98%
921
2 minutes
20
Background: Fluralaner, a novel pesticide that targets the γ-aminobutyric acid (GABA) receptor (GABAR) subunit of resistant to dieldrin (RDL), exhibits strong potential to be an insecticide to control agricultural insect pests. However, the risk and action of fluralaner to economic insects, e.g., honeybee Apis mellifera Linnaeus, remains unclear.
Results: In this study, both oral and contact toxicity of fluralaner to honeybee were found to be 0.13 μg adult . Abamectin, dieldrin, ethiprole, α-endosulfan, fipronil and fluralaner strongly inhibited the GABA-induced current in A. mellifera RDL (AmRDL), expressed in Xenopus laevis oocytes, with median inhibitory concentration (IC ) values of 7.99, 868.1, 27.10, 412.0, 11.21 and 13.59 nM, respectively. The binding free energy and electrophysiological response of AmRDL and insecticides were opposite. The correlation values between toxicity (to A. mellifera) and binding free energy/electrophysiological inhibition (to AmRDL) were at a moderate level.
Conclusion: In conclusion, we report for the first time the notable risk of fluralaner to honeybee in vivo and compared the actions of GABAR-targeted insecticides on the AmRDL receptor. © 2019 Society of Chemical Industry.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1002/ps.5483 | DOI Listing |
J Agric Food Chem
April 2025
State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Huaxi District, Guiyang 550025, China.
The isoxazoline insecticide, such as fluralaner, exhibits strong insecticidal activity against pests while showing no cross-resistance. However, due to its toxicity to bees, the use of Fluralaner is restricted in veterinary antiparasitic applications. Hence, how to modify the structure of fluralaner to maintain the insecticidal activity and reduce the toxicity to bees is vital and meaningful.
View Article and Find Full Text PDFJ Agric Food Chem
March 2025
State Key Laboratory of Green Pesticide, Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, College of Plant Protection, South China Agricultural University, Guangzhou 510642, P. R. China.
Isoxazoline insecticides exhibit broad-spectrum insecticidal activity against insect pests. However, the high toxicity to honeybees limits their application in pest management. To explore reducing the toxicity of isoxazoline derivatives to bees, a series of new isoxazoline cyclopropyl-picolinamide derivatives were designed and synthesized.
View Article and Find Full Text PDFPestic Biochem Physiol
September 2024
State Key Laboratory of Green Pesticide, Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, College of Plant Protection, South China Agricultural University, Guangzhou, Guangdong 510642, People's Republic of China. Electronic address:
Isoxazoline insecticides have shown broad-spectrum insecticidal activity against a variety of insect pests. However, the high toxicity of isoxazoline compounds towards honeybees restricts their application in crop protection. To mitigate this issue, a series of isoxazoline derivatives containing 2-phenyloxazoline were designed and synthesized.
View Article and Find Full Text PDFPestic Biochem Physiol
March 2024
National Key Laboratory of Green Pesticide, Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, South China Agricultural University, Guangzhou 510642, People's Republic of China. Electronic address:
Isoxazoline is a novel structure with strong potential for controlling agricultural insect pests, but its high toxicity to honeybees limits its development in agriculture. Herein, a series of N-phenylamide isoxazoline derivatives with low honeybee toxicity were designed and synthesized using the intermediate derivatization method. Bioassay results showed that these compounds exhibited good insecticidal activity.
View Article and Find Full Text PDFJ Agric Food Chem
October 2023
National Key Laboratory of Green Pesticide, Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, South China Agricultural University, Guangzhou 510642, People's Republic of China.
To develop highly effective, nontarget organism-friendly insecticides based on the isoxazoline scaffold, we rationally designed and synthesized 25 isoxazoline derivatives containing sulfonamides and sulfinamides. Their insecticidal activities against the diamondback moth (), fall armyworm (), beet armyworm (), and Fabricius () were evaluated. The trifluoromethyl sulfinamide-containing compound displayed excellent activities with LC values being 0.
View Article and Find Full Text PDF