Cytotoxic and Apoptosis‐inducing Activities of Taraxastane‐type Triterpenoid Derivatives in Human Cancer Cell Lines. Issue 8 (1st August 2016)

• Record Type: Journal Article
• Authors: Ukiya, Motohiko; Ohkubo, Chika; Kurita, Masahiro; Fukatsu, Makoto; Suzuki, Takashi; Akihisa, Toshihiro
• Is Part Of: Chemistry & biodiversity. Volume 13:Issue 8(2016:Aug.)
• Page Start: 1018
• Page End: 1029
• Publication Date: 2016-08-01
• Subjects: Taraxastane triterpenoid derivative -- Cytotoxic activity -- Apoptosis‐inducing activity -- Faradiol -- Amino acid conjugate; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Biodiversity -- Periodicals; 572
• DOI: 10.1002/cbdv.201500356
• Languages: English
• ISSNs: 1612-1872

Abstract

Abstract : Twenty‐eight taraxastane‐type triterpenoid derivatives4 – 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 compound31 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. Abstract : Cytotoxic and Apoptosis‐inducing Activities of Taraxastane‐type Triterpenoid Derivatives in Human Cancer Cell Lines M. Ukiya*, C. Ohkubo, M. Kurita, M. Fukatsu, T. Suzuki, T. Akihisa