4.4 Article

Euphorins A-H: bioactive diterpenoids from Euphorbia fischeriana

Journal

JOURNAL OF NATURAL MEDICINES
Volume 70, Issue 3, Pages 412-422

Publisher

SPRINGER JAPAN KK
DOI: 10.1007/s11418-016-0987-z

Keywords

Euphorbia fischeriana; Euphorbiaceae; Diterpenoid; Mammosphere formation; Cancer stem cells

Funding

  1. JSPS KAKENHI [25460136, 26460133]
  2. Grants-in-Aid for Scientific Research [26460133, 25460136] Funding Source: KAKEN

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Phytochemical investigation of the roots of Euphorbia fischeriana resulted in the isolation of 23 diterpenoids (1-23), which were classified into five subtypes, namely, ent-rosane (1-9), ent-abietane (10-16), ent-kaurane (17), ingenane (18-22), and lathyrane (23). The chemical structures of eight new compounds, namely, euphorin A (4), B (5), C (7), D (9), E (13), F (14), G (15), and H (16), were elucidated on the basis of extensive 1D and 2D NMR spectroscopic analyses, as well as single crystal X-ray structure analysis. A number of compounds (2, 6, 7, 10, 11, 13, 16, 19, 20, 22, and 23) showed inhibitory activity on the formation of mammospheres in human breast cancer MCF-7 cells at a final concentration of 10 mu M, suggesting the potential of these bioactive diterpenoids for further investigation of the action targeting cancer stem cells.

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