Muraminomicins, new lipo-nucleoside antibiotics from Streptosporangium sp. SANK 60501-structure elucidations of muraminomicins and supply of the core component for derivatization
| Autor: | Toshihiro Suzuki, Yasumasa Ogawa, Ryo Murakami, Masaaki Kizuka, Yasuhiro Suzuki, Suzuki Takashi, Tetsufumi Koga, Toshiyuki Konosu, Iizuka Mayumi, Toshio Takatsu, Yoshiko Kagoshima, Masuda Takeshi, Kunio Takasugi, Kazuko Saito, Yoko Fujita, Osamu Ishida, Toru Nakahira, Shuichi Endo, Akane Tokumitsu, Masami Miura, Shunichi Miyakoshi, Hideaki Nishigoori, Yasunori Muramatsu, Azusa Aoyagi |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Magnetic Resonance Spectroscopy
medicine.drug_class Antibiotics Transferases (Other Substituted Phosphate Groups) Myristic acid Microbial Sensitivity Tests Gram-Positive Bacteria Structure-Activity Relationship chemistry.chemical_compound Bacterial Proteins Transferases Actinomycetales Drug Discovery medicine Structure–activity relationship Enzyme Inhibitors Derivatization Pharmacology Chromatography Molecular Structure biology Fatty Acids biology.organism_classification Anti-Bacterial Agents chemistry Fermentation Antibacterial activity Nucleoside Bacteria |
| Zdroj: | The Journal of Antibiotics. 72:943-955 |
| ISSN: | 1881-1469 0021-8820 |
| DOI: | 10.1038/s41429-019-0215-7 |
| Popis: | We screened for bacterial phospho-N-acetylmuramyl-pentapeptide-translocase (MraY: EC 2.7.8.13) inhibitors with the aim of discovering novel antibiotics and observed inhibitory activity in the culture broth of an actinomycete, SANK 60501. The active compounds, muraminomicins A, B, C, D, E1, E2, F, G, H, and I exhibited strong inhibitory activity against MraY with IC50 values of 0.0105, 0.0068, 0.0104, 0.0099, 0.0115, 0.0109, 0.0089, 0.0134, 0.0186, and 0.0094 μg ml-1, respectively. Although muraminomicin F exhibited favorable antibacterial activity against drug-resistant Gram-positive bacteria, this activity was reduced with the addition of serum. To efficiently supply the core component for chemical modification studies, production was carried out in a controlled trial by adding myristic acid to the medium, and a purification method suitable for large-scale production was successfully developed. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full text from SpringerLink