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

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

扫码查看
原文链接
  • 国家科技期刊平台
  • NETL
  • NSTL
  • 万方数据
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 of 1,2,3,4-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 EC50 value 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 mg mL-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 broad-spectrum bactericides.

tetrahydro-β-carboline derivativesantibacterial activityROScell apoptosis

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

展开 >

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

国家自然科学基金国家自然科学基金国家自然科学基金贵州省科技计划the Guizhou Province,ChinaProgram of Introducing Talents of Discipline to Universities of China(111 Program)Guizhou University(GZU)Found for Newly Enrolled Talent,China

2187702132160661322023592018[4007]Qianjiaohe KY number2020004D20023202229

2024

10.1016/j.jia.2023.05.031

农业科学学报(英文)
中国农业科学院农业信息研究所

农业科学学报(英文)

CSTPCD
影响因子：0.576
ISSN：2095-3119
年,卷(期)：2024.23(4)
  • 57