丹参酮ⅡA结构修饰及其对HeLa细胞的抑制作用研究  

Preparation of Tanshinone ⅡA Derivatives and Their Proliferation Inhibitory Activity against HeLa Cells

作　　者：江城锋[1] 李瑞峰[1] 薛丹[1] 杨福军[1] 沈秀[1] 徐文清[1] 

机构地区：[1]北京协和医学院中国医学科学院放射医学研究所天津市分子核医学重点实验室,天津300192

出　　处：《天然产物研究与开发》2012年第3期385-388,共4页Natural Product Research and Development

基　　金：天津市应用基础及前沿技术研究计划(10JCYBJC14500);中国医学科学院放射医学研究所青年探索基金(ST1116)

摘　　要：本研究运用Mannich反应,得到了丹参酮ⅡA的16位被酯化氨基酸取代的5个衍生物,结构均经EI-MS、1H及13C NMR确证。经MTT法测定丹参酮ⅡA及其衍生物对HeLa细胞增殖的抑制作用,并计算出IC50。结果表明,5个衍生物的生物活性较丹参酮ⅡA均有所增强;即丹参酮ⅡA在16位进行结构修饰可以增强其对肿瘤细胞抑制活性。Five derivatives of Tanshinone Ⅱ A were prepared via Mannich reaction with esterified amino acid. Their structures were characterized by spectral data. The antipreliferative activities of Tanshinone Ⅱ A and the derivatives a- gainst HeLa cells were evaluated by M＇IT assay. All the five derivatives showed higher activity than Tanshinone Ⅱ A, which suggested that modification at C-16 of Tanshinone ⅡA could enhance its inhibitory activity on tumor cells.

关 键 词：丹参酮ⅡA 结构修饰 MANNICH反应 HELA细胞 细胞毒活性 

分 类 号：O629.9[理学—有机化学] Q946[理学—化学]