新型血管生成抑制剂Borrelidin抗肿瘤作用及其合成的研究进展  

Research Progress on the Anti-tumor Activities and Synthesis of the PotentAngiogenesis Inhibitors Borrelidin

作　　者：周明[1] 胡亮[1] 余聂芳[1] 

机构地区：[1]中南大学药学院,湖南长沙410013

出　　处：《肿瘤药学》2013年第2期82-86,95,共6页Anti-Tumor Pharmacy

基　　金：国家自然科学基金项目资助(81172927)

摘　　要：Borrelidin是从娄彻氏链霉菌代谢产物中分离得到的十八元大环内酯化合物,具有良好的抗菌、抗疟和抗病毒等活性。近年报道其具有血管生成抑制活性(IC50=0.8nM),是潜在的血管生成抑制剂,使Borrelidin再受瞩目,而血管生成抑制剂是目前抗肿瘤药物研究的热点之一,加之Borrelidin结构新颖独特,在药物科研开发领域再度引起了科技工作者的兴趣。本文就Borrelidin的抗肿瘤活性、作用机制及其合成的相关研究进行综述。Borrehdin, isolated from Streptomyces rochei, is a Cls macrolide compound, with several interesting and potent biological activities including antibacterial, antimalarial and antiviral activity. It has been reported in recent years that Borrehdin also has tumor growth inhibitory activity （IC50=0.8 riM） which may be attributed to inhibition of angiogenesis, and becomes a potential angiogenesis inhibitor. Angiogenesis research has become one of-the most attractive, exciting and promising areas in cancer research and treatment. The structural novelty and vital biological activities and its derivates have attracted a great amount of research devoted to the structural optimization in order to discover more potent compounds with fewer side effects. Herein, we reviewed its anti-tumor activities, mechanisms, as well as its synthesis, concentrating on recent case histories in oncology drug discovery.

关 键 词：Borrelidin ThrRS 血管生成抑制 

分 类 号：R730[医药卫生—肿瘤]