The mode of action of insecticidal acylurea compounds in the red flour beetle Tribolium castaneum

酰脲类化合物是选择性抑制几丁质合成的高效杀虫剂。抑制效力主要来源于几丁质形成缺陷及其异常表皮内沉积和蜕皮失败的后果。今天，酰基脲在害虫综合治理中发挥着重要作用。虽然已经确定酰脲类药物会干扰几丁质合成，但确切的作用机制尚不清楚。几个系列的实验表明，酰脲化合物不直接抑制催化，如无细胞几丁质合成昆虫系统中所示。酰基脲类药物不是直接抑制几丁质合成酶，而是可能改变囊泡运输或融合，阻断几丁质合成酶的底物供应，抑制几丁质聚合物跨膜易位或通过影响蜕皮甾体产生来干扰几丁质合成的激素调节。我们以前的研究表明，储藏物害虫赤拟谷盗（赤面甲虫）是一个很好的模式生物研究的生物活性物质，如酰脲和其他杀虫剂的作用方式。我们提出了一个全面的研究，利用基因组学，蛋白质组学，生物化学和免疫学的方法来澄清杀虫酰脲化合物的作用模式。

Acylurea compounds are highly potent insecticides that selectively inhibit chitin synthesis. Insecticide potency derives mainly from defects in chitin formation and its consequences of an abnormal endocuticular deposition and abortive molting. Today, acylureas play an important role in integrated pest management. Although it is well established that acylureas interfere in chitin synthesis, the precise mechanism of action is unknown. Several lines of experiments argue that acylurea compounds do not directly inhibit catalysis as evinced in cell-free chitin synthesizing insect systems. Rather than inhibiting the chitin synthase directly, acylureas may alter either vesicle transport or fusion, block the substrate supply for the chitin synthase, inhibit translocation of chitin polymers across the membrane or interfere in the hormonal regulation of chitin synthesis by influencing ecdysteroid production. Our previous studies revealed that the stored product pest Tribolium castaneum (red flour beetle) is a good model organism for investigating the mode of action of bioactive materials such as acylurea and other insecticides. We propose a comprehensive study utilizing genomic, proteomics, biochemical and immunological approaches to clarify the mode of action of insecticidal acylurea compounds.