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目的:研究中国南海总合草苔虫中的抗癌活性成分。方法:通过分级萃取和多种硅胶柱层析(Sephadex LH-20凝胶过滤、ODS反相层析和HPLC)追踪分离抗癌活性成分;利用电喷雾离子质谱(ESI-MS)和高分辨(600 MHz)核磁共振二维谱技术鉴定化合物的结构。结果:分离得到一个新的具有显著抗肿瘤活性的大环内酯bryostatin 19(1)。同时还首次自中国海域的该种苔虫中分离鉴定了5个bryostatins类大环内酯抗癌活性化合物:bryostatin 4,5,6,10,18。Bryostatin 19显示很强的体外抗癌活性,对U937细胞的ED50值为3.2 nmol／L。结论:我国南海总合草苔虫资源丰富,并且含有新结构的抗癌活性草苔虫内酯。本研究结果为今后的新药研制与开发提供了参考。
Objective: To study the anti-cancer active ingredients in C. ocellatus in the South China Sea. METHODS: Fractionated extractions and various silica gel column chromatography (Sephadex LH-20 gel filtration, ODS reverse phase chromatography, and HPLC) were used to trace the separation of anticancer active ingredients; electrospray ionization mass spectrometry (ESI-MS) and high resolution ( A 600 MHz) NMR two-dimensional spectrum technique was used to identify the structure of the compound. RESULTS: A novel macrolide bryostatin 19 (1) with significant antitumor activity was isolated. At the same time, five bryostatins macrolide anticancer active compounds were also isolated and identified from this species of Chinese seaweed for the first time: bryostatin 4,5,6,10,18. Bryostatin 19 showed strong anticancer activity in vitro with an ED50 value of 3.2 nmol/L for U937 cells. Conclusion: The total number of grassland weeds in the South China Sea is abundant, and contains a new structure of the anti-cancer activity of oxalidin. The results of this study provide a reference for the future development and development of new drugs.