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Design, synthesis and antifungal activity of arylhydrazine analogs containing diphenyl ether fragments. 含二苯醚片段的芳基肼类似物的设计、合成和抗真菌活性。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-10-28 DOI: 10.1002/ps.8498
Longjian Qiu, Yaru Liu, Lijuan Zhang, Aixi Hu, Jiao Ye, Zhongzhong Yan

Background: Succinate dehydrogenase (SDH) represents a critical target in the development of novel fungicides. To address the growing issue of resistance and safeguard the economic viability of agricultural production, the pursuit of new succinate dehydrogenase inhibitors (SDHIs) has emerged as a significant focus of contemporary research.

Results: In this project, 32 arylhydrazine derivatives containing diphenyl ether structural units were synthesized and evaluated for their fungicidal activities against Rhizoctonia solani, Sclerotinia sclerotiorum, Alternaria alternata, Gibberella zeae, Alternaria solani and Colletotrichum gloeosporioides. In an in vitro fungicidal activity assay, compound D6 showed significant inhibitory activity against R. solani with a half-maximum effective concentration (EC50) of 0.09 mg L-1. The in vivo fungicidal activity demonstrated that compound D6 inhibited R. solani by 95.39% in rice leaves, which was significantly better than that of boscalid (85.76%). The results of SDH enzyme assay, molecular docking simulation, mitochondrial membrane potential assay, cytoplasmic release studies and morphological observations demonstrated that the target compound D6 not only had significant SDH inhibitory activity, but also affected the membrane integrity of mycelium.

Conclusion: Bioactivity screening and validation of the mechanism of action indicated that compound D6 was a potentially unique SDHI, acting on SDH while also affecting cell membrane permeability, which deserved further study. © 2024 Society of Chemical Industry.

背景:琥珀酸脱氢酶(SDH)是开发新型杀菌剂的关键目标。为了解决日益严重的抗药性问题,保障农业生产的经济可行性,寻找新的琥珀酸脱氢酶抑制剂(SDHIs)已成为当代研究的一个重要焦点:本项目合成了 32 种含有二苯醚结构单元的芳基肼衍生物,并评估了它们对根瘤菌(Rhizoctonia solani)、硬粒菌(Sclerotinia sclerotiorum)、交替丝核菌(Alternaria alternata)、玉米赤霉病菌(Gibberella zeae)、茄属交替丝核菌(Alternaria solani)和球孢子菌(Colletotrichum gloeosporioides)的杀菌活性。在体外杀菌活性试验中,化合物 D6 对 R. solani 具有显著的抑制活性,其半最大有效浓度(EC50)为 0.09 mg L-1。体内杀菌活性表明,化合物 D6 对水稻叶片中 R. solani 的抑制率为 95.39%,明显优于啶酰菌胺(85.76%)。SDH酶测定、分子对接模拟、线粒体膜电位测定、细胞质释放研究和形态学观察结果表明,目标化合物D6不仅具有显著的SDH抑制活性,而且还影响菌丝体膜的完整性:结论:生物活性筛选和作用机制验证表明,化合物 D6 是一种潜在的独特 SDHI,在作用于 SDH 的同时也影响细胞膜的渗透性,值得进一步研究。© 2024 化学工业协会。
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引用次数: 0
Unveiling the functions of the Lim-domain binding protein MaPtaB in Metarhizium acridum. 揭示疟原虫中 Lim-domain结合蛋白MaPtaB的功能。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-10-29 DOI: 10.1002/ps.8488
Yanru Du, Meiwen Hu, Yuxian Xia, Kai Jin

Background: The Lim-domain binding protein PtaB, a homolog of Mfg1, governs conidiation and biofilm formation in several fungi. PtaB includes a conserved Lim-binding domain and two predicted nuclear localization sequences at its C terminus, and is co-regulated with the transcription factor Som1 downstream of the cyclic AMP-dependent protein kinase A (cAMP/PKA) pathway. However, the function of PtaB in entomopathogenic fungi remain poorly understood.

Results: Inactivation of PtaB in Metarhizium acridum resulted in delayed conidial germination, reduced conidial yield and increased sensitivities to cell wall disruptors, ultraviolet B irradiation and heat shock. In addition, the fungal virulence was significantly decreased after deletion of MaPtaB because of impairments in appressorium formation, cuticle penetration and evasion of insect immune responses in M. acridum. The MaPtaB-deletion and MaSom1-deletion strains showed similar phenotypes supporting that MaSom1/MaPtaB complex controls M. acridum normal conidiation and pathogenic progress. Upon loss of MaPtaB or MaSom1, the fungal sporulation mode in M. acridium shifted from microcycle conidiation to normal conidiation on SYA, a microcycle conidiation medium. Transcriptional analysis showed that more differentially expression genes were identified in MaSom1 RNA sequencing, and MaSom1 and MaPtaB may regulate the expression of genes for conidiation, nutrient metabolism and the cell cycle to control conidiation pattern shift.

Conclusion: These data corroborate a complex control function for MaPtaB as an important central factor interacting with MaSom1 in the cAMP/PKA pathway, which links stress tolerance, conidiation and virulence in the entomopathogenic fungus M. acridum. © 2024 Society of Chemical Industry.

背景:Lim结合域结合蛋白PtaB是Mfg1的同源物,在几种真菌中控制着分生和生物膜的形成。PtaB 的 C 端包括一个保守的 Lim 结合域和两个预测的核定位序列,并与转录因子 Som1 一起受环 AMP 依赖性蛋白激酶 A(cAMP/PKA)途径下游的共同调控。然而,人们对 PtaB 在昆虫病原真菌中的功能仍知之甚少:结果:钝化尖吻镰刀菌中的 PtaB 会导致分生孢子萌发延迟、分生孢子产量减少以及对细胞壁破坏剂、紫外线 B 照射和热休克的敏感性增加。此外,MaPtaB 基因缺失后,真菌的毒力明显下降,原因是尖吻蕈蚊的附着体形成、角质层穿透和逃避昆虫免疫反应的能力受损。缺失 MaPtaB 的菌株和缺失 MaSom1 的菌株表现出相似的表型,证明 MaSom1/MaPtaB 复合物控制着梭菌正常的分生和致病过程。缺失 MaPtaB 或 MaSom1 后,吖啶真菌的分生孢子模式从微循环分生转变为在微循环分生培养基 SYA 上正常分生。转录分析表明,在MaSom1 RNA测序中发现了更多的差异表达基因,MaSom1和MaPtaB可能调控分生、营养代谢和细胞周期基因的表达,从而控制分生模式的转变:这些数据证实了 MaPtaB 的复杂调控功能,它是与 MaSom1 在 cAMP/PKA 通路中相互作用的重要中心因子,将昆虫病原真菌 M. acridum 的胁迫耐受性、分生孢子和毒力联系在一起。
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引用次数: 0
Regulation of melanization in aphids by parasitoid wasp venom proteins enhances mummification. 寄生蜂毒液蛋白对蚜虫黑色素化的调控可促进木乃伊化。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-11-04 DOI: 10.1002/ps.8503
Jin Zhao, Zheng-Wu Wang, Guangmao Shen, Die Hu, Yi Zhong, Chao Ye, Jin-Jun Wang

Background: Interactions between parasitic insects and their hosts demonstrate the complexity of evolutionary processes. Specifically, the parasitoid wasp Aphidius ervi manipulates its host, the pea aphid Acyrthosiphon pisum, through strategic venom injection to enhance mummification. This study explores how this venom affects the aphid's immune system, particularly targeting the activity of the phenoloxidase (PO) enzyme.

Results: Following the injection of venom from A. ervi, significant changes were observed in the expression of immune-related genes in A. pisum, especially notable expression changes of ApPPOs and a reduction of PO activity. Multi-omics sequencing identified 74 potential venom proteins in the venom gland of A. ervi, including serine protease homolog 1 (AeSPH1) and serine protease inhibitor (AeSPN1), hypothesized to regulate PO activity. The injection of recombinant protein AeSPH1 and AeSPN1 into the A. pisum hemocoel selectively reduced the expression of ApPPO1, without affecting ApPPO2, and effectively suppressed melanization. Moreover, RNAi targeting AeSPH1 significantly reduced the mummification rate in A. pisum population parasitized by A. ervi.

Conclusion: Our findings clarify the complex biochemical mechanisms underlying host-wasp interactions and highlight potential avenues for developing targeted biological control strategies. © 2024 Society of Chemical Industry.

背景:寄生昆虫与其宿主之间的相互作用显示了进化过程的复杂性。具体来说,寄生蜂蚜茧蜂(Aphidius ervi)通过有策略地注射毒液来操纵宿主豌豆蚜(Acyrthosiphon pisum),以增强其木乃伊化。本研究探讨了这种毒液如何影响蚜虫的免疫系统,特别是针对酚氧化酶(PO)的活性:结果:注射 A. ervi 毒液后,观察到 A. pisum 免疫相关基因的表达发生了显著变化,尤其是 ApPPOs 的表达发生了明显变化,PO 活性降低。多组学测序确定了 A. ervi 毒腺中 74 种潜在的毒液蛋白,包括丝氨酸蛋白酶同源物 1(AeSPH1)和丝氨酸蛋白酶抑制物(AeSPN1),据推测这两种蛋白可调节 PO 活性。将重组蛋白 AeSPH1 和 AeSPN1 注入 A. pisum 血肠,可选择性地减少 ApPPO1 的表达,而不影响 ApPPO2 的表达,并有效抑制黑色素形成。此外,针对 AeSPH1 的 RNAi 能显著降低被 A. ervi 寄生的 A. pisum 群体的木乃伊化率:我们的研究结果阐明了寄主与黄蜂相互作用的复杂生化机制,并强调了开发有针对性的生物防治策略的潜在途径。© 2024 化学工业协会。
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引用次数: 0
Superior target genes and pathways for RNAi-mediated pest control revealed by genome-wide analysis in the beetle Tribolium castaneum. 通过对甲虫Tribolium castaneum的全基因组分析,发现RNAi介导的害虫控制的优良目标基因和途径。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-11-05 DOI: 10.1002/ps.8505
Benjamin Buer, Jürgen Dönitz, Martin Milner, Sonja Mehlhorn, Claudia Hinners, Janna Siemanowski-Hrach, Julia K Ulrich, Daniela Großmann, Doga Cedden, Ralf Nauen, Sven Geibel, Gregor Bucher

Background: An increasing human population, the emergence of resistances against pesticides and their potential impact on the environment call for the development of new eco-friendly pest control strategies. RNA interference (RNAi)-based pesticides have emerged as a new option with the first products entering the market. Essentially, double-stranded RNAs targeting essential genes of pests are either expressed in the plants or sprayed on their surface. Upon feeding, pests mount an RNAi response and die. However, it has remained unclear whether RNAi-based insecticides should target the same pathways as classic pesticides or whether the different mode-of-action would favor other processes. Moreover, there is no consensus on the best genes to be targeted.

Results: We performed a genome-wide screen in the red flour beetle to identify 905 RNAi target genes. Based on a validation screen and clustering, we identified the 192 most effective target genes in that species. The transfer to oral application in other beetle pests revealed a list of 34 superior target genes, which are an excellent starting point for application in other pests. Gene ontology (GO) and Kyoto encyclopedia of genes and genomes (KEGG) analyses of our genome-wide dataset revealed that genes with high efficacy belonged mainly to basic cellular processes such as gene expression and protein homeostasis - processes not targeted by classic insecticides.

Conclusion: Our work revealed the best target genes and target processes for RNAi-based pest control and we propose a procedure to transfer our short list of superior target genes to other pests. © 2024 The Author(s). Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

背景:随着人口的不断增长、杀虫剂抗药性的出现以及杀虫剂对环境的潜在影响,人们需要开发新的生态友好型害虫控制策略。随着首批产品进入市场,基于 RNA 干扰(RNAi)的杀虫剂已成为一种新的选择。从本质上讲,针对害虫重要基因的双链 RNA 要么在植物体内表达,要么喷洒在植物表面。害虫在摄食后会产生 RNAi 反应并死亡。然而,基于 RNAi 的杀虫剂是否应针对与传统杀虫剂相同的途径,或者不同的作用模式是否会有利于其他过程,目前仍不清楚。此外,对于最佳靶向基因也没有达成共识:结果:我们对红粉甲虫进行了全基因组筛选,确定了 905 个 RNAi 靶基因。根据验证筛选和聚类,我们确定了该物种中 192 个最有效的靶基因。将其转移到其他甲虫害虫的口服应用中,发现了 34 个优质靶基因,这是在其他害虫中应用的良好起点。对我们的全基因组数据集进行的基因本体(GO)和京都基因和基因组百科全书(KEGG)分析表明,高效基因主要属于基本细胞过程,如基因表达和蛋白质稳态--传统杀虫剂不针对这些过程:我们的工作揭示了基于 RNAi 的害虫控制的最佳靶基因和靶过程,我们还提出了一个将我们的优秀靶基因短名单应用于其他害虫的程序。© 2024 作者简介害虫管理科学》由 John Wiley & Sons Ltd 代表化学工业协会出版。
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引用次数: 0
Appropriate sampling to aid on-farm assessments of the haplotype composition of Zymoseptoria tritici populations. 进行适当的取样,以帮助在农场评估三尖杉蝽种群的单倍型组成。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-10-11 DOI: 10.1002/ps.8454
Catherine Harrison, Neil Boonham, Roy Macarthur, Michael David Parr, Femke van den Berg

Background: Zymoseptoria tritici causes Septoria tritici blotch (STB), which is the biggest threat to wheat in the UK. Azole fungicides have been used since the 1980s to control STB, but resistance to these chemicals is now widespread. The main resistance mechanism is based on the accumulation of CYP51 mutations, with 33 mutations reported. Hence, farmers need an accurate estimate of the haplotype composition of Z. tritici populations to develop effective fungicide treatments and resistance management.

Results: Isolates from Z. tritici lesions were collected from three fields across three commercial farms using two sampling approaches. Analysis of the isolate sequences revealed that the number of distinct haplotypes and the haplotype composition of the most dominant haplotypes varied only between and not within farms. Conventional W-shaped and point sampling both found the same percentage of distinct haplotypes and frequencies of the six most dominant haplotypes.

Conclusion: The results from this survey suggest that farm-resistance-management strategies should be based on farm-specific rather than national data, and that sampling within a single field is sufficient. W-shaped sampling is often recommended in sampling approaches, but this survey finds no evidence of this approach being more appropriate for detecting a greater percentage of distinct haplotypes which may aid the discovery of potential new resistance threats. © 2024 Fera Science Ltd. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

背景:三尖孢(Zymoseptoria tritici)会导致三尖孢(Septoria tritici)斑点病(STB),这是英国小麦面临的最大威胁。自 20 世纪 80 年代以来,唑类杀菌剂一直被用于控制 STB,但现在对这些化学品的抗性已十分普遍。主要的抗性机理是基于 CYP51 突变的积累,据报道有 33 种突变。因此,农民需要准确估计三尖杉属植物种群的单倍型组成,以制定有效的杀真菌剂处理和抗性管理方法:结果:采用两种取样方法,从三个商业农场的三块田地中采集了三尖杉病害分离株。对分离物序列的分析表明,不同单倍型的数量和最主要单倍型的单倍型组成只在农场之间有差异,而在农场内部没有差异。传统的 W 型采样和点式采样都发现了相同比例的独特单倍型和六个最主要单倍型的频率:本次调查的结果表明,农场抗性管理策略应基于特定农场而非全国数据,在单块田地内取样即可。取样方法中通常推荐 W 型取样,但本调查没有发现证据表明这种方法更适合检测更大比例的独特单倍型,这可能有助于发现潜在的新抗性威胁。© 2024 Fera Science Ltd.害虫管理科学》由 John Wiley & Sons Ltd 代表化学工业协会出版。
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引用次数: 0
Naturally-occurring nematicides of plant origin: two decades of novel chemistries. 源自植物的天然杀线虫剂:二十年的新型化学成分。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-11-06 DOI: 10.1002/ps.8504
Hashim Ibrahim, Vaderament-A Nchiozem-Ngnitedem, Louise-Marie Dandurand, Inna Popova

Plant-parasitic nematodes are among the most destructive plant pathogens, resulting in a global annual economic loss of about 358 billion dollars. Using synthetic nematicides to control plant-parasitic nematodes has resulted in broad-spectrum toxicity to the environment. Plant-derived secondary metabolites have recently emerged as viable options that provide effective, greener, and renewable routes for managing plant-parasitic nematodes in various cropping systems. However, limited comprehensive information on plant-derived secondary metabolites sources, chemical structures, and nematicidal activities is available. This study aims to compile and analyze data on plant-based secondary metabolites with nematicidal properties collected over the last two decades. In this review, we identified 262 plant-based metabolites with nematicidal activities that were isolated from 35 plant families and 65 plant species. Alkaloids, terpenoids, saponins, flavonoids, coumarins, thiophenes, and annonaceous acetogenins were among the most studied compounds. In addition to the structure-activity relation for specific metabolites with nematicidal potency, various techniques for their extraction and isolation from plant material are discussed. Our findings demonstrate the potential of plants as a feedstock for sourcing nematicidal compounds and discovering new chemistries that could potentially be used for developing the next generation of nematicides. © 2024 The Author(s). Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

植物寄生线虫是最具破坏性的植物病原体之一,每年给全球造成约 3580 亿美元的经济损失。使用合成杀线虫剂控制植物寄生线虫会对环境产生广谱毒性。植物提取的次生代谢物近来已成为一种可行的选择,为在各种种植系统中控制植物寄生线虫提供了有效、更环保和可再生的途径。然而,有关植物衍生次生代谢物的来源、化学结构和杀线虫活性的综合信息非常有限。本研究旨在汇编和分析过去二十年中收集的具有杀线虫特性的植物次生代谢物数据。在这篇综述中,我们发现了 262 种具有杀线虫活性的植物基代谢物,它们是从 35 个植物科和 65 个植物物种中分离出来的。研究最多的化合物包括生物碱、萜类化合物、皂苷、黄酮类化合物、香豆素、噻吩类化合物和壬基炔苷元。除了具有杀线虫效力的特定代谢物的结构-活性关系外,还讨论了从植物材料中提取和分离这些代谢物的各种技术。我们的研究结果表明,植物作为一种原料,具有寻找杀线虫化合物和发现新化学物质的潜力,有可能用于开发下一代杀线虫剂。© 2024 作者简介害虫管理科学》由 John Wiley & Sons Ltd 代表化学工业协会出版。
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引用次数: 0
DMI fungicide resistance in Zymoseptoria tritici is unlinked to geographical origin and genetic background: a case study in Europe. Zymoseptoria tritici 对 DMI 杀菌剂的抗性与地理来源和遗传背景无关:欧洲的一项案例研究。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-11-06 DOI: 10.1002/ps.8514
Eula Gems Oreiro, Berit Samils, Steven Kildea, Thies Heick, Pierre Hellin, Anne Legrève, Bernd Rodemann, Gunilla Berg, Lise N Jørgensen, Hanna Friberg, Anna Berlin, Jiasui Zhan, Björn Andersson

Background: The hemibiotrophic fungus Zymoseptoria tritici causing Septoria tritici blotch (STB), is a devastating foliar pathogen of wheat worldwide. A common group of fungicides used to control STB are the demethylation inhibitors (DMIs). DMI fungicides restrict fungal growth by inhibiting the sterol 14-α-demethylase, a protein encoded by CYP51 gene and essential for maintaining fungal cell permeability. However, the adaptation of Z. tritici populations in response to intensive and prolonged DMI usage has resulted in a gradual shift towards reduced sensitivity to this group of fungicides. In this study, 311 isolates were collected pre-treatment from nine wheat-growing regions in Europe in 2019. These isolates were analysed by high-throughput amplicon-based sequencing of nine housekeeping genes and the CYP51 gene.

Results: Analyses based on housekeeping genes and the CYP51 gene revealed a lack of population structure in Z. tritici samples irrespective of geographical origin. Minimum spanning network (MSN) analysis showed clustering of multilocus genotypes (MLGs) based on CYP51 haplotypes, indicating an effect of selection due to DMI fungicide use. The majority of the haplotypes identified in this study have been reported previously. The diversity and frequencies of mutations varied across regions.

Conclusion: Using a high-throughput amplicon-sequencing approach, we found several mutations in the CYP51 gene combined in different haplotypes that are likely to cause fungicide resistance. These mutations occurred irrespective of genetic background or geographical origin. Overall, these results contribute to the development of effective and sustainable risk monitoring for DMI fungicide resistance. © 2024 The Author(s). Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

背景:由三尖杉半知菌(Zymoseptoria tritici)引起的三尖杉斑点病(STB)是全世界小麦的一种毁灭性叶面病原菌。脱甲基化抑制剂(DMI)是一类常用的杀菌剂,用于控制 STB。DMI 类杀菌剂通过抑制甾醇 14-α-demethylase 来限制真菌生长,而甾醇 14-α-demethylase 是一种由 CYP51 基因编码的蛋白质,对维持真菌细胞的渗透性至关重要。然而,三尖杉属真菌种群对密集和长期使用 DMI 的适应性导致其对这一类杀真菌剂的敏感性逐渐降低。在这项研究中,2019 年从欧洲九个小麦种植区收集了 311 个处理前分离物。对这些分离物进行了基于高通量扩增子测序的九个看家基因和 CYP51 基因分析:结果:基于看家基因和 CYP51 基因的分析表明,Z. tritici 样本中缺乏种群结构,与地理来源无关。最小跨度网络(MSN)分析显示,基于CYP51单倍型的多焦点基因型(MLGs)聚类,表明使用DMI杀真菌剂产生了选择效应。本研究中发现的大多数单倍型此前已有报道。不同地区的变异多样性和频率各不相同:利用高通量扩增序列方法,我们在 CYP51 基因中发现了几种突变,它们结合在不同的单倍型中,很可能会导致杀菌剂抗性。这些突变的发生与遗传背景或地理来源无关。总之,这些结果有助于开发有效、可持续的 DMI 杀菌剂抗性风险监测。© 2024 作者。病虫害管理科学》由 John Wiley & Sons Ltd 代表化学工业协会出版。
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引用次数: 0
Unraveling the molecular mechanism of FgGcn5 inhibition by phenazine-1-carboxamide: combined in silico and in vitro studies. 揭示吩嗪-1-甲酰胺抑制 FgGcn5 的分子机制:硅学和体外联合研究。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-10-28 DOI: 10.1002/ps.8496
Lei Li, Qing Luo, Shuai Yang, Hancheng Wang, Yuguang Mu, Jingjing Guo, Feng Zhang

Background: Fusarium head blight (FHB), mainly caused by Fusarium graminearum (F. graminearum), remains a devastating disease worldwide. The histone acetyltransferase Gcn5 plays a crucial role in epigenetic regulation. Aberrant Gcn5 acetylation activity can result in serious impacts such as impaired growth and development in organisms. The secondary metabolite phenazine-1-carboxamide (PCN) inhibits F. graminearum by blocking the acetylation process of Gcn5 (FgGcn5), and is currently used to control FHB. However, the molecular basis of acetylation inhibition by PCN remains to be further explored.

Results: Our molecular dynamics simulations revealed that PCN binds to the cleft in FgGcn5 where histone H3 is bound, with key amino acid residues including Leu96 (L96), Arg121 (R121), Phe133 (F133), Tyr169 (Y169), and Tyr201 (Y201), preventing FgGcn5 from binding to histone H3 and affecting histone H3 from being acetylated. Experimental validation of key amino acid mutations further confirmed the impact of these mutations on the interaction of FgGcn5 with PCN and histone H3 peptide.

Conclusion: In summary, our study sheds light on the mechanism by which PCN inhibits the acetylation function of FgGcn5, providing a foundation for the development of drugs or fungicides targeting histone acetyltransferases. © 2024 Society of Chemical Industry.

背景:镰刀菌头枯病(FHB)主要由禾谷镰刀菌(F. graminearum)引起,目前仍是一种全球性的毁灭性病害。组蛋白乙酰转移酶 Gcn5 在表观遗传调控中起着至关重要的作用。异常的 Gcn5 乙酰化活性会导致生物体生长和发育受损等严重影响。次级代谢物酚嗪-1-甲酰胺(PCN)通过阻断 Gcn5(FgGcn5)的乙酰化过程来抑制禾谷粉虱,目前被用于防治禾谷粉虱。然而,PCN 抑制乙酰化的分子基础仍有待进一步探索:我们的分子动力学模拟发现,PCN与FgGcn5中组蛋白H3结合的裂隙结合,关键氨基酸残基包括Leu96 (L96)、Arg121 (R121)、Phe133 (F133)、Tyr169 (Y169)和Tyr201 (Y201),从而阻止FgGcn5与组蛋白H3结合,影响组蛋白H3乙酰化。关键氨基酸突变的实验验证进一步证实了这些突变对 FgGcn5 与 PCN 和组蛋白 H3 肽相互作用的影响:总之,我们的研究揭示了 PCN 抑制 FgGcn5 乙酰化功能的机制,为开发针对组蛋白乙酰转移酶的药物或杀菌剂奠定了基础。© 2024 化学工业协会。
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引用次数: 0
The miR-31b targets arylsulfatase B to regulate the ovarian development of Bactrocera dorsalis. miR-31b以芳基硫酸酯酶B为靶标,调控背带蝠的卵巢发育。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-11-04 DOI: 10.1002/ps.8513
Shan-Shan Yu, Qiang Zhang, Li-Yuan Zheng, Qian-Ping Xie, Jin-Jun Wang, Wei Dou

Background: Reproduction is the basis of insect population growth and evolution, and encompasses ovarian development, reproductive behavior, and fecundity. Bactrocera dorsalis is a globally significant agricultural pest that is subject to quarantine, with mated females that can lay over 3000 eggs. The post-transcriptional regulation of ovarian development remains unclear. Here, miR-31b is shown to be involved in regulating Bactrocera dorsalis ovarian development.

Results: CRISPR/Cas9 was used to generate miR-31b loss-of-function mutations in Bactrocera dorsalis. The removal of miR-31b resulted in severely impaired ovarian development in adults, with phenotypes that included dramatically reduced egg production and hatching rates. The relationship between miR-31b and its target gene arylsulfatase B (ARSB) was subsequently identified using the methods of bioinformatics, transcriptomic sequencing, quantitative polymerase chain reaction (qPCR), RNA pull-down and dual-luciferase reporter assay. Finally, miR-31b was confirmed to bind the target gene arylsulfatase B to affect metabolism and thereby further hindered ovarian development of Bactrocera dorsalis.

Conclusion: Overall, these results provide new insights into molecular mechanisms at the post-transcriptional level in regulating ovarian development and insect reproduction, consequently providing potential targets to control arthropod pests through the reproductive strategy. © 2024 Society of Chemical Industry.

背景:繁殖是昆虫种群增长和进化的基础,包括卵巢发育、繁殖行为和繁殖力。背腹扁虱是一种全球重要的农业害虫,需接受检疫,其交配雌虫可产卵 3000 多枚。卵巢发育的转录后调控仍不清楚。在这里,miR-31b 被证明参与调控背甲线虫的卵巢发育:结果:利用 CRISPR/Cas9 技术在蝙蝠卵巢发育过程中产生了 miR-31b 功能缺失突变。去除 miR-31b 会导致成虫卵巢发育严重受损,其表型包括产卵量和孵化率急剧下降。随后,利用生物信息学、转录组测序、定量聚合酶链式反应(qPCR)、RNA 下拉和双荧光素酶报告实验等方法,确定了 miR-31b 与其靶基因芳基硫酸酯酶 B(ARSB)之间的关系。最后,miR-31b 被证实与目标基因芳基硫酸酯酶 B 结合,影响新陈代谢,从而进一步阻碍了背甲双壳虫的卵巢发育:总之,这些结果为转录后水平调控卵巢发育和昆虫繁殖的分子机制提供了新的见解,从而为通过繁殖策略控制节肢动物害虫提供了潜在靶标。© 2024 化学工业协会。
{"title":"The miR-31b targets arylsulfatase B to regulate the ovarian development of Bactrocera dorsalis.","authors":"Shan-Shan Yu, Qiang Zhang, Li-Yuan Zheng, Qian-Ping Xie, Jin-Jun Wang, Wei Dou","doi":"10.1002/ps.8513","DOIUrl":"10.1002/ps.8513","url":null,"abstract":"<p><strong>Background: </strong>Reproduction is the basis of insect population growth and evolution, and encompasses ovarian development, reproductive behavior, and fecundity. Bactrocera dorsalis is a globally significant agricultural pest that is subject to quarantine, with mated females that can lay over 3000 eggs. The post-transcriptional regulation of ovarian development remains unclear. Here, miR-31b is shown to be involved in regulating Bactrocera dorsalis ovarian development.</p><p><strong>Results: </strong>CRISPR/Cas9 was used to generate miR-31b loss-of-function mutations in Bactrocera dorsalis. The removal of miR-31b resulted in severely impaired ovarian development in adults, with phenotypes that included dramatically reduced egg production and hatching rates. The relationship between miR-31b and its target gene arylsulfatase B (ARSB) was subsequently identified using the methods of bioinformatics, transcriptomic sequencing, quantitative polymerase chain reaction (qPCR), RNA pull-down and dual-luciferase reporter assay. Finally, miR-31b was confirmed to bind the target gene arylsulfatase B to affect metabolism and thereby further hindered ovarian development of Bactrocera dorsalis.</p><p><strong>Conclusion: </strong>Overall, these results provide new insights into molecular mechanisms at the post-transcriptional level in regulating ovarian development and insect reproduction, consequently providing potential targets to control arthropod pests through the reproductive strategy. © 2024 Society of Chemical Industry.</p>","PeriodicalId":218,"journal":{"name":"Pest Management Science","volume":" ","pages":"1094-1102"},"PeriodicalIF":3.8,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142567142","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Engineering the novel azobenzene-based molecular photoswitches for suppressing bacterial infection through dynamic regulation of biofilm formation. 设计新型偶氮苯分子光开关,通过动态调节生物膜的形成抑制细菌感染。
IF 3.8 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-02-01 Epub Date: 2024-10-07 DOI: 10.1002/ps.8453
Tai-Hong Zhang, Yi-Ke Yang, Yu-Mei Feng, Zhi-Jun Luo, Ming-Wei Wang, Pu-Ying Qi, Dan Zeng, Hong-Wu Liu, Yan-Mei Liao, Jiao Meng, Xiang Zhou, Li-Wei Liu, Song Yang

Background: Bacterial biofilm is a strong fortress for bacteria to resist harsh external environments, which can enhance their tolerance and exacerbate the drug/pesticide resistance risk. Currently, photopharmacology provides an advanced approach via precise spatiotemporal control for regulating biological activities by light-controlling the molecular configurations, thereby having enormous potential in the development of drug/pesticides.

Results: To further expand the photopharmacology application for discovering new antibiofilm agents, we prepared a series of light-controlled azo-active molecules and explored their photo isomerization, fatigue resistance, and anti-biofilm performance. Furthermore, their mechanisms of inhibiting biofilm formation were systematically investigated. Overall, designed azo-derivative A11 featured excellent anti-Xoo activity with an half-maximal effective concentration (EC50) value of 5.45 μg mL-1, and the EC50 value could be further elevated to 2.19 μg mL-1 after ultraviolet irradiation (converted as cis-configuration). The photo-switching behavior showed that A11 had outstanding anti-fatigue properties. An in-depth analysis of the action mechanism showed that A11 could effectively inhibit biofilm formation and the expression of relevant virulence factors. This performance could be dynamically regulated via loading with private light-switch property.

Conclusion: In this work, designed light-controlled azo molecules provide a new model for resisting bacterial infection via dynamic regulation of bacterial biofilm formation. © 2024 Society of Chemical Industry.

背景:细菌生物膜是细菌抵御外界恶劣环境的坚强堡垒,可增强细菌的耐受性,加剧耐药性/耐药性风险。目前,光药理学提供了一种先进的方法,通过精确的时空控制,以光控制分子构型来调节生物活性,从而在药物/杀虫剂的开发方面具有巨大潜力:为了进一步拓展光药理学在发现新型抗生物膜剂方面的应用,我们制备了一系列光控偶氮活性分子,并对其光异构化、抗疲劳性和抗生物膜性能进行了探索。此外,我们还系统地研究了它们抑制生物膜形成的机理。总体而言,所设计的偶氮衍生物 A11 具有优异的抗 Xoo 活性,其半最大有效浓度(EC50)值为 5.45 μg mL-1,在紫外线照射下(转换为顺式构型),EC50 值可进一步升高至 2.19 μg mL-1。光开关行为表明 A11 具有出色的抗疲劳特性。对其作用机制的深入分析表明,A11 能有效抑制生物膜的形成和相关毒力因子的表达。这种性能可以通过加载私人光开关特性进行动态调节:在这项工作中,设计的光控偶氮分子为通过动态调节细菌生物膜的形成来抵抗细菌感染提供了一种新的模式。© 2024 化学工业协会。
{"title":"Engineering the novel azobenzene-based molecular photoswitches for suppressing bacterial infection through dynamic regulation of biofilm formation.","authors":"Tai-Hong Zhang, Yi-Ke Yang, Yu-Mei Feng, Zhi-Jun Luo, Ming-Wei Wang, Pu-Ying Qi, Dan Zeng, Hong-Wu Liu, Yan-Mei Liao, Jiao Meng, Xiang Zhou, Li-Wei Liu, Song Yang","doi":"10.1002/ps.8453","DOIUrl":"10.1002/ps.8453","url":null,"abstract":"<p><strong>Background: </strong>Bacterial biofilm is a strong fortress for bacteria to resist harsh external environments, which can enhance their tolerance and exacerbate the drug/pesticide resistance risk. Currently, photopharmacology provides an advanced approach via precise spatiotemporal control for regulating biological activities by light-controlling the molecular configurations, thereby having enormous potential in the development of drug/pesticides.</p><p><strong>Results: </strong>To further expand the photopharmacology application for discovering new antibiofilm agents, we prepared a series of light-controlled azo-active molecules and explored their photo isomerization, fatigue resistance, and anti-biofilm performance. Furthermore, their mechanisms of inhibiting biofilm formation were systematically investigated. Overall, designed azo-derivative A11 featured excellent anti-Xoo activity with an half-maximal effective concentration (EC<sub>50</sub>) value of 5.45 μg mL<sup>-1</sup>, and the EC<sub>50</sub> value could be further elevated to 2.19 μg mL<sup>-1</sup> after ultraviolet irradiation (converted as cis-configuration). The photo-switching behavior showed that A11 had outstanding anti-fatigue properties. An in-depth analysis of the action mechanism showed that A11 could effectively inhibit biofilm formation and the expression of relevant virulence factors. This performance could be dynamically regulated via loading with private light-switch property.</p><p><strong>Conclusion: </strong>In this work, designed light-controlled azo molecules provide a new model for resisting bacterial infection via dynamic regulation of bacterial biofilm formation. © 2024 Society of Chemical Industry.</p>","PeriodicalId":218,"journal":{"name":"Pest Management Science","volume":" ","pages":"585-598"},"PeriodicalIF":3.8,"publicationDate":"2025-02-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"142379589","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":1,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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Pest Management Science
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