Advanced Agrochem最新文献

英文中文

Discovery of 4-Hydroxyphenylpyruvate dioxygenase inhibitors with novel pharmacophores 发现具有新药理作用的 4-羟基苯基丙酮酸二氧酶抑制剂

Advanced Agrochem

Pub Date : 2024-09-19 DOI: 10.1016/j.aac.2024.09.004

Tai-Li Yang , Jin Dong , Xin-Long Wang , Jiangqing Dong , Hong-Yan Lin

4-Hydroxyphenylpyruvate dioxygenase (HPPD) is pivotal in tyrosine metabolism and essential for plant survival. Its inhibition leads to leaf bleaching and plant death. While current HPPD inhibitors are effective, they pose phytotoxicity risks and may contribute to herbicide resistance. Here, we investigated the inhibitory potential of sethoxydim and atovaquone, which traditionally target acetyl-CoA carboxylase and the cytochrome bc1 complex, respectively. Both atovaquone and the degradation product of sethoxydim exhibited moderate HPPD inhibitory activity. But the mechanism by which sethoxydim inhibited HPPD remained unclear. Therefore, we embarked on an investigation into the crystal structure of the complex, with the aim of elucidating its precise binding mode. Our findings revealed that sethoxydim degrades in solution, producing dealkoxy sethoxydim as the active component in HPPD inhibition. Structural analysis elucidated the binding modes of atovaquone and dealkoxy sethoxydim with HPPD. These binding motifs represent novel pharmacophores and offer promising leads for developing HPPD inhibitors with improved pesticidal profiles.

4-Hydroxyphenylpyruvate dioxygenase（HPPD）在酪氨酸代谢中起着关键作用，对植物的生存至关重要。抑制该酶会导致叶片脱色和植物死亡。虽然目前的 HPPD 抑制剂很有效，但它们存在植物毒性风险，并可能导致除草剂抗药性。在这里，我们研究了sethoxydim 和阿托伐醌的抑制潜力，它们传统上分别以乙酰-CoA 羧化酶和细胞色素 bc1 复合物为靶标。阿托伐醌和sethoxydim 的降解产物都表现出中等程度的 HPPD 抑制活性。但sethoxydim抑制HPPD的机制仍不清楚。因此，我们开始研究该复合物的晶体结构，旨在阐明其精确的结合模式。我们的研究结果表明，sethoxydim 在溶液中降解，产生的脱烷氧基 sethoxydim 是抑制 HPPD 的活性成分。结构分析阐明了阿托伐醌和脱烷氧基sethoxydim与HPPD的结合模式。这些结合基团代表了新的药性，为开发具有更好杀虫特性的 HPPD 抑制剂提供了很好的线索。

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引用次数: 0

Design, synthesis and bioactivity of cyclic dinucleotides against Lepidoptera insects 针对鳞翅目昆虫的环状二核苷酸的设计、合成和生物活性

Advanced Agrochem

Pub Date : 2024-09-04 DOI: 10.1016/j.aac.2024.09.002

Zhiqiang Xie , Sijing An , Dejun Ma , Zhen Xi

Cyclic dinucleotides (CDNs) play important physiological roles in bacteria, mammals and insects as a novel class of signaling molecules. However, the application of CDNs in agricultural pest control has not been reported yet. To explore the potential bioactivity of CDNs on agricultural pests, we synthesized ten kinds of CDNs containing adenine and guanine bases with different internucleotide linkages (3′,3′; 2′,3′; 2′,2′). The target CDNs were used to determine the antifeedant and insecticidal activity against common Lepidoptera pests including S. frugiperda, M. separata, and H. armigera. The bioassay tests indicated that 3′,3′-c-di-AMP showed the highest antifeedant activity (EC₅₀ = 0.59 mg/L) against M. separata larvae among all the tested CDNs. Regarding insecticidal activity, 2′,3′-c-di-AMP showed higher insecticidal activity against M. separata larvae with LC₅₀ of 55.4 mg/L. RNA-seq further revealed that 3′,3′-c-di-AMP and 2′,3′-c-di-AMP exhibited a significant effect on the growth and development process of insects. More importantly, the bioactivity of 3′,3′-c-di-AMP was also closely correlated with the stimulation of insect immune inflammation. These results indicated that cyclic dinucleotides can affect the normal physiological process of insects, providing a new direction for managing pests.

环状二核苷酸（CDNs）作为一类新型信号分子，在细菌、哺乳动物和昆虫体内发挥着重要的生理作用。然而，CDNs 在农业害虫防治中的应用尚未见报道。为了探索 CDNs 对农业害虫的潜在生物活性，我们合成了 10 种含有腺嘌呤和鸟嘌呤碱基的 CDNs，它们具有不同的核苷酸间连接（3′,3′；2′,3′；2′,2′）。目标 CDNs 被用于测定对常见鳞翅目害虫（包括鞘翅目蚜虫、鳞翅目蚜虫和鞘翅目蚜虫）的抗飞虱和杀虫活性。生物测定结果表明，在所有测试的 CDNs 中，3′,3′-c-di-AMP 对 M. separata 幼虫的抗食性活性最高（EC50 = 0.59 mg/L）。在杀虫活性方面，2′,3′-c-二-AMP 对裂头蝇幼虫的杀虫活性较高，半数致死浓度为 55.4 毫克/升。RNA-seq进一步发现，3′,3′-c-di-AMP和2′,3′-c-di-AMP对昆虫的生长发育过程有显著影响。更重要的是，3′,3′-c-二-AMP 的生物活性还与刺激昆虫免疫炎症密切相关。这些结果表明，环状二核苷酸能影响昆虫的正常生理过程，为治理害虫提供了新的方向。

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引用次数: 0

Nature: Zinc-mediated regulation of nitrogen fixation through transcription factor filamentation in legumes 自然豆科植物中锌通过转录因子丝状化调控固氮作用

Advanced Agrochem

Pub Date : 2024-08-02 DOI: 10.1016/j.aac.2024.07.008

Le Yu, Ying Zhou

Plants maintain their fitness by adjusting their metabolism and gene expression to cope with fluctuating environmental conditions. In legumes, nitrogen homeostasis crucially relies on balancing nitrogen obtained from soil resources with nitrogen fixation performed by symbiotic bacteria within root nodules. Here, we highlight the recent advancements in nitrogen fixation research by Dugald Reid and his colleagues.

植物通过调整新陈代谢和基因表达来应对不断变化的环境条件，从而保持自身的适应能力。在豆科植物中，氮平衡主要依赖于平衡从土壤资源中获得的氮和根瘤内共生细菌的固氮作用。在此，我们重点介绍 Dugald Reid 及其同事在固氮研究方面取得的最新进展。

引用次数: 0

Antimicrobial metabolites produced by the plant growth-promoting rhizobacteria (PGPR): Bacillus and Pseudomonas 植物生长促进根瘤菌（PGPR）产生的抗菌代谢物：芽孢杆菌和假单胞菌

Advanced Agrochem

Pub Date : 2024-07-25 DOI: 10.1016/j.aac.2024.07.007

Yiheng Wang, Yongfu Pei , Xin Wang , Xiongfeng Dai, Manlu Zhu

Plant growth-promoting rhizobacteria (PGPR) such as Bacillus and Pseudomonas have drawn broad attention and interest due to their agricultural benefits. One of the major benefits of PGPR lies at their biocontrol capabilities against various plant pathogens. The biocontrol capability of PGPR is closely related to its capability of producing various kinds of antimicrobial substances. Major antimicrobial secondary metabolites secreted by PGPR include non-ribosomal lipopeptides (NRLPs), polyketides, ribosomal peptides, phenazines, pyrrolnitrins, etc. This review focuses on the major antimicrobial secondary metabolites produced by Bacillus and Pseudomonas including their classifications, structures, mechanisms of action and genetic regulations. We have also discussed their applications in plant biocontrol and provided insights into future development of improved biocontrol strains using synthetic biology approaches.

植物生长促进根瘤菌（PGPR），如芽孢杆菌和假单胞菌，因其对农业的益处而引起了广泛的关注和兴趣。PGPR 的主要益处之一在于它们对各种植物病原体的生物防治能力。PGPR 的生物防治能力与其产生各种抗菌物质的能力密切相关。PGPR 分泌的主要抗菌次生代谢物包括非核糖体脂肽（NRLPs）、多酮类化合物、核糖体肽、吩嗪类化合物、吡咯烷酮类化合物等。本综述重点介绍芽孢杆菌和假单胞菌产生的主要抗菌次级代谢产物，包括它们的分类、结构、作用机制和遗传调控。我们还讨论了它们在植物生物防治中的应用，并对未来利用合成生物学方法开发改良生物防治菌株提出了见解。

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引用次数: 0

Advanced Agrochem

Pub Date : 2024-07-24 DOI: 10.1016/j.aac.2024.07.006

Agus Wedi Pratama, Bambang Piluharto, Nurul Widiastuti, Melbi Mahardika

引用次数: 0

Ethylene and jasmonate as stimulants of latex yield in rubber trees (Hevea brasiliensis): Molecular and physiological mechanisms. A systematic approximation review 乙烯和茉莉酸作为橡胶树（Hevea brasiliensis）乳胶产量的促进剂：分子和生理机制。系统近似综述。

Advanced Agrochem

Pub Date : 2024-07-17 DOI: 10.1016/j.aac.2024.07.003

Nixon Florez-Velasco , Vanessa Florez Ramos , Stanislav Magnitskiy , Helber Balaguera-López

The rubber tree Hevea brasiliensis (Willd. Ex Adr. De Juss.) Müell Arg.] is an important source of latex for the production natural rubber. Natural rubber is an important biopolymer used in various industries, but aspects related to hormonal regulation in biosynthesis are still unknown, which would allow optimizing its production. We review the molecular and physiological mechanisms of increases latex regeneration and flow by the stimulation of rubber trees with exogenous applications of ethylene and jasmonate. We found that the increase in latex regeneration by ethylene is due to the increase in gene level expression and enzymatic activity of key photosynthesis and glycolysis enzymes for the generation of precursors in the first phase of rubber biosynthesis. Latex flow is supported by up-regulated genes in sucrose metabolism such as invertases, induction of sucrose transporters (SUT), and aquaporins (PIP) to maintain flow and turgor pressure in laticifers. Meanwhile, the increase in latex yield mediated by jasmonate may be due to the induction of laticifer differentiation in the long term and in the short term be mediated by the induction of small rubber particles (SRPP) as non-enzymatic cofactors in the production of latex. This information contributes to the knowledge of latex biosynthesis, which allows for a greater support for the exogenous application of jasmonates and ethylene to regulate its production.

橡胶树 Hevea brasiliensis (Willd. Ex Adr. De Juss.) Müell Arg.] 是生产天然橡胶的重要胶乳来源。天然橡胶是一种重要的生物聚合物，被广泛应用于各行各业，但与生物合成过程中的激素调节有关的方面仍然未知，而这些方面将有助于优化天然橡胶的生产。我们回顾了通过外源应用乙烯和茉莉酸盐刺激橡胶树来增加乳胶再生和流动的分子和生理机制。我们发现，乙烯促进乳胶再生的原因是，在橡胶生物合成的第一阶段，生成前体的关键光合作用和糖酵解酶的基因水平表达和酶活性增加。蔗糖代谢基因（如转化酶）的上调、蔗糖转运体（SUT）和水蒸气蛋白（PIP）的诱导支持了乳胶的流动，以维持流胶囊中的流动和张力压力。同时，茉莉酸盐介导的乳胶产量增加，从长期来看可能是由于诱导了胎生植物的分化，从短期来看则是由于诱导了小橡胶颗粒（SRPP）作为乳胶生产中的非酶辅助因子。这一信息有助于了解乳胶的生物合成，从而为外源应用茉莉酸盐和乙烯来调节乳胶的生产提供更多支持。

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引用次数: 0

Scenario-oriented nanopesticides: Shaping nanopesticides for future agriculture 以情景为导向的纳米农药：为未来农业打造纳米农药

Advanced Agrochem

Pub Date : 2024-07-16 DOI: 10.1016/j.aac.2024.07.002

Wenjie Shangguan , Huiping Chen , Pengyue Zhao, Chong Cao, Manli Yu, Qiliang Huang, Lidong Cao

Nanopesticides, as a promising technology, bring scientific and technological impetus to sustainable development and green revolution of agriculture. The excellent physicochemical properties, beneficial biological effects, and functional potential of nanopesticides have significantly contributed to improving utilization rates of pesticides, enhancing pest and disease management, and alleviating stresses. However, agricultural production and plant cultivation are diverse, leading to a wide range of application scenarios for pesticides. These application scenarios put forward more precise requirements and numerous innovative opportunities for the development of nanopesticides. Scenario-oriented nanopesticides are customized for various application scenarios and methods, aligning with the principles of economical, efficient, and sustainable future agriculture. This article outlines the development status of nanopesticides and then reviews the research progress of scenario-oriented nanopesticides, encompassing nine major application scenarios. Finally, the development priorities and prospects of scenario-oriented nanopesticides are summarized, offering innovative concepts for advancement of nanopesticides.

纳米农药作为一项前景广阔的技术，为农业的可持续发展和绿色革命带来了科技动力。纳米农药具有优异的理化性质、有益的生物效应和功能潜力，在提高农药利用率、加强病虫害防治和缓解胁迫等方面做出了重要贡献。然而，农业生产和植物栽培多种多样，导致农药的应用场景也多种多样。这些应用场景为纳米农药的发展提出了更精确的要求和众多创新机会。以应用场景为导向的纳米农药是为各种应用场景和方法量身定制的，符合经济、高效和可持续的未来农业原则。本文概述了纳米农药的发展现状，然后回顾了九大应用场景下情景导向纳米农药的研究进展。最后，总结了情景导向纳米农药的发展重点和前景，为纳米农药的发展提供了创新理念。

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引用次数: 0

Evaluation of mold, yeast and phage contamination of yogurt collected from North of Iran, measurement of their potent natamycin preservative 评估从伊朗北部采集的酸奶中的霉菌、酵母菌和噬菌体污染情况，测定其有效的纳他霉素防腐剂

Advanced Agrochem

Pub Date : 2024-07-01 DOI: 10.1016/j.aac.2024.07.001

Roghayeh Rezaeimalidareh, Mohammad Ahmadi, S. Shahidi, Sahar Aghamirzaei

引用次数: 0

Practical method for the large-scale synthesis of 4′-chloro-2-nitrobiphenyl: A key intermediate of Boscalid 大规模合成 4′-氯-2-硝基联苯的实用方法：Boscalid 的关键中间体

Advanced Agrochem

Pub Date : 2024-06-29 DOI: 10.1016/j.aac.2024.06.002

You Chen, Tong Meng, Rui Guo, Zhaoru Liu, Sixuan Meng, Jian Chen, Guang-Ao Yu

Boscalid is a pesticide with the advantages of broad spectrum bactericidal activity, high efficiency, low toxicity, and no cross-resistance with other fungicides currently available on the market. Herein, we report the synthesis of 4′-chloro-2-nitrobiphenyl, a key intermediate of Boscalid using a palladium-catalyzed Suzuki-Miyaura cross-coupling employing the 2-aryl-substituted indenyl phosphine ligand. 4′-Chloro-2-nitrobiphenyl was prepared in 94 % yield on a 100 g scale. This method allows for the industrial production of alimide and active substances bearing a biphenyl moiety.

Boscalid 是一种杀虫剂，具有广谱杀菌活性、高效、低毒以及与目前市场上的其他杀菌剂无交互抗性等优点。在此，我们报告了利用 2-芳基取代的茚基膦配体，通过钯催化的铃木-宫浦交叉偶联合成 4′-氯-2-硝基联苯的过程，这是 Boscalid 的关键中间体。在 100 克的规模上，4′-氯-2-硝基联苯的制备收率为 94%。利用这种方法可以工业化生产烯丙基酰胺和含有联苯分子的活性物质。

引用次数: 0

AI-driven drug discovery from natural products 人工智能驱动的天然产品药物研发

Advanced Agrochem

Pub Date : 2024-06-25 DOI: 10.1016/j.aac.2024.06.003

Feng-Lei Duan , Chun-Bao Duan , Hui-Lin Xu , Xin-Ying Zhao , Otgonpurev Sukhbaatar , Jie Gao , Ming-Zhi Zhang , Wei-Hua Zhang , Yu-Cheng Gu

The latest review published in Nature Reviews Drug Discovery by Michael W. Mullowney and co-authors focuses on the use of artificial intelligence techniques, specifically machine learning, in natural product drug discovery. The authors discussed various applications of AI in this field, such as genome and metabolome mining, structural characterization of natural products, and predicting targets and biological activities of these compounds. They also highlighted the challenges associated with creating and managing large datasets for training algorithms, as well as strategies to address these obstacles. Additionally, the authors examine common pitfalls in algorithm training and offer suggestions for avoiding them.

Michael W. Mullowney 和合著者在《自然-药物发现评论》（Nature Reviews Drug Discovery）上发表的最新综述重点介绍了人工智能技术（特别是机器学习）在天然产物药物发现中的应用。作者讨论了人工智能在这一领域的各种应用，如基因组和代谢组挖掘、天然产物的结构表征以及预测这些化合物的靶点和生物活性。他们还强调了与创建和管理用于训练算法的大型数据集相关的挑战，以及解决这些障碍的策略。此外，作者还探讨了算法训练中的常见误区，并提出了避免这些误区的建议。

引用次数: 0

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