RESUMEN
A novel aspochalasin, aspochalasin L (1), was isolated from the fermentation broth of a soil-derived fungal culture identified as Aspergillus flavipes (Deuteromycota). Structure elucidation of 1 was accomplished by detailed spectroscopic data analyses and by comparison with related cytochalasins. Aspochalasin L demonstrated activity against HIV integrase with an IC50 of 71.7microM.
Asunto(s)
Aspergillus/metabolismo , Citocalasinas/farmacología , Inhibidores de Integrasa VIH/farmacología , VIH-1/enzimología , Aspergillus/química , Fenómenos Químicos , Química Física , Medios de Cultivo , Citocalasinas/aislamiento & purificación , Fermentación , Inhibidores de Integrasa VIH/aislamiento & purificación , VIH-1/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Conformación Molecular , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría Infrarroja , Espectrofotometría Ultravioleta , Espectroscopía Infrarroja por Transformada de FourierRESUMEN
An HTS campaign aimed at the identification of inhibitors of HIV integrase showed that the methanol extract from the buds of a Eucalyptus globoidea was active. Bioassay guided fractionation of this extract resulted in the purification and structural elucidation of the lignan, globoidnan A (1) as the only compound in the extract responsible for the inhibition of HIV integrase. The compound was found to inhibit the combined 3' processing and strand transfer activity of HIV integrase with an IC50=0.64 microM.
Asunto(s)
Eucalyptus/química , Inhibidores de Integrasa VIH/aislamiento & purificación , Lignanos/aislamiento & purificación , Flores/química , Inhibidores de Integrasa VIH/farmacología , VIH-1/enzimología , Lignanos/farmacología , Estructura MolecularRESUMEN
To new triterpenes, trichomycins A (1) and B (2), were purified from the new species Tricholoma sp. AU1 by activity-guided fractionation following their antibacterial activity. The two compounds were found to have a hitherto unreported triterpenoid skeleton. The structures and relative stereochemistry of 1 and 2 were determined through extensive 2D NMR spectroscopy, while the inhibitory activity of 1 and 2 against two Gram-positive and two Gram-negative bacteria and a mammalian cell line was determined.
Asunto(s)
Antibacterianos/aislamiento & purificación , Basidiomycota/química , Triterpenos/aislamiento & purificación , Antibacterianos/química , Antibacterianos/farmacología , Australia , Ensayos de Selección de Medicamentos Antitumorales , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Humanos , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Triterpenos/química , Triterpenos/farmacología , Células Tumorales CultivadasRESUMEN
Chemical investigations of the crude MeOH extract of Physalis viscosa led to the identification of the novel acylated sucrose ester physaloside A (1). The structure of 1 was determined by 2D NMR analysis, and the absolute configuration was determined by chemical degradation and comparison with authentic standards.
Asunto(s)
Bacterias Grampositivas/efectos de los fármacos , Physalis/química , Plantas Medicinales/química , Sacarosa , Sacarosa/análogos & derivados , Sacarosa/aislamiento & purificación , Australia , Ensayos de Selección de Medicamentos Antitumorales , Ésteres/química , Ésteres/aislamiento & purificación , Ésteres/farmacología , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Sacarosa/química , Sacarosa/farmacologíaRESUMEN
The new diketopiperazine dimer 1, as well as the known compounds TMC-256A1 (2), TMC-256C1 (3), and demethylkotanin (4), were isolated from a culture of Aspergillus niger. The gross structure of 1 was determined by 2D NMR studies and comparison with literature data, and the absolute stereochemistry was elucidated by chiral HPLC analysis of the hydrolysis products.