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设计和合成扁桃酸衍生物以抑制柑橘溃疡病 T3SS 的毒力。

Design and Synthesis of Mandelic Acid Derivatives for Suppression of Virulence T3SS against Citrus Canker.

机构信息

National Key Laboratory of Green Pesticide, Integrative Microbiology Research Center, Guangdong Province Key Laboratory of Microbial Signals and Disease Control, College of Plant Protection, South China Agricultural University, Guangzhou 510642, China.

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. 2024 May 1;72(17):9611-9620. doi: 10.1021/acs.jafc.3c07681. Epub 2024 Apr 22.

Abstract

Citrus canker, a highly contagious bacterial disease caused by subsp. (), poses a substantial threat to citrus crops, leading to serious reductions in fruit yield and economic losses. Most commonly used bactericides against lead to the rapid development of resistant subpopulations. Therefore, it is imperative to create novel drugs, such as type III secretion system (T3SS) inhibitors, that specifically target bacterial virulence factors rather than bacterial viability. In our study, we designed and synthesized a series of mandelic acid derivatives including 2-mercapto-1,3,4-thiazole. Seven substances were found to reduce the level of transcription of without affecting bacterial viability. bioassays indicated that compound significantly inhibited hypersensitive response and pathogenicity. RT-qPCR assays showed that compound visibly suppressed the expression of T3SS-related genes as well as citrus canker susceptibility gene . Furthermore, the combination with compound and quorum-quenching bacteria HN-8 can also obviously alleviate canker symptoms.

摘要

溃疡病,一种由 亚种()引起的高度传染性细菌性疾病,对柑橘作物构成严重威胁,导致果实产量严重减少和经济损失。针对 ,最常用的杀细菌剂会导致抗药性亚群的迅速发展。因此,必须创造新型药物,如 III 型分泌系统(T3SS)抑制剂,这些药物专门针对细菌的毒力因子,而不是细菌的生存能力。在我们的研究中,我们设计并合成了一系列包括 2-巯基-1,3,4-噻唑的扁桃酸衍生物。发现七种物质可以在不影响细菌活力的情况下降低 的转录水平。生物测定表明,化合物 显著抑制了过敏性反应和致病性。RT-qPCR 检测表明,化合物 明显抑制了 T3SS 相关基因以及溃疡病易感性基因 的表达。此外,与化合物 和群体感应淬灭细菌 HN-8 的联合使用也能明显减轻溃疡病症状。

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