Key Laboratory of Marine Drugs, Chinese Ministry of Education, School of Medicine and Pharmacy, Ocean University of China, 266003, Qingdao, People's Republic of China.
Laboratory for Marine Drugs and Bioproducts of Qingdao Pilot National Laboratory for Marine Science and Technology, 266237, Qingdao, People's Republic of China.
J Antibiot (Tokyo). 2022 Jul;75(7):380-384. doi: 10.1038/s41429-022-00526-6. Epub 2022 Apr 25.
One new angucyclinone derivative, Kanglemycin N (1), and two new biogenetically related α-Pyrones, nocapyrones U-V (2-3), were isolated from a desert-derived Actinomycete Nocardiopsis dassonvillei HDN 154151. Their structures, including absolute configurations, were elucidated by extensive NMR, MS, and ECD analyses. Compound 1 exhibited potent antibacterial activity against Bacillus subtilis, Proteus sp., Vibrio Parahaemolyticus, Escherichia coli and Methicillin-resistant Staphylococcus aureus (MRSA) with MIC values ranging from 0.39 μM to 1.56 μM, and notably the effect of 1 against MRSA significantly exceeded the positive control ciprofloxacin. In addition, compound 1 also showed moderate cytotoxic activity against H69AR, MDA-MB-231, ASPC-1 and K562 cell lines, with IC values of 10.46, 8.78, 9.28 and 8.61 μM, respectively.
从沙漠来源的放线菌诺卡氏菌 Nocardiopsis dassonvillei HDN 154151 中分离得到一种新的安桥环酮衍生物康莱霉素 N(1)和两种新的生物相关的α-吡喃酮,nocapyrones U-V(2-3)。通过广泛的 NMR、MS 和 ECD 分析阐明了它们的结构,包括绝对构型。化合物 1 对枯草芽孢杆菌、变形杆菌、副溶血性弧菌、大肠杆菌和耐甲氧西林金黄色葡萄球菌(MRSA)表现出很强的抗菌活性,MIC 值范围为 0.39 μM 至 1.56 μM,值得注意的是,1 对 MRSA 的作用明显优于阳性对照环丙沙星。此外,化合物 1 对 H69AR、MDA-MB-231、ASPC-1 和 K562 细胞系也表现出中等的细胞毒性活性,IC 值分别为 10.46、8.78、9.28 和 8.61 μM。