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发现了与piperonyl结合的sulfoximines作为针对Amelα1/ratβ2复合物的新型低毒性蜜蜂毒剂

Qing Han¹, Yuxin Zhou², Yunjiang Zi¹

¹Innovation Center of Pesticide Research, Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, People's Republic of China; Key Laboratory of National Forestry and Grassland Administration on Pest Chemical Control, Beijing 100193, People's Republic of China.

International journal of biological macromolecules

|September 7, 2023

概括

新型硫胺衍生物对蜜蜂的毒性较低,为环保的虫控制提供了潜力. 这些化合物向尼古丁乙胆受体 (nAChRs),对于杀虫剂开发至关重要.

科学领域:

农业科学农业科学
昆虫学昆虫学是一门学科.
毒理学毒理学毒理学

背景情况:

尼古丁乙胆受体 (nAChRs) 是主要的杀虫剂点.
氨酸类药物和一些激动剂对nAChRs起作用.
了解nAChR相互作用对于开发更安全的杀虫剂至关重要.

研究的目的:

设计和合成针对Apis mellifera nAChR α1子单元的新型硫胺衍生物.
评估这些新化合物的杀虫活性和蜜蜂毒性.
阐明选择性毒性背后的分子机制.

主要方法:

基于nAChR结合腔的硫胺衍生物的合理设计.
新型硫胺化合物的化学合成 (7a-h).
在蜜蜂中进行电生理学测试 (双电极电压) 和急性接触毒性生物测试.
分子建模研究.分子建模研究.

主要成果:

合成了新的硫胺衍生物 (7a-h).
化合物7a-h的电生理反应低于硫 (SFX),这表明蜜蜂毒性降低.
化合物7b和7g证明了蜜蜂的低毒性 (LD50>11.0μg/蜜蜂).
分子建模确定了关键的氨基酸残留物 (Ile152,Ala151,Amelα1中的Val160;Lys144,Mpα1中的Trp80),影响了蜜蜂的毒性和杀虫活性.

结论:

该研究确定了新的硫胺支架,具有作为低毒性蜜蜂杀虫剂的潜力.
了解nAChR亚单元的相互作用,可以了解选择性杀虫剂的设计.
结果为开发针对nAChRs的环保杀虫剂铺平了道路.

关键词:

这种类型的杀虫剂是aphicide.蜜蜂的毒性蜜蜂的毒性电生理学反应反应电生理学反应硫胺衍生物硫胺衍生物在nAChR子单元中.

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