Li Benjie, Yan Ying, Yao Guangkai, Zhang Ling, Lin Fei, Xu Hanhong
National Key Laboratory of Green Pesticide/Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education South China Agricultural University, Guangzhou 510642, China.
The Affiliated Brain Hospital of Guangzhou Medical University, Guangzhou Huiai Hospital, Guangzhou 510370, China.
J Agric Food Chem. 2023 May 17;71(19):7250-7257. doi: 10.1021/acs.jafc.3c01270. Epub 2023 May 3.
In our previous study, a series of novel pyrazoloquinazolines were synthesized. Pyrazoloquinazoline showed high insecticidal activity against the diamondback moth () and no cross-resistance to fipronil. Patch clamp electrophysiology performed on pupae brains and two-electrode voltage clamp electrophysiology performed on oocytes indicated that might act on the ionotropic γ-aminobutyric acid (GABA) receptor (GABAR) and glutamate-gated chloride channel (GluCl). Moreover, 's potency on GluCl was about 15-fold higher than on fipronil, which may explain why there was no cross-resistance between and fipronil. Downregulation of the transcription level significantly enhanced the insecticidal activity of on . These findings shed light on the mode of action of and provide important insights into the development of new insecticides for agricultural applications.
在我们之前的研究中,合成了一系列新型吡唑并喹唑啉。吡唑并喹唑啉对小菜蛾表现出高杀虫活性,且与氟虫腈无交互抗性。对蛹脑进行的膜片钳电生理学研究以及对卵母细胞进行的双电极电压钳电生理学研究表明,其可能作用于离子型γ-氨基丁酸(GABA)受体(GABAR)和谷氨酸门控氯离子通道(GluCl)。此外,其对GluCl的效力比对氟虫腈高约15倍,这可能解释了其与氟虫腈之间不存在交互抗性的原因。下调该转录水平显著增强了其对小菜蛾的杀虫活性。这些发现揭示了其作用模式,并为农业应用新型杀虫剂的开发提供了重要见解。