title: Cytotoxic and Apoptosis-inducing Activities of Taraxastane-type Triterpenoid Derivatives in Human Cancer Cell Lines.
abstract: Twenty-eight taraxastane-type triterpenoid derivatives 4 - 31 were prepared from the naturally occurring triterpenoids faradiol (1) and heliantriol C (3). The cytotoxic activities of these compounds and arnidiol (2) were evaluated in leukemia (HL60), lung (A549), duodenal (AZ521), and breast (SK-BR-3) cancer cell lines. 21-Oxoarnidiol (18) and faradiol 3,16-di-O-l-alaninate (31) exhibited potent cytotoxicity, with 50% inhibitory concentrations of 0.5 - 2.7 μm. In particular, flow cytometric analysis indicated that compound 31 induced typical apoptotic cell death in HL60 cells. These results suggested that taraxastane-type triterpenoid derivatives might provide useful antitumor agents with apoptosis-inducing activity.
authors.affiliation: College of Science and Technology, Nihon University, 1-8-14 Kanda Surugadai, Chiyoda-ku, Tokyo, 101-8308, Japan. ukiya.motohiko@nihon-u.ac.jp.
authors.forename: Motohiko
authors.initials: M
authors.lastname: Ukiya
authors.affiliation: College of Science and Technology, Nihon University, 1-8-14 Kanda Surugadai, Chiyoda-ku, Tokyo, 101-8308, Japan.
authors.forename: Chika
authors.initials: C
authors.lastname: Ohkubo
authors.affiliation: College of Pharmacy, Nihon University, 7-7-1 Narashinodai, Funabashi-shi, Chiba, 274-8555, Japan.
authors.forename: Masahiro
authors.initials: M
authors.lastname: Kurita
authors.affiliation: College of Science and Technology, Nihon University, 1-8-14 Kanda Surugadai, Chiyoda-ku, Tokyo, 101-8308, Japan.
authors.forename: Makoto
authors.initials: M
authors.lastname: Fukatsu
authors.affiliation: College of Pharmacy, Nihon University, 7-7-1 Narashinodai, Funabashi-shi, Chiba, 274-8555, Japan.
authors.forename: Takashi
authors.initials: T
authors.lastname: Suzuki
authors.affiliation: College of Science and Technology, Nihon University, 1-8-14 Kanda Surugadai, Chiyoda-ku, Tokyo, 101-8308, Japan.|Akihisa Medical Clinic, 1086-3 Kamo, Sanda-shi, Hyogo, 669-1311, Japan.
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Akihisa
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D014315:Triterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D014315:Triterpenes
keywords: Amino acid conjugate; Apoptosis-inducing activity; Cytotoxic activity; Faradiol; Taraxastane triterpenoid derivative