期刊
JOURNAL OF ANTIBIOTICS
卷 75, 期 2, 页码 77-85出版社
SPRINGERNATURE
DOI: 10.1038/s41429-021-00492-5
关键词
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资金
- Ministry of Education, Culture, Sports, Science and Technology, Japan (JSPS KAKENHI) [JP 16H06276]
- JSPS KAKENHI [17K08777]
- Grants-in-Aid for Scientific Research [17K08777] Funding Source: KAKEN
The newly isolated bispolides C-E exhibit distinct structures from other known bispolides, and show antibacterial and cytotoxic activities against drug-resistant bacteria and tumor cells, indicating potential pharmaceutical value.
New three macrocyclic diolides, named bispolides C-E (1-3), were isolated from a fermentation broth of the actinomycete strain MG372-hF19, which produces an indole glycoside and leptomycins as we reported previously. The absolute structures of compounds 1-3 were elucidated by NMR and X-ray crystallography. Compounds 1-3 diverge from the known nine bispolides in their different alkylation patterns on the 20-membered macrocyclic diolide skeleton and the side chain in their planar structures. Furthermore, compounds 1-3 exhibited antibacterial activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococci and cytotoxic activity against human cancer cell lines. Among them, compound 3 has the most potent biological activities against bacteria and tumor cells. Additionally, using a membrane-potential-sensitive fluorescence probe, we found that compounds 1-3 and elaiophylin have a similar effect on membrane potential in A549 human lung cancer cells.
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