P-14 トポイソメラーゼII阻害活性を有するテルペノイド類の研究(ポスター発表の部)

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By many studies using specific inhibitors and mutant cell, functional significance of DNA topoisomerase II was shown to be involved in proliferative processes such as DNA replication, chromosome condensation, and chromosome segregation Therefore, topoisomerase II inhibitors were noted as cellular targets of anticancer and antimicrobial agents. In the course of our screening program of topoisomerase II inhibitors, we isolated many inhibitory terpenoid as well as eight new compounds (1-8) belonging to eudesmane type from the root of Cyperus rotundus, and friedelane, oleanane and ursane type from the stem of Maytenus diversifolia and Maytenus emaginata. Structure determination of these compounds was performed by various NMR technique, including COSY, HMBC and NOESY, and chemical methods. Particularly, some of them was found to show significant inhibitory activity against the enzyme, and the structure-activity relationship has become apparent by comparison with those dirivative. In the case of oleanane and ursane typed triterpenoid, topoisomerase II inhibitory activity required the presence of secondary hydroxyl groups at 3 and 22 position, and α-carboxyl group at 20 position. On the other hand, it was clear that the sulfonate group in friedelane type increased inhibitory activity. Those terpenoid did not stabilized the cleavable complex and did not intercalate into duplex DNA. Therefore, functional mechanism of them to topoisomerase II enzyme was different from those of conventional inhibitors such as VP-16 and VM-26.
天然有機化合物討論会の論文
1995-09-01

P-14 トポイソメラーゼII阻害活性を有するテルペノイド類の研究(ポスター発表の部)

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