穿心莲内酯抗肿瘤作用衍生物的合成研究进展  

Recent Progress in Synthesis of Andrographolide Derivatives with Anti-tumor Activities

作　　者：彭宇然[1,2] 孙亦诚 王德才[1] 韦萍[2] 欧阳平凯[2] 周国春[1] 

机构地区：[1]南京工业大学药学院,南京211816 [2]南京工业大学生物与制药工程学院,南京211816

出　　处：《有机化学》2015年第7期1451-1468,共18页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.30973621)资助项目~~

摘　　要：作为爵床科植物穿心莲的主要活性成分之一,穿心莲内酯具有广泛的药理活性.近年来,已有大量研究表明对穿心莲内酯进行结构改造可提升其抗肿瘤作用.因此,根据穿心莲内酯衍生物结构特点,将其按照基础骨架不同分为五类,分别为穿心莲内酯骨架衍生物、14-去氧穿心莲内酯骨架衍生物、脱水穿心莲内酯骨架衍生物、异穿心莲内酯骨架衍生物以及12-环替代的穿心莲内酯骨架衍生物.在此基础上,对穿心莲内酯衍生物的合成以及抗肿瘤活性结果进行综述,并初步总结其构效关系.最后,对衍生物未来的研究趋势进行了展望.As one of the major active constituents in Andrographis panniculata （Burm. f.） Nees of Acanthaceae family, andrographolide is proved to possess a wide range of biological activities. In recent years, numerous studies show that the structural modification of andrographolide could enhance its anti-tumor activities. Therefore, according to the structural properties of andrographolide derivatives, five types of derivatives classified by different basic skeletons are denoted as the skeleton of andrographolide derivatives, the skeleton of 14-deoxyandrographolide derivatives, the skeleton of dehydroandrographolide derivatives, the skeleton of isoandrographolide derivatives and the skeleton of 12-ring replaced andrographolide derivatives. On this basis, the synthesis and anti-tumor activities of andrographolide derivatives are reviewed, and the structure activity relationship are also summarized preliminarily. The future trends of the derivatives research are discussed in the end.

关 键 词：穿心莲内酯 衍生物 合成 抗肿瘤 

分 类 号：TQ460.1[化学工程—制药化工]