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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 isolate and purify the anti-tumor active components of Micromonospora C-3509 and elucidate its structural characteristics. METHODS: The anti-tumor activity of C-3509 was isolated and purified by a variety of chromatographic methods. Its structure was elucidated by UV-scan, high-resolution electrospray ionization mass spectrometry and proton nuclear magnetic resonance spectroscopy. The antitumor activity was detected by DNA cleavage. Results: The anti-tumor activity component C-3509B was isolated and purified by fermentation and activity test of C-3609 strain. The preliminary spectral analysis and structural identification of C-3509B were carried out. The results showed that the structure and anti-tumor activity of anti- Tumor antibiotics calicheamicinγ1I consistent. Conclusion: C-3509B is probably the γ1I component of ten-membered cycloalkyne diacetylenic calicheamicins.