文献类型：期刊文献

英文题名：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

作者：Zhao, Yong-Lian[1];Huang, Xing[1];Liu, Li-Wei[1];Wang, Pei-Yi[1];Long, Qing-Su[1];Tao, Qing-Qing[1];Li, Zhong[2];Yang, Song[1,2]

机构：[1]Guizhou Univ, Key Lab Green Pesticide & Agr Bioengn, State Key Lab Breeding Base Green Pesticide & Agr, Minist Educ,Ctr R&D Fine Chem, Guiyang 550025, Guizhou, Peoples R China;[2]East China Univ Sci & Technol, Coll Pharm, Shanghai 200237, Peoples R China

年份：2019

卷号：67

期号：26

起止页码：7512

外文期刊名：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY

收录：;EI(收录号：20193407331674);WOS:【SCI-EXPANDED(收录号:WOS:000474669600032)】；

基金：We acknowledge financial support from the National Natural Science Foundation of China (21877021, 21662009, 21702037, 31860516), the Research Project of Ministry of Education of China (20135201110005, 213033A), and Guizhou Provincial S&T Program ([2012]6012, LH [2017]7259, [2017]5788).

语种：英文

外文关键词：carbazole; isopropanolamine; antibacterial; proteomics; action mechanism

摘要：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 mu g/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.