - 3.12 nM）以及完美的AChE抑制剂（Ki在1.87 - 7.53 nM范围内）。
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