Establishment of a New Model for in Vitro Screening of Acetylcholinesterase Inhibitors Based on Immobilized Enzyme

CORC > 厦门大学 > 化学化工－已发表论文

	Establishment of a New Model for in Vitro Screening of Acetylcholinesterase Inhibitors Based on Immobilized Enzyme
	Chen Chen ; Shi Qian ; Chen Jun-Hui ; Zhang Ru-Tan ; Li Xin ; Zheng Li ; Wang Xiao-Ru ; Wang XR(王小如)
刊名	http://dx.doi.org/10.7503/cjcu20120772
	2013
关键词	ELECTROSPRAY MASS-SPECTROMETRY PESTICIDES REACTOR ORGANOPHOSPHATE CHOLINESTERASE MICROSPHERES
英文摘要	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 mu L, 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.
语种	英语
出版者	HIGHER EDUCATION PRESS
内容类型	期刊论文
源URL	[http://dspace.xmu.edu.cn/handle/2288/89036]
专题	化学化工－已发表论文
推荐引用方式 GB/T 7714	Chen Chen,Shi Qian,Chen Jun-Hui,et al. Establishment of a New Model for in Vitro Screening of Acetylcholinesterase Inhibitors Based on Immobilized Enzyme[J]. http://dx.doi.org/10.7503/cjcu20120772,2013.
APA	Chen Chen.,Shi Qian.,Chen Jun-Hui.,Zhang Ru-Tan.,Li Xin.,...&王小如.(2013).Establishment of a New Model for in Vitro Screening of Acetylcholinesterase Inhibitors Based on Immobilized Enzyme.http://dx.doi.org/10.7503/cjcu20120772.
MLA	Chen Chen,et al."Establishment of a New Model for in Vitro Screening of Acetylcholinesterase Inhibitors Based on Immobilized Enzyme".http://dx.doi.org/10.7503/cjcu20120772 (2013).