中国南海总合草苔虫抗癌活性成分研究──Ⅱ　总草苔虫内酯的超强抗癌活性  

STUDIES ON THE ANTINEOPLASTIC CONSTlTUENTS FROM MARINE BRYOZOAN BUGULA NERITINA INHABITING SOUTH CHINA SEA(Ⅱ):REMARKABLE ANTINEOPLASTIC ACTIVITIES OF ACTIVE PRINCIPALS

作　　者：林厚文[1] 易杨华 姚新生[2] 吴厚铭[3] 釜野德明[4] 

机构地区：[1]第二军医大学附属长征医院药材科,上海200003 [2]沈阳药科大学,沈阳100024 [3]中科院上海有机化学研究所 [4]日本神奈川大学理学部

出　　处：《中国海洋药物》2000年第2期1-3,共3页Chinese Journal of Marine Drugs

基　　金：国家自然科学基金!29672050

摘　　要：目的：研究中国南海草苔虫中的大环内酯类抗癌活性成分，从中寻找高效的新型抗癌剂。方法：以体外抗癌活性为指标，将活性评价与化学分离相结合，采用凝胶柱层析（SephadexLH－20），反相硅胶快速柱层析（CDS）和制备性高效液相层析等先进分离技术，对南中国海的总合草苔虫样本进行总活性成分的分离制备。采用MTT法考察总活性成分对K562、U937肿瘤细胞株的体外抑制活性。结果：从该动物中分离制备了纯度高达95％以上的总草苔虫内酯（bryostatins），此总活性成分对红白细胞白血病细胞株K562具有超强的杀灭作用（ED50＜10－18μg／ml），是天然产物中对K562肿瘤细胞抑制作用最强的化学成分。结论：我国南海总合草苔虫资源丰富，含有其独特的其超强抗癌活性的草苔虫内酯，为今后的新药研制与开发展示了美好前景。Objective:To study the antineoplastic constituents of rnarine bryozoan Bugula neritina inhabiting South China Sea and to search for new anticancer agents from this animal.Methods:The screening of active portions was preliminarily guided by bioassay method. Further isolation and purification of active principals were achieved by a combination of successive silica gel, Sephadex LH-20, octadecylsilanized (ODS)silica gel column chromatographies and preparative HPLC. Results: The active principals of the animal showed remarkable inhibiting activity against K562 cell line with IC50 value of 10-18μg/ml in vitro,while no substance with such strong cytotoxic activity against K562 cell line has been found in nature.Conclusion: Bugula neritina is abundant in South China Sea. It contains potential antineoplastic principals of bryostatin series,showing remarkable cell growth inhibitory activity against K562 cell line. The author believes that the marine bryozoan Bugula neritina,which was regarded as a common marine bio fouling before,will be developed as potentially useful source of anticancer in the future.

关 键 词：总合草苔虫 草苔虫内酯 抗癌活性 总活性成分 

分 类 号：R931.77[医药卫生—生药学] R979.1[医药卫生—药学]