目的 研究苦参Sophora flavescens根的化学成分及其体外抗肿瘤活性。方法 利用大孔树脂柱色谱、硅胶柱色谱、ODS柱色谱及半制备型HPLC等进行分离纯化，结合理化性质及波谱数据鉴定化合物的结构；评估了从苦参根提取物中分离得到的11个化合物对人乳腺鳞状癌HCC1806细胞，人乳腺癌MCF-7细胞，宫颈癌HeLa细胞，肺癌A549、H1299和H460细胞和人肝癌HepG2细胞的体外抑制活性。结果 从苦参根70%乙醇提取物中分离得到17个化合物，分别鉴定为8-（3，3-dimethylallyl） isorhamnetin（1）、6-lavandulyl-7，4-dimethoxy-5，2-dihydroxylflavanone（2）、sophoraflavanone B（3）、5-methyl-sophoraflavanone B（4）、苦参酮（5）、苦参醇U（6）、去甲脱水淫羊藿黄素（7）、槐果碱（8）、9α-羟基槐果碱（9）、槐胺碱（10）、臭豆碱（11）、胡椒酸（12）、1-（4-ethylphenyl）-1，2-ethanediol（13）、丁香酸（14）、1，2，4-苯三酚（15）、阿魏酸（16）、羟苄基酒石酸（17）。其中化合物5 对H1299和H460细胞的体外半数抑制浓度（median inhibition concentration，IC₅₀）分别为（22.6±1.2）、（13.6±0.5）μmol/L，其抑制效果强于阳性药顺铂。此外，化合物4 对A549细胞和化合物5 对MCF-7细胞的抑制效果与阳性药相当。结论 化合物1 为新的天然产物，化合物2 、12~15 首次从该属中分离得到；化合物5 对H1299细胞和H460细胞具有较好的抑制活性。苦参中的异戊烯基黄酮在抗肿瘤药物开发与应用上有良好的发展前景。

Objective To study the chemical constituents of Kushen (Sophora flavescens) and its antitumor activities in vitro. Methods The compounds were isolated and purified using macroporous resin column chromatography, silica gel column chromatography, ODS column chromatography and semi-preparative HPLC, and their structures were elucidated by means of physicochemical properties and spectroscopic analysis. And the 11 compounds were evaluated using relevant in vitro anti-tumor activities against breast squamous carcinoma cells (HCC1806), human breast cancer cells (MCF-7), human cervical cancer cells (HeLa), human lung cancer cells (A549, H1299 and H460), and human hepatoma cells (HepG2) in vitro. Results Seventeen compounds were isolated from 70% ethyl alcohol extract from the roots of S. flavescens and identified as 8-(3,3- dimethylallyl)isorhamnetin (1), 6-lavandulyl-7,4-dimethoxy-5,2-dihydroxylflavanone (2), sophoraflavanone B (3), 5- methylsophoraflavanone B (4), kurarinone (5), kushenol U (6), 8-prenylkaempferol (7), sophocarpine (8), 9α-hydroxysophocarpine (9), sophoramine (10), anagyrine (11), piperic acid (12), 1-(4-ethylphenyl)-1,2-ethanediol (13), syringic acid (14), 1,2,4-benzenetriol (15), ferulic acid (16), and piscidic acid (17). Compound 5 showed good inhibitory activities against H1299 and H460, and its inhibitory effect was stronger than that of cisplatin with IC₅₀values of (22.6 ±1.2) μmol/L and (13.6 ±0.5) μmol/L, respectively. In addition, the inhibitory activities of compound 4 against A549 cells and compound 5 against MCF-7 cells were comparable to that of the positive drug. Conclusion Among them, compound 1 is a new natural product, and compounds 2,12-15 are isolated from genus Sophora for the first time. Compound5 showed good inhibitory activities against H1299 and H460, which provide scientific basis for further research on new anti-tumor drugs of isopentenyl flavonoids in S. flavescens.

R284.1

国家重点研发计划项目（2017YFC1701200）；辽宁省“兴辽英才计划”项目（XLYC1902101）