| 氟啶虫酰胺作用靶标—内向整流钾离子通道研究进展 |
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投稿时间：2019-01-06
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| 引用本文：苏建亚.氟啶虫酰胺作用靶标—内向整流钾离子通道研究进展[J].农药学学报,2019,21(2):131-139. |
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| 基金项目:国家重点研发计划（2017YFD0200505） |
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| 中文摘要:氟啶虫酰胺是一种高选择性杀虫剂，主要用于防治刺吸式口器害虫。有关该杀虫剂的分子靶标长期未知。近年来随着研究的逐渐深入，相关作用靶标已逐步得到明确。早期研究表明，氟啶虫酰胺通过抑制剌吸式口器害虫的取食，造成害虫因饥饿而死亡；最新研究发现，其作用靶标是内向整流钾离子（Kir）通道，纳摩尔浓度级的氟啶虫酰胺即可阻断褐飞虱的Kir通道。氟啶虫酰胺通过抑制昆虫Kir通道，干扰昆虫细胞的离子稳态与平衡电位，尤其是破坏马氏管与唾液腺的正常分泌功能，从而影响昆虫的取食与排泄过程，最终导致害虫死亡。文章对氟啶虫酰胺的作用靶标、作用机制及应用等方面的研究进展进行了综述，总结分析了昆虫Kir通道的结构及其所参与的生理功能，分析了氟啶虫酰胺通过抑制该离子通道致使害虫死亡的具体作用机制，并介绍了针对靶向Kir通道药物的高通量筛选方法与研究进展，可为杀虫剂新靶标挖掘与靶向此类新靶标药剂的创制提供研究思路。 |
| 中文关键词:氟啶虫酰胺 分子靶标 内向整流钾离子通道 作用机制 高通量筛选 |
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| Molecular target of flonicamid: inward-rectifying potassium channels |
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| Abstract:Flonicamid is a selective insecticide, mainly registered to control sap-sucking insect pests. However, the mode of action for this insecticide is undefined for years. Recently, the molecular target of flonicamid was disclosed. The previous researches demonstrated that flonicamid caused the mortality of sap-sucking insects by inhibiting the feeding behavior of hemipteran pests. A recent study reported that the molecular target of flonicanmid was inward-rectifying potassium channels (Kir). Flonicamid in nanomole concentration inhibited the Kir channel of rice brown planthopper (Nilaparvata lugens) and disturbed the K+ homeostasis and the equilibrium potential across cell membrane, which then disrupted the physiological functions of salivary gland and Malpighian tubules, and finally lead to lethality of insect pests. In this review, the structure and physiological function of Kir channels in insects are summarized, and the mechanism for the mode of action of flonicamid by inhibiting the Kir channels is discussed. Finally, the research progress in high throughtput screening for novel small moleculars targeting at Kir channels of insects with thallium fluorescent probe is introduced, which will highlight the way to discover new insecticidal targets and to create the novel compounds with insecticidal activities. |
| Key words:flonicamid molecular target inward-rectifying potassium channel mode of action high throughput screening |
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