The discovery of new drugs that target cancer stem cells (CSCs) is a critical approach to overcome the major difficulties of the metastasis, chemotherapeutic resistance and recurrence for successful cancer therapy. Chemical investigation of the roots of Euphorbia fischeriana resulted in the isolation of eight ent-atisane diterpenoids (1-8), including two new compounds: 19-O-β-D-glucopyranosyl-ent-atis-16-ene-3,14-dione (7) and 19-O-(6-galloyl)-β-D-glucopyranosyl-ent-atis-16-ene-3,14-dione (8). The structures were elucidated on extensive spectroscopic analyses, as well as chemical transformations. ent-3β-Hydroxyatis-16-ene-2,14-dione (5), 7 and its aglycon, ent-19-hydroxy-atis-16-ene-3,14-dione (7a), showed significant inhibitory activity on mammosphere formation in human breast cancer MCF-7 cells at a final concentration of 10 μM.
Keywords: Cancer stem cells; Diterpenoid; Euphorbia fischeriana; Euphorbiaceae; Mammosphere formation; ent-Atisane.