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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (04): 515-527. 上一篇    下一篇

综述与进展

新型甾体血管新生抑制剂Cortistatin的结构、生物活性与合成

史勇，田伟生   

  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)
  • 收稿日期:2009-11-16 修回日期:2010-02-01 发布日期:2010-04-28
  • 通讯作者: 田伟生 E-mail:wstian@mail.sioc.ac.cn

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

Shi Yong Tian Weisheng   

  1. (Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032)
  • Received:2009-11-16 Revised:2010-02-01 Published:2010-04-28

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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.

关键词: 甾体生物碱, 血管新生抑制剂, 抗肿瘤, 合成, Cortistatin

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 angiogenesis. Cortistatin A and its analogues are a new kind of steroidal alkaloids with 9-(10,19)-abeo-androstane 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 concentrations (100 pmol/L to 1 μmol/L), in which the selective index is more than 3300-fold higher in comparison 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.

Key words: steroidal alkaloid, anti-angiogensis, antitumor, synthesis, cortistatin