Background: The limited amount of agrochemicals targeting plant bacterial diseases has motivated us to study innovative antibacterial surrogates with fresh modes of action. Notably, fabrication of violent apoptosis inducers to control the reproduction of pathogenic bacteria should be a feasible way to control plant bacterial diseases. To achieve this aim, we constructed a series of novel 18β-glycyrrhetinic piperazine amides based on the natural bioactive ingredient 18β-glycyrrhetinic acid to evaluate the in vitro and in vivo antibacterial activity and induced apoptosis behaviors on tested pathogens.
Results: Screening results suggested that these designed compounds were extremely bioactive against two notorious pathogens, Xanthomonas oryzae pv. oryzae and X. axonopodis pv. citri. This conclusion was highlighted by the biological effects of compounds A3 and B1 , affording the related EC50 values of 2.28 and 0.93 μg mL-1 . In vivo trials confirmed the prospective application for managing rice bacterial blight disease with control efficiency within 50.57-53.70% at 200 μg mL-1 . In particular, target compounds could induce the generation of excessive reactive oxygen species (ROS) in tested pathogens, subsequently leading to a strong apoptotic effect at a very low drug concentration (≤ 10 μg mL-1 ). This finding was consistent with the observed ROS-enhanced fluorescent images and morphological changes of pathogens from scanning electron microscopy patterns.
Conclusion: Given these features, we anticipate that these novel piperazine-tailored 18β-glycyrrhetinic hybrids can provide an perceptible insight for fighting bacterial infections by activation of the apoptosis mechanism. Novel 18β-glycyrrhetinic piperazine amides were reported to have excellent antibacterial efficacy toward phytopathogens Xanthomonas oryzae pv. oryzae and X. axonopodis pv. citri. A possible apoptosis mechanism was proposed from the remarkable apoptotic behaviors triggered by target compounds. © 2020 Society of Chemical Industry.
Keywords: 18β-glycyrrhetinic hybrids; ROS; antibacterial bioassays; apoptosis; mode of action.
© 2020 Society of Chemical Industry.