Proansamycin B derivatives from the post-PKS modification gene deletion mutant of Amycolatopsis mediterranei S699.
Xinyu MaFeng YeXiaochun ZhangZhan LiYanjiao DingChunhua LuYue-Mao ShenPublished in: The Journal of antibiotics (2024)
Ten new proansamycin B congeners (1-10) together with one known (11) were isolated and characterized on the basis of 1D and 2D NMR spectroscopic and HRESIMS data from the Amycolatopsis mediterranei S699 ΔPM::rifR+rif-orf19 mutant. Compounds 8 and 9 featured with six-membered ring and five-membered ring hemiketal, respectively. Compounds 1, 2, and 9 displayed antibacterial activity against MRSA (methicillin-resistant Staphylococcus aureus), with the MIC (minimal inhibitory concentration) values of 64, 8, and 128 µg/mL, respectively. Compound 1 showed significant cytotoxicity against MDA-MB-231, HepG2 and Panc-1 cell lines with IC 50 (half maximal inhibitory concentration) values of 2.3 ± 0.2, 2.5 ± 0.3 and 3.8 ± 0.5 μM, respectively.
Keyphrases
- methicillin resistant staphylococcus aureus
- staphylococcus aureus
- wild type
- magnetic resonance
- molecular docking
- air pollution
- particulate matter
- high resolution
- electronic health record
- genome wide
- breast cancer cells
- heart rate
- copy number
- big data
- heavy metals
- resistance training
- solid state
- polycyclic aromatic hydrocarbons
- blood pressure
- machine learning
- risk assessment
- cell death
- mycobacterium tuberculosis
- body composition
- mass spectrometry
- structure activity relationship
- signaling pathway
- high intensity