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基于杀螨剂靶标朱砂叶螨乙酰胆碱酯酶体外表达的新型杀螨活性化合物筛选

Screening new acaricidal compound based on In vitro expression of acaricidal target acetylcholinesterase of Tetranychus cinnabarinus
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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. 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.
作者 彭博 卜春亚 师光禄 李金玲 冯晓姣 韩晶玉 PENG Bo, BU Chunya , SHI Guanglu, LI Jinling, FENG Xiaojiao, HAN Jingyu(1. Plant Science and Technology College, Beijing University of Agriculture, Beijing 102206, China ;2College of Biologtcal Science and Engineering, Beijing University of Agriculture, Beijing 102206, China ;3.Key Laboratory of Urban Agriculture (North) of'Ministry of Agriculture P. R. China, Beijing University of Agriculture, Beijing 102206, China)
出处 《应用与环境生物学报》 CAS CSCD 北大核心 2016年第1期110-115,共6页 Chinese Journal of Applied and Environmental Biology
基金 国家自然科学基金项目(31200483) 教育部科学技术重点研究项目(212001) 北京市自然科学基金项目(6122005) 北京市教育委员会科技计划面上项目(KM201210020001)和北京市教育委员会平台项目(KCT2014001 KCT2015007)资助
关键词 朱砂叶螨 乙酰胆碱酯酶 酶动力学 AChE抑制剂 Tetranychus cinnabarinus acetylcholinesterase(AChE) enzyme kinetics AChE inhibitors
作者简介 通讯作者Corresponding author(E—mail:buchunya@163.com)
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