Fundación MEDINA, Centro de Excelencia en Investigación de Medicamentos Innovadores en Andalucía, Parque Tecnológico Ciencias de la Salud, Avda. del Conocimiento 34, 18016 Armilla, Granada, Spain.
Mar Drugs. 2018 Mar 16;16(3):95. doi: 10.3390/md16030095.
Phocoenamicins B and C ( and ), together with the known spirotetronate phocoenamicin (), were isolated from cultures of sp. The acetone extract from a culture of this strain, isolated from marine sediments collected in the Canary Islands, displayed activity against methicillin-resistant (MRSA), H37Ra and . Bioassay-guided fractionation of this extract using SP207ss column chromatography and preparative reversed-phased HPLC led to the isolation of the new compounds and belonging to the spirotetronate class of polyketides. Their structures were determined using a combination of HRMS, 1D and 2D NMR experiments and comparison with the spectra reported for phocoenamicin. Antibacterial activity tests of the pure compounds against these pathogens revealed minimal inhibitory concentration (MIC) values ranging from 4 to 64 µg/mL for MRSA, and 16 to 32 µg/mL for H37Ra, with no significant activity found against and vancomycin-resistant (VRE) at concentrations below 128 µg/mL, and weak activity detected against grown on agar plates.
从 sp. 的培养物中分离得到了 Phocoenamicins B 和 C（和），以及已知的螺缩酮类化合物 Phocoenamicin（）。从加那利群岛海洋沉积物中分离出的这种菌株的丙酮提取物对耐甲氧西林金黄色葡萄球菌（MRSA）、H37Ra 和 表现出活性。使用 SP207ss 柱层析和制备性反相 HPLC 对该提取物进行生物活性导向分离，得到了属于螺缩酮类聚酮化合物的新化合物和。通过 HRMS、1D 和 2D NMR 实验以及与报道的 Phocoenamicin 谱图的比较，确定了它们的结构。对这些纯化合物对这些病原体的抗菌活性测试表明，MRSA 的最小抑菌浓度（MIC）值范围为 4 至 64 µg/mL，H37Ra 的 MIC 值范围为 16 至 32 µg/mL，在低于 128 µg/mL 的浓度下对 和万古霉素耐药肠球菌（VRE）没有明显活性，在琼脂平板上对 检测到较弱的活性。
