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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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New antibacterial depsidones from an ant-derived fungus Spiromastix ***-1

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Chinese Journal of Natural Medicines 2022年第8期20卷 627-632页

作者： GUO Zhi-Kai HU Wen-Yong ZHAO Li-Xing CHEN Yan-Chi LI Sui-Jun CHENG Ping GE Hui-Ming TAN Ren-Xiang JIAO Rui-Hua State Key Laboratory of Pharmaceutical Biotechnology Institute of Functional BiomoleculesSchool of Life SciencesNanjing UniversityNanjing 210093China Hainan Key Laboratory of Tropical Microbe Resources Institute of Tropical Bioscience and BiotechnologyChinese Academy of Tropical Agricultural SciencesHaikou 571101China Yunnan Key Laboratory of Vaccine Research&Development on Severe Infectious Diseases Institute of Medical BiologyChinese Academy of Medical SciencesKunming 650118China Yunnan Institute of Microbiology Yunnan UniversityKunming 650091China

Six new(1–6)and seven known depsidones(7–13)were isolated from the culture of an ant(Monomorium chinensis)-derived fungus Spiromastix *** structures were elucidated by extensive spectroscopic analysis including high resolution MS,1D and 2D NMR *** new bromide depsidones were obtained through supplementing potassium bromide in the fermentation medium of Spiromastix *** isolated compounds showed various bioactivities against the tested phytopathogenic ***,new bromide compound 4,named spiromastixone S,exhibited the strongest activity against Xanthomonas oryzae *** with a MIC value of 5.2μmol·^L(−1).

关键词： Fungus Spiromastix sp Depsidones phytopathogenic bacteria Antibacterial

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