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Isolation of new derivatives of the 20-membered macrodiolide bispolide from Kitasatospora sp. MG372-hF19
- Source :
- The Journal of Antibiotics. 75:77-85
- Publication Year :
- 2021
- Publisher :
- Springer Science and Business Media LLC, 2021.
-
Abstract
- 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.
- Subjects :
- Methicillin-Resistant Staphylococcus aureus
Pharmacology
Antibiotics, Antineoplastic
Magnetic Resonance Spectroscopy
Alkylation
Molecular Structure
Streptomycetaceae
Vancomycin Resistance
Microbial Sensitivity Tests
Crystallography, X-Ray
Anti-Bacterial Agents
Actinobacteria
A549 Cells
Cell Line, Tumor
Drug Discovery
Humans
Macrolides
Drug Screening Assays, Antitumor
Enterococcus
Subjects
Details
- ISSN :
- 18811469 and 00218820
- Volume :
- 75
- Database :
- OpenAIRE
- Journal :
- The Journal of Antibiotics
- Accession number :
- edsair.doi.dedup.....7e451ca5effc35bffa212b83a55d689c