Tetranychus urticae, a highly destructive global pest, infests a wide range of plant species, including crucial food crops and ornamental plants. Effective control methods for this pest remain limited. Chitin synthase (CHS) is a key enzyme in the biosynthesis of chitin, which is essential for the growth and development of arthropods. However, the lack of detailed research on arthropod CHS proteins has hindered the development of targeted pesticides. In this study, we successfully expressed and purified the full-length TuCHS protein, which exhibited significant enzymatic activity in vitro. Utilizing this protein, we developed a reliable screening method to identify inhibitors targeting TuCHS. Two inhibitors, ZHZ-ZI-11 and SUY-SC-15, were identified. These compounds interfere with chitin translocation within the cell rather than inhibiting CHS enzyme activity. Both inhibitors demonstrated significant acaricidal efficacy, with improved performance when formulated as nanoemulsions. This study presents the first use of arthropod CHS protein for screening potential insecticides targeting chitin biosynthesis during mite development. Our findings provide a solid foundation for the development of novel, environmentally friendly pesticides aimed at CHS.

中文翻译：

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几丁质合酶抑制剂的发现和表征具有控制荨麻疹的新机制


荨麻疹 （Tetranychus urticae） 是一种极具破坏性的全球性害虫，侵染多种植物物种，包括重要的粮食作物和观赏植物。针对这种害虫的有效控制方法仍然有限。几丁质合酶 （CHS） 是几丁质生物合成的关键酶，对节肢动物的生长发育至关重要。然而，缺乏对节肢动物 CHS 蛋白的详细研究阻碍了靶向杀虫剂的开发。在这项研究中，我们成功表达和纯化了全长 TuCHS 蛋白，该蛋白在体外表现出显着的酶活性。利用这种蛋白质，我们开发了一种可靠的筛选方法来鉴定靶向 TuCHS 的抑制剂。确定了 ZHZ-ZI-11 和 SUY-SC-15 两种抑制剂。这些化合物会干扰细胞内的几丁质易位，而不是抑制 CHS 酶活性。两种抑制剂都表现出显著的杀螨功效，当配制成纳米乳剂时性能得到改善。本研究首次使用节肢动物 CHS 蛋白在螨虫发育过程中筛选针对甲壳素生物合成的潜在杀虫剂。我们的研究结果为开发针对 CHS 的新型环保农药奠定了坚实的基础。