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Assessment of species specificity of moulting accelerating compounds in Lepidoptera: comparison of activity between Bombyx mori and Spodoptera littoralis by in vitro reporter and in vivo toxicity assays

机译:鳞翅类蜕皮促进化合物的物种特异性评估:通过体外报告基因和体内毒性试验比较家蚕和斜纹夜蛾的活性

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BACKGROUND: Dibenzoylhydrazine analogues have been developed successfully as a new group of insect growth regulators, called ecdysone agonists or moulting accelerating compounds. A notable feature is their high activity against lepidopteran insects, raising the question as to whether species-specific analogues can be isolated. In this study, the specificity of ecdysone agonists was addressed through a comparative analysis in two important lepidopterans, the silkworm Bombyx mori L. and the cotton leafworm Spodoptera littoralis (Boisd.). RESULTS: When collections of non-steroidal ecdysone agonists containing different mother structures (dibenzoylhydrazine, acylaminoketone, tetrahydroquinoline) were tested, in vitro reporter assays showed minor differences using cell lines derived from both species. However, when compounds with high ecdysone agonist activity were examined in toxicity assays, larvicidal activity differed considerably. Of note was the identification of three dibenzoylhydrazine analogues with > 100-fold higher activity against Bombyx than against Spodoptera larvae. CONCLUSION: The present study demonstrated that species-specific ecdysone-agonist-based insecticides can be developed, but their species specificity is not based on differences in the activation of the ecdysone receptor but rather on unidentified in vivo parameters such as permeability of the cuticle, uptake/excretion by the gut or metabolic detoxification.
机译:背景:二苯甲酰肼类似物已成功开发为一组新的昆虫生长调节剂,被称为蜕皮激素激动剂或蜕皮促进化合物。一个显着的特征是它们对鳞翅目昆虫的高活性,这引发了是否可以分离出物种特异性类似物的问题。在这项研究中,蜕皮激素激动剂的特异性通过对两个重要的鳞翅类动物,蚕Bombyx mori L.和棉叶虫Spodoptera littoralis(Boisd。)的比较分析得以解决。结果:当测试了含有不同母体结构(二苯甲酰肼,酰氨酮,四氢喹啉)的非甾体蜕皮激素激动剂的收集物时,体外报告基因测定显示,使用源自两种物种的细胞系,差异很小。但是,当在毒性试验中检查具有高蜕皮激素激动剂活性的化合物时,杀幼虫剂的活性差异很大。值得注意的是,鉴定出的三种对苯甲酰肼的类似物对家蚕的活性比对夜蛾幼虫的活性高100倍以上。结论:本研究表明可以开发基于物种的蜕皮激素激动剂的杀虫剂,但其物种特异性并非基于蜕皮激素受体活化的差异,而是基于体内表皮渗透率等不确定的体内参数,肠道吸收或排泄或代谢排毒。

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