著者

中村 優一 加藤 光 塚本 佐知子

出版者

天然有機化合物討論会実行委員会

雑誌

天然有機化合物討論会講演要旨集

巻号頁・発行日

vol.53, pp.421-426, 2011

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In our laboratory, we search for drug leads from marine sponge, ascidian and fungus. The extract of the ascidian Didemnum sp., which collected in Indonesia in 2006, showed anti-fungal activity and inhibitory activity of p53-Mdm2 complex formation. p53, tumor suppressor, protein induced growth arrest and apoptosis, and Mdm2 is an E3 for p53 protein. Therefore, inhibition of p53-Mdm2 complex formation is a promising approach for treatment of cancer. Twelve new serinolipids, 1-12 were isolated from Indonesian ascidian Didemnum sp. 1D and 2D NMR spectrum and MS spectrum analysis was revealed the structures of these compounds possessing a 6,8-dioxabicyclo[3.2.1]octane ring, which was appeared in didemniserinolipid A, a glycerophosphocholine moiety and a serinol moiety containing sulfate. Compounds 1-12 demonstrated inhibition of p53-Mdm2 complex formation. Compounds 1 and 5 were the most potent inhibitors with an IC^<50> value of 2.0 μM, while compounds -2 and 10 exhibited weak inhibitors with IC^<50> values of 53 and 55 μM, respectively.