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氟虫腈对……的GABA受体亚基RDL的抑制作用

Inhibitory Effect of Fluralaner on GABA Receptor Subunit RDL of .

作者信息

Zhou Xiangyi, Chen Guoxing, Chen Keying, Xu Zhanyi, Qian Jiali, Yan Ru, Chen Bosheng, Wu Huiming, Chen Mengli

机构信息

Zhejiang Key Laboratory of Biology and Ecological Regulation of Crop Pathogens and Insects, College of Advanced Agricultural Sciences, Zhejiang A&F University, Hangzhou 311300, China.

Institute of Pesticide and Environmental Toxicology, College of Agriculture and Biotechnology, Zhejiang University, Hangzhou 310030, China.

出版信息

Insects. 2025 May 1;16(5):479. doi: 10.3390/insects16050479.

DOI:10.3390/insects16050479
PMID:40429192
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12112586/
Abstract

(Hendel) (Diptera: Tephritidae), a highly destructive pest, affects fruits and vegetables globally, leading to significant economic losses. As a homomeric subunit of γ-aminobutyric acid (GABA) receptors, RDL plays a crucial role in various physiological activities in insects. However, functional characterization of RDL from has not yet been elucidated. Here, we cloned the gene from , , and investigated the expression pattern of . The results showed that was highly expressed in pupae and the heads of male and female adults. Also, we characterized the BdRDL in through two-electrode voltage clamping. It turned out that the inward current of BdRDL induced by GABA was followed in a dose-dependent manner with a median effective concentration (EC) of 2.4 × 10 M. Additionally, we determined the mode action of fluralaner, a new insecticide, on BdRDL in oocytes. We found that fluralaner significantly inhibited the currents induced by GABA, suggesting that fluralaner worked as an antagonist of BdRDL. Furthermore, we found that fluralaner exhibited a comparable insecticidal activity to avermectin against adults. Lastly, the modeling and molecular docking predicted that fluralaner interacted with RDL via hydrogen bonds. Our results not only characterized the RDL of , but also revealed that fluralaner works as an antagonist of BdRDL and could be used as an effective strategy for control.

摘要

亨德尔实蝇(双翅目:实蝇科)是一种极具破坏性的害虫,在全球范围内影响水果和蔬菜,导致重大经济损失。作为γ-氨基丁酸(GABA)受体的同聚亚基,RDL在昆虫的各种生理活动中起着关键作用。然而,关于[某种实蝇]的RDL的功能特性尚未阐明。在此,我们从[某种实蝇]中克隆了[RDL]基因,并研究了其表达模式。结果表明,[RDL]在蛹以及雌雄成虫头部中高表达。此外,我们通过双电极电压钳技术对[某种实蝇]中的BdRDL进行了特性分析。结果发现,GABA诱导的BdRDL内向电流呈剂量依赖性,半数有效浓度(EC)为2.4×10⁻⁶M。另外,我们确定了新型杀虫剂氟虫腈对卵母细胞中BdRDL的作用方式。我们发现氟虫腈显著抑制GABA诱导的电流,这表明氟虫腈作为BdRDL的拮抗剂发挥作用。此外,我们发现氟虫腈对[某种实蝇]成虫表现出与阿维菌素相当的杀虫活性。最后,建模和分子对接预测氟虫腈通过氢键与RDL相互作用。我们的结果不仅对[某种实蝇]的RDL进行了特性分析,还揭示了氟虫腈作为BdRDL的拮抗剂发挥作用,并且可作为控制[某种实蝇]的有效策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/78ce6783b15a/insects-16-00479-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/c542ec9ff5dc/insects-16-00479-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/8d7938f9a46d/insects-16-00479-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/e7b2a2d5d84e/insects-16-00479-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/3941e6891d6b/insects-16-00479-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/ab43db73b752/insects-16-00479-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/78ce6783b15a/insects-16-00479-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/c542ec9ff5dc/insects-16-00479-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/8d7938f9a46d/insects-16-00479-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/e7b2a2d5d84e/insects-16-00479-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/3941e6891d6b/insects-16-00479-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/ab43db73b752/insects-16-00479-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72e1/12112586/78ce6783b15a/insects-16-00479-g006.jpg

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本文引用的文献

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Insect Biochem Mol Biol. 2025 Feb;177:104243. doi: 10.1016/j.ibmb.2024.104243. Epub 2024 Dec 5.
2
Isolation and characterization of the decreased cuticular penetration mechanism of fluralaner resistance in the house fly, Musca domestica.家蝇中氟虫腈抗性的表皮穿透能力降低机制的分离和特性。
Pestic Biochem Physiol. 2024 Nov;205:106154. doi: 10.1016/j.pestbp.2024.106154. Epub 2024 Sep 24.
3
N318L Blocks the Interaction of Fluralaner but Not Broflanilide or Fipronil with the Insect GABA Receptor .
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J Agric Food Chem. 2024 Oct 1. doi: 10.1021/acs.jafc.4c06478.
4
Lethal, Sublethal, and Offspring Effects of Fluralaner and Dinotefuran on Three Species of Fruit Flies.氟虫腈和呋虫胺对三种果蝇的致死、亚致死及子代效应
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