Discovery and structure-activity relationship studies of novel tetrahydro-β-carboline derivatives as apoptosis initiators for treating bacterial infections  

作　　者：Shanshan Su Hongwu Liu Junrong Zhang Puying Qi Yue Ding Ling Zhang Linli Yang Liwei Liu Xiang Zhou Song Yang 

机构地区：[1]National Key Laboratory of Green Pesticide/Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education/Center for R&D of Fine Chemicals,Guizhou University,Guiyang 550025,China

出　　处：《Journal of Integrative Agriculture》2024年第4期1259-1273,共15页农业科学学报（英文版）

基　　金：the supports from National Natural Science Foundation of China(21877021,32160661,and 32202359);the Guizhou Provincial S&T Project China(2018[4007]);the the Guizhou Province China[Qianjiaohe KY number(2020)004];the Program of Introducing Talents of Discipline to Universities of China(D20023,111 Program);the Guizhou University(GZU)Found for Newly Enrolled Talent China(202229)。

摘　　要：Developing and excavating new agrochemicals with highly active and safe is an important tactic for protecting crop health and food safety.In this paper,to discover the new bactericide candidates,we designed,prepared a new type of1,2,3,4-tetrahydro-β-carboline(THC)derivatives and evaluated the in vitro and in vivo bioactivities against the Xanthomonas oryzae pv.oryzae(Xoo),Xanthomonas axonopodis pv.citri(Xac),and Pseudomonas syringae pv.actinidiae(Psa).The in vitro bioassay results exhibited that most title molecules possessed good activity toward the three plant pathogenic bacteria,the compound A17 showed the most active against Xoo and Xac with EC50 values of 7.27 and 4.89 mg mL^(-1)respectively,and compound A8 exhibited the best inhibitory activity against Psa with EC50value of 4.87 mg mL^(-1).Pot experiments showed that compound A17 exhibited excellent in vivo antibacterial activities to manage rice bacterial leaf blight and citrus bacterial canker,with protective efficiencies of 52.67 and 79.79%at 200 mgmL^(-1),respectively.Meanwhile,compound A8 showed good control efficiency(84.31%)against kiwifruit bacterial canker at 200 mg mL^(-1).Antibacterial mechanism suggested that these compounds could interfere with the balance of the redox system,damage the cell membrane,and induce the apoptosis of Xoo cells.Taken together,our study revealed that tetrahydro-β-carboline derivatives could be a promising candidate model for novel broadspectrum bactericides.

关 键 词：tetrahydro-β-carboline derivatives antibacterial activity ROS cell apoptosis 

分 类 号：TQ455[化学工程—农药化工]