Computational insight on the binding and selectivity of target-subunit-dependent for neonicotinoid insecticides

Xu, Xiaoying; Yang, Zhaokai; Zhu, Kai; Li, Huilin; Qin, Zhaohai; Duan, Hongxia

doi:10.1016/j.jmgm.2020.107586

Cited by 16 publications

(17 citation statements)

References 18 publications

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“…A previous study also reported that there were no negative effects on the larvae development and foraging activity of honeybees with 4 ppm flupyradifurone [54]. Due to the unique binding mode of flupyradifurone to nAChR, flupyradifurone is considered to have low-toxicity to the honeybee [21].…”

Section: Discussionmentioning

confidence: 92%

“…Therefore, the appropriate use of this pesticide is considered safe for bumblebees, at least for the queenless microcolony studied here. Similarly, flupyradifurone (Sivanto, Bayer AG, Monheim am Rhein, Germany) was reported to be harmless for honeybees' taste and cognition behaviors under field conditions [21].…”

Section: Chronic Exposure To Flupyradifurone Shows No Detrimental Eff...mentioning

confidence: 99%

“…Flupyradifurone (4-[(2,2-difluoroethyl) amino]-2(5 H)-furanone) is a novel pesticide (commercial product Sivanto ® ), launched by Bayer AG (Monheim am Rhein, Germany) [20]. Compared to imidacloprid, flupyradifurone also acts as a reversible agonist on insect nAchR, while at a different site of action [21]. Flupyradifurone has been claimed to be "slightly toxic" to organisms in the environment, while it may evoke bees' motor disabilities and disturb normal motor behavior [20].…”

Section: Introductionmentioning

confidence: 99%

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Impacts of Imidacloprid and Flupyradifurone Insecticides on the Gut Microbiota of Bombus terrestris

et al. 2022

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Bumblebees are important pollinators for crops and wild flowering plants. Various pesticides have threatened the abundance and diversity of bumblebees. In addition to direct sublethal effects, pesticides may alter the gut microbial communities of bees. Imidacloprid and flupyradifurone insecticides both bind to the nicotinic acetylcholine receptor. However, the latter was assumed to be harmless for honeybees and can even be applied to flowering crops. In this study, we assessed the impacts of these two pesticides on queenless microcolonies and the gut microbiota of Bombus terrestris. We found that 10 μg/L imidacloprid significantly impeded syrup consumption, and postponed the egg-laying period, larvae, and pupae development. It decreased the relative abundance of the bumblebee-specific symbionts, Apibacter and Lactobacillus Firm-5. On the contrary, 10 μg/L flupyradifurone did not reduce syrup consumption, block larvae and pupae development in bumblebees. Although no significant phenotypes were observed, PICRUST revealed that flupyradifurone suppressed pathways, involving carbohydrate metabolism, nucleotide metabolism, translation, and membrane transport. Our findings suggest the appropriate use of this new pesticide may be considered safe for bumblebees, but the underlying mechanism warrants further investigation.

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Section: Discussionmentioning

confidence: 92%

Section: Chronic Exposure To Flupyradifurone Shows No Detrimental Eff...mentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Impacts of Imidacloprid and Flupyradifurone Insecticides on the Gut Microbiota of Bombus terrestris

et al. 2022

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“…Recent studies showed that flupyradifurone has a relatively lower impact on honeybees compared with neonicotinoids 16 . The electronegative butenolide group in flupyradifurone, as a surrogate of the nitro group in imidacloprid, is in a totally inverse orientation to stretch the α chain in honeybee nAChR, resulting in a weaker binding ability compared to neonicotinoids 17 . The safety of flupyradifurone use on flowering crops with actively foraging bees has been proven 18 .…”

Section: Introductionmentioning

confidence: 99%

Evaluation of flupyradifurone for the management of the Asian citrus psyllid Diaphorina citri via dripping irrigation systems

Wen

Meng

Zhao

et al. 2021

Pest Management Science

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BACKGROUND Chemical control is the most used and effective method to control Diaphorina citri, the vector of the phloem‐limited bacteria associated with citrus huanglongbing (HLB) disease. The objectives of this study were to determine the effectiveness of flupyradifurone applied via dripping irrigation systems on D. citri. Bioassays were conducted using leaves harvested on various dates post treatment, and insecticide residue in leaf tissue was quantified. RESULTS The drip application of flupyradifurone on citrus trees provided high‐level and long‐term control against D. citri adult, and the median lethal concentration (LC50) for ingestion of flupyradifurone in D. citri was 22.22 mg kg–1 (fresh leaf). Flupyradifurone residue was detected in leaf tissue within 3 days after treatment. The measured level of flupyradifurone peaked on day 40 day after application, and then showed a steady decline in subsequent days for all three applied dosages. The amounts of flupyradifurone in upper, middle, and lower leaves were similar, and trends in the change in concentration of flupyradifurone were consistent. CONCLUSIONS The results demonstrate that flupyradifurone can be a valuable new tool for D. citri management programs, and drip‐applied flupyradifurone provides an extended period of control efficacy. This paper could provide a reference to reduce the dependence on foliar‐applied insecticides, with associated benefits for non‐target exposure to workers and pollinators. © 2021 Society of Chemical Industry

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“…In honeybees, eleven genes encoding nAChR subunits have been identified, with 9 α subunits and 2 non-α (or β subunits) [ 21 ]. The subunit composition of nAChR subtypes is known to influence their pharmacological properties [ 20 ], as well as neonicotinoid binding and toxicity in honeybees [ 22 ].…”

Section: Introductionmentioning

confidence: 99%

Impairments in learning and memory performances associated with nicotinic receptor expression in the honeybee Apis mellifera after exposure to a sublethal dose of sulfoxaflor

et al. 2022

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Sulfoxaflor is a new insecticide which acts on the nicotinic acetylcholine receptor (nAChRs) in a similar way to neonicotinoids. However, sufloxaflor (SFX) is thought to act in a different manner and is thus proposed as an alternative in crop protection. The goal of this study is to evaluate the toxicity of SFX and its sublethal effect on the honeybee Apis mellifera after acute exposure. In toxicological assay studies, the LD50 value and sublethal dose (corresponding to the NOEL: no observed effect level) were 96 and 15 ng/bee, respectively. Using the proboscis extension response paradigm, we found that an SFX dose of 15 ng/bee significantly impairs learning and memory retrieval when applied 12 h before conditioning or 24 h after olfactory conditioning. SFX had no effect on honeybee olfactory performance when exposure happened after the conditioning. Relative quantitative PCR experiments performed on the six nicotinic acetylcholine receptor subunits demonstrated that they are differently expressed in the honeybee brain after SFX exposure, whether before or after conditioning. We found that intoxicated bees with learning defects showed a strong expression of the Amelβ1 subunit. They displayed overexpression of Amelα9 and Amelβ2, and down-regulation of Amelα1, Amelα3 and Amelα7 subunits. These results demonstrated for the first time that a sublethal dose of SFX could affect honeybee learning and memory performance and modulate the expression of specific nAChR subunits in the brain.

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Computational insight on the binding and selectivity of target-subunit-dependent for neonicotinoid insecticides

Cited by 16 publications

References 18 publications

Impacts of Imidacloprid and Flupyradifurone Insecticides on the Gut Microbiota of Bombus terrestris

Impacts of Imidacloprid and Flupyradifurone Insecticides on the Gut Microbiota of Bombus terrestris

Evaluation of flupyradifurone for the management of the Asian citrus psyllid Diaphorina citri via dripping irrigation systems

Impairments in learning and memory performances associated with nicotinic receptor expression in the honeybee Apis mellifera after exposure to a sublethal dose of sulfoxaflor

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