DNA旋转酶
化学
诺氟沙星
萘啶酸
异黄酮
生物化学
IC50型
柚皮苷
金黄色葡萄球菌
微生物学
环丙沙星
生物
细菌
大肠杆菌
体外
抗生素
类黄酮
抗氧化剂
色谱法
遗传学
基因
作者
Hongyan Lin,Jianqiang Hu,Mei Feng,Yahan Zhang,Yudi Ma,Qingqing Chen,Changyi Wang,Jiangyan Fu,Minkai Yang,Zhongling Wen,Xiaoming Wang,Jinliang Qi,Hongwei Han,Rongwu Yang,Yonghua Yang
摘要
Abstract Aims This study was conducted to evaluate 35 natural flavonoids for their in vitro susceptibility against E. coli (ATCC 25922), Ps. aeruginosa (ATCC 27853), B. subtilis (ATCC 530) and Staph. aureus (ATCC 6538) in search of a potential broad-spectrum antibiotic. Methods and Results Glabridin, a natural isoflavonoid isolated from Glycyrrhiza glabra L., was identified to be highly active with a MIC of 8–16 μg ml−1 against Staph. aureus, B. subtilis and E. coli. By the results of the docking simulation, we located the potential targets of glabridin as DNA gyrase and dihydrofolate reductase (DHFR). The subsequent DNA gyrase inhibition assays (glabridin: IC50 = 0.8516 μmol L−1, ciprofloxacin: IC50 = 0.04697 μmol L−1), DHFR inhibition assays (glabridin: inhibition ratio = 29%, methotrexate: inhibition ratio = 45% under 100 μmol L−1 treatment) and TUNEL confirmed that glabridin acted as DNA gyrase inhibitor and DHFR mild inhibitor, exerting bactericidal activity by blocking bacterial nucleic acid synthesis. CCK-8 and in silico calculations were also conducted to verify the low cytotoxicity and acceptable druggability of glabridin. Conclusion These findings suggest that glabridin represents the prototypical member of an exciting structural class of natural antimicrobial agents. Significance and Impact of the Study This study reports a novel mechanism of bactericidal activity of glabridin against Staph. aureus.
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