Pesticide Biochemistry and Physiology最新文献_第3页

Design, synthesis, and anti-fungicidal activities of sulfonyl fluoride functionalized SDHI analogs against plant pathogens 磺酰氟功能化SDHI类似物的设计、合成及其对植物病原体的抑菌活性

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-21 DOI: 10.1016/j.pestbp.2026.106973

Junjie Wei , Yunlong Chai , Yangyang Yuan, Jianxiang Wang, Guangkai Yao, Zhixiang Zhang, Hanhong Xu, Chen Zhao

Succinate dehydrogenase inhibitors (SDHIs) have been widely employed as agricultural fungicides due to their effectiveness and low toxicity. Recently, sulfonyl fluoride (R-OSO₂F) has emerged as a promising active moiety in pesticide development. Previously, our team identified aryl sulfonyl fluoride compounds with strong antifungal activity. Expanding on this, we incorporated the sulfonyl fluoride group into the heterocyclic amide scaffold of SDHIs, designing and synthesizing 56 novel aniline-based sulfonyl fluoride derivatives. Their structures were confirmed using ¹H NMR, ¹³C NMR, and high-resolution mass spectrometry (HRMS). Antifungal activity assays showed that compound 4a exhibited the highest inhibitory activity against Rhizoctonia solani (EC₅₀ = 2.89 μg/mL). In bioassays on rice leaves and pot experiments, compound 4a demonstrated 50.75% protective efficacy and 32.43% curative efficacy at 200 μg/mL, comparable to that of commercial SDHI fungicide boscalid. Enzyme inhibition assays confirmed its potent suppression of succinate dehydrogenase (SDH), and molecular docking studies demonstrated binding modes similar to boscalid, with improved binding affinity attributed to the sulfonyl fluoride moiety. We developed a novel sulfonyl fluoride series, identifying 4a as a potent antifungal lead with SDHI-like action. These findings provide valuable insights and new directions for the development of sulfonyl fluorides as next-generation fungicides.

琥珀酸脱氢酶抑制剂（SDHIs）因其高效、低毒等优点被广泛应用于农业杀菌剂。近年来，磺酰氟（R-OSO2F）已成为农药开发中一个很有前景的活性基团。此前，我们的团队发现芳基磺酰氟化合物具有很强的抗真菌活性。在此基础上，我们将磺酰氟基团引入到SDHIs的杂环酰胺支架中，设计并合成了56种新型苯胺基磺酰氟衍生物。它们的结构通过1H NMR， 13C NMR和高分辨率质谱（HRMS）进行了证实。抑菌活性实验表明，化合物4a对茄枯丝核菌的抑菌活性最高（EC50 = 2.89 μg/mL）。在水稻叶片生物测定和盆栽试验中，化合物4a在200 μg/mL浓度下的保护效果为50.75%，疗效为32.43%，与市售的SDHI杀菌剂boscalid相当。酶抑制实验证实了其对琥珀酸脱氢酶（SDH）的有效抑制，分子对接研究表明其结合模式类似于双硫醚，由于磺酰氟部分的存在，其结合亲和力得到了提高。我们开发了一种新的磺酰氟系列，确定4a是一种有效的抗真菌先导物，具有sdi样作用。这些发现为磺酰氟作为下一代杀菌剂的开发提供了有价值的见解和新的方向。

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引用次数: 0

Biocontrol of Apple Valsa Canker by Bacillus sp. H12 and modulation of the apple seedlings microbiome 芽孢杆菌H12对苹果溃疡病的防制及对苹果幼苗微生物群的调控

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-07 DOI: 10.1016/j.pestbp.2026.106946

Ling Sun , Jianxin Gao , Yawen Tan , Yiting Xia , Ruolin Wang , Ruiqi Liu , Xinmei Zhang , Xia Yan , Lili Huang

Apple Valsa Canker (AVC), caused by the fungal pathogen Cytospora mali, is the most devastating stem disease in East Asia apple production systems. As an eco-friendly alternative to chemical control, biological control strategies have attained prominence for mitigating environmental pollution and preventing pathogen resistance. In this study, a soil-derived bacterial strain significantly inhibited AVC and promoted plant growth. The strain was identified as Bacillus amyloliquefaciens using combined morphological and molecular characterization and designated as H12. The bacterium directly induces abnormal branching of C. mali hyphae, cytoplasmic leakage, and cell wall rupture, ultimately leading to mycelia death. H12 exhibits strong control efficacy against AVC on in vitro branches and the leaves of tissue-cultured seedlings. Notably, H12 upregulates immune-related gene expression in apple, enhances reactive oxygen species (ROS) accumulation, and increases callose deposition. Microbiome sequencing indicates that H12 modulates the structure of the apple phyllosphere bacterial community, enriches beneficial microorganisms, and enhances host resistance. Furthermore, the strain achieves a 55.56% disease control efficacy in field trials, demonstrating its potential for practical application as a promising microbial agent. In summary, H12 has dual functions, directly inhibiting pathogenic fungi and inducing host resistance, providing theoretical and practical support for the green management of AVC.

苹果溃疡病（AVC）是东亚苹果生产系统中最具破坏性的茎部病害，由真菌病原体马利细胞孢子虫（Cytospora mali）引起。生物防治作为一种替代化学防治的生态友好型防治策略，在减轻环境污染和预防病原菌耐药性方面已得到重视。在本研究中，一种土壤来源的菌株显著抑制AVC，促进植物生长。经形态学和分子鉴定，该菌株为解淀粉芽孢杆菌，编号为H12。该菌直接诱导马利梭菌菌丝分支异常，细胞质渗漏，细胞壁破裂，最终导致菌丝死亡。H12对离体枝和组培苗叶片的AVC有较强的防治效果。值得注意的是，H12上调苹果免疫相关基因的表达，增加活性氧（ROS）的积累，增加胼胝质沉积。微生物组测序结果表明，H12调节苹果层球细菌群落结构，丰富有益微生物，增强寄主抗性。此外，该菌株在田间试验中的防虫率达到55.56%，显示了其作为一种有前景的微生物剂的实际应用潜力。综上所述，H12具有直接抑制病原菌和诱导宿主抗性的双重功能，为AVC的绿色管理提供了理论和实践支持。

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引用次数: 0

Post-transcriptional regulation of UGT349A13 through a microRNA, PC-5p-86205_18, influences afidopyropen susceptibility in Aphis craccivora 通过微rna PC-5p-86205_18对UGT349A13的转录后调控影响豚鼠嗜核杆菌的敏感性

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-02 DOI: 10.1016/j.pestbp.2025.106939

Yuanxue Yang, Aiyu Wang, Chao Xue, Ming Zhao

As key detoxification enzymes, UDP-glycosyltransferases (UGTs) are known to underpin insecticide tolerance in pests such as Aphis craccivora. Yet, their post-transcriptional regulation by microRNAs (miRNAs) remains largely unexplored in this major crop pest. In the present study, we conducted a genomic analysis that identified 37 UGTs in Aphis craccivora. To investigate their role in susceptibility to the afidopyropen, we performed synergism bioassays following LC₅₀ concentration of afidopyropen exposure, combined with UGT activity measurements, revealed a critical contribution of UGTs to afidopyropen susceptibility. Exposure to afidopyropen resulted in more than a 2-fold increase in the expression levels of UGT343A37 and UGT349A13. Functional validation via RNA interference (RNAi) confirmed that suppression of UGT349A13 alone significantly increased the sensitivity of A. craccivora to afidopyropen. To elucidate the upstream regulatory mechanism, bioinformatic prediction identified candidate miRNAs targeting UGT349A13. To validate regulatory function, A. craccivora fed the synthetic agomir-PC-5p-86205_18, which reduced UGT349A13 transcript levels, correlating with increased susceptibility to afidopyropen. Then, molecular interaction specificity between PC-5p-86205_18 and UGT349A13 was definitively established by dual luciferase reporter assay. This finding demonstrated that PC-5p-86205_18 contributes to afidopyropen susceptibility in A. craccivora by post-transcriptionally regulating UGT349A13. This finding not only deepens our understanding of detoxification mechanisms but also provides a potential molecular target for developing strategies to manage afidopyropen resistance.

作为关键的解毒酶，已知udp -糖基转移酶（UGTs）是蚜虫（Aphis craccivora）等害虫对杀虫剂耐受的基础。然而，它们的转录后调控microRNAs （miRNAs）在这一主要作物害虫中仍未被广泛探索。在本研究中，我们进行了基因组分析，鉴定了37个ugt。为了研究它们在嗜酸纤维敏感性中的作用，我们在嗜酸纤维暴露LC50浓度后进行了协同生物测定，并结合UGT活性测量，揭示了UGT对嗜酸纤维敏感性的重要贡献。暴露于粘连素导致UGT343A37和UGT349A13的表达水平增加2倍以上。通过RNA干扰（RNAi）功能验证证实，单独抑制UGT349A13可显著提高A. craccivora对嗜酸性纤维的敏感性。为了阐明上游调控机制，生物信息学预测鉴定了靶向UGT349A13的候选mirna。为了验证调节功能，我们将A. craccivora饲养合成的agomir-PC-5p-86205_18，该基因降低了UGT349A13转录物的水平，与对嗜粘细胞的易感性增加相关。然后，通过双荧光素酶报告基因实验确定PC-5p-86205_18与UGT349A13的分子相互作用特异性。这一发现表明PC-5p-86205_18通过转录后调控UGT349A13参与了A. craccivora的嗜核杆菌敏感性。这一发现不仅加深了我们对解毒机制的理解，而且为开发管理嗜核细胞抗性的策略提供了潜在的分子靶点。

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引用次数: 0

Translocation, metabolism and distribution of multi-pesticides in rats 多种农药在大鼠体内的易位、代谢和分布

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-10 DOI: 10.1016/j.pestbp.2026.106954

Kai Cui , Liping Fang , Ruiyan Ding , Wanru Su , Shuai Guan , Jingyun Liang , Teng Li , Junhua Liu , Jian Wang , Zhan Dong , Xiaohu Wu , Yongquan Zheng

The use of pesticides has led to their widespread presence in food, making it unavoidable for the public to be exposed to pesticides through diet. However, few studies have focused on the in vivo distribution of pesticides after exposure. This study comprehensively investigated the residual behavior of nine pesticides and their five metabolites in rats after oral exposure and elucidated the relationship between their physicochemical properties and tissue-specific distribution. During the initial exposure, all tested pesticides and metabolites were detected in the serum and different tissues, with the highest concentration of 3294.03 μg/kg observed in the liver. However, after 48 h of exposure, a majority of the pesticides were undetectable. Correlation analysis revealed a strong negative correlation between pesticide residues detected in the serum, brain, heart, liver, lung, kidney, spleen, and urine as well as physicochemical properties such as molecular weight (Mw) and octanol–water partition coefficient (log Kow). Conversely, a positive correlation was observed between the residues and aqueous solubility (As). Pesticides with lower Mw and log Kow and higher As, such as acetamiprid, imidacloprid, and thiamethoxam, showed higher solubility in serum and higher residual deposition across different tissues. Water-soluble pesticides, such as acetamiprid, imidacloprid, and thiamethoxam, were predominantly excreted through urine, thereby achieving relatively rapid systemic clearance. However, fat-soluble pesticides, such as azoxystrobin, chlorantraniliprole, and pyraclostrobin, were primarily eliminated through the fecal route, which is a comparatively slow process. This study helps in understanding the residual behavior of pesticides in mammals, thereby providing valuable insights for pesticide safety evaluation.

农药的使用导致它们在食品中广泛存在，使公众不可避免地通过饮食接触到农药。然而，很少有研究关注农药暴露后的体内分布。本研究全面研究了9种农药及其5种代谢物在大鼠口腔暴露后的残留行为，并阐明了其理化性质与组织特异性分布的关系。初暴露时，血清和不同组织中均检测到所有农药及其代谢物，肝脏中浓度最高，为3294.03 μg/kg。然而，暴露48小时后，大多数农药无法检测到。相关分析显示，血清、脑、心、肝、肺、肾、脾、尿中农药残留量与分子质量（Mw）、辛醇-水分配系数（log Kow）等理化性质呈显著负相关。相反，残基与水溶解度（As）呈正相关。对乙酰咪唑啉、吡虫啉、噻虫嗪等低Mw、低log Kow、高As的农药在血清中的溶解度较高，在不同组织中的残留沉积也较高。水溶性农药，如啶虫脒、吡虫啉和噻虫嗪，主要通过尿液排出，从而实现相对快速的全身清除。而脂溶性农药，如偶氮虫胺、氯虫胺、吡虫胺等主要通过粪便途径清除，这是一个相对缓慢的过程。本研究有助于了解农药在哺乳动物体内的残留行为，从而为农药安全性评价提供有价值的见解。

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引用次数: 0

Biocontrol efficacy and mechanism of Bacillus subtilis PL5 against root rot of sweet potato: Insights into antifungal activity and metabolite function 枯草芽孢杆菌PL5对甘薯根腐病的生物防治效果及机制：抑菌活性及代谢物功能研究

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-08 DOI: 10.1016/j.pestbp.2026.106947

Yushun Liu , Zhenlin Han , Xinyu Li , Yinuo Tang , Bin Wang , Zunyang Song , Jingying Shi

Fusarium solani causes sweet potato root rot disease under optimal temperature conditions. Biocontrol using antagonistic microorganisms offers a sustainable and eco-friendly management strategy through dual mechanisms: direct pathogen suppression and induction of systemic plant resistance. Bacillus subtilis PL5 culture broth significantly reduced the plaque diameter of F. solani, impaired spore germination, and curtailed germ tube length. Furthermore, it triggered reactive oxygen species (ROS) accumulation, initiating apoptosis and membrane integrity disruption. In vivo experiments demonstrated that spraying with B. subtilis PL5 culture broth mitigated root rot incidence in sweet potato. It enhanced the activities of nicotinamide adenine dinucleotide phosphate oxidase (NOX), superoxide dismutase (SOD), catalase (CAT), ascorbate peroxidase (APX), and peroxidase (POD), thereby strengthening the antioxidative capacity of roots and balancing ROS levels, including hydrogen peroxide (H₂O₂) and superoxide anion radical (O₂^.-). Concurrently, B. subtilis PL5 culture broth modulated polyamines (PAs) metabolism, leading to significant elevations in putrescine (Put), spermidine (Spd), and spermine (Spm) levels, as well as enhanced activities of arginine decarboxylase (ADC), ornithine decarboxylase (ODC), and PA oxidase (PAO) and decline in diamine oxidase (DAO) activity. Natural disease occurrence studies showed that B. subtilis PL5 widely suppressed the disease progression in sweet potatoes. In addition, non-targeted metabolic and “Pearson” correlation analysis showed the metabolites in B. subtilis PL5 were closely related to the levels of ROS and PAs. Collectively, these findings elucidate the mechanism basis by which B. subtilis PL5 mediates pathogen suppression and enhances resistance, providing novel insights for developing sustainable sweet potato protection agent.

在最佳温度条件下，茄枯病菌可引起甘薯根腐病。利用拮抗微生物的生物防治通过双重机制提供了一种可持续和生态友好的管理策略：直接抑制病原体和诱导系统植物抗性。枯草芽孢杆菌PL5培养液显著降低了茄枯菌菌斑直径，抑制了孢子萌发，缩短了芽管长度。此外，它还会引发活性氧（ROS）积累，引发细胞凋亡和膜完整性破坏。体内试验表明，施用枯草芽孢杆菌PL5培养液可减轻甘薯根腐病的发生。增强烟酰胺腺嘌呤二核苷酸磷酸氧化酶（NOX）、超氧化物歧化酶（SOD）、过氧化氢酶（CAT）、抗坏血酸过氧化物酶（APX）和过氧化物酶（POD）活性，从而增强根的抗氧化能力，平衡过氧化氢（H2O2）和超氧阴离子自由基（O2.-）等活性氧水平。同时，枯草芽孢杆菌PL5培养液调节了多胺（PAs）代谢，导致腐胺（Put）、亚精胺（Spd）和精胺（Spm）水平显著升高，精氨酸脱羧酶（ADC）、鸟氨酸脱羧酶（ODC）和PA氧化酶（PAO）活性增强，二胺氧化酶（DAO）活性下降。自然发病研究表明，枯草芽孢杆菌PL5广泛抑制甘薯病害进展。此外，非靶向代谢和“Pearson”相关分析显示，枯草芽孢杆菌PL5的代谢物与ROS和PAs水平密切相关。这些发现阐明了枯草芽孢杆菌PL5介导病原菌抑制和增强抗性的机制基础，为开发可持续的甘薯保护剂提供了新的见解。

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引用次数: 0

Divergent impacts of conventional and biodegradable microplastics on pesticide fate and toxicity in a soil–chive system, underscoring a soil-plant-microbe disruption 传统和可生物降解微塑料对土壤-韭菜系统中农药命运和毒性的不同影响，强调土壤-植物-微生物的破坏

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-20 DOI: 10.1016/j.pestbp.2026.106971

Jing Yang , Guy Smagghe , Xiaomao Wu , Wanping Zhang , Xiangsheng Chen

Microplastics (MPs) and pesticides increasingly co-occur in agricultural soils, yet their combined effects on soil biology and plant–soil interactions remain poorly understood. Here we provide the evidence that biodegradable polylactic acid (PLA) MPs, despite their eco-friendly reputation, fundamentally reshape soil microbial and biochemical dynamics under pesticide stress. In a soil–chive system, PLA, but not conventional polyethylene (PE), significantly delayed iprodione (IPR) degradation (up to 7.7-fold), increased the persistence of its toxic metabolite 3,5-dichloroaniline (3,5-DCA), and enhanced plant uptake of 3,5-DCA (up to 59%). Mechanistically, PLA disrupted beneficial bacterial enrichment, altered microbial community composition, and interfered with plant detoxification pathways, notably glutathione metabolism and amino acid biosynthesis. These interactions intensified phytotoxicity, stunted plant growth, and reduced soil–plant resilience. Our findings reveal a previously overlooked ecological trade-off: biodegradable MPs can amplify pesticide risks by destabilizing soil microbial processes and stress-response mechanisms. This work advances understanding of how novel contaminants interact in soils and highlights the importance of integrating soil biological functions into sustainability assessments of alternative plastics.

微塑料（MPs）和农药越来越多地共同出现在农业土壤中，但它们对土壤生物学和植物-土壤相互作用的综合影响仍然知之甚少。在这里，我们提供的证据表明，可生物降解的聚乳酸（PLA） MPs尽管具有环保的声誉，但在农药胁迫下从根本上重塑了土壤微生物和生化动力学。在土壤-韭菜体系中，聚乳酸（PLA）显著延缓了异丙二酮（IPR）的降解（高达7.7倍），增加了其有毒代谢产物3,5-二氯苯胺（3,5- dca）的持久性，并提高了植物对3,5- dca的吸收率（高达59%）。在机制上，聚乳酸破坏了有益细菌的富集，改变了微生物群落的组成，干扰了植物的解毒途径，特别是谷胱甘肽代谢和氨基酸的生物合成。这些相互作用加剧了植物毒性，阻碍了植物生长，降低了土壤植物的恢复力。我们的研究结果揭示了一个以前被忽视的生态权衡：可生物降解的MPs可以通过破坏土壤微生物过程和应激反应机制来放大农药风险。这项工作促进了对新污染物如何在土壤中相互作用的理解，并强调了将土壤生物功能整合到替代塑料可持续性评估中的重要性。

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引用次数: 0

Breaking the trade-off: Trichoderma effector Tahfb1 dual-targets growth and defense pathways via Hsp70L 打破取舍：木霉效应物Tahfb1通过Hsp70L双重靶向生长和防御途径

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-20 DOI: 10.1016/j.pestbp.2026.106972

Yaping Yin, Yuhang Fu, He Wu, Liping Feng, Lijuan He, Runmao Lin, Rui Wang, Zhengbin Tang, Baoping Zhu, Jumei Hou, Jing Zhao, Tong Liu

Beneficial microbes like Trichoderma can help plants balance growth and defense, but the key signaling molecules and mechanisms underlying this balance remain unclear. In the present study, we demonstrated that Trichoderma asperellum promotes tomato growth and enhances resistance to Botrytis cinerea. Interaction transcriptomics revealed a 156-fold upregulation of Tahfb1, a gene encoding a class II hydrophobin. Application of exogenous Tahfb1 protein increased lateral root growth and reduced lesion area on tomato leaves. A CRISPR/Cas9-mediated knockout of Tahfb1 resulted in a 32% reduction in lateral roots and a 39% increase in lesion size. Conversely, overexpression strains significantly enhanced lateral root growth by 97% and decreased lesion area by 40%. Pot experiments further confirmed that Tahfb1 increased the number of lateral roots by 42% and reduced lesion area by 58%. Furthermore, yeast two-hybrid (Y2H), co-immunoprecipitation (Co-IP), and bimolecular fluorescence complementation (BiFC) confirmed that Tahfb1 directly interacts with the tomato heat shock protein Hsp70L. RNAi silencing of Hsp70L significantly compromised Tahfb1-induced lateral root development by 53% and increased lesion size by 62%. Quantitative analysis indicated that Tahfb1 modulates auxin signaling pathway (ARF19/PIN1/CYCB1;2), and the jasmonic acid/ethylene pathway (LOX/ETR1) to synergistically promote growth and immunity. Our results identify the Tahfb1-Hsp70L module as a key mediator of the synergistic enhancement of growth and defense in Trichoderma-plant interactions.

像木霉这样的有益微生物可以帮助植物平衡生长和防御，但这种平衡背后的关键信号分子和机制尚不清楚。在本研究中，我们证明了曲霉能促进番茄生长，增强番茄对灰霉病的抗性。相互作用转录组学显示，编码II类疏水蛋白的基因Tahfb1上调了156倍。施用外源Tahfb1蛋白可促进番茄侧根生长，减少叶片损伤面积。CRISPR/ cas9介导的Tahfb1基因敲除导致侧根减少32%，病变大小增加39%。相反，过表达菌株显著促进侧根生长97%，损伤面积减少40%。盆栽实验进一步证实，Tahfb1使侧根数量增加42%，损伤面积减少58%。此外，酵母双杂交（Y2H）、共免疫沉淀（Co-IP）和双分子荧光互补（BiFC）证实Tahfb1直接与番茄热休克蛋白Hsp70L相互作用。RNAi沉默Hsp70L显著降低tahfb1诱导的侧根发育53%，病变大小增加62%。定量分析表明Tahfb1可调节生长素信号通路（ARF19/PIN1/CYCB1;2）和茉莉酸/乙烯通路（LOX/ETR1），协同促进生长和免疫。我们的研究结果表明，Tahfb1-Hsp70L模块是木霉与植物相互作用中协同增强生长和防御的关键中介。

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引用次数: 0

Corrigendum to “Both target-site and non-target-site resistance mechanisms confer mesosulfuron-methyl resistance in Silene conoidea L.” [Pesticide Biochemistry and Physiology 218(2026) 106905] “靶点和非靶点抗性机制都赋予了Silene conoidea L.中硫隆-甲基抗性”的勘误表[农药生物化学与生理218(2026)106905]。

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-23 DOI: 10.1016/j.pestbp.2026.106964

Xinhui Xue , Hailan Cui , Shen'ao Hu , Hong Ma , Shouhui Wei , Hongjuan Huang , Xiangju Li , Zhaofeng Huang

引用次数: 0

Herbicidal activity mechanism and ecotoxicological study of novel triazolinone PPO inhibitors based on plant-derived allelochemical cinnamic acid 基于植物化感化学物质肉桂酸的新型三唑啉酮类PPO抑制剂除草活性机制及生态毒理学研究

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-06 DOI: 10.1016/j.pestbp.2026.106945

Li-Xia Zhao , Xian-Da Guo , Jia-Xiao Li , Yue-Li Zou , Shuang Gao , Ying Fu , Fei Ye

Chemical herbicides are crucial for weed control, affecting crop growth and yield. Yet, their extended use has caused environmental harm and resistance concerns. Developing novel, highly efficient, low-toxicity herbicides with unique mechanisms is imperative. Protoporphyrinogen oxidase (PPO) is vital for chlorophyll and heme synthesis, while targeted PPO inhibitors are favoured for their low toxicity to mammals. In this study, 44 phenyltriazolinone-cinnamoyl derivatives were synthesised from cinnamic acid using an active substructure splicing strategy to explore their herbicidal activity and ecotoxicity as PPO inhibitors. Most compounds were more effective against broadleaf weeds than against grass weeds. Compound VII-6 notably inhibited various weeds by over 80% at 37.5 g a.i. ha⁻¹, displaying superior in vitro Echinochloa crus-galli PPO (EcPPO) inhibitory activity (IC₅₀ = 0.180 ± 0.003 μM) compared to sulfentrazone. VII-6 was safe for soybean, maize, and other crops but caused slight injury to cotton, and it exhibited a broad herbicidal spectrum against 24 weeds species, comparable to that of sulfentrazone. ADMET predictions indicated pharmacokinetic properties of VII-6 akin to sulfentrazone. Predicted ecotoxicity showed VII-6 to be relatively low toxicity to several species of animals, non-toxicity to bees and low environmental persistence. Molecular studies showed stable interactions of VII-6 with NtPPO, forming hydrogen bonds and hydrophobic interactions with lower binding free energy than sulfentrazone. In this study, compound VII-6 was initially developed as a novel PPO inhibiting herbicide molecule with low ecotoxicity and sustainable green agriculture prospect.

化学除草剂是控制杂草的关键，影响作物生长和产量。然而，它们的长期使用已经引起了环境危害和耐药性问题。开发具有独特作用机理的新型、高效、低毒除草剂势在必行。原卟啉原氧化酶（PPO）对叶绿素和血红素的合成至关重要，而靶向PPO抑制剂因其对哺乳动物的低毒性而受到青睐。本研究以肉桂酸为原料，采用活性亚结构剪接策略合成了44个苯基三唑啉-肉桂基衍生物，以考察其作为PPO抑制剂的除草活性和生态毒性。多数化合物对阔叶杂草的防治效果优于禾本科杂草。在37.5 g a.i. ha−1条件下，化合物7 -6对多种杂草的抑制率达80%以上，其体外EcPPO抑制活性（IC50 = 0.180±0.003 μM）优于磺胺曲酮。7 -6对大豆、玉米等作物安全，对棉花危害较小，对24种杂草有较宽的除草谱，与磺胺酮相当。ADMET预测显示VII-6的药代动力学性质类似于磺胺酮。预测生态毒性表明，VII-6对几种动物毒性较低，对蜜蜂无毒，环境持久性较低。分子研究表明，7 -6与NtPPO相互作用稳定，形成氢键和疏水相互作用，其结合自由能低于磺胺曲酮。在本研究中，化合物VII-6是一种具有低生态毒性和可持续绿色农业前景的新型PPO抑制除草剂分子。

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引用次数: 0

Precision pest management: Genome editing tools, specifically CRISPR/Cas9 and future prospects 精确害虫管理：基因组编辑工具，特别是CRISPR/Cas9和未来展望

IF 4 1区农林科学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY

Pesticide Biochemistry and Physiology

Pub Date : 2026-03-01 Epub Date: 2026-01-07 DOI: 10.1016/j.pestbp.2026.106941

Ankush Saini , Neha Sharma , Nidhi Sharma , Neha Kumari , Muskaan Sharma , Brajesh Singh , Ajay Kumar Thakur

The growing resistance to synthetic insecticides and Bt toxins, alongside persistent crop losses despite heavy pesticide application, highlights the urgent need for safer, sustainable and efficient pest management strategies. This review presents genome editing as a precise and versatile approach to reduce pest impact by altering fertility, feeding patterns or vulnerability, while protecting beneficial organisms. Among the genome editing tools, CRISPR/Cas9 (Clustered Regularly Interspaced Short Palindromic Repeats/CRISPR-associated protein 9) is one of the most promising genome editing techniques in insects. It facilitates targeted functional studies, integration with RNAi and dual-expression systems and gene drive applications. Deployment is envisioned in two phases, initial laboratory modification followed by regulated field release, with a strong emphasis on biosafety through terminator genes, marked individuals for gene flow monitoring, optimized dosages, stringent screening and long-term ecological surveillance, along with transparency and adherence to international safety protocols. Significant challenges encompass delivery efficiency, identification of edits, off-target mutations, dose-related efficacy and sterility, unstable transmission and resistance development. Innovations such as base and prime editing minimize unintended mutations by circumventing double-stranded breaks (DSBs), while paratransgenic strategies targeting gut symbionts offer supplementary avenues; plant-mediated insect gene editing emerges as a promising frontier. Overall, carefully regulated trials aligned with policy frameworks and stakeholder involvement are vital to assess effectiveness in natural environments and achieve targeted, dependable and ecologically responsible pest control.

对合成杀虫剂和Bt毒素的耐药性日益增强，加之尽管大量施用农药，作物仍持续损失，这突出表明迫切需要更安全、可持续和有效的病虫害管理战略。这篇综述介绍了基因组编辑作为一种精确和通用的方法，通过改变生育力、喂养模式或脆弱性来减少有害生物的影响，同时保护有益生物。在基因组编辑工具中，CRISPR/Cas9 （Clustered Regularly Interspaced Short Palindromic Repeats/CRISPR-associated protein 9）是最有前途的昆虫基因组编辑技术之一。它促进了有针对性的功能研究，与RNAi和双表达系统以及基因驱动应用的集成。部署计划分两个阶段进行，首先在实验室进行初步修改，然后进行规范的现场释放，重点强调通过终止基因的生物安全性，标记个体进行基因流监测，优化剂量，严格筛选和长期生态监测，以及透明度和遵守国际安全协议。重大挑战包括递送效率、编辑鉴定、脱靶突变、剂量相关功效和不育、不稳定传播和耐药性发展。碱基和引物编辑等创新通过规避双链断裂（dsb）来最大限度地减少意外突变，而针对肠道共生体的准转基因策略提供了补充途径；植物介导的昆虫基因编辑成为一个有前途的前沿。总体而言，与政策框架和利益攸关方参与相一致的精心监管的试验对于评估自然环境中的有效性和实现有针对性、可靠和对生态负责的虫害防治至关重要。

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