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Discovery of cryptolepine derivatives as novel promising agents against phytopathogenic bacteria

Frontiers of Chemical Science and Engineering 2023年第2期17卷 156-166页

作者： Ying-Hui He Qing-Ru Chu Shao-Yong Zhang Li-Rong Guo Yue Ma Bao-Qi Zhang Zhi-Jun Zhang Wen-Bin Zhao Yong-Mei Hu Chen-Jie Yang Sha-Sha Du Tian-Lin Wu Ying-Qian Liu Key Laboratory of Vector Biology and Pathogen Control of Zhejiang Province College of Life ScienceHuzhou UniversityHuzhou 313000China School of Pharmacy Lanzhou UniversityLanzhou 730000China Laboratory of Grassland Agro-ecosystems Lanzhou UniversityLanzhou 730000China

To ensure the production of food crops,a series of cryptolepine derivatives were synthesised,after which their antibacterial activities and mechanism of action against three plant pathogens were *** bioassay results indicated that most of the target compounds displayed potent inhibitory effects against Xanthomonas oryzae(***)and Xanthomonas axonopodis ***(*** pv.c.).Remarkably,compound 9 exhibited the best in vitro antibacterial activity against ***,with a minimum inhibitory concentration(MIC)value of 0.78μg·mL^(-1).Compound 2 exhibited the best in vitro antibacterial activity against *** pv.c.,with an MIC value of 0.39μg·mL^(-1).These activities were superior to those of copper quinolate(MIC=6.25,25μg·mL^(-1))and thiodiazole copper(MIC=100,200μg·mL^(-1))against *** and *** *** vivo experiments demonstrated the promising applicability of compound 9 for the control of rice bacterial ***,compound 9 was selected as a candidate to conduct preliminary analyses of the antibacterial mechanisms of cryptolepine *** electron microscopy and transmission electron microscopy observations,extracellular polysaccharide production,biofilm formation,transcriptomic,quantitative reverse transcription-polymerase chain reaction analyses,and molecular docking assays were ***,our findings demonstrated that compound 9 might act via multifarious mechanisms to down-regulate virulence factors and cause cell death.

关键词： cryptolepine derivatives phytopathogenic bacteria antibacterial activity mechanism of action

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