RESUMEN
Five novel tigliane-type diterpenes, stelleracins A-E (3-7), a novel flavanone dimer, chamaeflavone A (8), and six known compounds were isolated from the roots of Stellera chamaejasme. Their structures were elucidated by extensive spectroscopic analyses. The isolated compounds were evaluated for anti-HIV activity in MT4 cells. New compounds 3-5 showed potent anti-HIV activity (EC90 0.00056-0.0068 µM) and relatively low or no cytotoxicity (IC50 4.4-17.2 µM). These new compounds represent promising new leads for development into anti-AIDS clinical trial candidates.
Asunto(s)
Fármacos Anti-VIH/aislamiento & purificación , Fármacos Anti-VIH/farmacología , Diterpenos/aislamiento & purificación , Diterpenos/farmacología , Flavanonas/aislamiento & purificación , Flavanonas/farmacología , Thymelaeaceae/química , Síndrome de Inmunodeficiencia Adquirida/tratamiento farmacológico , Fármacos Anti-VIH/química , Supervivencia Celular/efectos de los fármacos , Diterpenos/química , Flavanonas/química , Estructura Molecular , Nepal , Resonancia Magnética Nuclear Biomolecular , Raíces de Plantas/químicaRESUMEN
Three novel 1-alkyldaphnane-type diterpenes, stelleralides A-C (4-6), and five known compounds were isolated from the roots of Stellera chamaejasme L. The structures of 4-6 were elucidated by extensive spectroscopic analyses. Several isolated compounds showed potent anti-HIV activity. Compound 4 showed extremely potent anti-HIV activity (EC(90) 0.40 nM) with the lowest cytotoxicity (IC(50) 4.3 µM) and appears to be a promising compound for development into anti-AIDS clinical trial candidates.