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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

NlCYP417A1 is a critical regulator of molting by governing ecdysone homeostasis in the brown planthopper

Xiaowei Yuan,Hanlin Wang,Jiawen Du,Xiaojuan Liu,Haoli Gao,Zewen Liu

BACKGROUND The brown planthopper (BPH), Nilaparvata lugens , is a destructive rice pest across Asia. Suppressing insect development is enduring goals in insect pest management, underpinning the action of existing insecticides and guiding the design of new ones. Insect molting, which is tightly regulated by ecdysteroid signaling, is essential for insect growth and development. Cytochrome P450 (CYP) enzymes play critical roles in ecdysteroid biosynthesis, and identifying P450 genes involved in this process may provide new insights into insect developmental regulation and potential targets for pest control. RESULTS Here, we identify NlCYP417A1, a planthopper specific P450, as an essential regulator of molting and cuticle remodeling. NlCYP417A1 is predominantly expressed in the cuticle. RNA interference-mediated knockdown severely impairs ecdysis, leading to incomplete cuticle shedding, elongated body shape, and final lethality. Mechanistically, NlCYP417A1 silencing suppresses Halloween family gene expression, reducing 20-hydroxyecdysone (20E) titers and disrupting downstream 20E signaling, including ecdysone receptor ( EcR )/ultraspiracle ( USP ), early response genes ( E93 , E75 , E74A ), HR3 , and FTZ-F1 . Finally, silencing NlCYP417A1 down-regulates chitinolytic enzyme genes and multiple cuticular protein genes, which provides a compelling explanation for the abnormal molting observed in the test insects. CONCLUSION Our study reveals an essential role of NlCYP417A1 in regulating ecdysteroid biosynthesis and nymphal molting, expanding our understanding of CYP450-mediated developmental regulation in insects. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Transforming agricultural waste into intelligent biopesticide delivery: soil-disintegrable tea saponin microcapsules for sustainable crop protection

Ying Liu,Yi Ding,Long Xu,Chao Wang,Huanhuan Yao,Huili Zhang,Xiujun Tang,Min Liao,Haiqun Cao,Junfan Niu

BACKGROUND In order to achieve intelligent and sustainable delivery of tea tree oil (TTO) for tea pest control, we developed a soil-disintegrable, pH-responsive microcapsule system (TMS) with an average particle size of 2.05 μm using 15.6% tea saponin as the shell precursor via interfacial polymerization. RESULTS Optimized TMS (1–2 μm) achieved 97.4% encapsulation efficiency. The system exhibited accelerated TTO release under acidic conditions (78.8% at pH 5.0), enabling targeted delivery to fungal infection sites. It demonstrated superior foliar adhesion and rainfastness (84.5% retention) compared to free TTO. Biological evaluations revealed potent dual bioactivity: antifungal efficacy against Colletotrichum camelliae [median effective concentration (EC 50 ) = 0.87 mg mL −1 ] and Phyllosticta theaefolia (EC 50 = 2.3 mg mL −1 ), alongside significant insecticidal activity against Ectropis obliqua larvae (90.0% mortality at 3 mg mL −1 ). CONCLUSIONS This work demonstrates substantial macroscopic disintegration and no apparent phytotoxicity, with the potential to reduce persistent microplastic accumulation, providing a potential strategy to improve its formulation and delivery while retaining its biological activity. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Characterization of the Dermanyssus gallinae octopamine receptor DgOctβ2R as the molecular target for synthetic and natural acaricides

Zihan Cheng,Yanbing Zhu,Jinwei Liu,Mingxiang Zhang,Rui Li,Ailing Liu,Jia Huang

BACKGROUND The poultry red mite ( Dermanyssus gallinae ) seriously threatens the global poultry industry. Reliance on chemical acaricides has led to resistance, and plant essential oils represent an eco-friendly alternative, but their mode of action remains unclear. Amitraz targets the β2-adrenergic-like octopamine receptor (Octβ2R). This study aimed to clone and characterize Octβ2R from D. gallinae , elucidate the mechanism of amitraz and essential oils, and support resistance monitoring. RESULTS We cloned DgOctβ2R. Evolutionary analysis revealed that DgOctβ2R clusters with other mite Octβ2Rs, distinct from insect orthologs. Functional assays in HEK293T cells demonstrated that amitraz and its metabolite N′-(2,4-dimethylphenyl)-N-methylformamidine(DPMF) potently activated DgOctβ2R, with DPMF acting as a full agonist. The plant essential oil component thymol also exhibited agonist activity at micromolar concentrations. Molecular docking revealed that DPMF and thymol bind the orthosteric pocket via a hydrogen bond with D 3.32 , whereas octopamine additionally engages S 5.46 . CONCLUSION This study successfully identified and functionally characterized DgOctβ2R from D. gallinae , providing molecular evidence that amitraz and DPMF target this receptor. The differential potency between synthetic and natural compounds reveals distinct agonistic profiles. These findings establish a molecular basis for rational use of amitraz, resistance surveillance, and structure-based design of novel and environmentally friendly acaricides targeting DgOctβ2R. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Design, synthesis, and anti-oomycete, antifungal and nematicidal activities of novel paeonol ether derivatives containing isoxazoline/isoxazole moiety

Xiaxia Ban,Yihao Guo,Xiaobo Huang,Yuee Tian,Lin Zhou,Zhiping Che

BACKGROUND Paeonol is the main active ingredient in root bark of Paeonia suffruticosa , with broad-spectrum bioactivity. Additionally, isoxazoline/isoxazole is becoming the core skeleton for creating efficient and green pesticides today owing to its unique structural advantages and bioactivity potential. RESULTS In order to discover biorational natural product-based pesticides, 26 novel paeonol ether derivatives ( 3a–q and 5a , c , d , f–j , m ) were synthesized by ingeniously introducing an isoxazoline/isoxazole ring, and their structures were well-characterized by proton and carbon nuclear magnetic resonance (NMR), and high-resolution mass spectrometry (HRMS). The stereochemical configurations of five target compounds 3a , 3g , 3j , 5a and 5h were unambiguously subjected to single-crystal X-ray diffraction (XRD) analysis. Furthermore, we screened the bioactivities of these compounds as anti-oomycete, antifungal and nematicidal agents. Amongst evaluated derivatives, (1) compounds 2 and 4 displayed promising anti-oomycete against the plant pathogen Phytophthora capsici , with median effective concentration (EC 50 )values of 28.51 and 42.52 mg L –1 , respectively. (2) Compounds 2 and 4 also exhibited excellent antifungal activity against the plant pathogen Fusarium graminearum , with EC 50 values of 29.11 and 31.23 mg L –1 , respectively. (3) Nine compounds ( 3f–h , j , o–q and 5f , g ) showed significant nematicidal activity against Heterodera glycines , with LC 50 values all <30.00 mg L –1 . Especially for compound 3g , its LC 50 value is the smallest, at 21.78 mg L –1 . CONCLUSION The research results indicate that, on the one hand, introducing an allyl or propargyl group at the hydroxyl position of paeonol can effectively enhance its anti-oomycete and antifungal activities. On the other hand, further introduction of an isoxazoline/isoxazole ring into the structural skeleton of paeonol can significantly enhance its nematicidal activity. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Design of bioactive peptides by amino acid combination strategy against peanut southern blight caused by Sclerotium rolfsii

Yayu Ren,Youwu Hao,Guangyao Li,Yaru Song,Xiaohan Wang,Qiya Wang,Meizi Wang

BACKGROUND Peanut southern blight, caused by Sclerotium rolfsii Sacc., is a destructive soil-borne disease that severely threatens peanut yield and production safety. In response to the growing demand for environmentally compatible fungicides with low resistance risk, bioactive peptides have emerged as promising alternatives for disease management. RESULTS In this study, two novel peptides, wmz-1 and wmz-2 , were designed using an amino acid combination strategy, and their bioactivities were systematically evaluated. Although both peptides exhibited moderate in vitro inhibition rates of 28.48% and 26.46% against S. rolfsii at 400 mg L −1 , they showed superior in vivo performance in pot experiments. At 200 mg L −1 , wmz-1 demonstrated protective and curative efficacies of 62.79% and 65.68%, respectively, whereas wmz-2 achieved 53.74% and 46.06%, respectively. To investigate the discrepancy between in vitro and in vivo activity, their effects on peanut plants were further examined. The results showed that both wmz-1 and the amino acid combination significantly promoted plant growth and enhanced the activities of defense-related enzymes, thereby providing experimental evidence supporting the involvement of plant growth promotion and induced defense responses. Moreover, both peptides exhibited low cytotoxicity toward human LO2 liver cells. CONCLUSION These findings highlight the potential of wmz-1 and wmz-2 as effective, low-toxicity and environmentally friendly biopesticide candidates for the sustainable management of peanut southern blight, providing a theoretical basis for further development of peptide-based fungicides. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Integrated cell–mouse metabolomics reveals toxicity mechanisms and biomarkers of prothioconazole exposure

Linlin Shi,Wenhui Li,Xiandan Zhu,Heng Zhang,Lei Yang,Siyu Chen,Jinjing Xiao,Xiude Hua,Haiqun Cao,Qingkui Fang

BACKGROUND Prothioconazole (PTC) is one of the most widely used triazole fungicides worldwide, while its major metabolite, prothioconazole-desthio (dPTC), exhibits enhanced toxicological potential. However, the metabolic perturbations induced by chronic PTC exposure and sensitive biomarkers for exposure monitoring remain poorly understood. This study aimed to elucidate the metabolic toxicity mechanisms of PTC and identify reliable biomarkers using integrated in vitro and in vivo metabolomics. RESULTS Cytotoxicity assays demonstrated significant differences in the toxicity of eight representative pesticides toward L-02 hepatocytes, with half-maximal inhibitory concentration (IC 50 ) values of 102.8 and 167.3 μmol L −1 for PTC and dPTC, respectively. Untargeted metabolomics revealed that PTC exposure significantly disturbed lipid metabolism, nicotinate metabolism, amino acid metabolism, and mitochondrial energy homeostasis. Corticosterone, equol, and uric acid exhibited excellent discriminatory performance (area under the curve (AUC) > 0.95) and were identified as potential cellular biomarkers of exposure. In C57BL/6J mice, chronic PTC exposure for 28 days induced systemic metabolic disturbances involving the tricarboxylic acid cycle, lysine degradation, and host–microbiota co-metabolism. Targeted metabolomics further validated significant increases in succinic acid, heptanedioic acid, and 2-oxohexanedioic acid, together with a marked decrease in indole-3-propionic acid, consistent with the untargeted metabolomics results. These metabolites demonstrated high sensitivity and specificity for discriminating PTC exposure. CONCLUSIONS This study demonstrates that chronic PTC exposure disrupts mitochondrial energy metabolism and multiple metabolic pathways, leading to systemic metabolic dysfunction. The identified metabolic biomarkers provide promising tools for pesticide biomonitoring and mechanistic toxicity assessment, improving exposure surveillance and health risk evaluation of triazole fungicides. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Azelaic acid from Pseudomonas nicosulfuronedens MiC45 as an effective compound against Meloidogyne incognita in susceptible pepper

Jia Xiao,Xiufang Deng,Wei Zhao,Lingyun Zhang,Keying Xie,Lei Chen,Jiaqi Wan,Hongdong Liao

BACKGROUND Globally restricted high-toxic chemical nematicides have triggered an urgent demand for ecologically compatible biocontrol alternatives. Antagonistic microbes and their bioactive metabolites serve as eco-friendly candidates to manage Meloidogyne incognita . This study aimed to screen rhizosphere antagonistic bacteria, characterize their primary nematicidal metabolite, and validate their nematicidal efficacy. RESULTS Strain Pseudomonas nicosulfuronedens MiC45, isolated from the rhizosphere soil of healthy pepper in nematode-infested fields, exhibited potent nematicidal activity, yielding a corrected second-stage juvenile mortality rate of 89.54% at 48 h post-treatment. Liquid chromatography–mass spectrometry (LC–MS) analysis identified azelaic acid as the critical bioactive constituent within its ethyl acetate fermentation extract, with a detected concentration of 505.73 μg/mL. In vitro tests showed that azelaic acid exhibited dose-dependent lethal activity against M. incognita . At 500 μg/mL, the nematodes mortality reached 84.22%, surpassing the positive control abamectin (76.75%). In addition, concentrations ≥ 300 μg/mL greatly suppressed nematode egg hatching, with an inhibition index of 98.71% at 500 μg/mL after 11 days. Moreover, scanning electron microscopy (SEM) and transmission electron microscopy (TEM) imaging revealed cuticle disruption and ultrastructural damage in treated nematodes. Azelaic acid also induced dose-dependent reactive oxygen species (ROS) generation within nematodes. Pot experiments demonstrated that both MiC45 fermentation broth and azelaic acid significantly reduced root gall numbers and nematode invasion, while the fermentation broth simultaneously enhanced pepper biomass. CONCLUSION Azelaic acid from strain MiC45 suppresses M. incognita by destroying body structures and triggering oxidative stress. These findings provide a theoretical foundation for developing novel biopesticides for pepper production and offer a solid basis for environmentally friendly alternatives to conventional chemical nematicides. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Synthesis, antibacterial evaluation, and mechanism study of piperazine-bearing oxime ether derivatives

Yuguo Zheng,Mei Chen,Hua Sun,Bicheng Lou,Renfeng Zhang,Guanglong Zhang,Wei Xue

BACKGROUND The persistent proliferation of bacterial phytopathogens presents a significant threat to global food security and agricultural sustainability. Among these pathogens, species belonging to the genus Xanthomonas are particularly destructive. Xanthomonas oryzae pv . oryzae ( Xoo ), the causal agent of bacterial leaf blight in rice, is recognized as one of the most devastating phytopathogens. This strongly indicates that there is an urgent need to create green small-molecule pesticides specifically targeting Xoo . RESULTS Herein, we designed and synthesized 20 oxime ether derivatives containing piperazine fragments and systematically evaluated their antibacterial activity. Bioassay results revealed that compound L1 exhibited notable antibacterial efficacy, with a half-maximal effective concentration (EC 50 ) of 7.32 μg mL −1 , significantly outperforming control agents such as thiodiazole-copper (96.90 μg mL −1 ) and bismerthiazol (47.20 μg mL −1 ). The underlying mechanism of action was investigated using an integrated approach involving molecular docking, morphological observation, three-dimensional quantitative structure–activity relationship modeling, and transcriptome profiling. In addition, the phytotoxicity study results indicate that compound L1 exhibits low toxicity towards plants. The findings of this research provide theoretical insights and experimental guidance for designing novel, potent, and environment-friendly small-molecule antibacterial agents. CONCLUSION Compound L1 represents a promising class of antibacterial agents with potent activity against Xoo . It possesses the dual advantages of high bactericidal efficacy and ecological friendliness, demonstrating great potential to replace traditional agricultural chemicals and promote green prevention and control of plant diseases. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Design and synthesis of oxathiapiprolin derivatives containing acetal fragments as potent fungicide candidates

Hong-Hao Li,Jin-Peng Yang,Chuan-Xiang Cheng,Lan Zhang,Chao Gong,Ying Ye,Xi-Li Liu,WM Wishwajith W. Kandegama,Xiao-Lei Zhu

BACKGROUND Oxysterol-binding proteins (OSBPs) serve as critical regulators throughout the oomycete life cycle. Oxathiapiprolin (OXA), a potent OSBP-targeting fungicide, represents the first commercially developed piperidine-thiazole-isooxazoline (PTI) product. Despite extensive structural modification focused on OXA, very few analogs with improved fungicidal activity have been identified to date. RESULTS In this study, a series of OXA derivatives were designed and synthesized by introducing a flexible acetal fragment into OXA. The compounds B3 and B5 respectively exhibited excellent 77.78% and 94.44% control efficiency against cucumber downy mildew (CDM) at 0.02 mg/L concentration. The field trials showed that compounds B3 and B5 took on higher control efficiency than OXA at the same concentration. The result of environmental toxicological risk assessment indicated that compounds B3 and B5 have lower toxicity to aquatic lives than OXA. Computational chemistry indicated that the binding mode of compound B3 with Phytophthora capsici OSBP ( Pc OSBP) is similar to that of OXA, and kept the main binding interaction with OSBPs. CONCLUSION Our findings suggested that a strategy focused on increasing molecular flexibility could be advantageous for optimizing OSBP inhibitors. The chemical structure of compound B3 may serve as a promising new starting point for the development of further OSBP inhibitors. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

β-Substitution and prodrug derivation leading to identification of fosmidomycin analogs with improved herbicidal activity

Zili Yang,Liru Zheng,Qinping Hu,Mengwei Bu,Jiang Duan,Weiguo Li,Aidong Zhang

BACKGROUND The rapid evolution and spread of herbicide resistance poses a great challenge to the sustainability of modern agriculture and finding new herbicides based on novel modes of action (MOA) has become an urgent need. The enzyme 1-deoxy- d -xylulose-5-phosphate reductoisomerase (DXR) in the 2- C -methyl- d -erythritol 4-phosphate (MEP) pathway is considered an ideal novel target for developing new herbicides and therefore its natural inhibitor fosmidomycin (FOS) is an excellent starting point from which to design new herbicidal candidates. RESULTS This work presents the design and synthesis of a series of β -substituted FOS analogs 10a – m and 11a – m and a prodrug 15i , the diethyl ester of 11i , for evaluating their herbicidal activity. Most compounds exhibited high inhibition activity toward the DXR enzyme in the MEP pathway, and 11i and 11l were among the most active, with half-maximal inhibitory concentrations of 0.24 and 0.27 μ m , respectively. In pre- and post-emergence tests on model plants, ten compounds had higher activities than FOS, and 15i achieved more than tenfold pre-emergence and twofold post-emergence activity against the test weeds. The MEP pathway rescue of Arabidopsis inhibited by 11i as a representative had a higher rescue rate than that by FOS, while molecular docking revealed binding enhancement in the DXR active site due to β -substitution, suggesting that β -substituted FOS analogs may be herbicidally active by targeting DXR, like the MOA of FOS. CONCLUSION The combination of β -substitution with prodrug derivation to modify the lead structure FOS is an effective strategy for developing herbicide-active FOS analogs. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Field-dose fenitrothion impairs gut function and survival in the bumble bees (Bombus terrestris)

Yutong Liu,Yang Yang,Jiasen Wang,Sa Yang,Zuren Li,Lianyang Bai,Zachary Y Huang,Changsheng Ma

BACKGROUND Fenitrothion is a widely used insecticide, yet its effects on the health of bumble bees ( Bombus terrestris ) have not been reported until now. We carried out experiments to investigate the impact of field-realistic concentrations of fenitrothion on food consumption, body weight, survival probability, gut structure, gut detoxification enzyme activity, gut microbial diversity, gut transcriptional and gut metabolic profiles of Bombus terrestris . RESULTS Exposure to 500 μg kg −1 fenitrothion significantly reduced survival probability, induced gut damage as evidenced by hematoxylin and eosin staining, decreased cytochrome P450 (P450) activity while increasing glutathione S-transferase (GST) activity, and down-regulated AChE1 expression in gut tissue. Furthermore, 16S rRNA sequencing revealed a decline in gut microbial diversity, while transcriptomic and metabolomic analyses indicated disruptions in gut gene and metabolic expression. Molecular docking revealed that fenitrothion binds within a hydrophobic pocket formed by residues Trp148, Ser186, Tyr185, and Gly182 of the AChE1 protein. CONCLUSION These multiple sublethal alterations in bee behavior and physiology indicate that fenitrothion is likely to exert complex yet detrimental effects on Bombus terrestris health under field conditions. © 2026 Society of Chemical Industry.

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PEST MANAGEMENT SCIENCE · 2026 · IF 4.2

Novel histone deacetylase-inhibiting 5-(trifluoromethyl)-1,2,4-oxadiazole derivatives with exceptional efficacy against Phakopsora pachyrhizi

Chunlan Li,Yuandong Liu,Yuxin Huang,Fanqi Meng,Jing Zhang,Lixin Zhang

BACKGROUND Asian soybean rust caused by Phakopsora pachyrhizi ( P. pachyrhizi ) poses a serious threat to global soybean production, and resistance to conventional fungicides is increasing. Therefore, new fungicides with novel modes of action are urgently needed. This study aimed to design and optimize potent 5-(trifluoromethyl)-1,2,4-oxadiazole (TFMO) derivatives inspired by fungal histone deacetylase inhibition. RESULTS Forty-two TFMO derivatives were synthesized through bioisosteric modification and linker optimization. Among them, FM-17888 showed the highest activity against P. pachyrhizi , with an EC 50 value of 0.0583 mg·L −1 , approximately eightfold lower than that of flufenoxadiazam. Under the tested greenhouse conditions, FM-17888 also showed good crop safety and selective activity against Puccinia triticina . Molecular docking and DFT analyses suggested that its improved activity may be associated with favorable binding geometry, additional π -sulfur interactions, and a reduced HOMO-LUMO energy gap. CONCLUSION FM-17888 is a potent and selective TFMO lead compound for soybean rust control. Together with the greenhouse bioassay, docking, and DFT results, these findings support FM-17888 as a promising candidate for further development against rust diseases, while direct target-validation studies are still needed to confirm its precise mode of action. © 2026 Society of Chemical Industry.

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