光致异构杀虫剂的创制及其对靶酶和昆虫的实时调控

The frequent application of insecticides causes side effects to nontarget organism and environmental contamination. Normally, the activity of a conventional insecticide cannot be controlled intentionally once administrated, making it difficult to elucidate the timing and location of its activity and to study the mechanism of insecticide-target or insecticide-inset interactions. This uncontrollable property leads to many undesirable secondary effects after application, such as occurrence of resistance and food and environmental contamination. Base on photopharmacology, this project is planning to introduce the photoisomerizable subunit into the insecticidal molecule, with a view to realize the spatiotemporal regulation on the insecticide performance by light. By studying the differences of physiochemical properties, activity, toxicity, stability and modes of action upon irradiation, we wish to develop novel functional insecticides, explore the rule of insecticide-insects interactions, the optical control over the insect behavior and the factors influencing the activity in order to provide guiders to insecticide development.

杀虫剂的过度频繁使用危害非靶标生物及生态环境，传统杀虫剂施用后，其性能不可主观调控，这为研究杀虫剂-靶标、杀虫剂-昆虫相互作用的生物学机制带来一定难度，同时也导致杀虫剂不可控的毒性、环境生态危害等系列负面效应。本项目基于光药理学，将光致异构基团引入到杀虫剂分子中，实现对杀虫剂分子及其生物效应的时空调控。研究杀虫剂在光控下的物化性质、生物活性、有益生物毒性、光热稳定性、作用机制等的差异。探寻杀虫剂-昆虫作用规律及其活性的关键调控机制和技术途径，研究其对作用靶酶和昆虫活体行为的实时调控，为杀虫剂创新及害虫绿色防控提供理论指导。

本项目将光药理学与农药研究相结合，开发了系列活性可控的农药分子。本项目共设计合成了10个系列约100多个化合物，共发表SCI论文11篇，其中一区论文8篇，申请专利9项，应邀撰写书籍1章；发现具有商品化价值的高活性杀菌剂1个；培养硕士生8名，博士生3名；发现了nAChR高通量筛选技术1项，为探索农药活性影响机制、农药-靶标互作机制和农药的精准释放提供了新的方法。