Fundación MEDINA, Centro de Excelencia en Investigación de Medicamentos Innovadores en Andalucía, Avda. del Conocimiento 3, Parque Tecnológico de Ciencias de la Salud, E-18016 Granada, Spain.
Departamento de Biología Funcional, Área de Microbiología, and Instituto Universitario de Oncología del Principado de Asturias, Universidad de Oviedo, 33006 Oviedo, Spain.
Mar Drugs. 2018 Oct 8;16(10):371. doi: 10.3390/md16100371.
Fractionation of the bioactive extract of a culture of the marine derived actinomycete M-157 led to the isolation of the known 3-hydroxyquinaldic acid (), its amide () and three new derivatives (⁻) containing different amino acid residues. The structures of the new molecules (⁻), including their absolute configuration, were determined by the analysis of their ESI-TOF MS and one-dimensional (1D) and two-dimensional (2D) NMR spectra and advanced Marfey's analysis of their hydrolyzation products. Compound spontaneously dimerized in solution to give the disulfide derivative . Unfortunately, none of the new compounds isolated confirmed the antimicrobial activity found in the bacterial extract, perhaps indicating that such antibacterial activity might be due to presence in the extract at the trace level of larger bioactive 3-hydroxyquinaldic acid derivatives from which compounds ⁻ are biosynthetic precursors. Cytotoxicity tests confirmed the moderate and weak IC values of 15.6 and 51.5 µM for compounds and , respectively.
从海洋来源放线菌 M-157 的培养物的生物活性提取物中进行分段分离，得到了已知的 3-羟基喹哪啶酸（）、其酰胺（）和三个含有不同氨基酸残基的新衍生物（⁻）。新分子（⁻）的结构，包括它们的绝对构型，通过分析它们的 ESI-TOF MS 和一维（1D）和二维（2D）NMR 谱以及对其水解产物的高级 Marfey 分析来确定。化合物在溶液中自发二聚化生成二硫化物衍生物。不幸的是，分离得到的任何新化合物都没有证实在细菌提取物中发现的抗菌活性，这可能表明这种抗菌活性可能是由于提取物中痕量存在更大的生物活性 3-羟基喹哪啶酸衍生物，而化合物 ⁻ 则是其生物合成前体。细胞毒性测试证实化合物和分别具有中等和弱的 IC 值 15.6 和 51.5 µM。
