Identification of Racemic and Chiral Carbazole Derivatives Containing an Isopropanolamine Linker as Prospective Surrogates against Plant Pathogenic Bacteria: In Vitro and In Vivo Assays and Quantitative Proteomics,Journal of Agricultural and Food Chemistry

当前位置： X-MOL 学术 › J. Agric. Food Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Identification of Racemic and Chiral Carbazole Derivatives Containing an Isopropanolamine Linker as Prospective Surrogates against Plant Pathogenic Bacteria: In Vitro and In Vivo Assays and Quantitative Proteomics
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2019-06-10 00:00:00 , DOI: 10.1021/acs.jafc.9b02036
Yong-Liang Zhao ₁ , Xing Huang ₁ , Li-Wei Liu ₁ , Pei-Yi Wang ₁ , Qing-Su Long ₁ , Qing-Qing Tao ₁ , Zhong Li ₂ , Song Yang _{1,

2}

Affiliation

Recent observations on the emergence of drug-resistant plant pathogenic bacteria have highlighted and elicited an acute campaign to develop novel, highly efficient antibiotic surrogates for managing bacterial diseases in agriculture. Thus, a type of racemic and chiral carbazole derivative containing an isopropanolamine pattern was systematically synthesized to discover low-cost and efficient antibacterial candidates. Screening results showed that compounds 2f, 6c, and 2j could significantly suppress the growth of tested plant pathogens, namely Xanthomonas oryzae pv oryzae, X. axonopodis pv citri, and Pseudomonas syringae pv actinidiae, and provided the corresponding EC₅₀ values of 1.27, 0.993, and 0.603 μg/mL, which were significantly better than those of existing commercial drugs. In vivo studies confirmed their prospective applications for controlling plant bacterial diseases. Label-free quantitative proteomics analysis indicated that compound 2f could dramatically induce the up- and down-regulation of a total of 247 differentially expressed proteins, which was further validated by the parallel reaction monitoring technique. Moreover, fluorescence spectra and SEM images were obtained to further explore the antibacterial mechanism.

中文翻译：

鉴定含有异丙醇胺接头的外消旋和手性咔唑衍生物作为针对植物病原细菌的前瞻性替代物：体内和体内分析以及定量蛋白质组学

关于抗药性植物病原菌的出现的最新观察结果突出并引发了一项急性运动，以开发新颖，高效的抗生素替代物来管理农业中的细菌性疾病。因此，系统地合成了一种包含异丙醇胺模式的消旋和手性咔唑衍生物，以发现低成本和有效的抗菌药物候选物。筛选结果表明，化合物2f中，图6C，和图2J能显著抑制测试植物病原体，即生长黄单胞菌PV菌，X. axonopodis PV螨，和丁香假单胞菌PV猕猴桃，并提供相应的EC ₅₀值1.27、0.993和0.603μg/ mL，显着优于现有商业药物的EC ₅₀值。体内研究证实了其在控制植物细菌疾病方面的前瞻性应用。无标记定量蛋白质组学分析表明，化合物2f可以显着诱导总共247个差异表达蛋白的上调和下调，这已通过平行反应监测技术进一步验证。此外，获得了荧光光谱和SEM图像以进一步探索其抗菌机理。

更新日期：2019-06-10

点击分享查看原文

点击收藏

阅读更多本刊新发论文本刊介绍/投稿指南