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	基于固定化酶的乙酰胆碱酯酶抑制剂体外筛选模型的建立; Establishment of a New Model for in Vitro Screening of Acetylcholinesterase Inhibitors Based on Immobilized Enzyme
	陈晨 ; 史倩 ; 陈军辉 ; 张茹潭 ; 李鑫 ; 郑立 ; 王小如
	2013-05-10
关键词	固定化酶 乙酰胆碱酯酶抑制剂 靶酶抑制剂筛选 Immobilized enzyme Acetylcholinesterase inhibitor Target enzyme inhibitor screening
英文摘要	以可重复使用的固定化酶代替游离态酶,建立一种基于比色分析的乙酰胆碱酯酶(ACHE)抑制剂体外筛选新模型.采用以氨基化硅胶为载体固定的ACHE优化了实验条件,用ACHE抑制剂阳性对照物他克林和毒扁豆碱对该模型进行验证,还对模型技术参数进行评价,并将新模型用于单体化合物及天然产物粗提物ACHE抑制活性评价.结果表明,最佳实验条件为:固定化酶用量55μl,底物浓度5 MMOl/l,甲醇、乙醇及体积分数不高于6%的二甲基亚砜水溶液均可作为样品溶剂;模型验证及模型技术参数评价结果良好,该模型对ACHE抑制剂筛选有较好的特异性和灵敏度,可用于筛选ACHE抑制剂.该模型具有适用性强、固定化酶可重复使用及结果可靠等优点,是单体化合物及天然产物粗提物ACHE抑制剂活性评价的有效方法.; An economical model for rapid in vitro screening of acetylcholinesterase(AChE) inhibitors was developed,which used Ellman's reaction-based assay with reusable immobilized AChE.AChE-immobilized aminated silica gel microspheres were applied to develop new screening method.Firstly,the experimental conditions were optimized.And then,the inhibitory activity on immobilized AChE of tacrine and eserine(positive controls) was tested to validate the effectiveness of the new model.Multiple technical parameters of this new model were also evaluated.Finally,the inhibitory activity on AChE of monomeric compounds and natural products was evaluated by the proposed new model.The results show that the optimal conditions included the followings: 55 μL of immobilized AChE as the appropriate dose,5 mmol/L acetylthiocholine iodide as substrate,methanol and ethanol as well as dimethyl sulfoxide which was under 6% as sample solvent.The obtained results also demonstrated that this new model was sensitive and specific for rapid screening of AChE inhibitors.Good model validation and multiple parameters evaluation results were obtained.The proposed model has many advantages: good applicability,continuous reuse of the immobilized AChE,with reliable results,etc.This model is a powerful tool for identification of AChE inhibitors from natural products or chemical libraries produced by combinatorial chemistry.; 国家自然科学基金(批准号:20905017); 国家“八六三”计划项目(批准号:2007AA092001-10)资助
语种	zh_CN
内容类型	期刊论文
源URL	[http://dspace.xmu.edu.cn/handle/2288/106821]
专题	化学化工－已发表论文
推荐引用方式 GB/T 7714	陈晨,史倩,陈军辉,等. 基于固定化酶的乙酰胆碱酯酶抑制剂体外筛选模型的建立, Establishment of a New Model for in Vitro Screening of Acetylcholinesterase Inhibitors Based on Immobilized Enzyme[J],2013.
APA	陈晨.,史倩.,陈军辉.,张茹潭.,李鑫.,...&王小如.(2013).基于固定化酶的乙酰胆碱酯酶抑制剂体外筛选模型的建立..
MLA	陈晨,et al."基于固定化酶的乙酰胆碱酯酶抑制剂体外筛选模型的建立".(2013).

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