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Discovery of novel pyridine carboxamides with antifungal activity as potential succinate dehydrogenase inhibitors. 具有抗真菌活性的新型吡啶类羧胺类琥珀酸脱氢酶抑制剂的发现。
IF 2.4 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-08-20 DOI: 10.1584/jpestics.D22-017
Zhongzhong Yan, Zihui Yang, Longjian Qiu, Yan Chen, Aijun Li, Taopeng Chang, Xinzhe Niu, Jingyan Zhu, Shihao Wu, Feng Jin

Fifteen novel pyridine carboxamide derivatives bearing a diarylamine-modified scaffold were designed, synthesized, and their antifungal activity was evaluated. Preliminary bioassay results showed that some of the synthesized compounds exhibited moderate to good in vitro antifungal activity. Further, compound 6-chloro-N-(2-(phenylamino)phenyl)nicotinamide (3f) displayed good in vivo antifungal activity against Botrytis cinerea. The enzymatic test on B. cinerea succinate dehydrogenase (SDH) showed that the inhibitory activity possessed by compound 3f equally matches that of thifluzamide. Molecular docking results demonstrated that compound 3f could commendably dock with the active site of SDH via stable hydrogen bonds and hydrophobic interactions, suggesting the possible binding modes of the title compounds with SDH. The results above revealed that the target compounds would be the leading fungicide compound for further investigation.

设计、合成了15种新型二芳胺修饰吡啶羧胺衍生物,并对其抗真菌活性进行了评价。初步的生物试验结果表明,部分合成的化合物具有中等到良好的体外抗真菌活性。此外,化合物6-氯- n -(2-(苯基氨基)苯基)烟酰胺(3f)在体内对灰霉病菌具有良好的抗真菌活性。酶学试验表明,化合物3f对葡萄球菌琥珀酸脱氢酶(SDH)的抑制活性与硫氟唑胺相当。分子对接结果表明,化合物3f可以通过稳定的氢键和疏水相互作用与SDH活性位点很好地对接,提示了标题化合物与SDH可能的结合方式。上述结果表明,目标化合物将是进一步研究的主要杀菌剂化合物。
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引用次数: 0
Emerging technologies for the chemical control of root parasitic weeds. 根寄生杂草化学防治的新技术。
IF 2.4 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-08-20 DOI: 10.1584/jpestics.D22-045
Kojiro Kawada, Tomoyuki Koyama, Ikuo Takahashi, Hidemitsu Nakamura, Tadao Asami

Parasitic plants in the Orobanchaceae family include devastating weed species, such as Striga, Orobanche, and Phelipanche, which parasitize major crops, drastically reduces crop yields and cause economic losses of over a billion US dollars worldwide. Advances in basic research on molecular and cellular processes responsible for parasitic relationships has now achieved steady progress through advances in genome analysis, biochemical analysis and structural biology. On the basis of these advances it is now possible to develop chemicals that control parasitism and reduce agricultural damage. In this review we summarized the recent development of chemicals that can control each step of parasitism from strigolactone biosynthesis in host plants to haustorium formation.

寄生虫科的寄生植物包括具有破坏性的杂草物种,如斯特里加、Orobanche和菲利潘切,它们寄生在主要作物上,严重降低作物产量,并在全球造成超过10亿美元的经济损失。通过基因组分析、生化分析和结构生物学的进展,寄生关系的分子和细胞过程的基础研究取得了稳步进展。在这些进展的基础上,现在有可能开发出控制寄生和减少农业损害的化学品。本文综述了近年来控制寄生各阶段的化学物质的研究进展,从寄主植物的独角兽内酯生物合成到吸器的形成。
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引用次数: 0
Biological soil disinfestation compatible with renewable energy production for sustainable agriculture. 生物土壤消毒与可再生能源生产兼容,促进可持续农业。
IF 1.5 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-08-20 DOI: 10.1584/jpestics.D22-010
Shaohua Chen, Tatsuya Hirano, Yoshiaki Hayashi, Hiroto Tamura

Biological soil disinfestation (BSD) is biotechnology to control soil-borne plant pathogens based on the anaerobic-reducing environment in soil and the functions of indigenous microbes. A new sustainable agricultural technology, the GET system, which produces and recovers methane as renewable energy from paddy fields, has a structure and principles similar to those of BSD technology. To confirm the potential of the GET system as BSD technology, the microbial community structures in the GET system were analyzed using next-generation sequencing. Thirty-four phyla were detected: 31 bacterial and 3 archaeal. Firmicutes dominated during the experimental period, which plays an important role in BSD functions such as organic decomposition, nitrate removal, and soil-borne pathogen elimination. The ability of the GET system to control soil-borne pathogens as well as produce renewable energy was demonstrated.

土壤生物消毒(BSD)是一种基于土壤中的厌氧还原环境和本地微生物的功能来控制土传植物病原体的生物技术。一种新的可持续农业技术,即 GET 系统,可从稻田中生产和回收甲烷作为可再生能源,其结构和原理与 BSD 技术相似。为了证实 GET 系统作为 BSD 技术的潜力,我们使用新一代测序技术分析了 GET 系统中的微生物群落结构。共检测到 34 个门类:31 个细菌门和 3 个古细菌门。在实验期间,固着菌占主导地位,在有机物分解、硝酸盐去除和土传病原体消除等 BSD 功能中发挥着重要作用。GET 系统在控制土传病原体和生产可再生能源方面的能力得到了证明。
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引用次数: 0
Development of a rice herbicide, fenquinotrione. 水稻除草剂芬喹诺酮的研制。
IF 2.4 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-08-20 DOI: 10.1584/jpestics.J22-02
Atsushi Nagamatsu, Ken Ueda, Ryuji Tamai, Shinki Tani, Shunsuke Yamamoto

Fenquinotrione is a novel rice herbicide that was discovered and developed by Kumiai Chemical Industry Co., Ltd. It can control a wide range of broadleaf and sedge weeds with excellent rice selectivity at 30 g a.i./10 a and is as effective as the wild type on acetolactate synthase inhibitor-resistant weeds. Our metabolic and molecular biological studies showed that CYP81A6-mediated demethylation and subsequent glucose conjugation are responsible for the safety of fenquinotrione in rice. Fenquinotrione was registered in Japan in 2018, and various products containing fenquinotrione have been launched. With its high efficacy and excellent rice selectivity, we believe that fenquinotrione will contribute to efficient food production in the future.

芬喹诺酮是Kumiai化学工业有限公司发现并开发的一种新型水稻除草剂。对阔叶杂草和莎草杂草有广泛的防治作用,对水稻有很好的选择性。/10 a,对抗乙酰乳酸合酶抑制剂杂草的效果与野生型相同。我们的代谢和分子生物学研究表明,cyp81a6介导的去甲基化和随后的葡萄糖偶联是芬喹诺酮在水稻中的安全性的原因。芬喹诺酮于2018年在日本注册,并推出了多种含有芬喹诺酮的产品。我们相信,芬喹诺酮具有高效的药效和优异的水稻选择性,将为未来的高效粮食生产做出贡献。
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引用次数: 0
Structural insights into the interaction between gabazine (SR-95531) and Laodelphax striatellus GABA receptors. gabazine (SR-95531)与纹状线虫GABA受体相互作用的结构研究。
IF 2.4 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-05-20 DOI: 10.1584/jpestics.D22-007
Yuki Fujie, Genyan Liu, Fumiyo Ozoe, Yoshihisa Ozoe

γ-Aminobutyric acid receptors (GABARs) mediate fast inhibitory neurotransmission and are targets for insecticides. GABARs are composed of five subunits, the composition of which dictates the pharmacological characteristics of GABARs. Both competitive and noncompetitive GABAR antagonists can be used as insecticides. Gabazine is a potent competitive antagonist of mammalian α1β2γ2 GABARs; however, it is less potent against insect GABARs. To explore how gabazine interacts with GABARs, we examined whether the sensitivity of the small brown planthopper (Laodelphax striatellus) RDL GABAR (LsRDLR) to gabazine is increased when its amino acid residues are substituted with α1β2γ2 GABAR residues. In the results, two of the generated mutants showed enhanced gabazine sensitivity. Docking simulations of gabazine using LsRDLR homology models and an α1β2γ2 GABAR cryo-EM structure revealed that the accommodation of gabazine into the "aromatic box" in the orthosteric site lowered the binding energy. This information may help in designing GABAR-targeting insecticides with novel modes of action.

γ-氨基丁酸受体(gabar)介导快速抑制性神经传递,是杀虫剂的靶点。gabar由五个亚基组成,它们的组成决定了gabar的药理学特性。竞争性和非竞争性GABAR拮抗剂都可用作杀虫剂。Gabazine是一种有效的哺乳动物α1β2γ2 gabar的竞争性拮抗剂;然而,它对昆虫gabar的作用较弱。为了探究gabazine与GABARs的相互作用机制,我们检测了当小褐飞虱(Laodelphax striatellus) RDL GABAR (LsRDLR)的氨基酸残基被α1β2γ2 GABAR残基取代时,gabazine对gabazine的敏感性是否增加。结果显示,产生的两个突变体显示出增强的gabazine敏感性。利用LsRDLR同源模型和α1β2γ2 GABAR低温电镜结构对gabazine进行对接模拟,结果表明,gabazine被安置在正构位的“芳香盒子”中,降低了结合能。这些信息可能有助于设计具有新型作用模式的gabar靶向杀虫剂。
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引用次数: 0
Permeability of the fish intestinal membrane to bulky chemicals. 鱼类肠膜对大体积化学物质的渗透性。
IF 1.5 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-05-20 DOI: 10.1584/jpestics.D21-055
Chiyoko Miyata, Yoshihide Matoba, Makiko Mukumoto, Yoshiaki Nakagawa, Hisashi Miyagawa

The ability to predict the environmental behavior of chemicals precisely is important for realizing more rational regulation. In this study, the bioaccumulation of nine chemicals of different molecular weights absorbed via the intestinal tract was evaluated in fish using the everted gut sac method. The amounts of chemicals that passed through the intestinal membrane after a 24-hr exposure were significantly decreased for chemicals with MW≥548 and Dmax min≥15.8 Å (or Dmax aver≥17.2 Å). These thresholds are consistent with those previously proposed in terms of MW (>800) and molecular size (Dmax min>15.6 Å or Dmax aver>17.1 Å) for the limit of permeable chemicals through the gill membrane. The results show that the same MW and Dmax criteria can be used to predict low bioaccumulation through both the gill membrane and the intestinal tract. These findings are helpful in reducing the need to conduct animal tests in environmental safety studies.

准确预测化学品的环境行为对于实现更合理的监管非常重要。本研究采用常温肠囊法评估了鱼类经肠道吸收的九种不同分子量化学物质的生物累积性。在暴露 24 小时后,通过肠膜的化学物质的数量在截留分子量≥548 和最小截留分子量≥15.8 Å(或平均截留分子量≥17.2 Å)的化学物质中显著减少。这些阈值与之前提出的化学物质通过鳃膜的渗透极限的截留分子量(>800)和分子大小(最小截留分子量>15.6 Å 或平均截留分子量>17.1 Å)一致。结果表明,相同的 MW 和 Dmax 标准可用于预测通过鳃膜和肠道的低生物蓄积性。这些发现有助于减少在环境安全研究中进行动物试验的必要性。
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引用次数: 0
Effects of temperature and humidity on the contact angle of pesticide droplets on rice leaf surfaces. 温度和湿度对水稻叶片表面农药滴接触角的影响。
IF 2.4 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-05-20 DOI: 10.1584/jpestics.D21-068
Jiantao Zhang, Tengyuan Zhou, Jiajun Zeng, Xuanchun Yin, Yubin Lan, Sheng Wen

The effects of external factors such as temperature, humidity, pesticide formulation, and pesticide concentration on the contact angle of pesticide droplets on rice leaf surfaces were analyzed. The experiments showed that there were significant differences in the contact angles of droplets on the leaf surfaces under different temperatures and humidity. As the ambient temperature increased, the contact angle first decreased and then increased, reaching a minimum value at 25°C. With a gradual increase in humidity, the contact angle significantly increased and reached a maximum at 100% humidity. Finally, it was concluded that both the formulation and concentration of the pesticide had a significant effect on the contact angle of droplets on rice leaf surfaces. The experiments also illustrated that the effects of the pesticide formulation and concentration on the contact angle were more significant than those of temperature and humidity.

分析了温度、湿度、农药配方、农药浓度等外界因素对水稻叶片表面农药液滴接触角的影响。实验表明,不同温度和湿度条件下,液滴在叶片表面的接触角存在显著差异。随着环境温度的升高,接触角先减小后增大,在25℃时达到最小值。随着湿度的逐渐增大,接触角显著增大,在100%湿度时达到最大值。最后得出结论,农药配方和浓度对水稻叶片表面雾滴接触角有显著影响。实验还表明,农药配方和浓度对接触角的影响比对温度和湿度的影响更为显著。
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引用次数: 4
Mortality of Orius insidiosus by contact with spinosad in the laboratory as well as in the field and a perspective of these as controllers of Frankliniella occidentalis. 实验室和野外与棘球菊接触对隐孔螟死亡率的影响及其防治西富兰克林蝇的效果观察。
IF 2.4 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-05-20 DOI: 10.1584/jpestics.D22-012
Samuel Cruz-Esteban, Irais Brito-Bonifacio, David Estrada-Valencia, Edith Garay-Serrano

Orius insidiosus, known as the pirate bug, is widely distributed throughout the Americas. It is employed for the biological control of Frankliniella occidentalis in organic berry crops in Mexico. In conventional crops, spinosad is the main control method for this pest. The LD50 of spinosad on O. insidiosus was determined. In addition, we monitored the population density of F. occidentalis in blackberry crops under two types of management (biochemical+mass trapping, and biological control). The LD50 was 225.65 ppm 3.8 times greater than the 60 ppm dose commonly used in blackberry crops. Both types of control are efficient; however, spinosad is less effective and should be combined with other environmentally friendly strategies. The possibility of combining chromatic traps+spinosad application and chromatic traps+strategic release of O. insidiosus to effectively control thrips without compromising fruit quality is discussed.

Orius insidiosus,被称为海盗虫,广泛分布在整个美洲。该方法用于墨西哥有机浆果作物的西富兰克林菌生物防治。在常规作物中,多酚是防治这种害虫的主要方法。测定了棘糖苷对毒蛾的LD50。此外,我们还监测了两种管理方式(生化+质量诱捕和生物防治)下黑莓作物中西叶蚜的种群密度。LD50为225.65 ppm,是黑莓作物中常用的60 ppm剂量的3.8倍。这两种控制都是有效的;然而,spinosad效果较差,应与其他环境友好型战略结合使用。探讨了色诱+施棘糖和色诱+策略放生在不影响果实品质的前提下有效防治蓟马的可能性。
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引用次数: 0
Studies on the inhibition of methanogenesis and dechlorination by (4-hydroxyphenyl) chloromethanesulfonate. 研究(4-羟基苯基)氯甲烷磺酸盐对甲烷生成和脱氯的抑制作用。
IF 1.5 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-05-20 DOI: 10.1584/jpestics.D21-071
Yudai Hotta, Chizu Yagoshi, Ryo Okazaki, Mitsumasa Ikeda

The purpose of this study was to demonstrate the inhibitory effect of chemicals on methane emissions in paddy soil. We found that (4-hydroxyphenyl) chloromethanesulfonate (C-1) has a methanogenic inhibition activity, and we studied its inhibition mechanism using laboratory tests. The study found that C-1 treatment of flooded soil did not significantly affect the bacterial community but rather the archaeal community; particularly, Methanosarcina spp. C-1 strongly inhibited the aceticlastic methanogenesis route. It was suggested that the inhibitory target of C-1 was different from the well-known methanogenic inhibitor 2-bromoethanesulfonate, which targets methyl-coenzyme M reductase of methanogen. In addition, C-1 had a secondary effect of inhibiting the dechlorination of chlorophenols. Although field trials are required as the next development step, C-1 can be used to reduce methane emissions from paddy fields, one of the largest sources in the agricultural sector.

本研究的目的是证明化学物质对稻田土壤中甲烷排放的抑制作用。我们发现(4-羟基苯基)氯甲磺酸盐(C-1)具有抑制甲烷生成的活性,并通过实验室试验研究了其抑制机制。研究发现,C-1 对淹水土壤的处理对细菌群落没有明显影响,但对古细菌群落有明显影响,尤其是对 Methanosarcina spp. C-1 对醋酸菌甲烷生成途径有强烈的抑制作用。研究表明,C-1 的抑制靶标不同于著名的甲烷生成抑制剂 2-溴乙基磺酸盐,后者的靶标是甲烷菌的甲基辅酶 M 还原酶。此外,C-1 还具有抑制氯酚脱氯的副作用。虽然下一步开发工作还需要进行实地试验,但 C-1 可用于减少农业部门最大的甲烷排放源之一--水稻田的甲烷排放。
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引用次数: 0
Engineering of Bacillus thuringiensis insecticidal proteins. 苏云金芽孢杆菌杀虫蛋白的工程研究。
IF 2.4 4区 农林科学 Q2 ENTOMOLOGY Pub Date : 2022-05-20 DOI: 10.1584/jpestics.D22-016
Takashi Yamamoto

Bacillus thuringiensis (Bt) has been used as sprayable pesticides for many decades. Bt strains utilized in these products produce multiple insecticidal proteins to complement a narrow insect specificity of each protein. In the late 1990s, genes encoding Bt insecticidal proteins were expressed in crop plants such as cotton and corn to protect these crops from insect damage. The first Bt protein used in transgenic cotton was Cry1Ac to control Heliothis virescens (tobacco budworm). Cry1Ab was applied to corn to control Ostrinia nubilalis (European corn borer). Since these insects have developed resistance to Cry1Ac and Cry1Ab, new Bt proteins are required to overcome the resistance. In order to protect corn furthermore, it is desired to control Diabrotica virgifera (Western corn rootworm), Helicoverpa zea (corn earworm) and Spodoptera frugiperda (fall armyworm). Recently, many new Bt insecticidal proteins have been discovered, but most of them require protein engineering to meet the high activity standard for commercialization. The engineering process for higher activity necessary for Bt crops is called optimization. The seed industry has been optimizing Bt insecticidal proteins to improve their insecticidal activity. In this review, several optimization projects, which have led to substantial activity increases of Bt insecticidal proteins, are described.

苏云金芽孢杆菌(Bacillus thuringiensis, Bt)作为喷雾农药已经使用了几十年。这些产品中使用的Bt菌株产生多种杀虫蛋白,以补充每种蛋白的狭窄昆虫特异性。在20世纪90年代末,编码Bt杀虫蛋白的基因在棉花和玉米等作物中表达,以保护这些作物免受昆虫的伤害。第一个用于转基因棉花的Bt蛋白是用于防治烟草芽虫的Cry1Ac。将Cry1Ab用于玉米防治欧洲玉米螟(Ostrinia nubilalis)。由于这些昆虫已经对Cry1Ac和Cry1Ab产生了抗性,因此需要新的Bt蛋白来克服这种抗性。为了进一步保护玉米,应防治玉米根虫、玉米耳虫和秋粘虫。近年来,人们发现了许多新的Bt杀虫蛋白,但它们大多需要通过蛋白质工程才能达到较高的活性标准。Bt作物所需的提高活性的工程过程被称为优化。种业一直在优化Bt杀虫蛋白,以提高其杀虫活性。本文综述了几个优化项目,这些项目已导致Bt杀虫蛋白活性的大幅提高。
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引用次数: 3
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Journal of Pesticide Science
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