RESUMEN
During a chemical investigation of Wikstroemia scytophylla, three new [wikstrocins A-C (1-3)] and three known tigliane diterpenoids (4-6) were isolated. The structures of the new compounds were elucidated from extensive physiochemical and spectroscopic analysis. The correlations between the ECD Cotton effects and B ring structures of tiglianes were also evaluated. The isolated compounds were assessed for their anti-HIV activity against HIV-1 infection of MT4 cells, and two compounds (4 and 6) showed potent anti-HIV activity with IC50 values of 3.8 and 12.8 nM, respectively.
Asunto(s)
Fármacos Anti-VIH/farmacología , Diterpenos/farmacología , Forboles/farmacología , Wikstroemia/química , Fármacos Anti-VIH/química , Fármacos Anti-VIH/aislamiento & purificación , Línea Celular , Diterpenos/aislamiento & purificación , Humanos , Análisis Espectral/métodosRESUMEN
Macrocyclic daphnane orthoesters (MDOs) have attracted significant research interest for the drug discovery to cure HIV infection based on the "Shock and Kill" strategy. In the present study, the first chemical study on Wikstroemia ligustrina (Thymelaeaceae) was carried out by LC-MS analysis and phytochemical investigation. Nine daphnane diterpenoids (1-9) including seven MDOs were detected by LC-MS analysis. Further phytochemical investigation resulted in the isolation and structural elucidation of five daphnanes (1, 2, 5, 8, and 9) with potent anti-HIV activity. Taking the isolated MDO (1) as a model compound, the MS/MS fragmentation pathway was also elucidated.