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J Nat Prod ; 77(3): 497-502, 2014 Mar 28.
Artículo en Inglés | MEDLINE | ID: mdl-24428261

RESUMEN

Bacteria continue to evade existing antibiotics by acquiring resistance by various mechanisms, leading to loss of antibiotic effectiveness. To avoid an epidemic from infections of incurable drug-resistant bacteria, new antibiotics with new modes of action are desperately needed. Using a genome-wide mechanism of action-guided whole cell screening approach based on antisense Staphylococcus aureus fitness test technology, we report herein the discovery of altersolanol P (1), a new tetrahydroanthraquinone from an unknown fungus from the Hypocreales isolated from forest litter collected in Puerto Rico. The structure was elucidated by high-resolution mass spectrometry and 2D NMR spectroscopy. Relative stereochemistry was established by NOESY correlations, and absolute configuration was deduced by the application of MPA ester-based methodology. Observed (1)H and (13)C NMR shifts were well aligned with the corresponding chemical shifts predicted by DFT calculations. Altersolanol P exhibited Gram-positive antibacterial activity (MIC range 1-8 µg/mL) and inhibited the growth of Gram-negative Haemophilus influenzae (MIC 2 µg/mL). The isolation, structure elucidation, and antibacterial activity of altersolanol P are described.


Asunto(s)
Antraquinonas/aislamiento & purificación , Antraquinonas/farmacología , Antibacterianos/aislamiento & purificación , Antibacterianos/farmacología , Hypocreales/química , Staphylococcus aureus/efectos de los fármacos , Antraquinonas/química , Antibacterianos/química , Farmacorresistencia Bacteriana/efectos de los fármacos , Haemophilus influenzae/efectos de los fármacos , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Puerto Rico
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