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[摘要]
目的 分離箭葉淫羊藿中的化學(xué)成分并對(duì)8-異戊烯基黃酮類化合物進(jìn)行體外抗腫瘤活性篩選。方法 采用硅膠柱色譜、凝膠柱色譜和HPLC制備色譜方法分離純化,根據(jù)理化性質(zhì)和波譜分析方法鑒定其結(jié)構(gòu),利用MTT法對(duì)分離得到的異戊烯基黃酮類化合物進(jìn)行體外抗腫瘤活性篩選。結(jié)果 分離得到7個(gè)黃酮類化合物,分別鑒定為淫羊藿苷(1)、淫羊藿素(2)、寶藿苷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)。體外抗腫瘤結(jié)果表明,在0.5~100 μmol/L濃度,化合物2、3、4、6對(duì)人乳腺癌MDA-MB-231細(xì)胞增殖具有明顯抑制作用,并隨濃度的增加抑制作用更加明顯,48 h的IC50分別為12.43、35.44、11.53、16.31 μmol/L,化合物1、7活性很弱。結(jié)論 化合物3、4為首次從箭葉淫羊藿植物分離得到,化合物3有望成為靶向抗乳腺癌的候選藥物。
[Key word]
[Abstract]
Objective To investigate the chemical constituents from Epimedium sagittatum and screen in vitro antitumor activity for 8-prenylated flavonoids. Methods Chemical constituents were isolated and purified by chromatography on silica gel, Sephadex LH-20 colums, and preparative HPLC. Their structures were identified by physicochemical constants and spectroscopic methods. The in vitro antitumor activities of the isolated prenylated compounds were evaluated by MTT assay. Results Seven flavonoids were isolated and their structures were identified as icariin (1), icaritin (2), baohuosideⅠ (3), desmethylicaritin (4), tricin (5), IcarisideⅠ (6), and epimedin C (7). In vitro antitumor results showed that compounds 2-4 and 6 showed the enhanced inhibition on the cell proliferation of human breast cancer cell line MDA-MB-231 in 0.5 — 100 μmol/L with concentration increasing. The IC50 value for 48 h was 12.43, 35.44, 11.53, and 16.31 μmol/L respectively, the activity of compound 1 and 7 were very weak. Conclusion Compounds 3 and 4 are isolated from E. sagittatum for the first time. Compound 3 is expected to become one of the anti-breast cancer drug candidates.
[中圖分類號(hào)]
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