多杀菌素类杀虫剂的环境降解及抗性机制研究进展

Research progresses on environmental degradation and resistance mechanism of spinosyn insecticides

多杀菌素类杀虫剂具有高效低毒、杀虫谱广及环境友好等优点,在害虫综合防治中具有很好的应用前景。近年的研究明确了多杀菌素和乙基多杀菌素的环境/农作物的降解代谢物及降解动力学,重点阐明了多杀菌素和乙基多杀菌素的代谢及靶标抗性机制,对多杀菌素类杀虫剂的合理使用和抗性治理提供了科学依据。同时,在杀虫活性更好、防治谱更广的乙基多杀菌素的开发过程中,计算建模、生物路径调控及化学合成等技术的综合应用发挥了巨大作用,为进行天然产物结构改造、开发新型杀虫剂提供了重要参考。本文论述了多杀菌素和乙基多杀菌素的结构特点及环境降解特性,综述了多杀菌素和乙基多杀菌素抗性机制的研究进展。

Spinosyn insecticides with advantages of high efficacy, low toxicity, broad spectrum and environmentally benign, are promising insecticides for the integrated pest management of pest insects.In recent years, the environmental degradation fate of spinosad and spinetoram including major metabolites and the degradation dynamics in soil, water and crops were reported. Moreover, the resistance mechanisms of insects to spinosad and spinetoram, especially metabolic resistance and targetmutation related resistance, were elucidated. These information is useful for rational application and resistance management of spinosad and spinetoram. Furthermore, technologies such as computational model-based quantitative structure-activity relationship（QSAR） analysis, the regulation of biosynthesis pathways and the organic synthesis played key roles in the discovery of spinetoram with much higher efficacy and broader insecticidal spectrum by modifying the structures of insecticidal natural products.In the review, the chemical structure characteristics and the research progresses on the environmental degradation of spinosad and spinetoram were summarized. Additionally, the achievements in the studies of resistance mechanisms to spinosad and spinetoram were also reviewed.