Cu(Ⅱ)离子诱导的β-淀粉样蛋白聚集抑制剂筛选及分子构效关系分析

doi:10.11944/j.issn.1000-0518.2016.07.150375

摘要/Abstract

摘要：

阿尔茨海默症药物的开发对该疾病的治疗非常重要。利用纳米金为探针研究了13种化合物抑制Cu²⁺诱导的β-淀粉样蛋白聚集的能力,筛选出了10种有效的抑制剂,并获得了抑制剂抑制能力与其分子结构间的关系,利用筛选出的抑制剂实现了β淀粉样蛋白聚集过程的抑制和H₂O₂产生量的减少,对阿尔茨海默症的研究具有重要意义。

关键词: 阿尔茨海默症, 纳米金, 抑制剂

Abstract:

It is very important to develop efficient drugs for the cure of Alzheimer's disease. Here, gold nanoparticle probes were utilized to acquire the ability of 13 kinds of compounds to inhibit the Cu²⁺ induced β-amyloid peptide aggregation. Ten of then were screened as the effective inhibitors. The relationships between the chemical structures and their inhibitory efficiencies were also studied as well. We also used the screened molecules to regulate the morphology changes of Cu²⁺-β-amyloid aggregates and to decrease the production of H₂O₂ formed by the interaction of Cu²⁺ and β-amyloid peptide. This research is significant to the study of Alzheimer's disease.

Key words: Alzheimer's disease, gold nanoparticles, inhibitor

王承克, 王振新. Cu(Ⅱ)离子诱导的β-淀粉样蛋白聚集抑制剂筛选及分子构效关系分析[J]. 应用化学, 2016, 33(7): 834-840.

WANG Chengke, WANG Zhenxin. Screening of Cu(Ⅱ) Ion Induced β-Amyloid Peptide Aggregation Inhibitor and Their Molecular Structure Analysis[J]. Chinese Journal of Applied Chemistry, 2016, 33(7): 834-840.

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