关键词: [1,2,4]triazolo[3,4‐b][1,3,4]thiadiazole moiety antimicrobial activity label‐free proteomic mechanisms of action

来  源:   DOI:10.1002/ps.8266

Abstract:
BACKGROUND: Plant pathogens cause substantial crop losses annually, posing a grave threat to global food security. Fungicides have usually been used for their control, but the rapid development of pesticide resistance renders many ineffective, therefore the search for novel and efficient green pesticides to prevent and control plant diseases has become the top priority in crop planting.
RESULTS: The results of bioassay studies indicated that most of the target compounds showed certain antimicrobial activity in vitro. In particular, compound X7 showed high inhibitory activity against Xanthomonas oryzae pv. oryzae (Xoo), with an EC50 value of 27.47 μg mL-1, surpassing conventional control agents such as thiazole zinc (41.55 μg mL-1) and thiodiazole copper (53.39 μg mL-1). Further studies on molecular docking showed that X7 had a strong binding affinity with 2FBW. The morphological change observed by scanning electron microscopy indicated that the surface of Xoo appears wrinkled and cracked under X7 treatment and a total of 2662 proteins were identified by label-free proteomic analysis. Three experiments have elucidated the mechanism whereby X7 induced considerable changes in the physiological and biochemical properties of Xoo, which in turn affected the reproduction and growth of bacteria.
CONCLUSIONS: This work represents a pivotal advancement, offering important reference for the research and development therapeutics in combating plant pathogens. © 2024 Society of Chemical Industry.
摘要:
背景:植物病原体每年造成大量作物损失,对全球粮食安全构成严重威胁。杀菌剂通常用于控制它们,但是农药抗性的快速发展使许多无效,因此,寻找新型高效的绿色农药来预防和控制植物病害已成为农作物种植的重中之重。
结果:生物测定研究的结果表明,大多数目标化合物在体外表现出一定的抗菌活性。特别是,化合物X7对水稻黄单胞菌pv具有较高的抑制活性。稻米(Xoo),EC50值为27.47μgmL-1,超过了噻唑锌(41.55μgmL-1)和噻二唑铜(53.39μgmL-1)等常规对照剂。对分子对接的进一步研究表明,X7与2FBW具有很强的结合亲和力。通过扫描电子显微镜观察到的形态变化表明,在X7处理下,Xoo的表面出现皱纹和破裂,通过无标记蛋白质组分析总共2662个蛋白质。三个实验阐明了X7诱导Xoo生理和生化特性发生重大变化的机制,进而影响细菌的繁殖和生长。
结论:这项工作代表了关键的进步,为防治植物病原体的研究和开发提供了重要的参考。©2024化学工业学会。
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