College of Plant Protection, Southwest University, Chongqing, China.
Key Laboratory of Agricultural Biosafety and Green Production of Upper Yangtze River (Ministry of Education), Southwest University, Chongqing, China.
Pest Manag Sci. 2023 Sep;79(9):3211-3217. doi: 10.1002/ps.7500. Epub 2023 May 30.
Amitraz is a broad-spectrum formamidine acaricide proven to be effective against mites in all development stages. Under acidic conditions, amitraz is hydrolyzed to N -(2,4-dimethylphenyl)-N -methyformamidine (DPMF), an active metabolite for mite control. Octopamine and tyramine receptors are well known targets of amitraz. Until now, no research has been conducted about the amitraz target in Tetranychus cinnabarinus. This study aimed to identify the target genes of amitraz in T. cinnabarinus and reveal the mechanisms behind the differential acaricidal activities of amitraz and DPMF.
Analysis of the toxicity, stress expression, target sensitivity and binding site of amitraz against T. cinnabarinus showed that TcOctβ2R was the main target gene of amitraz. DPMF had more potent acaricidal activity against T. cinnabarinus and was more effective at activating TcOctβ2R than amitraz. Furthermore, the three synergists had no significant effect on amitraz and DPMF, indicating that the detoxification metabolism was not related to the difference in acaricidal activity.
In this study, TcOctβ2R was identified as the main target gene of amitraz against T. cinnabarinus. The divergence of target binding was responsible for the difference in acaricidal activity between amitraz and DPMF. The results also revealed the physiological and pharmacological functions of octopamine receptors (OARs) in T. cinnabarinus and could provide a basis for the design of new acaricides, with OARs as a special target. © 2023 Society of Chemical Industry.
咪鲜胺是一种广谱脒类杀螨剂,已被证明对所有发育阶段的螨虫都有效。在酸性条件下,咪鲜胺会水解为 N -(2,4-二甲基苯基)-N -甲基脒(DPMF),这是一种控制螨虫的活性代谢物。章鱼胺和酪胺受体是咪鲜胺的已知靶标。到目前为止,还没有关于朱砂叶螨中咪鲜胺靶标的研究。本研究旨在鉴定朱砂叶螨中咪鲜胺的靶标基因,并揭示咪鲜胺和 DPMF 杀虫活性差异的机制。
分析咪鲜胺对朱砂叶螨的毒性、应激表达、靶标敏感性和结合位点表明,TcOctβ2R 是咪鲜胺的主要靶标基因。DPMF 对朱砂叶螨具有更强的杀螨活性,比咪鲜胺更能激活 TcOctβ2R。此外,三种增效剂对咪鲜胺和 DPMF 没有明显影响,表明解毒代谢与杀虫活性的差异无关。
在这项研究中,鉴定了 TcOctβ2R 是咪鲜胺防治朱砂叶螨的主要靶标基因。靶标结合的差异导致了咪鲜胺和 DPMF 杀虫活性的差异。研究结果还揭示了章鱼胺受体(OARs)在朱砂叶螨中的生理和药理学功能,为以 OARs 为特殊靶标设计新型杀螨剂提供了依据。© 2023 化学工业协会。