Role of the phenolic hydroxyl group in the biological activities of simplified analogue of aplysiatoxin with antiproliferative activity |
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| Authors: | Ryo C. Yanagita Hiroaki Kamachi Keisuke Tanaka Akira Murakami Yu Nakagawa Harukuni Tokuda Hiroshi Nagai Kazuhiro Irie |
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| Affiliation: | 1. Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Kyoto 606-8502, Japan;2. Synthetic Cellular Chemistry Laboratory, Advanced Science Institute, RIKEN (The Institute of Physical and Chemical Research), Wako 351-0198, Japan;3. Graduate School of Medical Science, Kanazawa University, Kanazawa 920-8640, Japan;4. Tokyo University of Marine Science and Technology, Minato-ku, Tokyo 108-8477, Japan |
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| Abstract: | The 18-deoxy derivative (3) of a simplified analogue (1) of aplysiatoxin with antiproliferative activity was synthesized to examine the role of the phenolic hydroxyl group at position 18 in the biological activities of 1. Compound 3 as well as 1 showed significant affinity for protein kinase Cδ (PKCδ), and the antiproliferative activity of 3 was slightly higher than that of 1. However, the anti-tumor-promoting activity of 3 was less than that of 1 in vitro, suggesting that the phenolic hydroxyl group of 1 is necessary for the anti-tumor-promoting activity but not for the binding of PKCδ and antiproliferative activity. Moreover, PKC isozyme selectivity of 3 was similar to that of 1, suggesting non-PKC receptors for these compounds to play some roles in the anti-tumor-promoting activity of 1. |
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