Insects
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2025
·Vol. 16
·期 5
·479
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IF 2.9
Xiangyi Zhou,Guoxing Chen,Keying Chen,Zhanyi Xu,Jiali Qian,Ru Yan,Bosheng Chen,Huiming Wu,Mengli Chen
Simple SummaryBactrocera dorsalis(Hendel) (Diptera: Tephritidae), a highly invasive pest with high transmissibility and adaptability, causes severe damage to various commercial vegetables and fruits. RDL, as the homomeric subunit of γ-aminobutyric acid (GABA) receptors, is the target of several insecticides. In this study, we found thatBdRdlwas highly expressed in the pupae and heads of male and female adult insects. Also, BdRDL was functionally characterized inXenopus oocytesby two-electrode voltage clamping and we found that fluralaner worked as an antagonist of BdRDL. Furthermore, we found that fluralaner exhibited a comparable insecticidal activity to avermectin againstB. dorsalisadults. Finally, the modeling and molecular docking predicted that fluralaner interacted with BdRDL via hydrogen bonds. These results suggested that fluralaner, as an antagonist of BdRDL, could be used to controlB. dorsalis.Bactrocera dorsalis(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 fromB. dorsalishas not yet been elucidated. Here, we cloned theRdlgene fromB. dorsalis,BdRdl, and investigated the expression pattern ofBdRdl. The results showed thatBdRdlwas highly expressed in pupae and the heads of male and female adults. Also, we characterized the BdRDL inXenopus oocytesthrough 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 (EC50) of 2.4 × 10−4M. 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 againstB. dorsalisadults. Lastly, the modeling and molecular docking predicted that fluralaner interacted with RDL via hydrogen bonds. Our results not only characterized the RDL ofB. dorsalis, but also revealed that fluralaner works as an antagonist of BdRDL and could be used as an effective strategy forB. dorsaliscontrol.
研究领域:
昆虫学
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分子生物学
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PubMed
高影响因子
PEST MANAGEMENT SCIENCE
·
2019
·Vol. 76
·期 3
·888-893
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IF 3.255
Kipchoge Leviticus,Li Cui,Han Ling,Zhong-Qiang Jia,Qiu-Tang Huang,Zhao-Jun Han,Chun-Qing Zhao,Lu Xu
BACKGROUND Two-spotted spider mite (TSSM), Tetranychus urticae Koch is a serious agricultural pest and has developed high levels of resistance to many acaricides. Hence, screening new acaricides is important in the control of TSSM. Fluralaner, a novel isoxazoline, has high activity against agricultural and ectoparasitic pests; however, little information is available about its effects on agricultural mites. Lethal and sublethal effects of fluralaner towards TSSM eggs and female adults were therefore evaluated in this study. RESULTS Fluralaner exhibited higher activity towards TSSM female adults (LC 50 , 0.49 mg L −1 ) compared with commercial acaricides including fenpyroximate, pyridaben and hexythiazox, and also excellent activity towards eggs (LC 50 , 0.36 mg L −1 ). The results of a sublethal effect study showed a significant reduction in the duration and fecundity of female adults with increases in the tested concentrations. The net reproductive rate ( R 0 ) decreased to 67.34 ± 3.96 and 50.29 ± 3.40 offspring per individual in LC 10 and LC 30 treatments compared with control (108.31 ± 7.61 offspring per individual). The intrinsic rate of increase ( r ) and finite rate of increase ( λ ) in the controls (0.30 and 1.36 d −1 ) were significantly higher than in the LC 30 treatment (0.25 and 1.29 d −1 ); whereas, they were almost identical to values for the LC 10 treatment. No change in mean generation time ( T ) was observed at sublethal concentrations treatments. CONCLUSION Our results demonstrated that fluralaner has high acaricidal activity and could be considered a potential acaricide for TSSM management. © 2019 Society of Chemical Industry
研究领域:
农业科学
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害虫管理
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植物保护
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高影响因子
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
·
2025
·
IF 6.2
Ziyi Chen,Chunyan Yin,Falong Wang,Xinlin Sun,Wishwajith Kandegama,Zhenyu Wang,Guangfu Yang
The green peach aphid (Myzus persicae, Hemiptera: Aphididae) is a globally important pest. Isocycloseram (a novel isooxazoline) and fluralaner (a benzamide/sulfonamide) are novel insecticides. A Hainan-resistant population (HNR), exhibited 459- and 316-fold resistance to isocycloseram and fluralaner, respectively, compared with a Yunnan susceptible population (YNS). Synergist bioassays and enzyme activity analyses indicated that enhanced cytochrome P450 monooxygenase activity contributed to resistance. Transcriptomic and qRT-PCR analyses revealed that CYP6CY3 was upregulated 16.4- and 10.8-fold in HNR compared with YNS. RNA interference of CYP6CY3 significantly restored susceptibility to both insecticides. In vitro recombinant enzyme assays confirmed CYP6CY3-mediated metabolism of isocycloseram and fluralaner, and gene copy number analysis demonstrated a 7.09-fold amplification. These results reveal CYP6CY3-mediated cross-resistance to isocycloseram and fluralaner, representing the first mechanistic evidence of isoxazoline resistance in M. persicae.
研究领域:
昆虫学
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农药科学
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分子生物学
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昆虫生物化学
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毒理学
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高影响因子
JOURNAL OF FOOD COMPOSITION AND ANALYSIS
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2024
·
IF 4
Can Cui,Xiaojun Jiao,Xianbin Xu,Jiongzhou Gong,Jiaxin Zhou,Ge Tian,Liwei Lu,Li Li,Xianhui Huang
The presence of residues of veterinary drugs in eggs is an ongoing and significant issue of concern. Fluralaner is widely used in the prevention of ectoparasites, including the poultry red mite, but no analytical method has been reported for detection of its residues in eggs. An HPLC-MS/MS method was established for the determination of fluralaner residues in whole eggs and validated for LOD, LOQ, specificity, linearity, accuracy, precision, and matrix effects. LOD was 5 μg•kg −1 and LOQ was 65 μg•kg −1 . Recovery ranged from 97.7% to 103.7% (spiked at 65, 650, 1300, and 2600 μg•kg −1 ), while intra-assay and inter-assay coefficients of variation were consistently below 1.5%. A drug withdrawal trial was conducted with 16 laying hens administered a therapeutic dose of fluralaner in drinking water on days 0 and 7, with eggs being analyzed for 23 days. The highest concentration, 1235 μg•kg −1 , was detected on day 13. This was below the European Union maximum residue limit for fluralaner in edible chicken tissues and eggs (1300 μg•kg −1 ). Residues were detectable up to two weeks after cessation of treatment. This method is suitable for routine compliance monitoring of fluralaner residues in egg matrices and may be adapted for analysis of other edible tissues.
研究领域:
兽医学
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食品科学
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高影响因子
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
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2022
·
IF 4.966
Ting Xiong,Si-quan Ling,Jia-li Liu,Xin-nian Zeng
The red imported fire ant ( Solenopsis invicta ), a worldwide invasive and polyphagous pest, and often nests in residential areas. Finding an alternative pesticide that is both effective on S. invicta and environmentally friendly is urgent and crucial. Fluralaner, a novel isoxazoline insecticide, has been proven to possess selective toxicity for insects versus mammals and has been safe for mammals and non-target organisms, suggesting its potential in pest management. However, little toxicity information is available for the controlment of S. invicta. In this article, we studied the toxicity of fluralaner against S. invicta systematically, and the roles of metabolism-related enzymes in the metabolism process of fluralaner. The toxicity results showed that the topical application and feeding application were all effective for S. invicta . Moreover, fluralaner can be transmitted among workers by contacting and feeding which leads to a toxic reaction among nestmates. By exploring the biochemistry change, we found cytochrome P450 monooxygenase ( P450 ) may be involved in the detoxification of fluralaner as well as carboxylesterase ( CarE ), but not glutathione S-transferase ( GST ). Synergism assays gave solid evidence in which piperonyl butoxide , an activity inhibitor of P450, increased the toxicity of fluralaner to S. invicta . Importantly, with the RNAi treatment, four of S.invicta P450 genes were significantly inhibited and showed more sensitivity to fluralaner at LC 50 concentration. Our result indicated that fluralaner could be a potential alternative pesticide in S. invicta control . And CYP9AS16 , CYP6AS161 , CYP6SQ20 , and CYP336A45 genes were closely associated with the metabolism process of fluralaner.
研究领域:
昆虫学
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毒理学
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生物化学
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害虫管理
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高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
·
2023
·Vol. 24
·期 21
·15627
·
IF 5.6
Leyi Shao,Wei Wang,Xin Gong,Yinghao Yu,Junao Xue,Xinnian Zeng,Jiali Liu
The red imported fire ant (RIFA),Solenopsis invicta, is an invasive pest that causes damage to agricultural and ecological environments worldwide. Fluralaner is a new isoxazoline pesticide with the potential to become a control agent against RIFA. However, it is not clear whetherS. invictaresponds the same way to fluralaner at different reproductive stages. The present study firstly evaluated the toxicity of fluralaner toS. invictaat different developmental stages, finding that fourth instar larvae (LD50, 1744.23 mg/kg) and worker ants (LD50, 8.62 mg/kg) were differently susceptible to fluralaner, while the mortality rate of fourth instar larvae was significantly lower at the same concentration of 10 mg/L (5.56 ± 3.14%) than that of worker ants (62.22 ± 3.14%), demonstrating a greater tolerance to fluralaner. Subsequently, the metabolic responses of worker and larval ants to fluralaner stress (10 mg/L) were investigated using non-targeted metabolomics, which indicated that the amount of differential metabolites and the KEGG metabolic pathways enriched were different between workers and larvae when exposed to the same dose (10 mg/L) of fluralaner. Differential metabolites of larvae and worker ants under fluralaner stress were mainly concentrated in organic acids and their derivatives, lipids and lipid-like molecules, nucleosides, nucleotides, and analogues, combined with the enriched metabolic pathways, revealed that the differential metabolic responses of larvae and worker ants were mainly in energy metabolism, detoxification metabolism, and neurotransmitter ligands. Workers consumed more substrates in the arginine synthesis pathway (l-glutamic acid,l-aspartic acid, and fumaric acid) to provide energy for the detoxification (glutathione) of pesticides when exposed to fluralaner stress, and the high accumulation ofl-aspartic acid induced excitotoxicity in the worker ants. Larval ants consumed more arachidonic acid to synthesize PG D2, and changes in the metabolism of antioxidants such as catechins, hesperidin, andl-ascorbic acid suggested that larvae were more capable of scavenging the ROS response than worker ants. The results of non-targeted metabolomics successfully revealed differences in the sensitivity of larvae and workers to fluralaner agents, providing insights into the fluralaner control ofSolenopsis invicta.Keywords:contacting activity;fluralaner stress;invasive pest;metabolome;tolerance
研究领域:
昆虫学
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毒理学
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生态学
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PubMed
高影响因子
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