In vitro activities of arylomycin natural-product antibiotics against Staphylococcus epidermidis and other coagulase-negative staphylococci.
In vitro activities of arylomycin natural-product antibiotics against Staphylococcus epidermidis and other coagulase-negative staphylococci.
复制标题
arylomycin 天然产物抗生素对表皮葡萄球菌和其他凝固酶阴性葡萄球菌的体外活性。
DOI：
10.1128/aac.01459-10
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发表时间：
2011
影响因子：
4.9
通讯作者：
Romesberg,FloydE
中科院分区：
文献类型：
--
作者：
Smith,PeterA;Powers,MichaelE;Roberts,TuckerC;Romesberg,FloydE
芳基霉素是一类天然产物抗生素，其通过抑制I型信号肽酶（SPase）起作用，并且我们已经在多种细菌中发现，它们的活性受到SPase中存在的赋予抗性的Pro残基的限制，该残基减少抑制剂结合。我们还证明了表皮葡萄球菌缺乏这种Pro残基，对芳香霉素非常敏感。在这里，为了进一步探索芳基霉素的潜在效用，我们报告了一个合成的芳基霉素衍生物，芳基霉素C16，对临床分离的S。表皮病和其他凝固酶阴性葡萄球菌（CoNS）来自不同的地理位置。对许多重要的物种的CoNS，包括S。表皮葡萄球菌S. haemolyticus、S. lugdunensis和S.人，我们发现芳基霉素C16的活性等于或大于万古霉素，万古霉素是最常用于治疗CoNS感染的抗生素。虽然易感性通常与之前鉴定的Pro残留物的缺乏相关，但在几个病例中发现了其他因素似乎也有贡献。
The arylomycins are a class of natural-product antibiotics that act via the inhibition of type I signal peptidase (SPase), and we have found in diverse bacteria that their activity is limited by the presence of a resistance-conferring Pro residue in SPase that reduces inhibitor binding. We have also demonstrated thatStaphylococcus epidermidis, which lacks this Pro residue, is extremely susceptible to the arylomycins. Here, to further explore the potential utility of the arylomycins, we report an analysis of the activity of a synthetic arylomycin derivative, arylomycin C16, against clinical isolates ofS. epidermidisand other coagulase-negative staphylococci (CoNS) from distinct geographical locations. Against many important species of CoNS, includingS. epidermidis,S. haemolyticus,S. lugdunensis, andS. hominis, we find that arylomycin C16exhibits activity equal to or greater than that of vancomycin, the antibiotic most commonly used to treat CoNS infections. While the susceptibility was generally correlated with the absence of the previously identified Pro residue, several cases were identified where additional factors also appear to contribute.