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作用于DNA拓扑异构酶的抗癌物质中,已知有来源于喜树碱等植物的活性物质,但为数甚少。作者此次以探索具有拓扑依存DNA切断活性的植物成分为目的进行了如下研究。实验:运用由胞质遗传体与乳牛胸腺精制的拓扑Ⅰ及Ⅱ,对形成拓扑DNA切断复合体的植物成分进行了探索。结果:①从日本产黄连中发现拓扑Ⅱ抑制活性,从中国产黄连(味连、雅连)中发现拓扑Ⅰ,拓扑Ⅱ两方面的抑制活性。②黄连的拓扑阻碍活性为小檗碱系生物碱所致。对关于各种小檗碱系生物碱的构—效关系进行研究的结果表明,
Among the anticancer substances that act on DNA topoisomerases, active substances derived from plants such as camptothecin are known, but few are known. The authors conducted the following study for the purpose of exploring plant components with topologically dependent DNA cutting activity. Experiments: The use of topological I and II, which are purified from cytoplasmic herpes and cow thymus, explored the plant components that form topological DNA cleavage complexes. RESULTS: 1 Topological II inhibitory activity was found in Japanese Rhizoma Coptidis. The inhibitory activities of topological I and Topological II were discovered from Chinese produced Coptis (Zililian and Yalian). 2 The topological inhibitory activity of Coptis chinensis is caused by berberine alkaloids. The results of studies on the structure-effect relationships of various berberine alkaloids show that