RESUMEN

Eleven previously undescribed abietane-type diterpenoids, named caryopincanoids A-K (1-11), together with five known compounds, were isolated from the EtOH extract of the aerial parts of Caryopteris incana (Thunb.) Miq. Their structures were elucidated on the basis of comprehensive spectroscopic data, NMR calculations, and ECD calculations. The inhibitory activities of all compounds against HIF-2α gene expression in 786-O cells were tested by luciferase assay. Compounds 7, 9, 15, and 16 showed significant inhibitory effects with IC50 values ranging from 12.73 to 23.80 µM. The preliminary structure-activity relationship of these compounds was also discussed.

Asunto(s)

Abietanos , Factores de Transcripción con Motivo Hélice-Asa-Hélice Básico , Abietanos/química , Abietanos/farmacología , Abietanos/aislamiento & purificación , Relación Estructura-Actividad , Humanos , Factores de Transcripción con Motivo Hélice-Asa-Hélice Básico/antagonistas & inhibidores , Factores de Transcripción con Motivo Hélice-Asa-Hélice Básico/metabolismo , Estructura Molecular , Componentes Aéreos de las Plantas/química , Relación Dosis-Respuesta a Droga