期刊
JOURNAL OF ANTIBIOTICS
卷 73, 期 8, 页码 542-547出版社
SPRINGERNATURE
DOI: 10.1038/s41429-020-0307-4
关键词
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资金
- Program of Guangzhou Science and Technology Plan [201707010454]
- National Natural Science Foundation of China [41676151]
- Key Special Project for Introduced Talents Team of Southern Marine Science and Engineering Guangdong Laboratory (Guangzhou) [GML2019ZD0406]
- National Key Research and Development Program of China [2017YFD0201401]
- Special Fund for Strategic Pilot Technology of Chinese Academy of Sciences [XDA13020302-2]
Two new chlorinated bis-indole alkaloids, dionemycin (1) and 6-OMe-7 ',7 ''-dichorochromopyrrolic acid (2), along with seven known analogs 3-9, were isolated from the deep-sea derived Streptomyces sp. SCSIO 11791. Their structures were elucidated by extensive HRESIMS, and 1D and 2D NMR data analysis. In vitro antibacterial and cytotoxic assays revealed that, compound 1, shows anti-staphylococcal activity with an MIC range of 1-2 mu g/mL against six clinic strains of methicillin-resistant Staphylococcus aureus (MRSA) isolated from human and pig. Additionally, compound 1 displayed cytotoxic activity against human cancer cell lines NCI-H460, MDA-MB-231, HCT-116, HepG2, and noncancerous MCF10A with an IC50 range of 3.1-11.2 mu M. Analysis of the structure-activity relationship reveals that the chlorine atom at C-6 '' could be pivotal for conferring their bioactivities, thus providing hints on chemical modifications on bis-indole alkaloid scaffold in drug design.
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