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
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
复制标题
鉴定含有异丙醇胺接头的外消旋和手性咔唑衍生物作为抗植物病原细菌的潜在替代物：体外和体内测定以及定量蛋白质组学
DOI：
10.1021/acs.jafc.9b02036
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发表时间：
2019
影响因子：
6.1
通讯作者：
Yang Song
中科院分区：
文献类型：
--
作者：
Zhao Yong Liang;Huang Xing;Liu Li Wei;Wang Pei Yi;Long Qing Su;Tao Qing Qing;Li Zhong;Yang Song
最近对耐药植物病原菌的出现的观察突出了并引发了一场激烈的运动，以开发用于管理农业细菌性疾病的新型高效抗生素替代物。因此，系统地合成了一类含有异丙醇胺结构的外消旋手性咔唑衍生物，以寻找低成本和有效的抗菌候选物。筛选结果表明，化合物2f、6c和2 j对水稻黄单胞菌（Xanthomonasoryzaepvoryzae）、水稻黄单胞菌（Xanthomonasoryzae）、水稻黄单胞菌（Xanthomonas结果表明，它们对柑橘类细菌性病害的EC_（50）分别为1.27、0.993和0.603 μg/mL，明显优于现有的商品化药物，在植物细菌性病害防治中具有广阔的应用前景。无标记定量蛋白质组学分析表明，化合物2f可显著上调和下调共247个差异表达蛋白，平行反应监测技术进一步验证了这一点。此外，还通过荧光光谱和扫描电镜照片进一步探讨了其抗菌机理。
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 compounds2f,6c, and2jcould significantly suppress the growth of tested plant pathogens, namelyXanthomonas oryzaepvoryzae,X. axonopodispvcitri, andPseudomonas syringaepvactinidiae, and provided the corresponding EC50values of 1.27, 0.993, and 0.603 μg/mL, which were significantly better than those of existing commercial drugs.In vivostudies confirmed their prospective applications for controlling plant bacterial diseases. Label-free quantitative proteomics analysis indicated that compound2fcould 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.