Cytotoxic and Apoptosis‐inducing Activities of Taraxastane‐type Triterpenoid Derivatives in Human Cancer Cell Lines |
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| Authors: | Motohiko Ukiya Chika Ohkubo Masahiro Kurita Makoto Fukatsu Takashi Suzuki Toshihiro Akihisa |
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| Affiliation: | 1. +81 2. 3 3. 32590816+81 4. 32937572;5. College of Science and Technology, Nihon University, Chiyoda‐ku, Tokyo, Japan;6. College of Pharmacy, Nihon University, Funabashi‐shi, Chiba, Japan;7. Akihisa Medical Clinic, Sanda‐shi, Hyogo, Japan |
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| 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. |
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| Keywords: | Taraxastane triterpenoid derivative Cytotoxic activity Apoptosis‐inducing activity Faradiol Amino acid conjugate |
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