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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 Q1 Agricultural and Biological Sciences 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 Q1 Agricultural and Biological Sciences 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 Q1 Agricultural and Biological Sciences 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 Q1 Agricultural and Biological Sciences 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
Temporal and regional variability of cumulative ecological risks of pesticides in Japanese river waters for 1990–2010 1990-2010年日本河流农药累积生态风险的时空变异特征
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-02-20 DOI: 10.1584/jpestics.d21-054
T. Nagai, Shunji Yachi, K. Inao
We quantitatively evaluated the cumulative ecological risks from multiple pesticides used in paddy fields in Japan. Moreover, we visualized the temporal and regional variability of those risks for 1990–2010. Considering the region-specific parameters of environmental conditions, region-specific predicted environmental concentrations were estimated at 350 river-flow monitoring sites in Japan. Then the multi-substance potentially affected fraction (msPAF) was calculated as a risk index of multiple pesticides by using the computation tool NIAES-CERAP. The median msPAF values for insecticides and herbicides decreased by 92.4% and 53.1%, respectively, from 1990 to 2010. This substantial reduction in ecological risk was attributed to the development of low-risk pesticides by manufacturers, the efforts of farmers in risk reduction, and tighter regulation by the Japanese government. In particular, the substantial reduction of the ecological risk from insecticides was largely due to the decrease in the use of organophosphorus insecticides.
我们定量评估了日本稻田使用多种杀虫剂的累积生态风险。此外,我们可视化了1990-2010年这些风险的时间和区域变化。考虑到特定区域的环境条件参数,对日本350个河流流量监测点的特定区域预测环境浓度进行了估算。然后利用NIES-CERAP计算工具,将多物质潜在影响因子(msPAF)计算为多种农药的风险指数。从1990年到2010年,杀虫剂和除草剂的msPAF中值分别下降了92.4%和53.1%。生态风险的大幅降低归功于制造商开发的低风险农药、农民在降低风险方面的努力以及日本政府更严格的监管。特别是,杀虫剂的生态风险大幅降低,主要是由于有机磷杀虫剂的使用减少。
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引用次数: 0
Insect growth regulators with hydrazide moiety inhibit strigolactone biosynthesis in rice 具有酰肼部分的昆虫生长调节剂抑制水稻中三羟内酯的生物合成
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-02-20 DOI: 10.1584/jpestics.D21-063
Kojiro Kawada, Yasuyuki Sasaki, T. Asami, S. Yajima, S. Ito
Strigolactones (SLs) are carotenoid-derived plant hormones involved in several growth and developmental processes. Also, SLs are allelochemicals that induce the seed germination of root parasitic plants and the hyphal branching of arbuscular mycorrhizal fungi. In this study, to identify novel lead chemicals that inhibit SL biosynthesis, we evaluated the effect of agrochemicals on SL biosynthesis. We found that the diacylhydrazine insect growth regulator, chromafenozide, reduced the endogenous level of 4-deoxyorobanchol (4DO), a major SL in rice. Furthermore, treatment with the same class of insect growth regulator, methoxyfenozide, also resulted in the reduction of 4DO levels in rice root exudates. These results suggest that chromafenozide and methoxyfenozide are novel lead inhibitors of SL biosynthesis.
Strigolactones(SL)是类胡萝卜素衍生的植物激素,参与多种生长发育过程。此外,SL是诱导根寄生植物种子发芽和丛枝菌根真菌菌丝分枝的化感物质。在本研究中,为了鉴定抑制SL生物合成的新型先导化学品,我们评估了农用化学品对SL生物合成的影响。我们发现,昆虫生长调节剂二酰肼chromafenozide降低了水稻中主要SL 4-脱氧欧班醇(4DO)的内源水平。此外,用同一类昆虫生长调节剂甲氧基苯并咪唑处理也降低了水稻根系分泌物中的4DO水平。这些结果表明,色马菲酰肼和甲氧基非诺肼是SL生物合成的新的主要抑制剂。
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引用次数: 2
Synthesis and antifungal activity of the proposed structure of a volatile compound isolated from the edible mushroom Hypsizygus marmoreus 一种从食用菌Hypsizygus marmoreus中分离的挥发性化合物的合成及其抗真菌活性
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-02-20 DOI: 10.1584/jpestics.D21-061
Nguyen Thi Ngoc Anh, Daisuke Miyaji, Kumiko Osaki-Oka, Tatsuo Saito, A. Ishihara, A. Yajima
We synthesized the proposed structure of an antifungal compound detected in the culture broth of the edible mushroom Hypsizygus marmoreus. Using the Evans aldol and Abiko–Masamune aldol reactions as the key steps, we synthesized all of the stereoisomers of the compound with high stereoselectivity. The GC retention times and the fragmentation patterns in the mass spectra of the synthesized isomers did not match those of the natural product. Therefore, this result may imply that it is necessary to reisolate the natural product and reconsider its structure. All of the synthesized isomers were found to exhibit antifungal activity against the phytopathogenic fungus Alternaria brassicicola. Due to their simple structures, the obtained isomers could be lead compounds for new pesticides.
我们合成了一种在食用菌海绵菌培养液中检测到的抗真菌化合物的拟议结构。以Evans羟醛和Abiko–Masamune羟醛反应为关键步骤,合成了该化合物所有具有高立体选择性的立体异构体。合成异构体的GC保留时间和质谱中的碎片模式与天然产物的不匹配。因此,这一结果可能意味着有必要重新分离天然产物并重新考虑其结构。所有合成的异构体都对植物病原真菌油菜链格孢具有抗真菌活性。由于其结构简单,所获得的异构体可能是新农药的先导化合物。
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引用次数: 0
Root exudation of prometryn and its metabolites from Chinese celery (Apium graveolens) 芹菜中prometryn及其代谢产物的根分泌物
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-02-20 DOI: 10.1584/jpestics.d21-035
Yingai Gui, Wei-Dong Yu, Xiangwu Ge, Haiyan Li, Chengpeng Sun, Xiqin Mao, Kuijing Yuan
Root exudates from Chinese celery (Apium graveolens) and Chinese cabbage (pak choi, Brassica chinensis) plants treated by prometryn, an herbicide, were qualitatively and quantitatively investigated and compared under hydroponic cultivation. Prometryn and its metabolites released into the nutrient solution were analyzed by ultra-performance liquid chromatograph coupled with orbitrap mass spectrometer to investigate whether this xylem-mobile herbicide is exuded from the roots. The results showed that celery and pak choi had different root exudation profiles. Celery metabolized prometryn to prometryn sulfoxide and released both compounds from the roots. In contrast, pak choi barely metabolized or actively released prometryn from the roots. The concentration of prometryn sulfoxide released from celery after 96 hr was 21 µg/L, which was nearly one-third that of released prometryn. Our results indicate that the root exudation and translocation of xylem-mobile herbicides could be significant in plants and are highly species dependent compared with phloem-mobile herbicides.
在水培条件下,对异丙灵处理的芹菜(Apium graveolens)和大白菜(pak choi,Brassica chinensis)根系分泌物进行了定性和定量研究和比较。采用超高效液相色谱联用orbittrap质谱仪对Prometryn及其代谢产物释放到营养液中进行分析,以研究这种木质部流动除草剂是否从根部渗出。结果表明,芹菜和小白菜的根系分泌物特征不同。芹菜将异丙素代谢为异丙素亚砜,并从根中释放出这两种化合物。相比之下,小白菜几乎没有代谢或从根部主动释放异丙素。芹菜96年后释放的异丙素亚砜浓度 小时为21 µg/L,几乎是释放的异丙肾上腺素的三分之一。我们的研究结果表明,木质部流动除草剂的根系渗出和移位在植物中可能是显著的,并且与韧皮部流动除草剂相比具有高度的物种依赖性。
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引用次数: 2
期刊
Journal of Pesticide Science
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