Tetramic acid based alkaloids from Aspergillus amoenus Roberg strain UP197-antibiotic properties and new pyranterreones
| Autor: | Bengt Guss, Anders Broberg, Christina Nord, Jolanta J. Levenfors, Joakim Bjerketorp, Bo Öberg |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2022 |
| Předmět: |
medicine.drug_class
Antibiotics Plant Science Fungus Tetramic acid alkaloids 01 natural sciences Biochemistry Analytical Chemistry Microbiology Aspergillus amoenus cytotoxic medicine Organisk kemi biology Strain (chemistry) 010405 organic chemistry Chemistry Organic Chemistry Biochemistry and Molecular Biology pyranterreone biology.organism_classification 0104 chemical sciences 010404 medicinal & biomolecular chemistry antibacterial Medicinal Chemistry Biokemi och molekylärbiologi |
| Popis: | The fungus Aspergillus amoenus Roberg strain UP197 was shown to produce antibacterial tetramic acid based alkaloids. Two new compounds, pyranterreone I and J (1 and 2), were isolated and characterized, in addition to the known compounds cordylactam, 7-hydroxycordylactam, pyranterreone C, D, F and G. Neither the pyranterreones nor the cordylacctams had previously been tested for antimicrobial activity. Thus, all isolated compounds were tested against a panel of clinically important bacteria and fungi. Pyranterreone C was active against Gram-positive and Gram-negative bacteria, with minimal inhibitory concentrations (MIC) between 1 and 8 µg/mL, whereas the MICs for all other compounds were >32 µg/mL. Pyranoterreone C was cytotoxic towards HepG2 cells, and since pyranterreone C reacted rapidly with the nucleophile cysteine, it is likely that the observed antibacterial activity is due to the chemical reactivity rather than enzymatic affinity, making it unsuitable for development as an antibacterial drug. |
| Databáze: | OpenAIRE |
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