Merck & Co. Inc., Rahway, NJ, 07065, USA.
Charles A Dana Research Institute of Scientist Emeriti, Drew University, Madison, NJ, 07054, USA.
J Antibiot (Tokyo). 2024 Oct;77(10):679-684. doi: 10.1038/s41429-024-00757-9. Epub 2024 Aug 1.
Boxazomycins A-C are potent broad-spectrum antibiotics isolated from Actinomycetes strain G495-1 in 1987. We now report that boxazomycin A inhibits bacterial growth by selectively inhibiting protein synthesis, its effect is bacteriostatic, and it is equally active against drug resistant bacterial strains. No cross-resistance to protein synthesis inhibitors was observed suggesting that its inhibition is distinct from clinical protein synthesis inhibitors. We also report in vivo efficacy in a Staphylococcus aureus murine infection model supported by corresponding pharmacokinetic studies.
1987 年，从放线菌菌株 G495-1 中分离出了强效广谱抗生素博沙霉素 A、B 和 C。我们现在报告说，博沙霉素 A 通过选择性抑制蛋白质合成来抑制细菌生长，其作用是抑菌的，并且对耐药菌菌株同样有效。没有观察到对蛋白质合成抑制剂的交叉耐药性，这表明其抑制作用与临床蛋白质合成抑制剂不同。我们还报告了在金黄色葡萄球菌感染小鼠模型中的体内疗效，并通过相应的药代动力学研究提供了支持。
