Imidacloprid Crystal Polymorphs for Disease Vector Control and Pollinator Protection
Imidacloprid Crystal Polymorphs for Disease Vector Control and Pollinator Protection
复制标题
DOI：
10.1021/jacs.1c07610
复制
发表时间：
2021-10-12
影响因子：
15
通讯作者：
Kahr, Bart
中科院分区：
文献类型：
--
作者：
Zhu, Xiaolong;Hu, Chunhua T.;Kahr, Bart
吡虫啉是世界上最主要的杀虫剂，最近已被批准用于控制传染病媒介；然而，在农业环境中，它与传粉媒介的可怕下降有关。这表明需要采取策略来大幅减少吡虫啉对环境的影响。当作为接触性杀虫剂使用时，吡虫啉的有效性依赖于其晶体表面与昆虫跗关节之间的物理接触。本文报道了七种新的吡虫啉晶体多晶型，增加了两种已知的形式。预计昆虫对吡虫啉分子的吸收将取决于晶体多形态表面各自的自由能，对亚稳态晶体形式的昆虫击倒时间的测量比商业形式对伊蚊、按蚊、库蚊以及果蝇的作用快9倍。这些结果表明，在空间喷洒中，用三种新的多晶型（IV、VI、IX）中的任何一种取代市售吡虫啉晶体（又称I型），都可以抑制媒介传播的疾病传播，同时减少环境暴露和对非目标生物的伤害。
Imidacloprid, the world's leading insecticide, has been approved recently for controlling infectious disease vectors; yet, in agricultural settings, it has been implicated in the frightening decline of pollinators. This argues for strategies that sharply reduce the environmental impact of imidacloprid. When used as a contact insecticide, the effectiveness of imidacloprid relies on physical contact between its crystal surfaces and insect tarsi. Herein, seven new imidacloprid crystal polymorphs are reported, adding to two known forms. Anticipating that insect uptake of imidacloprid molecules would depend on the respective free energies of crystal polymorph surfaces, measurements of insect knockdown times for the metastable crystal forms were as much as nine times faster acting than the commercial form against Aedes, Anopheles, and Culex mosquitoes as well as Drosophila (fruit flies). These results suggest that replacement of commercially available imidacloprid crystals (a.k.a. Form I) in space-spraying with any one of three new polymorphs, Forms IV, VI, IX, would suppress vector-borne disease transmission while reducing environmental exposure and harm to nontarget organisms.