一株新的小单孢菌C-3509抗肿瘤活性成分的分离、纯化和结构鉴定  

Separation,purification and structure identification of the antitumor antibiotic component from fermentation broth of a new micromonospora C-3509

作　　者：赵春燕[1] 张文军[1] 高瑞娟[1] 金莲舫[1] 李电东[1] 邵荣光[1] 

机构地区：[1]中国医学科学院北京协和医学院医药生物技术研究所,北京100050

出　　处：《中国新药杂志》2010年第7期564-568,共5页Chinese Journal of New Drugs

基　　金：国家重大新药创制专项(2009ZX09301-003);国家自然科学基金(30772583);国家973项目(2009CB521807);国家高技术研究发展计划(863)基金(2006AA02A255)

摘　　要：目的:分离纯化小单孢菌C-3509中的抗肿瘤活性成分,并阐明其结构特征。方法:采用多种层析法进行C-3509抗肿瘤活性成分的分离纯化;通过紫外扫描、高分辨电喷雾质谱和核磁共振氢谱揭示其结构特征;利用DNA断裂法检测其抗肿瘤活性。结果:通过对C-3609菌株发酵和活性检测,分离、纯化得到了抗肿瘤活性成分C-3509B;进一步对C-3509B组分进行初步光谱分析与结构鉴定,结果显示该组分结构特征与抗肿瘤抗生素calicheamicinγ1I一致。结论:C-3509B可能是十元环烯二炔calicheamicins的γ1I组分。Objective：To identify the antitumor component extracted from the fermentation broth of a new micromonospora C-3509.Methods：Many kinds of chromatography were used to separate and purify the antitumor component.Then,the identification of the active antitumor component was performed by ultraviolet （UV） scanning,high-resolution electrospray ionization mass spectrometry （HR-ESI-MS） and proton nuclear magnetic resonance spectorscopy （1H-NMR）.Finally,its antitumor effect was analyzed by DNA damage.Results：The antitumor component C-3509B was obtained after the fermentation,detection,isolation and purification of C-3509 strain.Furthermore,the preliminary results of spectral analysis and structural identification for the component C-3509B showed that the structural characteristic of the component was consistent with antitumor antibiotic calicheamicin γ1^I.Conclusion：C-3509B may be the calicheamicin γ1^I,a kind of 10-membered cyclic enediynes.

关 键 词：小单孢菌C-3509 烯二炔 抗肿瘤抗生素 calicheamicin 

分 类 号：R979.14[医药卫生—药品]