AVIRU, EXIST Transfer of Research, OC II, Lichtenbergstraße 4, 85747 Garching (Germany).
ChemMedChem. 2014 Apr;9(4):710-3. doi: 10.1002/cmdc.201300325. Epub 2014 Feb 20.
Skin infections caused by Staphylococcus aureus are a major clinical concern, especially if they are caused by multi-resistant strains. In these cases, a spread into deeper soft tissues or the bloodstream results in life-threatening conditions that are difficult to treat by conventional antibiotics. Previous in vitro experiments with a small β-lactone-based molecule demonstrated that antibiotic-sensitive and -resistant S. aureus strains are effectively disarmed in their virulence and corresponding pathogenicity. In this work, in vivo mouse studies show that this methodology is effective for the treatment of skin abscesses in mice. A single dose of the β-lactone significantly decreased abscess size even when applied 6 h post-infection. Although the molecule requires pharmacological optimization (improved stability, for example), this study emphasizes the potential value of antivirulence therapies.
金黄色葡萄球菌引起的皮肤感染是一个主要的临床关注点，特别是如果它们是由多耐药菌株引起的。在这些情况下，感染扩散到更深的软组织或血液中会导致危及生命的情况，这使得传统抗生素难以治疗。之前对一种基于小β-内酰胺的分子进行的体外实验表明，抗生素敏感和耐药的金黄色葡萄球菌菌株在其毒力和相应的致病性方面被有效地解除武装。在这项工作中，体内小鼠研究表明，这种方法对治疗小鼠皮肤脓肿是有效的。即使在感染后 6 小时给予单剂量的β-内酰胺，脓肿的大小也显著减小。尽管该分子需要药理学优化（例如提高稳定性），但这项研究强调了抗毒力治疗的潜在价值。
