水牛脑胱氨酸与阿尔茨海默氏症药物多奈哌齐相互作用的研究。

Q1 Neuroscience
International Journal of Alzheimer's Disease Pub Date : 2013-01-01 Epub Date: 2013-08-25 DOI:10.1155/2013/842689
Fakhra Amin, Bilqees Bano
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引用次数: 0

摘要

当药物与蛋白质结合时,分子内结构会发生改变,从而导致蛋白质构象的改变。多奈哌齐是一种乙酰胆碱酯酶抑制剂(AChE),通常用于治疗阿尔茨海默氏症(AD)患者,以增强胆碱能神经传递。它是治疗阿尔茨海默病的 "一线 "药物,用于改善阿尔茨海默病的认知功能。本研究采用碱处理、40% 至 60% 硫酸铵分馏和 Sephadex G-75 凝胶过滤色谱法从水牛脑中分离出一种半胱氨酸蛋白酶抑制剂(胱抑素),产率为 64.13%,纯化倍数为 384.7。纯化的抑制剂(Buffalo Brain Cystatin, (BBC))被洗脱为单一的木瓜蛋白酶抑制峰,在原生 PAGE 上迁移为单一条带;然而,在添加和不添加 β-巯基乙醇(β ME)的 SDS-PAGE 上,BBC 得到两条 M W 分别为 31.6 和 12.4 KDa 的条带。凝胶过滤测定的分子量为 43.6 KDa。胱抑素与多奈哌齐作用时的紫外光谱表明蛋白质发生了构象变化。胱抑素-多奈哌齐复合体的荧光光谱显示出结构变化,表明在多奈哌齐的存在下,胱抑素的荧光强度显著增加,发生了 40 nm 的红移,表明胱抑素在相互作用时发生了折叠,这表明多奈哌齐在使用该药物期间会产生副作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Studies on interaction of buffalo brain cystatin with donepezil: an Alzheimer's drug.

Studies on interaction of buffalo brain cystatin with donepezil: an Alzheimer's drug.

Studies on interaction of buffalo brain cystatin with donepezil: an Alzheimer's drug.

Studies on interaction of buffalo brain cystatin with donepezil: an Alzheimer's drug.

When drugs bind to a protein, the intramolecular structures can be altered, resulting in conformational change of the protein. Donepezil, an Acetyl Cholinesterase inhibitor (AChE), is commonly prescribed to patients with Alzheimer's disease (AD) to enhance cholinergic neurotransmission. It is the "first-line" agents in the treatment of Alzheimer's disease used to improve cognitive function in the disease. In the present study, a cysteine protease inhibitor (cystatin) has been isolated from buffalo brain using alkaline treatment, 40 to 60% ammonium sulphate fractionation and gel filtration chromatography on Sephadex G-75 with % yield of 64.13 and fold purification of 384.7. The purified inhibitor (Buffalo Brain Cystatin, (BBC)) was eluted as a single papain inhibitory peak which migrated as single band on native PAGE; however, on SDS-PAGE with and without beta mercaptoethanol ( β ME) BBC gave two bands of M W 31.6 and 12.4 KDa, respectively. The molecular weight determined by gel filtration came out to be 43.6 KDa. The UV spectra of cystatin on interaction with donepezil suggested a conformational change in the protein. The fluorescence spectra of BC-donepezil composite show structural changes indicating 40 nm red shift with significant increase in fluorescence intensity of cystatin in the presence of donepezil representing an unfolding of cystatin on interaction, which is an indication of side effect of donepezil during the use of this drug.

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来源期刊
International Journal of Alzheimer's Disease
International Journal of Alzheimer's Disease Neuroscience-Behavioral Neuroscience
CiteScore
10.10
自引率
0.00%
发文量
3
审稿时长
11 weeks
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