Chitin-degrading enzymes are critical components in regulating the molting process of the Asian corn borer and serve as potential targets for controlling this destructive pest of maize. Here, we used a scaffold-hopping strategy to design a series of efficient naphthylimide insecticides. Among them, compound 8c exhibited potent inhibition of chitinase from OfChi-h and OfChtI at low nanomolar concentrations (IC₅₀ = 1.51 and 9.21 nM, respectively). Molecular docking simulations suggested that 8c binds to chitinase by mimicking the interaction of chitin oligosaccharide substrates with chitinase. At low ppm concentrations, compound 8c performed comparably to commercial insecticides in controlling the highly destructive plant pest, the Asian corn borer. Tests on a wide range of nontarget organisms indicate that compound 8c has very low toxicity. In addition, the effect of inhibitor treatment on the expression of genes associated with the Asian corn borer chitin-degrading enzymes was further investigated by quantitative real-time polymerase chain reaction. In conclusion, our study highlights the potential of 8c as a novel chitinase-targeting insecticide for effective control of the Asian corn borer, providing a promising solution in the quest for sustainable pest management.

中文翻译：

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通过生物等排体取代和支架跳跃设计针对几丁质降解酶的抑制剂，用于选择性控制亚洲玉米螟

几丁质降解酶是调节亚洲玉米螟蜕皮过程的关键成分，也是控制这种破坏性玉米害虫的潜在目标。在这里，我们采用支架跳跃策略设计了一系列高效的萘酰亚胺杀虫剂。其中，化合物8c在低纳摩尔浓度下表现出对Of Chi-h和Of ChtI的几丁质酶的有效抑制作用（IC ₅₀分别为1.51和9.21 nM）。分子对接模拟表明，8c通过模拟几丁质寡糖底物与几丁质酶的相互作用来与几丁质酶结合。在低 ppm 浓度下，化合物8c在控制极具破坏性的植物害虫亚洲玉米螟方面的效果与商业杀虫剂相当。对多种非目标生物体的测试表明，化合物8c的毒性非常低。此外，通过定量实时聚合酶链反应进一步研究了抑制剂处理对亚洲玉米螟几丁质降解酶相关基因表达的影响。总之，我们的研究强调了8c作为一种新型几丁质酶靶向杀虫剂在有效控制亚洲玉米螟方面的潜力，为寻求可持续害虫管理提供了一个有前途的解决方案。