Li Ru-Jia, Qin Chun, Huang Gan-Rong, Liao Li-Juan, Mo Xiao-Qiang, Huang Yan-Qiang
Research Center for the Prevention and Treatment of Drug Resistant Microbial Infecting, Youjiang Medical University for Nationalities, Baise, China.
Front Microbiol. 2022 Apr 28;13:863624. doi: 10.3389/fmicb.2022.863624. eCollection 2022.
With the widespread use and abuse of antibiotics, () has become seriously drug resistant. The development of new antibiotics is an important way to solve 's drug resistance. Screening antibacterial ingredients from natural products is a convenient way to develop new antibiotics. Phillygenin, an effective antibacterial component, was selected from the natural product, forsythia, in this study. Its minimal inhibitory concentration (MIC) for 18 strains was 16-32 μg/ml. The minimum bactericidal concentration (MBC) of G27 was 128 μg/ml; the higher the drug concentration and the longer the time, the better the sterilization effect. It was non-toxic to gastric epithelial cell (GES)-1 and BGC823 cells at the concentration of 100 μg/ml. It presented a better antibacterial effect on in an acidic environment, and after 24 days of induction on with 1/4 MIC of phillygenin, no change was found in the MIC of . In the mechanism of action, phillygenin could cause ATP leakage and inhibit the biofilm formation; the latter was associated with the regulation of and genes. In addition, phillygenin could regulate the genes of , and , leading to the weakening of 's acid resistance and virulence, the diminishing of 's capacity for drug efflux, 's DNA methylation, the initiation of human immune response, and the ATP leakage of , thus accelerating the death of . In conclusion, phillygenin was a main ingredient inhibiting in , with a good antibacterial activity, high safety, strong specificity, better antibacterial effect under acidic conditions, and low risk of resistance development by . Its mechanism of action was mainly associated with inhibiting the biofilm formation and resulting in ATP leakage. In addition, phillygenin was shown to be able to reduce the acid resistance and virulence of .
随着抗生素的广泛使用和滥用,(某菌)已产生严重耐药性。开发新型抗生素是解决(某菌)耐药性问题的重要途径。从天然产物中筛选抗菌成分是开发新型抗生素的便捷方法。本研究从天然产物连翘中筛选出一种有效的抗菌成分连翘酯苷。其对18株(某菌)的最低抑菌浓度(MIC)为16 - 32μg/ml。G27的最低杀菌浓度(MBC)为128μg/ml;药物浓度越高、作用时间越长,杀菌效果越好。在100μg/ml浓度下对胃上皮细胞(GES)-1和BGC823细胞无毒。在酸性环境中对(某菌)呈现出较好的抗菌效果,用1/4 MIC的连翘酯苷对(某菌)诱导24天后,(某菌)的MIC未发生变化。在作用机制方面,连翘酯苷可导致ATP泄漏并抑制生物膜形成;后者与(某些)基因的调控有关。此外,连翘酯苷可调节(某些)基因,导致(某菌)的耐酸性和毒力减弱以及药物外排能力降低、(某菌)的DNA甲基化、人体免疫反应启动以及(某菌)的ATP泄漏,从而加速(某菌)死亡。总之,连翘酯苷是抑制(某菌)的主要成分,具有良好的抗菌活性、高安全性、强特异性、在酸性条件下抗菌效果较好以及(某菌)产生耐药性的风险较低。其作用机制主要与抑制生物膜形成和导致ATP泄漏有关。此外,连翘酯苷还能降低(某菌)的耐酸性和毒力。