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新型 1,3,4-噁二唑类农用杀菌剂先导化合物的发现:利用Ⅲ型分泌系统诱导的细菌饥饿机制防治植物细菌病害

New Inspiration of 1,3,4-Oxadiazole Agrochemical Candidates: Manipulation of a Type III Secretion System-Induced Bacterial Starvation Mechanism to Prevent Plant Bacterial Diseases.

机构信息

National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.

出版信息

J Agric Food Chem. 2023 Feb 15;71(6):2804-2816. doi: 10.1021/acs.jafc.2c07486. Epub 2023 Feb 6.

DOI:10.1021/acs.jafc.2c07486
PMID:36744848
Abstract

Discovering new anti-virulent agents to control plant bacterial diseases by preventing bacterial pathogenesis/pathogenicity rather than affecting bacterial growth is a sensible strategy. However, the effects of compound-manipulated bacterial virulence factors on host response are still not clear. In this work, 35 new 1,3,4-oxadiazole derivatives were synthesized and systematically evaluated for their anti-phytopathogenic activities. Bioassay results revealed that compound possessed outstanding antibacterial activity in vitro (half-maximal effective concentration: 0.80 μg/mL) against pv. () and acceptable bioactivity in vivo toward rice bacterial leaf blight. Furthermore, virulence factor-related biochemical assays showed that was a promising anti-virulent agent. Interestingly, could indirectly reduce the inducible expression of host genes and thereby alleviate nutrient supply in the infection process of phytopathogenic bacteria. Our results highlight the potential of 1,3,4-oxadiazole-based agrochemicals for manipulating type III secretion system-induced phytopathogenic bacteria starvation mechanisms to prevent plant bacterial diseases.

摘要

通过阻止细菌的发病机制/致病性而不是影响细菌生长来发现新的抗毒剂以控制植物细菌性疾病是一种明智的策略。然而,化合物操纵的细菌毒力因子对宿主反应的影响仍不清楚。在这项工作中,合成了 35 种新的 1,3,4-噁二唑衍生物,并对其抗植物病原活性进行了系统评价。生物测定结果表明,化合物 对 pv. ()具有出色的体外抗菌活性(半数有效浓度:0.80μg/mL),对水稻细菌性叶斑病具有可接受的体内生物活性。此外,与毒力因子相关的生化测定表明 是一种有前途的抗毒剂。有趣的是, 可以间接降低宿主 基因的诱导表达,从而减轻感病细菌感染过程中的营养供应。我们的研究结果强调了基于 1,3,4-噁二唑的农用化学品在操纵 III 型分泌系统诱导的植物病原细菌饥饿机制以预防植物细菌性疾病方面的潜力。

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