Production of Antitubercular Depsipeptides via Biosynthetic Engineering of Cinnamoyl Units

Two new cyclodecapeptides, atratumycins B (1) and C (2), containing substituted cinnamoyl side chains were generated by converging elements of the atratumycin (3) and atrovimycin (4) biosynthetic pathways. The structures of 1 and 2 were determined on the basis of HRESIMS, 1D and 2D NMR data, and X-ray single-crystal diffraction studies. Atratumycin B (1) is active against autoluminescent Mycobacterium tuberculosis H37Rv, displaying a minimum inhibitory concentration of 3.1 μg/mL (2.3 μM).

本研究通过融合阿特拉霉素（atratumycin，3）与阿特罗霉素（atrovimycin，4）的生物合成途径元件，成功获得了两个携带取代肉桂酰基侧链的新型环十肽（cyclodecapeptides）——阿特拉霉素B（1）与阿特拉霉素C（2）。借助高分辨电喷雾电离质谱（HRESIMS）、一维（1D）与二维（2D）核磁共振（NMR）谱学数据以及X射线单晶衍射分析，研究人员确定了化合物1与2的化学结构。活性测试表明，阿特拉霉素B（1）对自发光结核分枝杆菌（Mycobacterium tuberculosis）H37Rv具有抗菌活性，其最低抑菌浓度为3.1 μg/mL（2.3 μM）。