Structure Modification for Reduced Toxicity Derivatives and Anticancer Activity of Vinblastine Zu Yuangang, Fu Yujie，Luo Meng*, Mu Fansong (Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, China) Abstract Vinblastine is one of the alkaloids from catharanthus roseus. As an antimitotic drug it can inhibit microtubule assembly and induce tubulin self-association into coiled spiral aggregates. Several semisynthesis vinblastine analogues were prepared and lots of them have pharmacological activities, some even changed significantly. But the relationship between chemical structure and pharmacological activity of vinblastine are still unknown. So in this paper we summarized some mechanism of vinblastine analogues with microtubules and proteins and the reactive center of vinblastine through the successful chemical structure modification cases previously. We also suggest the possible successful chemical structure modification methods of vinblastine in this study. Key words Vinblastine, Anticancer activity, Derivatives, Chemical structure modification Reactive center 长春碱的抗癌活性及其降低毒性的结构修饰 祖元刚 付玉杰 罗 猛* 牟璠松 (东北林业大学森林植物生态学教育部重点实验室 哈尔滨 150040) 摘要 长春碱是长春花中所含生物碱的一种。作为一种抗有丝分裂药物，它能够抑制微管聚合并诱导自缔合的微管蛋白形成盘绕的螺旋形聚合体。目前人们已经合成了一系列长春碱类衍生物，其中大多数具有药理活性，有一些甚至产生极大变化。但长春碱类药物的构效关系至今仍不清楚。本文结合长春碱类生物碱衍生物与微管及相关蛋白质的作用机制并通过前人对长春碱成功修饰的范例总结了长春碱的活性作用点，同时也对长春碱可能进行的化学结构修饰提出建议。 关键词 长春碱 抗癌活性 化学结构修饰 活性作用点 祖元刚 男，48 岁，教授，主要从事药用植物和植物药的研究工作。E-mail:zygorl@public.hr.hl.cn *联系人 2003-03-15 收稿，2003-10-08 接受 (PDF全文下载c04027)