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The structure–activity relationship of aryloxyacetylthioureas for the inhibition of <i>Orobanche minor</i> radicle elongation 芳基氧乙酰硫脲抑制&lt;i&gt;小环切菌&lt;/i&gt的构效关系胚根伸长
4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2023-01-01 DOI: 10.1584/jpestics.d23-034
Atsushi Okazawa, Shizuki Noda, Yusuke Mimura, Kotaro Fujino, Takatoshi Wakabayashi, Daisaku Ohta, Yukihiro Sugimoto, Motohiro Sonoda
Orobanchaceae root parasitic weeds cause significant damage to agriculture and become threats to global food security. Integrated pest management is a key concept in modern agriculture and requires chemicals with various modes of action. Planteose accumulates as a storage carbohydrate in the dry seeds of root parasitic weeds. In Orobanche minor seeds, planteose is hydrolyzed by an α-galactosidase, OmAGAL2, during germination. It was found that the OmAGAL2 inhibitor, PI-28, suppressed the radicle elongation of germinating O. minor seeds. This inhibitory activity against O. minor radicle elongation was evaluated for a series of aryloxyacetylthioureas synthesized based on the structure of PI-28. Compounds with a 3-Cl or 4-Cl substituent on the benzene ring in the phenoxy moiety in PI-28 exhibited more potent activity than the parent PI-28. This is the first report on the effect of aryloxyacetylthioureas on a root parasitic weed and will contribute to the development of control reagents for root parasitic weeds.
根寄生杂草对农业造成严重危害,对全球粮食安全构成威胁。有害生物综合治理是现代农业的一个重要概念,需要多种作用方式的化学品。植物糖作为储存碳水化合物在根寄生杂草的干燥种子中积累。在Orobanche minor种子中,植物糖在萌发时被α-半乳糖苷酶OmAGAL2水解。发现OmAGAL2抑制剂PI-28抑制萌发的O. minor种子的胚根伸长。以PI-28的结构为基础合成了一系列芳基乙酰硫脲,并对其自由基伸长的抑制活性进行了评价。PI-28苯氧基部分苯环上含有3-Cl或4-Cl取代基的化合物比母体PI-28具有更强的活性。本文首次报道了芳基乙酰硫脲对根寄生杂草的防治作用,为根寄生杂草防治试剂的开发提供参考。
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引用次数: 0
Fugacity model incorporating computational fluid dynamics for analyzing the behavior of an insecticide sprayed indoors 结合计算流体动力学的逸度模型用于分析室内喷洒杀虫剂的行为
4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2023-01-01 DOI: 10.1584/jpestics.d23-011
Sayuri Tanaka, Yoshihide Matoba, Hiroaki Kondo, Tomohiko Ihara
Fugacity models are used widely to predict the time-dependent behaviors of chemicals in environments containing several media (e.g., air, sediment, soil, and water). However, these fugacity models work on the assumption that the concentration of a chemical in each medium is uniform, so they cannot describe the spatial distribution of the chemical. We developed a new fugacity model, termed InPestCFD, incorporating computational fluid dynamics to describe both the time-dependent distribution and the spatial distribution of a chemical in a medium. InPestCFD was used to calculate the behavior of an insecticide released from an aerosol canister in a room. Indoor airflow and aerosol particle behavior were calculated via computational fluid dynamics and using a Lagrangian dispersion model. Transport of the insecticide among media (aerosol particles, air, ceiling, floor, and walls) was calculated using the fugacity model. The time-dependent distributions and spatial distributions of the insecticide in the media agreed well with real measurements.
逸度模型被广泛用于预测化学物质在含有多种介质(如空气、沉积物、土壤和水)的环境中随时间变化的行为。然而,这些逸度模型是在假设每种介质中化学物质的浓度是均匀的前提下工作的,因此它们不能描述化学物质的空间分布。我们开发了一种新的逸度模型,称为InPestCFD,它结合了计算流体动力学来描述介质中化学物质的时间依赖性分布和空间分布。InPestCFD用于计算室内气溶胶罐中释放的杀虫剂的行为。通过计算流体力学和拉格朗日色散模型计算了室内气流和气溶胶颗粒的行为。使用逸度模型计算杀虫剂在介质(气溶胶颗粒、空气、天花板、地板和墙壁)之间的迁移。杀虫剂在介质中的时空分布与实测结果吻合较好。
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引用次数: 0
Characteristics biological activities of the novel acaricide flupentiofenox against phytophagous mites 新型杀螨剂氟虫腈对植食性螨的生物学活性研究
4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2023-01-01 DOI: 10.1584/jpestics.d23-033
Shingo Yoshimura, Shigeyuki Mukawa
Flupentiofenox, which has a unique chemical structure, is a novel acaricide that has been developed by the Kumiai Chemical Industry Co., Ltd. Flupentiofenox exerted significant acaricidal activities against spider mites Tetranychus urticae and Panonychus citri at all developmental stages even at extremely low concentrations, as compared with its practical concentration (80 ppm) for use in mites and was effective against spider mite populations that are resistant to widely used commercial acaricides. These results suggested that flupentiofenox could be used effectively for the control and prevention of spider mite infestation. Additionally, flupentiofenox had a more rapid effect than acetyl CoA carboxylase inhibitors, but it had a relatively slower effect than mitochondrial electron transport inhibitors and glutamate-gated chloride channel modulators. Overall, flupentiofenox is assumed to have a new mode of action.
fluupentiofenox是Kumiai化学工业有限公司开发的一种新型杀螨剂,具有独特的化学结构。与螨虫的实际使用浓度(80 ppm)相比,氟虫芬诺在所有发育阶段对荨叶螨和柑橘全爪螨都具有显著的杀螨活性,并且对对广泛使用的商业杀螨剂产生抗性的蜘蛛螨种群有效。结果表明,氟虱螨可有效防治蜘蛛螨的侵害。此外,氟哌啶芬诺比乙酰辅酶a羧化酶抑制剂起效更快,但比线粒体电子传递抑制剂和谷氨酸门控氯通道调节剂起效相对较慢。总的来说,fluupentiofenox被认为具有一种新的作用模式。
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引用次数: 0
Discovery of a novel acaricide, acynonapyr 发现一种新的杀螨剂,无虫螨
4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2023-01-01 DOI: 10.1584/jpestics.d23-028
Isami Hamamoto, Masahiro Kawaguchi, Takehiko Nakamura, Makio Yano, Keiji Koizumi, Jun Takahashi
Acynonapyr, discovered by Nippon Soda Co., Ltd., is a novel acaricide with N-pyridyloxy azabicycle as a unique core structure. Acynonapyr exhibits high activity against the spider mite species in the genera Tetranychus and Panonychus, with good efficacy at all life stages. Early in this research, cyclic amines substituted with (hetero)aryl(oxy) moieties were designed as target molecules and diversely synthesized, and 4-[4-(trifluoromethyl)phenoxy]-1-[5-(trifluoromethyl)-2-pyridyl]piperidine was found to show weak acaricidal activity. The structural optimization of this acaricidal active piperidine as the first lead compound led to the discovery of acynonapyr. In this report, our research process that led to the discovery of acynonapyr is described.
Acynonapyr是日本汽水公司发现的一种新型杀螨剂,其独特的核心结构为n -吡啶氧基氮杂二环。对叶螨属和全爪螨属的螨类均有较强的杀灭作用,且在各个生命阶段均有良好的杀灭效果。本研究早期以(杂)芳基(氧)基取代的环胺为靶分子,进行了多种合成,发现4-[4-(三氟甲基)苯氧基]-1-[5-(三氟甲基)-2-吡啶]哌啶具有较弱的杀螨活性。该杀螨活性胡椒碱作为第一个先导化合物进行结构优化,从而发现了刺虫精。在这篇报告中,我们的研究过程导致了acynonapyr的发现。
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引用次数: 0
A simple reliable quantification of glyphosate in human urine using MonoSpin TiO extraction and isotope dilution mass spectrometry 单旋钛萃取和同位素稀释质谱法测定人尿中草甘膦的简单可靠的定量
4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2023-01-01 DOI: 10.1584/jpestics.d23-030
Takamitsu Otake, Keisuke Nakamura, Nobuyasu Hanari
A method of quantifying glyphosate (Gly) in human urine by means of MonoSpin TiO extraction and 9-fluorenylmethoxycarbonyl chloride (FMOC-Cl) derivatization with isotope dilution mass spectrometry (IDMS) was investigated and optimized. The method’s quantification limit under optimized conditions was 0.3 µg/kg for FMOC-Gly, which was comparable to or lower than those described in previous studies. When a spike test using human urine samples was carried out with optimized analytical conditions, the trueness for FMOC-Gly was as follows: 101.6–104.9% for a spike level of 0.5 µg/kg and 99.2–101.0% for a spike level of 30 µg/kg. The intra-day repeatability and inter-day reproducibility were <6.5%. The spike test results for validation between the “with” and “without” derivatization methods were comparable at 1 µg/kg. Our results indicate that using MonoSpin TiO extraction and FMOC-Cl derivatization with IDMS is an accurate method for analyzing Gly in human urine.
研究了单旋TiO萃取- 9-氟酰甲氧羰基氯(FMOC-Cl)衍生-同位素稀释质谱法(IDMS)测定人尿中草甘膦(Gly)含量的方法并进行了优化。优化条件下,FMOC-Gly的定量限为0.3µg/kg,与前人研究结果相当或更低。在优化的分析条件下,对人尿样品进行尖峰检测,FMOC-Gly的准确率为:尖峰水平为0.5µg/kg时为101.6 ~ 104.9%,尖峰水平为30µg/kg时为99.2 ~ 101.0%。日内重复性和日内重复性均<6.5%。“有”衍生化和“没有”衍生化方法之间验证的峰值测试结果在1µg/kg时具有可比性。本研究结果表明,单旋体TiO萃取和IDMS - FMOC-Cl衍生化是一种准确分析人尿中甘氨酸的方法。
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引用次数: 0
Basic Technology and Recent Trends in Agricultural Formulation and Application Technology. 农业配方与应用技术的基础技术与最新趋势。
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-11-20 DOI: 10.1584/jpestics.D22-055
Takeo Ohkouchi, Kozo Tsuji

Recent requirements of the pesticide industry have become much severer, and pesticides (formulated products) are required to satisfy higher safety to both human beings and the environment, higher biological efficacy, lower price, and labor-saving. This review explains the outline of basic pesticide formulation technology, followed by recent advances in developing new formulations and application technologies. Labor-saving formulations and application technologies, environmental load reduction technologies, and user-friendly formulations and application technologies are elucidated.

近年来,农药行业对农药的要求越来越高,要求农药(配方产品)对人类和环境的安全性更高、生物功效更高、价格更低、更省力。本文概述了农药基本配方技术,并介绍了新配方的开发和应用技术的最新进展。阐述了省力配方及应用技术、环保减载技术、人性化配方及应用技术。
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引用次数: 1
Author Index to Volume 47, 2022 作者索引到第47卷,2022年
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-11-20 DOI: 10.1584/jpestics.a22-03
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引用次数: 0
Reconfiguring the online tool of SkinSensPred for predicting skin sensitization of pesticides. 重新配置SkinSensPred在线工具,用于预测农药的皮肤致敏性。
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-11-20 DOI: 10.1584/jpestics.D22-043
Chia-Chi Wang, Shan-Shan Wang, Chun-Lin Liao, Wei-Ren Tsai, Chun-Wei Tung

Adverse outcome pathway (AOP)-based computational models provide state-of-the-art prediction for human skin sensitizers and are promising alternatives to animal testing. However, little is known about their applicability to pesticides due to scarce pesticide data for evaluation. Moreover, pesticides traditionally have been tested on animals without human data, making validation difficult. Direct application of AOP-based models to pesticides may be inappropriate since their original applicability domains were designed to maximize reliability for human response prediction on diverse chemicals but not pesticides. This study proposed to identify a consensus chemical space with concordant human responses predicted by the SkinSensPred online tool and animal testing data to reduce animal testing. The identified consensus chemical space for non-sensitizers achieved high concordance of 85% and 100% for the cross-validation and independent test, respectively. The reconfigured SkinSensPred can be applied as the first-tier tool for identifying non-sensitizers to reduce. animal testing for pesticides by 19.6%.

基于不良结果通路(AOP)的计算模型为人类皮肤致敏剂提供了最先进的预测,是动物试验的有希望的替代方案。然而,由于缺乏农药评价数据,人们对其在农药中的适用性知之甚少。此外,农药传统上是在没有人体数据的情况下在动物身上进行试验的,这使得验证变得困难。将基于aop的模型直接应用于农药可能是不合适的,因为它们最初的适用范围是为了最大限度地提高人类对各种化学品(而不是农药)的反应预测的可靠性。本研究建议通过SkinSensPred在线工具和动物试验数据预测,确定一个具有一致人类反应的一致化学空间,以减少动物试验。在交叉验证和独立测试中,非敏化剂的共识化学空间分别达到了85%和100%的高一致性。重新配置的SkinSensPred可以用作识别要减少的非敏化剂的第一级工具。农药动物试验减少19.6%。
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引用次数: 0
Acute toxicity of fipronil to an invasive ant, Lepisiota frauenfeldi. 氟虫腈对入侵蚂蚁的急性毒性研究。
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-11-20 DOI: 10.1584/jpestics.D22-049
Daisuke Hayasaka, Masayoshi K Hiraiwa, Yu Maebara, Yugo Seko

Slow-acting fipronil is one of the best components for controlling invasive ants. However, its efficacy against invasive Lepisiota frauenfeldi, which recently invaded Japan, remains unclear. Here, its acute toxicity to Le. frauenfeldi was assessed, and its lethal concentrations were compared with those against other invasive ants (Linepithema humile and Solenopsis invicta). The LC10 and LC50 values of fipronil for Le. frauenfeldi were significantly lower than the previously reported values for Li. humile and/or S. invicta, and its LC90 value against Le. frauenfeldi was in the same range as that required for Li. humile extermination. Additionally, Le. frauenfeldi can be more sensitive to fipronil than non-target arthropods. Therefore, recent fipronil-based Li. humile and S. invicta eradication/control programs may be effective against Le. frauenfeldi as well. Moreover, applying fipronil at dosages appropriate for Le. frauenfeldi would lead to effective Le. frauenfeldi extermination/control with low damage to other native species/ants.

缓效氟虫腈是控制入侵蚂蚁的最佳成分之一。然而,它对最近入侵日本的入侵性狼斑绦虫(Lepisiota frauenfeldi)的功效尚不清楚。在此,其急性毒性为乐。测定了弗劳恩费尔迪的致死浓度,并比较了其对其他入侵蚂蚁(矮腰线蚁和invicopsis)的致死浓度。氟虫腈的LC10和LC50值。fraenfeldi明显低于先前报道的Li值。对赤霉素和/或赤霉素的LC90值。弗劳恩费尔迪与李的要求相同。种灭绝。此外,勒。与非目标节肢动物相比,弗劳恩费尔迪对氟虫腈更敏感。因此,最近基于氟虫腈的Li。对紫锥虫和红锥虫的根除/控制计划可能有效。还有弗劳恩费尔迪。此外,使用氟虫腈的剂量适合Le。弗劳恩费尔迪将导致有效的乐。灭杀/控制弗劳恩费尔迪,对其他本地物种/蚂蚁的损害较小。
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引用次数: 1
Synthesis of fluorescently labeled pyrazole derivative induceing a triple response in Arabidopsis seedlings. 荧光标记吡唑衍生物在拟南芥幼苗中诱导三重反应的合成。
IF 2.4 4区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2022-11-20 DOI: 10.1584/jpestics.D22-006
Keimei Oh, Kai Jiang

A fluorescent labeled pyrazole derivative with a dansyl moiety (EH-DF) was synthesized. Design of EH-DF was carried out by using a dansyl moiety to substitute the naphthalene moiety of the parent compound (EH-1). At a concentration of 30 µM, EH-DF displayed biological activity on inducing a triple response in Arabidopsis seedlings. Compared with the non-chemical treated control, the hypocotyl length of EH-DF-treated Arabidopsis seedlings was reduced from approximately 9.2±0.7 mm to 2.4±0.2 mm. The length of the roots was reduced from 1.7±0.1 mm to 1.0±0.1 mm, and the curvature of the hook of Arabidopsis seedlings increased from 60±16 degrees to 245±35 degrees. The maxim excitation wavelength and emission wavelength of EH-DF were 350 and 535 nm, respectively. Data obtained via fluorescent microscope analysis indicated that intensive fluorescent signals of EH-DF were observed in the shoot of Arabidopsis seedlings.

合成了一种荧光标记的丹酰吡唑衍生物。EH-DF的设计是用丹酰部分代替母体化合物EH-1的萘部分。在浓度为30µM时,EH-DF在拟南芥幼苗中表现出诱导三重反应的生物活性。与未经化学处理的对照相比,eh - df处理的拟南芥幼苗下胚轴长度从约9.2±0.7 mm缩短至2.4±0.2 mm。根长从1.7±0.1 mm减少到1.0±0.1 mm,拟南芥幼苗钩曲率从60±16度增加到245±35度。EH-DF的最大激发波长为350 nm,最大发射波长为535 nm。荧光显微镜分析数据表明,EH-DF在拟南芥幼苗的茎部中观察到强烈的荧光信号。
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引用次数: 0
期刊
Journal of Pesticide Science
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