昆虫乙酰胆碱受体β亚基氨基酸环D、E、F环在新烟碱类杀虫剂选择性中的作用
Roles of D, E and F of insect nicotinic acetylcholine receptor β subunit on the neonicotinoid selectivity
在脊椎动物和无脊椎动物的神经系统中，乙酰胆碱受体(nAChRs)是对神经递质乙酰胆碱起快速反应的一种神经递质门控离子通道。为了研究新烟碱类杀虫剂的选择性机制，在杂合表达受体中（褐飞虱Nlα1和小鼠β2亚基），将昆虫特异氨基酸环D、E、F分别引入到小鼠β2亚基的相应位置，构建β2亚基嵌合体，并与Nlα1共表达。与野生型N1α1-β2相比，引入昆虫特异氨基酸环D、E、F到小鼠β2亚基构建嵌合体，均导致乙酰胆碱受体N1α1-β2嵌合体对吡虫啉的敏感性上升，反映在EC50值的减小。同时，对乙酰胆碱的影响很小。研究结果表明，昆虫特异氨基酸环D、E、F在新烟碱类杀虫剂的选择性中起重要作用，研究结果对阐明新烟碱类杀虫剂选择性和高选择性杀虫剂开发具有重要意义。
Nicotinic acetylcholine (ACh) receptors (nAChRs) are ligand-gated ion channels which mediate fast cholinergic synaptic transmission in insect and vertebrate nervous systems. To investigate the mechanism of neonicotinoid selectivity, we have examined the effects of altering insect-specific loops D, E and F in hybrid nAChRs containing insect and mammalian subunits (Nlα1 from the brown planthopper Nilaparvata lugens and β2 from rat). Introduction of the insect-specific loops D, E or F into rat β2 subunit resulted in a leftward shift of the imidacloprid dose-response curves for nAChRs Nlα1-β2 chimeras, reflecting decreases in EC50, compared to wildtype nAChRs Nlα1-β2. By contrast, the influences on ACh potency were minimal or negligible. These results indicated the insect-specific loops D, E and F each played important roles in neonicotinoids selectivity. This study contributes to our understanding of the molecular mechanism underlying selectivity of neonicotinoids against insects over vertebrates.
刘泽文、姚香梅、张懿熙
昆虫学生物科学研究方法、生物科学研究技术分子生物学
农业昆虫与害虫防治烟碱型乙酰胆碱受体β1亚基新烟碱类杀虫剂选择性
agricultural insect and pest controlnicotinic acetylcholine receptorβ1 subunitneonicotinoids selectivity
刘泽文,姚香梅,张懿熙.昆虫乙酰胆碱受体β亚基氨基酸环D、E、F环在新烟碱类杀虫剂选择性中的作用[EB/OL].(2012-02-15)[2025-08-20].http://www.paper.edu.cn/releasepaper/content/201202-434.点此复制
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