丹参素的抗癌活性研究anticancer activity of denshensu.pdf

- 180 - Drug Evaluation Research Vol.33 No.6 June 2010 丹参素的抗癌活性研究 * 赵广荣 ，田莉莉，王长松 系统生物工程教育部重点实验室，天津市生物与制药工程重点实验室，天津大学化工学院制药工程系，天津 300072 摘 要 目的：建立体外抗癌天然药物筛选模型，评价丹参素的抗癌活性。方法：以遗传物质DNA 为靶标，溴化乙锭（EB ） 为致癌物质，丹参素为试药，利用荧光光谱检测丹参素对 EB-DNA 体系的荧光猝灭效应；利用圆二色谱技术检测 丹参素对 EB-DNA 体系的干扰作用。结果：丹参素能明显抑制 EB-DNA 体系的荧光强度，且具有浓度依赖性；丹 参素能够有效阻断 EB 嵌入 DNA 的碱基对中，维持DNA 分子的正常构象。结论：丹参素抑制致癌剂对 DNA 链的 嵌合，从而起抗癌活性。该模型可应用于抗癌功效的天然药物的筛选中。 关键词 筛选模型；抗癌天然药物；丹参素；荧光光谱；圆二色谱；DNA 构象 中图分类号：R979.1 文献标志码：A 文章编号：1674–6376 （2010 ）03–0180–03 Anticancer activity of denshensu * ZHAO Guang-rong , TIAN Li-li, WANG Chang-song Key Laboratory of Systems Bioengineering, Ministry of Education; Tianjin Key Laboratory of Biological and Pharmaceutical Engineering; Department of Pharmaceutical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, P. R. China Abstract Objective: To establish in vitro screening model for natural anticancer drugs and evaluate the anticancer activity of denshensu on carcinogenic damaged DNA. Methods: Genetic material DNA was used as target, ethidium bromide (EB) as carcinogen, quenching effect of denshensu on fluorescence spectrum of EB-DNA was detected. Interfering effect of denshensu on circular dichroism spectra of EB-DNA was measured. Results: Denshensu strongly quenched the fluorescent intensity at a dose-dependent manner. The circular dichroism spectra showed that denshensu could inhibit the insertion of EB to base pairs of DNA, and maintain the normal conformation of DNA. Conclusion: Denshensu possesses strong anticancer activity by inhibiting insertion of carcinogens into genetic DNA. This model would be applicable for screening natural anti