苦参碱衍生物的生物转化制备及其抗肿瘤活性研究

摘要

目的：制备新的具有抗肿瘤活性的苦参碱衍生物。方法：采用生物转化方法，制备苦参碱衍生物；采用凝胶柱层析、高效液相色谱等分离技术对转化产物进行分离；采用波谱技术进行化合物结构鉴定；采用MTT法进行细胞毒活性测试。结果：得到5个苦参碱衍生物：13-羟基苦参碱（1）、13，14-二羟基苦参碱（2）、12-羟基苦参碱（3）、13-羰基苦参碱（4）、12-羰基苦参碱（5）。结论：化合物3~5为新的苦参碱衍生物，为首次报道其结构；所得产物均有一定抗肿瘤活性。%Objective: To prepare anti-tumor derivatives of matrine by biotransformation. Methods:Biotransformation technology was applied to prepare matrine derivatives, chromatography technologies were used to isolate the products, spectroscopy techniques were used to determine their structures and MTT method was used to test their cytotoxicity activity. Results: Five matrine derivatives were obtained, including 13-hydroxymatrine (1), 13,14-dihydroxymatrine (2), 12-hydroxymatrine (3), 13-carbonylmatrine (4) and 12-carbonylmatrine (5). Conclusion: Compounds 3-5 were new matrine derivatives and all the obtained compounds showed good anti-tumor activity in bioactivity test.