title: ent-Atisane diterpenoids from Euphorbia fischeriana inhibit mammosphere formation in MCF-7 cells.
abstract: 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.
authors.affiliation: Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi, Chiba, 274-8510, Japan.
authors.forename: Xinzhu
authors.initials: X
authors.lastname: Kuang
authors.affiliation: Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi, Chiba, 274-8510, Japan. liwei@phar.toho-u.ac.jp.
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.affiliation: Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi, Chiba, 274-8510, Japan.
authors.forename: Yuichiro
authors.initials: Y
authors.lastname: Kanno
authors.affiliation: Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi, Chiba, 274-8510, Japan.
authors.forename: Naoya
authors.initials: N
authors.lastname: Yamashita
authors.affiliation: Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi, Chiba, 274-8510, Japan.
authors.forename: Kiyomitsu
authors.initials: K
authors.lastname: Nemoto
authors.affiliation: Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba, 278-8510, Japan.
authors.forename: Yoshihisa
authors.initials: Y
authors.lastname: Asada
authors.affiliation: Faculty of Pharmaceutical Sciences, Toho University, Miyama 2-2-1, Funabashi, Chiba, 274-8510, Japan.
authors.forename: Kazuo
authors.initials: K
authors.lastname: Koike
mesh_terms: D004224:Diterpenes / Q000737:chemistry / Q000494:pharmacology*; D028481:Euphorbia / Q000737:chemistry*; D006801:Humans; D061986:MCF-7 Cells; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018517:Plant Roots / Q000737:chemistry; D018874:Spheroids, Cellular / Q000187:drug effects*; D014407:Tumor Cells, Cultured
chemical_list: D004224:Diterpenes; D010936:Plant Extracts
keywords: Cancer stem cells; Diterpenoid; Euphorbia fischeriana; Euphorbiaceae; Mammosphere formation; ent-Atisane