Fermentation of Acremonium tubakii W. Gams isolated from a soil sample collected from the University of Utah led to the isolation and characterization of six new linear pentadecapeptides, emerimicins V–X (1–6). Peptaibols containing 15-residues are quite rare, with only 22 reported. Genome mining and bioinformatic analysis were used to identify the emerimicin 60 kbp eme biosynthetic cluster harboring a single 16-module hybrid polyketide-nonribosomal peptide synthetase. A detailed bioinformatic investigation of the corresponding 15 adenylation domains, combined with 1D and 2D NMR experiments, LC-MS/MS data, and advanced Marfey’s method, allowed for the elucidation and absolute configuration of all proteinogenic and nonproteinogenic amino acid residues in 1–6. As some peptaibols possess cytotoxic activity, a zebrafish embryotoxicity assay was used to evaluate the toxicity of the six emerimicins and showed that emerimicin V (1) and VI (2) exhibit the most potent activity. Additionally, out of the six emerimicins, 1 displayed modest activity against Enterococcus faecalis, methicillin-resistant Staphylococcus aureus, and vancomycin-resistant Enterococcus faecium with MIC values of 64, 32, and 64 μg/mL, respectively.

中文翻译：

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Emerimicins V–X, 15-Residue Peptaibols 从 Acremonium sp. 中发现。通过综合基因组和化学方法

从犹他大学收集的土壤样品中分离出的Acremonium tubakii W. Gams发酵导致了六种新的线性十五肽 Emerimicins V-X (1-6 )的分离和表征。含有 15 个残基的 Peptaibols 非常罕见，仅报道了 22 个。基因组挖掘和生物信息学分析用于鉴定 emerimicin 60 kbp eme含有单个 16 模块杂合聚酮化合物-非核糖体肽合成酶的生物合成簇。对相应的 15 个腺苷酸化结构域进行详细的生物信息学研究，结合 1D 和 2D NMR 实验、LC-MS/MS 数据和先进的 Marfey 方法，可以阐明和绝对构型1-6中的所有蛋白质和非蛋白质氨基酸残基. 由于一些 peptaibols 具有细胞毒活性，斑马鱼胚胎毒性试验用于评估六种 Emerimicins 的毒性，并显示 Emerimicin V ( 1 ) 和 VI ( 2 ) 表现出最有效的活性。此外，在 6 种 emerimicins 中，1种表现出适度的抗粪肠球菌、耐甲氧西林金黄色葡萄球菌和耐万古霉素粪肠球菌，MIC 值分别为 64、32 和 64 μg/mL。