肿瘤药学
腫瘤藥學
종류약학
ANTI-TUMOR PHARMACY
2013年
2期
82-86
,共5页
Borrelidin%ThrRS%血管生成抑制
Borrelidin%ThrRS%血管生成抑製
Borrelidin%ThrRS%혈관생성억제
Borrelidin%ThrRS%Inhibition of angiogenesis
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.
Borrelidin 是從婁徹氏鏈黴菌代謝產物中分離得到的十八元大環內酯化閤物,具有良好的抗菌、抗瘧和抗病毒等活性.近年報道其具有血管生成抑製活性(IC50=0.8 nM),是潛在的血管生成抑製劑,使 Borrelidin 再受矚目,而血管生成抑製劑是目前抗腫瘤藥物研究的熱點之一,加之 Borrelidin 結構新穎獨特,在藥物科研開髮領域再度引起瞭科技工作者的興趣.本文就 Borrelidin 的抗腫瘤活性、作用機製及其閤成的相關研究進行綜述.
Borrelidin 시종루철씨련매균대사산물중분리득도적십팔원대배내지화합물,구유량호적항균、항학화항병독등활성.근년보도기구유혈관생성억제활성(IC50=0.8 nM),시잠재적혈관생성억제제,사 Borrelidin 재수촉목,이혈관생성억제제시목전항종류약물연구적열점지일,가지 Borrelidin 결구신영독특,재약물과연개발영역재도인기료과기공작자적흥취.본문취 Borrelidin 적항종류활성、작용궤제급기합성적상관연구진행종술.
@@@@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, mechanisms, as well as its synthesis, concentrating on recent case histories in oncology drug discovery.