新型甾体血管新生抑制剂Cortistatin的结构、生物活性与合成  

Structure, Bioactivity and Synthesis of Cortistatin, a New Kind of Steroidal Angiogenesis Inhibitors

作　　者：史勇[1] 田伟生[1] 

机构地区：[1]中国科学院上海有机化学研究所天然产物有机合成化学重点实验室,上海200032

出　　处：《有机化学》2010年第4期515-527,共13页Chinese Journal of Organic Chemistry

摘　　要：由于肿瘤的生长与转移高度依赖于血管新生,因此发现和发明新型血管新生抑制剂对肿瘤疾病治疗有重要意义.以Cortistatin A为代表的Cortistatin类海洋天然产物是一类化学结构新颖、具有显著血管新生抑制作用的甾体化合物.它们具有9-(10,19)-abeo-雄甾烷骨架和氧原子桥连七元B环结构,Cortistatin A对人脐静脉内皮细胞(HUVEC)增殖具有nmol/L级的抑制活性和相对其他细胞系大于3300的选择性指数.综述了Cortistatin及其类似物自发现来两年期间的合成进展情况.The discovery and invention of new type of anti-angiogenesis agents are very important for the treatment of a variety of tumors due to a fact that growth and metastasis of tumor highly depended upon an- giogenesis. Cortistatin A and its analogues are a new kind of steroidal alkaloids with 9-（lO,19）-abeo-andro- stane skeleton and a bridged seven-membered B ring of marine origin. Cortistatin A shows cytostatic anti-proliferative activity against human umbilical vein endothelial cell （HUVEC） at very wide range con- centrations （100 pmol/L to 1 μmol/L）, in which the selective index is more than 3300-fold higher in com- parison with those of several other cell lines. This review summarizes the synthetic progress of cortistatin A and its analogues since their discovery in 2006-2007.

关 键 词：甾体生物碱 血管新生抑NN 抗肿瘤 合成 CORTISTATIN 

分 类 号：TQ464[化学工程—制药化工]