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依替米星作为一种新型抑制剂。

Etamycin as a Novel Inhibitor.

机构信息

Molecular Mechanisms of Antibiotics, Division of Life Science, Research Institute of Life Science, Division of Applied Life Science (BK21plus Program), Gyeongsang National University, Jinju 52828, Korea.

Department of Environmental Toxicology and Chemistry, Korea Institute of Toxicology, Jinju 52843, Korea.

出版信息

Int J Mol Sci. 2020 Sep 21;21(18):6908. doi: 10.3390/ijms21186908.

Abstract

The increase in drug-resistant , which has become resistant to existing standard-of-care agents, is a major concern, and new antibacterial agents are strongly needed. In this study, we introduced etamycin that showed an excellent activity against . We found that etamycin significantly inhibited the growth of wild-type strain, three subspecies, and clinical isolates in vitro and inhibited the growth of that resides in macrophages without cytotoxicity. Furthermore, the in vivo efficacy of etamycin in the zebrafish () infection model was greater than that of clarithromycin, which is recommended as the core agent for treating infections. Thus, we concluded that etamycin is a potential anti- candidate for further development as a clinical drug candidate.

摘要

耐药性的增加,即对现有标准治疗药物产生耐药性,是一个主要关注点,因此强烈需要新的抗菌药物。在这项研究中,我们引入了艾米霉素,它对 表现出优异的活性。我们发现艾米霉素在体外显著抑制了 野生型菌株、三个亚种和临床分离株的生长,并且对驻留在巨噬细胞中的没有细胞毒性。此外,艾米霉素在斑马鱼()感染模型中的体内疗效优于克拉霉素,克拉霉素被推荐为治疗 感染的核心药物。因此,我们得出结论,艾米霉素是一种有潜力的抗 候选药物,可进一步开发为临床药物候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/21d7/7555287/da68f82120eb/ijms-21-06908-g001.jpg

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