中文摘要：

乙酰胆碱酯酶（Acetylcholinesterase,AChE）是保证神经信号在生物体内正常传递的关键酶,是有机磷和氨基甲酸酯类农药的作用靶标.本研究在前期朱砂叶螨乙酰胆碱酯酶基因原核表达及最适反应条件摸索的基础上,大规模表达纯化朱砂叶螨AChE,进一步研究其酶学性质.研究结果显示,在温度为25℃、其他条件最适的情况下,测定酶Km值为0.67 mmol/L,K（cat）/Km值为13.53 mmol L^-1） s^-1.随后,从SPECS化学库筛选到了55个候选AChE抑制性化合物,获得了9个抑制活性优于或相当于毒扁豆碱的朱砂叶螨AChE抑制化合物,并且它们对朱砂叶螨有较好的毒性.本研究为乙酰胆碱酯酶抑制剂的筛选以及以乙酰胆碱酯酶为靶标的农药开发提供了理论依据和实验基础.

英文摘要：

Carmine spider mite,Tetranychus cinnabarinus Boisduval（Acari：Tetranychidae） is one of the most important polyphagous pest mites in agriculture throughout the world.Acetylcholinesterase（AChE） plays a key role in maintaining normal nerve impulse transmission in the synaptic gap,and is the target of organic phosphorus and carbamate insecticides.We previously reported the in vitro expression of T.cinnabarinus AChE and its enzyme assay optimization.In this resesarch we studied mass expression and purification of T.cinnabarinus AChE.The enzy me activity of the recombinant mite AChE was measured with a Km value of 0.67 mmol/L and K（cat）/Km of 13.53 mmol L^-1 s^-1.According to the structure of T.cinnabarinus AChE,55 compounds with high affinity with mite AChE were screened from SPECS chemical lead-compound database.Among them 9 compounds were found to have high inhibitory activity against AChE of T.cinnabarinus comparable to that of eserine.The bioassay data indicated that they confer high toxicity to Tetranychus cinnabarinus.This study lays a solid foundation in empirical data and conceptual understanding for screening new AChE inhibitors and development of anticholinesterase pesticides.