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发现2-硝基-3-芳基丙烯酸乙酯分子作为III型分泌系统抑制剂可降低植物致病细菌的毒力

Discovery of Ethyl 2-Nitro-3-Arylacrylates Molecules as T3SS Inhibitor Reducing the Virulence of Plant Pathogenic Bacteria .

作者信息

Jiang Shan, Li Hui, Ahmed Wasim, Xiang Xuwen, Song Gaopeng, Cui Zi-Ning

机构信息

State Key Laboratory for Conservation and Utilization of Subtropical Agro-Bioresources, Integrative Microbiology Research Centre, Guangdong Province Key Laboratory of Microbial Signals and Disease Control, South China Agricultural University, Guangzhou, China.

College of Materials and Energy, South China Agricultural University, Guangzhou, China.

出版信息

Front Microbiol. 2019 Aug 20;10:1874. doi: 10.3389/fmicb.2019.01874. eCollection 2019.

Abstract

pv. () is a gram-negative pathogen which causes leaf blight disease. Known traditional bactericides are not much more effective in inhibiting this bacteria than before. Selecting the virulence factor of the bacteria as the target without affecting their growth has been considered as a novel method for developing new anti-microbial drugs. Type III secretion systems (T3SS) are one of the important and highly conserved virulence factors in most gram-negative pathogens, which has been considered as an effective target to develop new anti-microbial drugs. In order to discover potential anti-microbial drugs against pathogens, a series of ethyl 2-nitro-3-arylacrylates compounds were screened. Among them, the compounds I-9, I-12, and I-13 could highly inhibit the promoter activity of a harpin gene , which were used to further check for the influence on bacterial growth and on the hypersensitive response (HR) caused by bacteria on non-host plants. The results showed that above compounds could reduce HR without affecting bacterial growth and survival. Moreover, qRT-PCR analysis indicated that treatment with the three inhibitors (I-9, I-12, and I-13) could suppress the expression of the T3SS in different extent. The mRNA levels of representative genes in the cluster, including the key regulatory genes and , were decreased. Last but not least, test ensured that the above compounds reduced the disease symptoms of on the rice and on the Chinese radish.

摘要

pv.()是一种革兰氏阴性病原菌,可引起叶枯病。已知的传统杀菌剂对这种细菌的抑制效果并不比以前好多少。选择该细菌的毒力因子作为靶点且不影响其生长,已被视为开发新型抗菌药物的一种新方法。III型分泌系统(T3SS)是大多数革兰氏阴性病原菌中重要且高度保守的毒力因子之一,已被视为开发新型抗菌药物的有效靶点。为了发现针对该病原菌的潜在抗菌药物,筛选了一系列2-硝基-3-芳基丙烯酸乙酯化合物。其中,化合物I-9、I-12和I-13能够高度抑制harpin基因的启动子活性,被用于进一步检测其对细菌生长以及该细菌在非寄主植物上引起的过敏反应(HR)的影响。结果表明,上述化合物可降低过敏反应,而不影响细菌的生长和存活。此外,qRT-PCR分析表明,用这三种抑制剂(I-9、I-12和I-13)处理可在不同程度上抑制T3SS的表达。该菌簇中代表性基因的mRNA水平,包括关键调控基因和,均有所下降。最后但同样重要的是,试验证实上述化合物减轻了该病原菌在水稻上以及在白萝卜上的病害症状。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ba48/6710329/51f7028da3ef/fmicb-10-01874-g001.jpg

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