期刊
MARINE DRUGS
卷 10, 期 11, 页码 2388-2402出版社
MDPI AG
DOI: 10.3390/md10112388
关键词
marine Streptomyces fradiae; fradimycins A and B; fradic acids A and B; antibacterial and antitumor activities
资金
- National Science Foundation of China [81273428]
- Cross-Disciplinary Research for Ocean Science of Zhejiang University [2012HY018B]
Capoamycin-type antibiotics (2-5) and polyene acids (6, 7) were isolated from marine Streptomyces fradiae strain PTZ0025. Their structures were established by extensive nuclear magnetic resonance (NMR) and high resolution electron spray ionization mass spectroscopy (HRESIMS) analyses and chemical degradation. Compounds 3, 4, 6, 7 were found to be new and named as fradimycins A (3) and B (4), and fradic acids A (6) and B (7). Compounds 3-5 showed in vitro antimicrobial activity against Staphylococcus aureus with a minimal inhibitory concentration (MIC) of 2.0 to 6.0 mu g/mL. Interestingly, Compounds 3-5 also significantly inhibited cell growth of colon cancer and glioma with IC50 values ranging from 0.13 to 6.46 mu M. Fradimycin B (4), the most active compound, was further determined to arrest cell cycle and induce apoptosis in tumor cells. The results indicated that fradimycin B (4) arrested the cell cycle at the G(0)/G(1) phase and induced apoptosis and necrosis in colon cancer and glioma cells. Taken together, the results demonstrated that the marine natural products 3-5, particularly fradimycin B (4), possessed potent antimicrobial and antitumor activities.
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