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研究几种苯并咪唑类药物对乙酰胆碱酯酶和丁酰胆碱酯酶的毒性和抑制作用。

Investigation of the toxicological and inhibitory effects of some benzimidazole agents on acetylcholinesterase and butyrylcholinesterase enzymes.

机构信息

Health Services Vocational School, Igdır University, Igdır, Turkey.

出版信息

Arch Physiol Biochem. 2021 Apr;127(2):97-101. doi: 10.1080/13813455.2019.1618341. Epub 2019 May 28.

Abstract

Benzimidazole, an anthelmintic used in the manufacture of human and veterinary drugs, is an important heterocyclic compound. In this work, I investigated the effect of drugs such as ricobendazole, thiabendazole, albendazole, and oxfendazole, on Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE) enzyme activity. As kinetic studies, K and IC values were calculated separately for each drug, respectively. Study findings have shown that benzimidazoles inhibit both AChE and BChE enzymes at the nanomolar level. The compound that best was inhibited the AChE enzyme ricobendazole, and it was that the best inhibited the BChE enzyme thiabendazole. IC and K values were calculated 123.02 nM, 28.68 ± 8.46 nM for AChE and 64.26 nM, 12.08 ± 2.18 nM for BChE respectively. The types of inhibition indicated by the drugs were investigated and they were found to show non-competitive inhibition.

摘要

苯并咪唑是一种用于制造人类和兽医药物的驱虫药,是一种重要的杂环化合物。在这项工作中,我研究了苯并咪唑类药物如瑞苯达唑、噻苯达唑、阿苯达唑和奥芬达唑对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)酶活性的影响。作为动力学研究,分别为每种药物单独计算了 K 和 IC 值。研究结果表明,苯并咪唑类化合物在纳摩尔水平上抑制 AChE 和 BChE 两种酶。抑制 AChE 酶效果最好的化合物是瑞苯达唑,而抑制 BChE 酶效果最好的化合物是噻苯达唑。IC 和 K 值分别计算为 123.02 nM 和 28.68 ± 8.46 nM。BChE 的 IC 和 K 值分别为 64.26 nM 和 12.08 ± 2.18 nM。研究了药物的抑制类型,发现它们表现为非竞争性抑制。

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