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目的分离筛选黑海参中具有抗肿瘤活性的三萜皂苷成分。方法采用萃取、大孔树脂吸附和正反相硅胶色谱和HPLC对黑海参中具有抗肿瘤活性成分进行提取分离,根据所得化合物的理化性质和波谱数据鉴定其结构;以MTT法检测肿瘤细胞活性,以PI染色及Hoechst 33258染色检测肿瘤细胞周期及凋亡。结果从黑海参中分离获得9个组分A-I,其中组分C、E、F有明显的抑制人肺癌细胞A549和白血病细胞株HL60的活性,而对肝癌BEL7402和MOLT-4细胞无影响;组分C诱导A549细胞周期阻滞在G0/G1和细胞凋亡。据此从组分C中分离并鉴定了3个化合物(1~3)。结论黑海参皂苷组分C中含有抑制人肺癌细胞的活性成分,进一步筛选和分离有可能获得具有抗癌活性的皂苷单体;化合物1~3为首次从黑海参中分离得到。
Objective To isolate and screen triterpenoid saponins with anti-tumor activity in black sea cucumber. METHODS Extraction, macroporous resin adsorption, forward and reverse phase silica gel chromatography and HPLC were used to extract and separate anti-tumor active ingredients of black sea cucumber. The structures of the compounds were identified by the physicochemical properties and spectral data of the obtained compounds. The activity of tumor cells was measured by MTT assay PI staining and Hoechst 33258 staining were used to detect tumor cell cycle and apoptosis. Results Nine components AI were isolated from black sea cucumber. Components C, E and F significantly inhibited the activity of human lung cancer cell line A549 and leukemia cell line HL60, but had no effect on BEL7402 and MOLT-4 cells. Sub-C induced A549 cell cycle arrest at G0 / G1 and apoptosis. Accordingly, three compounds (1-3) were isolated and identified from component C. CONCLUSIONS: Black sea ginsenoside component C contains the active ingredient that inhibits human lung cancer cells, and further screening and isolation may obtain saponin monomers with anticancer activity. Compounds 1 to 3 were isolated from black sea cucumber for the first time.