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[苯并咪唑衍生物在不同底物存在下对动物胆碱酯酶的抑制作用]

[Inhibitory effect of benzimidazole derivatives on cholinesterases of animals in the presence of different substrates].

作者信息

Basova N E, Kormilitsyn B N, Perchenok A Iu, Rosengart E V, Saakov V S, Suvorov A A

出版信息

Ukr Biochem J. 2014 Sep-Oct;86(5):47-55.

Abstract

Specifically synthesized group of benzimidazole derivatives possessing varying degrees of delocalization of the positive charge in the cation group of the molecule has been studied in order to search for potential cholinergically active compounds and to study the role of the Coulomb interaction in cholinesterase catalysis. These compounds were reversible inhibitors of cholinesterase (ChE) of human erythrocytes, horse serum, brain of the frog Rana temporaria and visual ganglia of the Pacific squid Todarodes pacificus in the presence of acetylthiocholine iodide and propionylthiocholine iodide as substrates. The differences in the nature of reversible inhibitory effect were observed. The effect of the inhibitor structure and substrate nature, specific for each of the studied inhibitors, on the character of the process of reversible inhibition was found.

摘要

为了寻找潜在的胆碱能活性化合物并研究库仑相互作用在胆碱酯酶催化中的作用,对特定合成的一组苯并咪唑衍生物进行了研究,这些衍生物在分子的阳离子基团中具有不同程度的正电荷离域。在以碘化乙酰硫代胆碱和碘化丙酰硫代胆碱为底物的情况下,这些化合物是人类红细胞、马血清、青蛙(泽蛙)脑和太平洋鱿鱼(太平洋褶柔鱼)视觉神经节中胆碱酯酶(ChE)的可逆抑制剂。观察到可逆抑制作用性质的差异。发现了每种研究抑制剂特有的抑制剂结构和底物性质对可逆抑制过程特征的影响。

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