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Design, synthesis and bioactivity studies of flavonol bio‐containing β ‐amino alcohols 生物含β氨基醇类黄酮醇的设计、合成及生物活性研究
IF 4.1 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-12-22 DOI: 10.1002/ps.70353
Yujiao Qiu, Chunmei Hu, Qing Zhou, Qingxue Hu, Jieyu Li, Dan Shen, Xianghui Ruan, Wei Xue
BACKGROUND The escalating field resistance to triazole fungicides has established the development of novel, environmentally benign antifungal agents with distinct mechanisms of action, high efficacy, and low toxicity as an urgent research priority in agricultural chemistry. RESULTS Based on natural flavonol leads, a series of β‐amino alcohol‐containing flavonoid derivatives were synthesized and screened against nine plant pathogenic fungi. Some of them showed good inhibitory effects against Phytophthora capsici , Sclerotinia sclerotiorum , and Phytophthora kiwifruit anopheles ( Phytophthora homopsis sp.). It is noteworthy that compound 5q exhibited significant inhibitory activity against P. capsici , its half‐maximal effective concentration (EC 50 ) was 5.2 μg/mL, the protective and curative activities of compound 5q against eggplants were 85.7% and 77.8% at 200 μg/mL in vivo , which were better than that of azoxystrobin (Az, 42.9% and 35.5%). In addition, scanning electron microscopy (SEM) revealed that compound 5q caused mycelial breakage and crumpling, thereby disrupting normal growth. Malondialdehyde (MDA) content indicated that compound 5q compromised the integrity of fungal cell membranes, and accelerated apoptosis. Molecular docking and dynamics simulations confirmed that compound 5q binds to the cytochrome bc₁ complex with higher structural stability and compactness than Az. CONCLUSION Flavonols derivatives containing β‐amino alcohol moieties exhibit strong potential as novel fungicidal agents. © 2025 Society of Chemical Industry.
背景:随着三唑类杀菌剂耐药性的不断上升,开发作用机制明确、高效、低毒、对环境无害的新型抗真菌药物已成为农业化学研究的当务之急。结果以天然黄酮醇先导物为基础,合成了一系列含β -氨基醇类黄酮衍生物,并对9种植物病原真菌进行了抑菌筛选。其中部分对辣椒疫霉、菌核病疫霉和猕猴桃按蚊疫霉有较好的抑制作用。值得注意的是,化合物5q对辣椒辣椒病菌表现出显著的抑制活性,其一半最大有效浓度(EC 50)为5.2 μg/mL,在200 μg/mL时,化合物5q对茄子的体内保护和治疗活性分别为85.7%和77.8%,优于偶氮嘧菌酯(Az, 42.9%和35.5%)。此外,扫描电镜(SEM)显示化合物5q导致菌丝断裂和皱缩,从而破坏正常生长。丙二醛(MDA)含量表明,化合物5q破坏了真菌细胞膜的完整性,加速了细胞凋亡。分子对接和动力学模拟证实,化合物5q与细胞色素bc₁配合物结合,具有比Az更高的结构稳定性和致密性。结论含β -氨基醇的黄酮醇衍生物具有很强的作为新型杀真菌剂的潜力。©2025化学工业协会。
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引用次数: 0
Nanoselenium and Melatonin Diminish Bensulfuron-methyl Toxicity in Field Wheat by Regulating Interaction among Rhizosphere Soil Allelochemicals, Bacterial Community, and Plant Metabolites. 纳米硒和褪黑素通过调节根际土壤化感物质、细菌群落和植物代谢物之间的相互作用,降低田间小麦苯磺隆-甲基毒性。
IF 6.1 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2025-12-22 DOI: 10.1021/acs.jafc.5c13561
Chunran Zhou,Dong Li,Peijuan Miao,Qinyong Dong,Xiaoying Wan,Huan Yu,Haiyan Cheng,Canping Pan
The crop yield loss and quality decline due to herbicides' unreasonable application seriously threaten global food security. Nanoselenium (nano-Se) and melatonin have been shown to improve plants' tolerance to abiotic stress. Here, this study investigated the effects of nano-Se and melatonin on wheat growth, metabolism, and resistance under bensulfuron-methyl stress through field experiment. Nano-Se and melatonin application activated the indole alkaloid metabolism and increased the contents of tryptamine, 5-hydroxytryptamine, DIMBOA-Glc, and HDMBOA-Glc in leaves, roots, rhizosphere soil, and grains at different wheat growth stages. This increased wheat height (22.3%) and the weight of thousand grains (8.1%) when exposed to bensulfuron. The contents of allelochemicals (jasmonic acid and DIMBOA-Glc), microbial communities (Alphaproteobacteria, Gammaproteobacteria, Bacteroidia, and Gemmatimonadetes), and soil-lipase (21.3%), and soil-fluorescein diacetate (16.4%) were also significantly increased by nano-Se and melatonin biofortification during the wheat ripening stage under bensulfuron treatment. Changes in microbial communities were closely linked to the plant metabolites and soil allelochemicals (benzoxazinoids (BXs)), which promoted wheat growth and lessened the harmful effects of bensulfuron-methyl. In summary, nano-Se and melatonin might reduce phytotoxicity by promoting plant metabolism (BXs) and improving the soil microenvironment and signal transduction in the rhizosphere soil and wheat plants.
由于除草剂的不合理使用,导致作物减产和品质下降,严重威胁着全球粮食安全。纳米硒(nano-Se)和褪黑素已被证明可以提高植物对非生物胁迫的耐受性。本研究通过田间试验研究了纳米硒和褪黑素对苯甲磺隆胁迫下小麦生长、代谢和抗性的影响。纳米硒和褪黑激素激活了吲哚类生物碱代谢,增加了小麦不同生育期叶片、根系、根际土壤和籽粒中色胺、5-羟色胺、DIMBOA-Glc和HDMBOA-Glc的含量。当暴露于苯磺隆时,小麦高(22.3%)和千粒重(8.1%)增加。在苯磺隆处理下,化感物质(茉莉酸和DIMBOA-Glc)、微生物群落(Alphaproteobacteria、Gammaproteobacteria、Bacteroidia和gemmatimonades)、土壤脂酶(21.3%)和土壤荧光素(16.4%)含量均显著提高。微生物群落的变化与植物代谢物和土壤化感物质(苯并恶嗪类化合物)密切相关,它们促进小麦生长,减轻苯并磺隆-甲基的有害影响。综上所述,纳米硒和褪黑激素可能通过促进植物代谢、改善根际土壤和小麦植株的土壤微环境和信号转导来降低植物毒性。
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引用次数: 0
Lactiplantibacillus plantarum JY039 Ameliorates Necrotizing Enterocolitis via Intestinal Stem Cell Regeneration. 植物乳杆菌JY039通过肠道干细胞再生改善坏死性小肠结肠炎。
IF 6.1 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2025-12-22 DOI: 10.1021/acs.jafc.5c09843
Jinfeng Guo,Ying Zhao,Kaiqi Gao,Yilin Sun,Feng Zhao,Yu Zhang,Yujun Jiang
Necrotizing enterocolitis (NEC) is a serious condition in premature infants, driven by dysbiosis-induced inflammation and barrier damage. This study screened probiotics for efficient 2'-fucosyllactose (2'-FL) utilization and intestinal repair potential. Lactiplantibacillus plantarum JY039 (L. plantarum JY039, JY039) was selected from 25 strains (p < 0.05) based on 2'-FL metabolism, intestinal adhesion, and Lgr5 induction in TNF-α-damaged organoids. JY039 showed versatile carbon metabolism and sensitivity to 11 antibiotics, indicating its clinical safety. In TNF-α-injured organoids, it elevated intestinal stem cell (ISC) markers (Olfm4 and Ascl2, 4-fold) and proliferation markers (c-Myc, Ki67, and cyclins, 3-fold), with EdU intensity increasing 4-fold versus NEC models. In NEC rats, JY039 (109 CFU/mL) reduced pathology scores and permeability, restored tight junctions, modulated cytokines (TNF-α, IL-6, myeloperoxidase decreased; and IL-10 increased, p < 0.05), activated ISC regeneration, and enriched Lactococcus and Akkermansia. JY039 effectively maintained epithelial regeneration and improved the microbial imbalance, representing a safe NEC candidate. It also offers guidance for producing a functional infant formula.
坏死性小肠结肠炎(NEC)是早产儿的一种严重疾病,由生态失调引起的炎症和屏障损伤驱动。本研究筛选了具有2′-聚焦乳糖(2′- fl)高效利用和肠道修复潜力的益生菌。根据2′-FL代谢、肠道粘附、Lgr5诱导TNF-α-损伤的类器官,从25株菌株中筛选出植物乳杆菌JY039 (L. plantarum JY039, JY039)。JY039碳代谢多样,对11种抗生素敏感,临床安全性较高。在TNF-α-损伤的类器官中,它升高了肠干细胞(ISC)标志物(Olfm4和Ascl2, 4倍)和增殖标志物(c-Myc, Ki67和cyclins, 3倍),EdU强度比NEC模型增加了4倍。在NEC大鼠中,JY039 (109 CFU/mL)降低病理评分和通透性,恢复紧密连接,调节细胞因子(TNF-α、IL-6、髓过氧化物酶降低,IL-10升高,p < 0.05),激活ISC再生,并富集乳球菌和Akkermansia。JY039有效维持上皮再生,改善微生物失衡,是一种安全的NEC候选药物。它还为生产功能性婴儿配方奶粉提供了指导。
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引用次数: 0
Natural Dietary Flavonoid Apigenin Mitigates Ulcerative Colitis via Modulating the AMPK/NF-κB/NLRP3 Signaling Axis. 天然膳食黄酮类芹菜素通过调节AMPK/NF-κB/NLRP3信号轴减轻溃疡性结肠炎。
IF 6.1 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2025-12-22 DOI: 10.1021/acs.jafc.5c15405
Mengsha Zhou,Xiaoshuang Mao,Lin-En Zou,Ying Yang,Wenli Zhao,Yinan Yang,Shihao Sun,Zhongyi Mao,Peng Li,Guihong Qi
Ulcerative colitis (UC) is a challenging inflammatory disease with higher relapse and lower remission rates, urgently requiring effective and safe complementary treatment options. Apigenin (Api), a natural flavonoid from parsley and celery, exhibits potent antioxidant and anti-inflammatory activities. In mice with 2.5% DSS-induced acute colitis, Api markedly alleviated weight loss, colon shortening, and elevated DAI scores, while restoring mucosal integrity and reducing oxidative stress and inflammation. Mechanistically, Api can directly bind to AMPK to activate it, thereby alleviating oxidative stress and suppressing the NF-κB pathway, which in turn inhibits NLRP3 inflammasome activation. Moreover, Api directly binds to NLRP3, thereby inhibiting inflammasome activation. Through dual targeting of AMPK and NLRP3, Api cooperatively suppresses oxidative stress and inflammation in UC mice. Collectively, these findings demonstrate that Api protects against colitis via modulation of the AMPK/NF-κB/NLRP3 axis, highlighting its potential as a natural anti-inflammatory agent for intestinal health.
溃疡性结肠炎(UC)是一种具有高复发率和低缓解率的挑战性炎症性疾病,迫切需要有效和安全的补充治疗方案。芹菜素(Apigenin, Api)是一种从欧芹和芹菜中提取的天然类黄酮,具有很强的抗氧化和抗炎活性。在2.5% dss诱导的急性结肠炎小鼠中,Api显著缓解体重减轻、结肠缩短和DAI评分升高,同时恢复粘膜完整性,减少氧化应激和炎症。在机制上,Api可直接与AMPK结合激活AMPK,从而缓解氧化应激,抑制NF-κB通路,进而抑制NLRP3炎性体的激活。此外,Api直接与NLRP3结合,从而抑制炎症小体的激活。Api通过双重靶向AMPK和NLRP3,共同抑制UC小鼠的氧化应激和炎症。总的来说,这些发现表明Api通过调节AMPK/NF-κB/NLRP3轴来预防结肠炎,突出了其作为肠道健康天然抗炎剂的潜力。
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引用次数: 0
Design and synthesis of N ‐heterocycle‐fused azolyl selenoureas against Rhizoctonia solani and its mode‐of‐action N -杂环融合偶氮基硒脲的设计、合成及其作用方式
IF 4.1 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-12-22 DOI: 10.1002/ps.70478
Li Dong, Xuefen Zheng, Chuxin Rong, Lantu Xiong, Bo Yang, Ri‐Yuan Tang
BACKGROUND Rhizoctonia solani , a deleterious fungal pathogen, significantly impedes global crop productivity. This investigation focused on designing and synthesizing novel N ‐heterocycle‐fused azolyl selenoureas to assess their antifungal efficacy and molecular mode‐of‐action against R. solani . RESULTS A series of N ‐heterocycle‐fused azolyl selenoureas were synthesized. Most compounds demonstrated significant antifungal activity (median effective concentration 2.3–13.4 mg L −1 ). Compound 2 exhibited potent in vitro and in vivo efficacy. Its curative and protective effects on detached rice leaves were concentration‐dependent, with maximal efficacy at 100 mg L −1 (80.8 and 81.2%, respectively) exceeding azoxystrobin. Notably, it substantially inhibited sclerotial germination (45.3% at 6.25 mg L −1 ). Mechanistic investigations revealed severe disruption of hyphal tissue structure, and increased membrane permeability and cytoplasmic leakage, resulting in cellular mortality. Additionally, it induced reactive oxygen species generation, dissipated mitochondrial membrane potential and reduced nuclear count. Transcriptomic analysis demonstrated significant downregulation of MCM2‐7 and PCNA genes associated with DNA replication pathways. CONCLUSION N ‐heterocycle‐fused azolyl selenoureas, particularly compound 2 , demonstrate potential as multimechanistic agents for R. solani management in agricultural pathology. © 2025 Society of Chemical Industry.
茄枯丝核菌是一种有害的真菌病原体,严重阻碍了全球作物的生产力。本研究旨在设计和合成新型N -杂环融合偶氮基硒脲,并对其抗真菌效果和分子作用模式进行研究。结果合成了一系列N -杂环熔融偶氮基硒脲。大多数化合物表现出显著的抗真菌活性(中位有效浓度为2.3-13.4 mg L−1)。化合物2具有较强的体内外药效。其对水稻离体叶片的治疗和保护作用呈浓度依赖性,在100 mg L−1时的最大效果(分别为80.8%和81.2%)超过氮嘧菌酯。值得注意的是,在6.25 mg L−1时,它显著抑制了菌核萌发(45.3%)。机制研究显示菌丝组织结构严重破坏,膜通透性增加,细胞质渗漏,导致细胞死亡。此外,它诱导活性氧的产生,消散线粒体膜电位,减少核计数。转录组学分析显示,与DNA复制途径相关的MCM2‐7和PCNA基因显著下调。结论N -杂环融合偶氮基硒脲,特别是化合物2,在农业病理中具有多机制治疗茄蚜的潜力。©2025化学工业协会。
{"title":"Design and synthesis of N ‐heterocycle‐fused azolyl selenoureas against Rhizoctonia solani and its mode‐of‐action","authors":"Li Dong, Xuefen Zheng, Chuxin Rong, Lantu Xiong, Bo Yang, Ri‐Yuan Tang","doi":"10.1002/ps.70478","DOIUrl":"https://doi.org/10.1002/ps.70478","url":null,"abstract":"BACKGROUND <jats:italic>Rhizoctonia solani</jats:italic> , a deleterious fungal pathogen, significantly impedes global crop productivity. This investigation focused on designing and synthesizing novel <jats:italic>N</jats:italic> ‐heterocycle‐fused azolyl selenoureas to assess their antifungal efficacy and molecular mode‐of‐action against <jats:italic>R. solani</jats:italic> . RESULTS A series of <jats:italic>N</jats:italic> ‐heterocycle‐fused azolyl selenoureas were synthesized. Most compounds demonstrated significant antifungal activity (median effective concentration 2.3–13.4 mg L <jats:sup>−1</jats:sup> ). Compound 2 exhibited potent <jats:italic>in vitro</jats:italic> and <jats:italic>in vivo</jats:italic> efficacy. Its curative and protective effects on detached rice leaves were concentration‐dependent, with maximal efficacy at 100 mg L <jats:sup>−1</jats:sup> (80.8 and 81.2%, respectively) exceeding azoxystrobin. Notably, it substantially inhibited sclerotial germination (45.3% at 6.25 mg L <jats:sup>−1</jats:sup> ). Mechanistic investigations revealed severe disruption of hyphal tissue structure, and increased membrane permeability and cytoplasmic leakage, resulting in cellular mortality. Additionally, it induced reactive oxygen species generation, dissipated mitochondrial membrane potential and reduced nuclear count. Transcriptomic analysis demonstrated significant downregulation of <jats:italic>MCM2‐7</jats:italic> and <jats:italic>PCNA</jats:italic> genes associated with DNA replication pathways. CONCLUSION <jats:italic>N</jats:italic> ‐heterocycle‐fused azolyl selenoureas, particularly compound 2 , demonstrate potential as multimechanistic agents for <jats:italic>R. solani</jats:italic> management in agricultural pathology. © 2025 Society of Chemical Industry.","PeriodicalId":218,"journal":{"name":"Pest Management Science","volume":"361 1","pages":""},"PeriodicalIF":4.1,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145801264","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
VvU2A' -mediated circRNA biogenesis confers salt tolerance in grapevine via the VvcircHMA1 -VvmiR167b- VvARF6 pathway VvU2A'介导的circRNA生物发生通过VvcircHMA1 - vvmir167b - VvARF6途径赋予葡萄耐盐性
IF 8.7 1区 农林科学 Q1 Agricultural and Biological Sciences Pub Date : 2025-12-22 DOI: 10.1093/hr/uhaf355
Zhen Gao, Le Zheng, Yeqi Li, Jing Li, Yuanpeng Du
Circular RNAs (circRNAs) play important roles in plant stress responses, yet their dynamic regulation during stress remains unclear. This study elucidates a molecular mechanism whereby the grapevine U2 snRNP core component VvU2A' enhances salt tolerance through a circRNA-mediated post-transcriptional network. We found that VvU2A' expression is induced by salt stress and positively regulates salt tolerance in grapevine. CircRNA sequencing revealed 497 VvU2A'-regulated differentially expressed circRNAs, including downregulated VvcircHMA1. Mechanistic investigation revealed that VvcircHMA1 acts as a competitive endogenous RNA (ceRNA) by sequestering VvmiR167b, thereby attenuating its cleavage activity on the target mRNA VvARF6. Functional analyses revealed that both VvcircHMA1 and VvARF6 negatively regulate salt tolerance, while VvmiR167b positively regulates it. Collectively, our study reveals a novel mechanism by which the splicing factor VvU2A' enhances salt stress response through the VvcircHMA1-VvmiR167b-VvARF6 cascade, providing promising molecular targets for breeding salt-resistant grapevines.
环状rna (circRNAs)在植物逆境反应中发挥重要作用,但其在逆境中的动态调控尚不清楚。本研究阐明了葡萄U2 snRNP核心组分VvU2A'通过circrna介导的转录后网络增强耐盐性的分子机制。我们发现VvU2A的表达受盐胁迫诱导,并正向调节葡萄的耐盐性。CircRNA测序显示497个VvU2A'调控的差异表达CircRNA,包括下调的VvcircHMA1。机制研究表明,VvcircHMA1通过隔离VvmiR167b作为竞争性内源性RNA (ceRNA),从而减弱其对靶mRNA VvARF6的切割活性。功能分析显示,VvcircHMA1和VvARF6负调控耐盐性,而VvmiR167b正调控耐盐性。总之,我们的研究揭示了剪接因子VvU2A'通过VvcircHMA1-VvmiR167b-VvARF6级联增强盐胁迫响应的新机制,为培育耐盐葡萄提供了有希望的分子靶点。
{"title":"VvU2A' -mediated circRNA biogenesis confers salt tolerance in grapevine via the VvcircHMA1 -VvmiR167b- VvARF6 pathway","authors":"Zhen Gao, Le Zheng, Yeqi Li, Jing Li, Yuanpeng Du","doi":"10.1093/hr/uhaf355","DOIUrl":"https://doi.org/10.1093/hr/uhaf355","url":null,"abstract":"Circular RNAs (circRNAs) play important roles in plant stress responses, yet their dynamic regulation during stress remains unclear. This study elucidates a molecular mechanism whereby the grapevine U2 snRNP core component VvU2A' enhances salt tolerance through a circRNA-mediated post-transcriptional network. We found that VvU2A' expression is induced by salt stress and positively regulates salt tolerance in grapevine. CircRNA sequencing revealed 497 VvU2A'-regulated differentially expressed circRNAs, including downregulated VvcircHMA1. Mechanistic investigation revealed that VvcircHMA1 acts as a competitive endogenous RNA (ceRNA) by sequestering VvmiR167b, thereby attenuating its cleavage activity on the target mRNA VvARF6. Functional analyses revealed that both VvcircHMA1 and VvARF6 negatively regulate salt tolerance, while VvmiR167b positively regulates it. Collectively, our study reveals a novel mechanism by which the splicing factor VvU2A' enhances salt stress response through the VvcircHMA1-VvmiR167b-VvARF6 cascade, providing promising molecular targets for breeding salt-resistant grapevines.","PeriodicalId":13179,"journal":{"name":"Horticulture Research","volume":"1 1","pages":""},"PeriodicalIF":8.7,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145801223","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
Novel cinnamic acid‐ribavirin conjugates: design, synthesis, antiviral activity against tobacco mosaic virus and mechanistic study 新型肉桂酸-利巴韦林缀合物:设计、合成、抗烟草花叶病毒活性及机制研究
IF 4.1 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-12-22 DOI: 10.1002/ps.70462
Min Luo, Chen Chen, Min Xu, Wen‐Xin Lv, Yonggui Robin Chi
BACKGROUND Plant viral diseases represent a serious threat to global agricultural productivity and sustainable development. Most commercially available antiviral agents function primarily as protectants. However, the long‐term and repetitive application of conventional broad‐spectrum antiviral agents has led to the emergence of resistance, diminishing their field efficacy. To discover new antiviral drugs, we designed and synthesized 31 novel ribavirin derivatives incorporating cinnamic acid motifs via a lead optimization strategy and evaluated their anti‐tobacco mosaic virus (TMV) activity. RESULTS Biological assays revealed that compound A23 exhibited potent protective activity against TMV, with an EC₅₀ of 131.1 μg/mL, which was significantly lower than that of ribavirin (529.9 μg/mL) and ningnanmycin (248.4 μg/mL). Further research indicated that compound A23 significantly enhanced the activity of defense‐related enzymes and regulated the plant hormone signal transduction pathway as well as the plant‐pathogen interaction pathway in tobacco plants. Notably, it upregulated the expression of key genes NPR1 and PR‐1 in the salicylic acid (SA) signaling pathway, thereby effectively enhancing the plant's defense response and resistance against TMV. CONCLUSION These results demonstrate that compound A23 possesses remarkable bioactivity and effectively controls TMV infection by inducing host plant immunity. Its promising efficacy supports its potential as a candidate agent for controlling plant viral diseases and warrants further investigation. © 2025 Society of Chemical Industry.
植物病毒性病害对全球农业生产力和可持续发展构成严重威胁。大多数市售抗病毒药物主要起保护作用。然而,长期和重复使用常规广谱抗病毒药物导致耐药性的出现,降低了它们的田间疗效。为了发现新的抗病毒药物,我们采用先导优化策略设计并合成了31种含有肉桂酸基序的利巴韦林衍生物,并对其抗烟草花叶病毒(TMV)活性进行了评价。结果生物实验表明,化合物A23对TMV具有较强的保护作用,其EC₅0为131.1 μg/mL,显著低于利巴韦林(529.9 μg/mL)和宁南霉素(248.4 μg/mL)。进一步研究表明,化合物A23可显著增强烟草植株防御相关酶的活性,调控植物激素信号转导通路和植物-病原体互作通路。值得注意的是,它上调了水杨酸(SA)信号通路中关键基因NPR1和PR‐1的表达,从而有效增强了植物对TMV的防御反应和抗性。结论化合物A23具有显著的生物活性,可通过诱导寄主植物免疫来有效控制TMV感染。其良好的药效支持其作为防治植物病毒性疾病的候选药剂的潜力,值得进一步研究。©2025化学工业协会。
{"title":"Novel cinnamic acid‐ribavirin conjugates: design, synthesis, antiviral activity against tobacco mosaic virus and mechanistic study","authors":"Min Luo, Chen Chen, Min Xu, Wen‐Xin Lv, Yonggui Robin Chi","doi":"10.1002/ps.70462","DOIUrl":"https://doi.org/10.1002/ps.70462","url":null,"abstract":"BACKGROUND Plant viral diseases represent a serious threat to global agricultural productivity and sustainable development. Most commercially available antiviral agents function primarily as protectants. However, the long‐term and repetitive application of conventional broad‐spectrum antiviral agents has led to the emergence of resistance, diminishing their field efficacy. To discover new antiviral drugs, we designed and synthesized 31 novel ribavirin derivatives incorporating cinnamic acid motifs <jats:italic>via</jats:italic> a lead optimization strategy and evaluated their anti‐tobacco mosaic virus (TMV) activity. RESULTS Biological assays revealed that compound A23 exhibited potent protective activity against TMV, with an EC₅₀ of 131.1 μg/mL, which was significantly lower than that of ribavirin (529.9 μg/mL) and ningnanmycin (248.4 μg/mL). Further research indicated that compound A23 significantly enhanced the activity of defense‐related enzymes and regulated the plant hormone signal transduction pathway as well as the plant‐pathogen interaction pathway in tobacco plants. Notably, it upregulated the expression of key genes <jats:italic>NPR1</jats:italic> and <jats:italic>PR‐1</jats:italic> in the salicylic acid (SA) signaling pathway, thereby effectively enhancing the plant's defense response and resistance against TMV. CONCLUSION These results demonstrate that compound A23 possesses remarkable bioactivity and effectively controls TMV infection by inducing host plant immunity. Its promising efficacy supports its potential as a candidate agent for controlling plant viral diseases and warrants further investigation. © 2025 Society of Chemical Industry.","PeriodicalId":218,"journal":{"name":"Pest Management Science","volume":"30 1","pages":""},"PeriodicalIF":4.1,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145801262","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
Propyl Gallate Mitigates Gastric Injury Caused by Indomethacin in Wistar Rats. 没食子酸丙酯减轻吲哚美辛致Wistar大鼠胃损伤。
IF 6.1 1区 农林科学 Q1 AGRICULTURE, MULTIDISCIPLINARY Pub Date : 2025-12-22 DOI: 10.1021/acs.jafc.5c13909
Felix Widodo,Yun-Ya Wang,Tsair-Bor Yen,Kuo-Chan Tseng,Yu-Hsiang Chen,Shih-Chao Lin,Pei-Shan Tsai,Yu-Kuo Chen
Propyl gallate (PG) is an edible food-grade antioxidant, but its gastroprotective potential has not been extensively evaluated. This study evaluated the protective effects of PG on indomethacin-induced gastric mucosal injury in Wistar rats. Male rats were assigned to control (C), vehicle (Vehicle), PG-treated (20, 40, and 100 mg/kg; LPG, MPG, and HPG), and positive control (omeprazole, 30 mg/kg; OM). Following 7 days of pretreatment, indomethacin (100 mg/kg) was administered to all groups except group C, and the gastric tissues were collected for further analysis. PG pretreatment significantly reduced ulcer area in a dose-dependent manner (p < 0.05). PG also suppressed gastric inflammatory protein expression (NF-κB, COX-2, TNF-α, IL-6, and iNOS), restoring prostaglandin E2 (PGE2) levels, and enhanced antioxidant defenses, as evidenced by increased glutathione (GSH) levels and superoxide dismutase (SOD) activity. These findings demonstrate that PG exerts marked gastroprotective effects through combined anti-inflammatory and antioxidant mechanisms.
没食子酸丙酯(PG)是一种可食用的食品级抗氧化剂,但其胃保护作用尚未得到广泛的评价。本研究评价PG对吲哚美辛致Wistar大鼠胃粘膜损伤的保护作用。雄性大鼠分为对照组(C)、对照组(vehicle)、pg处理组(20、40和100 mg/kg; LPG、MPG和HPG)和阳性对照组(奥美拉唑,30 mg/kg; OM)。预处理7 d后,除C组外,其余各组均给予吲哚美辛(100 mg/kg),并收集胃组织进行进一步分析。PG预处理显著减少溃疡面积,呈剂量依赖性(p < 0.05)。PG还能抑制胃炎症蛋白(NF-κB、COX-2、TNF-α、IL-6和iNOS)的表达,恢复前列腺素E2 (PGE2)水平,增强抗氧化防御能力,表现为谷胱甘肽(GSH)水平和超氧化物歧化酶(SOD)活性的升高。这些结果表明,PG通过抗炎和抗氧化的联合机制具有明显的胃保护作用。
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引用次数: 0
Iron plaque in paddy: formation, properties, functions, and applications 水稻中的铁质斑块:形成、性质、功能及应用
IF 9.7 1区 农林科学 Q1 SOIL SCIENCE Pub Date : 2025-12-22 DOI: 10.1016/j.soilbio.2025.110075
Zhao-Feng Yuan, Tida Ge, Dong-Xing Guan, Bin He, Xiaokai Zhang, Yongfu Li, Zhenke Zhu, Gang Li, Pil Joo Kim, Georg Guggenberger, Minggang Xu, Jianping Chen, Yakov Kuzyakov
Iron (Fe) plaque is a ubiquitous feature formed on root surfaces of wetland plants (e.g., rice), resulting from the oxidation of Fe2+ to Fe3+ driven by radial oxygen loss from roots. Fe plaque formation is primarily driven by abiotic pathways: influx of water with dissolved Fe2+ from bulk soil to roots and rhizosphere, wherein Fe2+ is oxidized by O2 released from aerenchyma, and reactive species (e.g., ∙HO, ∙NO2, ∙NO) produced by electron transport from Fe2+ within Fe plaque. Biotic pathways, mediated mainly by Fe-reducing and Fe-oxidizing bacteria in rhizosphere, regulate Fe plaque formation. Fe plaque is mainly composed of ferrihydrite (Fe2O3∙nH2O), goethite (α-FeOOH), lepidocrocite (γ-FeOOH), but may include siderite (FeCO3), and vivianite (Fe3(PO4)2). Soil properties, plant species, developmental stages and redox fluctuations substantially influence Fe plaque composition and formation rate, as well its dissolution. As a microbial and biogeochemical hotspot in paddy ecosystems, Fe plaque interacts extensively with nutrients and contaminants, influencing their bioavailability and plant uptake. With extensive reactive surface area and abundant functional groups, Fe plaque functions as both a barrier and reservoir for nutrients and contaminants. We developed the concept of “Fe circuit” to describe its dual functions on elemental cycling in rice rhizosphere. Fe plaque can be utilized for in-situ immobilizing or removing contaminants in paddy soil. This review offers a comprehensive perspective on Fe plaque and its potential to remediate contaminants in paddy soil and other wetlands.
铁(Fe)斑块是湿地植物(如水稻)根表面普遍存在的特征,是由根系径向氧损失驱动Fe2+氧化为Fe3+造成的。铁斑块的形成主要由非生物途径驱动:从大块土壤中溶解的Fe2+的水流入根部和根际,其中Fe2+被空气组织释放的O2氧化,以及铁斑块内Fe2+的电子传递产生的活性物质(例如∙HO,∙NO2,∙NO)。生物途径主要由根际铁还原菌和铁氧化菌介导,调控铁斑块的形成。铁斑块主要由水合铁(Fe2O3∙nH2O)、针铁矿(α-FeOOH)、绢云母(γ-FeOOH)组成,但也可能包括菱铁矿(FeCO3)和橄榄石(Fe3(PO4)2)。土壤性质、植物种类、发育阶段和氧化还原波动对铁斑块的组成和形成速率以及其溶解有很大影响。作为水稻生态系统中微生物和生物地球化学热点,铁斑块与养分和污染物广泛相互作用,影响其生物利用度和植物吸收。铁斑块具有广泛的活性表面积和丰富的官能团,既是营养物质和污染物的屏障,也是其储存库。我们提出了“铁回路”的概念来描述其在水稻根际元素循环中的双重功能。铁膜可用于水稻土的原位固定化或去除污染物。本文综述了稻田土和其他湿地中铁斑块及其修复污染物的潜力。
{"title":"Iron plaque in paddy: formation, properties, functions, and applications","authors":"Zhao-Feng Yuan, Tida Ge, Dong-Xing Guan, Bin He, Xiaokai Zhang, Yongfu Li, Zhenke Zhu, Gang Li, Pil Joo Kim, Georg Guggenberger, Minggang Xu, Jianping Chen, Yakov Kuzyakov","doi":"10.1016/j.soilbio.2025.110075","DOIUrl":"https://doi.org/10.1016/j.soilbio.2025.110075","url":null,"abstract":"Iron (Fe) plaque is a ubiquitous feature formed on root surfaces of wetland plants (e.g., rice), resulting from the oxidation of Fe<sup>2+</sup> to Fe<sup>3+</sup> driven by radial oxygen loss from roots. Fe plaque formation is primarily driven by abiotic pathways: influx of water with dissolved Fe<sup>2+</sup> from bulk soil to roots and rhizosphere, wherein Fe<sup>2+</sup> is oxidized by O<sub>2</sub> released from aerenchyma, and reactive species (e.g., ∙HO, ∙NO<sub>2</sub>, ∙NO) produced by electron transport from Fe<sup>2+</sup> within Fe plaque. Biotic pathways, mediated mainly by Fe-reducing and Fe-oxidizing bacteria in rhizosphere, regulate Fe plaque formation. Fe plaque is mainly composed of ferrihydrite (Fe<sub>2</sub>O<sub>3</sub>∙nH<sub>2</sub>O), goethite (α-FeOOH), lepidocrocite (γ-FeOOH), but may include siderite (FeCO<sub>3</sub>), and vivianite (Fe<sub>3</sub>(PO<sub>4</sub>)<sub>2</sub>). Soil properties, plant species, developmental stages and redox fluctuations substantially influence Fe plaque composition and formation rate, as well its dissolution. As a microbial and biogeochemical hotspot in paddy ecosystems, Fe plaque interacts extensively with nutrients and contaminants, influencing their bioavailability and plant uptake. With extensive reactive surface area and abundant functional groups, Fe plaque functions as both a barrier and reservoir for nutrients and contaminants. We developed the concept of “Fe circuit” to describe its dual functions on elemental cycling in rice rhizosphere. Fe plaque can be utilized for <em>in-situ</em> immobilizing or removing contaminants in paddy soil. This review offers a comprehensive perspective on Fe plaque and its potential to remediate contaminants in paddy soil and other wetlands.","PeriodicalId":21888,"journal":{"name":"Soil Biology & Biochemistry","volume":"3 1","pages":""},"PeriodicalIF":9.7,"publicationDate":"2025-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145801472","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
Evolving resistance patterns in Tetranychus urticae and Bemisia tabaci in Greece 希腊荨麻疹叶螨和烟粉虱抗性模式的进化
IF 4.1 1区 农林科学 Q1 AGRONOMY Pub Date : 2025-12-22 DOI: 10.1002/ps.70475
Anastasia Kampouraki, Aris Ilias, Kiriaki‐Maria Papapostolou, Styliani Malliaraki, Ioannis Pirgianakis, Evangelia Karakosta, John Vontas, Anastasia Tsagkarakou, Konstantinos Mavridis
BACKGROUND Pesticide resistance in agricultural pests remains a major barrier to effective and sustainable crop protection. In this study, we assessed the current resistance status of two key pests, Tetranychus urticae and Bemisia tabaci , in major agricultural regions of Greece. A total of 25 field populations (19 of T. urticae and six of B. tabaci ) were collected between 2023 and 2025 and tested using single‐dose bioassays and droplet digital PCR (ddPCR) for target‐site resistance mutations. RESULTS The results revealed significant variability in susceptibility to multiple acaricides and insecticides. Several T. urticae populations displaying reduced sensitivity to abamectin, hexythiazox, and fenpyroximate. Resistance mutations such as I321T ( GluCl3 ), I1017F ( CHS1 ), F1538I ( vgsc ), and G126S ( cytb ) were detected simultaneously at high frequencies in several T. urticae populations, indicating multi‐resistant phenotypes. A widespread occurrence of F331W ( ace1 ), L925I/T929V ( vgsc ), and A2083V ( acc ) mutations were recorded in B. tabaci , showing the dynamics of resistance to organophosphates, pyrethroids, and ketoenols, respectively. CONCLUSION Our findings underscore the ongoing evolution of resistance in these pests and highlight the need for integrated management strategies that include regular resistance monitoring and judicious pesticide use. This study provides resistance surveillance data to guide pest control decisions and promote sustainable Integrated Pest Management (IPM) in Greece. © 2025 The Author(s). Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.
农业害虫的农药抗性仍然是有效和可持续作物保护的主要障碍。在本研究中,我们评估了两种主要害虫荨麻疹叶螨和烟粉虱在希腊主要农业区的抗性现状。在2023年至2025年期间,共收集了25个野外种群(19个荨麻疹T.和6个烟粉虱),并使用单剂量生物测定法和液滴数字PCR (ddPCR)对目标位点抗性突变进行了检测。结果对多种杀螨剂和杀虫剂的敏感性存在显著差异。一些荨麻疹种群对阿维菌素、己噻唑和苯吡肟的敏感性降低。耐药突变如I321T (GluCl3)、I1017F (CHS1)、F1538I (vgsc)和G126S (cytb)在几个荨麻疹种群中同时高频率检测到,表明多重耐药表型。F331W (ace1)、L925I/T929V (vgsc)和A2083V (acc)突变在烟粉虱中广泛存在,分别表现出对有机磷、拟除虫菊酯和酮醇的抗性动态。结论我们的研究结果强调了这些害虫抗性的持续演变,并强调了综合管理策略的必要性,包括定期监测抗性和明智地使用农药。本研究提供了抗性监测数据,以指导希腊害虫防治决策和促进可持续的害虫综合治理(IPM)。©2025作者。《有害生物管理科学》由John Wiley &; Sons Ltd代表化学工业协会出版。
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