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Rare  ent -abietane-rosane diterpenoid heterodimers, Bisebracteolasins A and B ( 1  and  2 , respectively), were isolated from the roots of  Euphorbia ebracteolata  Hayata. Their structures and absolute configurations were elucidated from spectroscopic data and X-ray diffraction analysis. Compounds  1  and  2  exhibited moderate cytotoxic effects against five cancer cell lines. Compound  1  showed more effective antiproliferative activities against human tumour cells, HL-60 and SMMC-7721, with IC 50  values of 2.61 and 4.08  μ M, respectively, than  2 . Both compounds  1  and  2  inhibit the colorectal cancer stem cell line P6C with IC 50  values of 16.48 and 34.76  μ M, respectively. Moreover, preliminary biological tests showed compound  1  exhibited inhibitory activity towards tumoursphere formation and migration of the P6C cell line. Overall, we identified two novel diterpenoid heterodimers, and Bisebracteolasin A exhibits therapeutic potential in impeding tumour growth and metastatic ability of cancer stem cells.

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Two novel diterpenoid heterodimers, Bisebracteolasins A and B, from Euphorbia ebracteolata Hayata, and the cancer chemotherapeutic potential of Bisebracteolasin A