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水牛脑胱抑素与多奈哌齐(一种治疗阿尔茨海默病的药物)相互作用的研究

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

作者信息

Amin Fakhra, Bano Bilqees

机构信息

Department of Biochemistry, Faculty of Life Sciences, Aligarh Muslim University, Aligarh 202002, Utar Pradesh, India.

出版信息

Int J Alzheimers Dis. 2013;2013:842689. doi: 10.1155/2013/842689. Epub 2013 Aug 25.

Abstract

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.

摘要

当药物与蛋白质结合时,分子内结构可能会发生改变,从而导致蛋白质的构象变化。多奈哌齐是一种乙酰胆碱酯酶抑制剂(AChE),常用于治疗阿尔茨海默病(AD)患者,以增强胆碱能神经传递。它是治疗阿尔茨海默病用于改善该疾病认知功能的“一线”药物。在本研究中,通过碱性处理、40%至60%硫酸铵分级分离以及在Sephadex G - 75上进行凝胶过滤色谱,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。纯化后的抑制剂(水牛脑胱抑素,(BBC))以单个木瓜蛋白酶抑制峰洗脱,在天然聚丙烯酰胺凝胶电泳(PAGE)上迁移为单一条带;然而,在有和没有β - 巯基乙醇(βME)的十二烷基硫酸钠 - 聚丙烯酰胺凝胶电泳(SDS - PAGE)上,BBC分别给出了分子量为31.6和12.4 kDa的两条带。通过凝胶过滤测定的分子量为43.6 kDa。胱抑素与多奈哌齐相互作用的紫外光谱表明该蛋白质发生了构象变化。BC - 多奈哌齐复合物的荧光光谱显示结构变化,表明在多奈哌齐存在下,胱抑素的荧光强度显著增加,出现40 nm红移,这代表胱抑素在相互作用时发生了展开,这是使用该药物期间多奈哌齐产生副作用的一个迹象。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4471/3767058/27e23af54114/IJAD2013-842689.001.jpg

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