RESUMEN
Five new diterpenoids, named euphorfischerins A-E, were isolated from the roots of Euphorbia fischeriana. Their chemical structures and absolute configurations were determined by interpretation of NMR, HR-ESI-MS, ECD and X-ray diffraction data. Euphorfischerin A showed cytotoxicity against the human cancer cell lines HeLa, H460 and Namalwa with IC50 values of 4.6, 11.5 and 16.4â µM, respectively, while euphorfischerin B gave comparable IC50 values of 9.5, 17.4 and 13.3â µM against the three cancer cell lines, respectively.
Asunto(s)
Antineoplásicos Fitogénicos/química , Antineoplásicos Fitogénicos/farmacología , Diterpenos/química , Diterpenos/farmacología , Euphorbia/química , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Humanos , Modelos Moleculares , Neoplasias/tratamiento farmacológico , Raíces de Plantas/químicaRESUMEN
Three new diterpenoids (1-3) (two abietane type diterpenoids and a paralianone type diterpenoid), together with four known compounds (4-7) were isolated from the whole plants of Euphorbia peplus. Their structures were elucidated through spectroscopic analysis and physicochemical characteristics. The cytotoxic activities of compounds 1-7 against five human tumour cell lines were evaluated, however, they were inactive at the concentration of 40 µM. The compound 3 enhanced lysosomal biogenesis with Lyso Tracker staining intensity of 132.6%.
Asunto(s)
Antineoplásicos Fitogénicos , Diterpenos , Euphorbia , Abietanos , Antineoplásicos Fitogénicos/farmacología , Diterpenos/farmacología , Humanos , Estructura MolecularRESUMEN
The first phytochemical investigation of the seeds of Euphorbia peplus led to the isolation and characterization of five new (1-5), named euphopepluanones A-E, and five known diterpenoids (6-10). Their structures were established by extensive spectroscopic analysis and X-ray crystallographic experiments. Euphopepluanones A-E (1-3) feature a very rare 5/11/5-tricyclic skeleton, and euphopepluanones D-E (4-5) represent the first report of lathyrane type diterpenoids found in E. peplus. The new compounds 1-5 were assessed for their activities to induce lysosomal biogenesis through LysoTracker Red staining, in which compounds 1 and 3 could significantly induce lysosomal biogenesis. In addition, compounds 1 and 3 could promote the nuclear translocation of TFEB, a master transcriptional factor of lysosomal genes, indicating that compounds 1 and 3 induced lysosomal biogenesis through activation of TFEB.