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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Screening and biological activities of pedopeptins, novel inhibitors of LPS produced by soil bacteria
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Screening and biological activities of pedopeptins, novel inhibitors of LPS produced by soil bacteria

机译：土壤细菌产生的脂多糖新型抑制剂pedopeptins的筛选和生物学活性

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Lipopolysaccharide (LPS) is a strong endotoxin and is delivered to the cell surface signaling receptor, Toll-like receptor 4 and MD-2 complex, via soluble cluster of differentiation (CD) 14 or membranous CD14, resulting in the induction of the inflammatory response. To obtain new compounds that block LPS binding to CD14, we designed a high-throughput screening based on time-resolved intermolecular fluorescence resonance energy transfer. This cell-free screening system successfully led to the discovery of novel inhibitors of LPS-CD14 interaction from the library of the secondary metabolites of microorganisms. We identified the novel compounds pedopeptin A, B and C from a culture broth of Pedobacter sp. SANK 72003. Pedopeptins blocked LPS binding to CD14 in vitro with IC 50 values of 20, 11 and 47 nM, respectively, and also inhibited LPS binding to the cells expressing CD14, leading to the suppression of cytokine production. Moreover, they showed antimicrobial activities against Escherichia coli with minimum inhibitory concentration ranging from 2 to 4 μg ml -1.
机译：脂多糖（LPS）是一种强内毒素，通过可溶性分化（CD）14或膜CD14传递至细胞表面信号受体，Toll样受体4和MD-2复合物，从而诱导炎症反应。为了获得阻断LPS与CD14结合的新化合物，我们设计了基于时间分辨的分子间荧光共振能量转移的高通量筛选。这种无细胞的筛选系统成功地导致了微生物次级代谢产物库中LPS-CD14相互作用的新型抑制剂的发现。我们从Pedobacter sp。的培养液中鉴定了新型化合物pedopeptin A，B和C。 SANK72003。肽肽在体外以200、11和47 nM的IC 50值阻断LPS与CD14的结合，还抑制LPS与表达CD14的细胞的结合，从而抑制细胞因子的产生。而且，它们显示出对大肠杆菌的抗菌活性，最低抑菌浓度范围为2至4μgml -1。

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