两个斑点的蜘蛛螨,荨麻疹科赫,具有广泛的寄主植物范围,并具有开发农药抗性的极端能力,成为农业的主要经济害虫。抗胆碱酯酶杀虫剂仍然占全球杀虫剂销售的很大一部分。然而,人们越来越关注抗胆碱酯酶杀虫剂的严重耐药性问题及其非目标毒性。在这项研究中,进行基于结构的虚拟筛选,以从ChemBridge数据库中发现选择性AChE抑制剂,并获得了39种潜在的针对荨麻疹AChE的物种特异性AChE抑制剂,但不是人类ACHE。其中,化合物编号8抑制荨麻疹的AChE,但不是来自人类,并且具有与eserine相当的抑制活性。化合物编号8在载玻片浸渍试验中对荨麻疹具有剂量依赖性毒性,在盆栽实验中具有明显的螨防治效果。但需要高浓度才能达到与螺氯芬相似的控制效果。毒性评估表明化合物No.在我们的测定中,8对传粉者蜜蜂和天然捕食者N.californicus没有急性毒性,并且不影响草莓的生长。化合物编号图8是用于开发具有降低的非目标毒性的新型杀螨剂的潜在先导化合物。
The two-spotted spider mite, Tetranychus urticae Koch, has a broad host plant range and presents an extreme capacity for developing pesticide resistance, becoming a major economic pest in agriculture.
Anticholinesterase insecticides still account for a big part of global insecticide sales. However, there is a growing concern about the serious resistance problems of
anticholinesterase insecticides and their nontarget toxicity. In this study, structure-based virtual screening was performed to discover selective AChE inhibitors from the ChemBridge database, and 39 potential species-specific AChE inhibitor were obtained targeting T. urticae AChE, but not human AChE. Among them, compound No. 8 inhibited AChE from T. urticae, but not from human, and had an inhibitory activity comparable to that of eserine. Compound No. 8 had dose-dependent toxicity to T. urticae in glass slide-dipping assay and had significant mite control effects in a pot experiment, but required a high concentration to achieve similar control effects to spirodiclofen. The toxicity evaluation suggested that compound No. 8 had no acute toxicity on pollinator honey bees and natural predator N. californicus and did not affect strawberry growth in our assay. Compound No. 8 is a potential lead compound for developing novel acaricides with reduced nontarget toxicity.