新型血管生成抑制剂Borrelidin抗肿瘤作用及其合成的研究-肿瘤药学.PDFVIP

- 82 - 肿瘤药学 2013 年 4 月第 3 卷第 2 期　Anti-tumor Pharmacy, April 2013, Vol. 3, No. 2 ●综　　述● 新型血管生成抑制剂 Borrelidin 抗肿瘤作用及其合 成的研究进展★ 周　 明，胡　 亮，余聂芳* （中南大学药学院，湖南 长沙，4 100 13 ） 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=0.8 nM），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。 关键词：Borrelidin；ThrRS；血管生成抑制 中图分类号：R730　文献标识码 ：A　文章编号：2095-1264（2013）02-0082-06 doi：10.3969/j.issn.2095-1264.2013.019 Research Progress on the Anti-tumor Activities and Synthesis of the Potent Angiogenesis Inhibitors Borrelidin ★ Zhou Ming, Hu Liang, Yu Nief ang* ( School of Pharmacy Sciences, Central South University, Changsha, Hunan, 410013, China ) Abstract: Borrelidin, isolated from Streptomyces rochei, is a C18 macrolide compound, with several interesting and potent biological activities including antibacterial, antimalarial and antiviral activity. It has been reported in recent years that Borrelidin also has tumor growth inhibitory activity (IC50=0.8 nM) 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 ef- fects. Herein, we reviewed its anti-tumor activities, mechanis