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目的分离箭叶淫羊藿中的化学成分并对8-异戊烯基黄酮类化合物进行体外抗肿瘤活性筛选。方法采用硅胶柱色谱、凝胶柱色谱和HPLC制备色谱方法分离纯化,根据理化性质和波谱分析方法鉴定其结构,利用MTT法对分离得到的异戊烯基黄酮类化合物进行体外抗肿瘤活性筛选。结果分离得到7个黄酮类化合物,分别鉴定为淫羊藿苷(1)、淫羊藿素(2)、宝藿苷Ⅰ(3)、去甲淫羊藿素(4)、苜蓿素(5)、淫羊藿次苷Ⅰ(6)和朝藿定C(7)。体外抗肿瘤结果表明,在0.5～100μmol/L浓度,化合物2、3、4、6对人乳腺癌MDA-MB-231细胞增殖具有明显抑制作用,并随浓度的增加抑制作用更加明显,48h的IC50分别为12.43、35.44、11.53、16.31μmol/L,化合物1、7活性很弱。结论化合物3、4为首次从箭叶淫羊藿植物分离得到,化合物3有望成为靶向抗乳腺癌的候选药物。
OBJECTIVE To isolate the chemical constituents from Epimedium sagittatum and screen the 8-isopentenyl flavonoids for antitumor activity in vitro. Methods The compounds were isolated by silica gel column chromatography, gel column chromatography and HPLC. The structures of the compounds were identified by physico-chemical properties and spectral analysis. Results Seven flavonoids were isolated and identified as icariin (1), icariin (2), icariin Ⅰ (3), demecaimuronin (4), alfalfa (5 ), Epimedium Ⅰ (6) and Epimedin C (7). The antitumor results in vitro showed that compounds 2, 3, 4, and 6 inhibited the proliferation of human breast cancer MDA-MB-231 cells at a concentration of 0.5-100 μmol / L, and the inhibitory effect was more pronounced with increasing concentration. IC50 were 12.43,35.44,11.53,16.31μmol / L, compound 1,7 activity is weak. Conclusion Compounds 3 and 4 were isolated from Epimedium arborescens for the first time. Compound 3 is expected to be a candidate drug for breast cancer targeting.