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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 macrolide anticancer active ingredients in the grass weevil of the South China Sea, and to find a new type of anti-cancer agent. METHODS: In vitro anticancer activity was used as an index to combine activity evaluation with chemical separation using gel column chromatography (SephadexLH-20), reverse phase silica gel flash column chromatography (CDS) and preparative high performance liquid chromatography. Advanced Separation Technology for Separation and Preparation of Total Active Constituents from Total Weeds of the South China Sea MTT assay was used to examine the in vitro inhibitory activity of total active ingredients against K562 and U937 tumor cell lines. RESULTS: Total bryostatins with a purity of more than 95% were isolated and prepared from this animal. This total active ingredient has a superior killing effect on the red and white cell leukemia cell line K562 (ED50<10-18 μg/mL). Ml) is the chemical component of natural products that has the strongest inhibitory effect on K562 tumor cells. Conclusion: The resources of weed moss in China’s South China Sea are abundant, and its unique anti-cancer lactoferrin has unique anti-cancer activity for the future development and development of new drugs.