Molecular Mechanisms of Antibiotics, Division of Life Science, Research Institute of Life Science, Gyeongsang National University, Jinju 52828, Korea.
Division of Applied Life Science (BK21plus Program), Gyeongsang National University, Jinju 52828, Korea.
Molecules. 2020 Mar 31;25(7):1597. doi: 10.3390/molecules25071597.
is the most difficult-to-treat nontuberculous mycobacteria because of its resistance to many antibiotics. In this study, we screened the Korea Chemical Bank library for a bioluminescent reporter assay to identify molecules capable of acting against On application of the assay, rifamycin O showed excellent in vitro activity with a narrow range of the minimum inhibitory concentration required to inhibit the growth of 90% of the bacterium (MIC = 4.0-6.2 μM); its in vivo efficacy in the zebrafish () infection model was comparable to that of rifabutin at 25 μM. Furthermore, rifamycin O did not show significant toxicity in cells and the zebrafish model. These results are the first in vivo indication that rifamycin O may be a drug candidate for treating infections.
是最难治疗的非结核分枝杆菌，因为它对许多抗生素具有耐药性。在这项研究中，我们筛选了韩国化学银行文库中的生物发光报告测定法，以鉴定能够对抗的分子。在应用该测定法时，利福霉素 O 表现出优异的体外活性，其抑制 90%细菌生长所需的最小抑菌浓度范围很窄（MIC = 4.0-6.2 μM）；其在斑马鱼（）感染模型中的体内疗效与 25 μM 的利福布汀相当。此外，利福霉素 O 在细胞和斑马鱼模型中没有显示出显著的毒性。这些结果首次在体内表明，利福霉素 O 可能是治疗 感染的候选药物。
