五柱五桠果的化学成分及其体外抗肿瘤抗缺氧活性

目的 研究五柱五桠果的化学成分及其抗肿瘤抗缺氧活性。方法 利用各种色谱技术分离化学成分，根据理化性质与光谱数据鉴定结构，利用MTT法测试抗肿瘤活性。结果 从五柱五桠果果实中分离鉴定了白桦酸 (1)、白桦醇 (2)、羽扇豆醇 (3)、谷甾醇 (4)、没食子酸 (5)、没食子酸乙酯 (6)、原儿茶酸 (7)、原儿茶酸甲酯 (8)。化合物1~3、5和6对K562细胞增殖有抑制活性，其中1、2、5的作用较强，IC50分别为31 μg&;#8226;mL-1、29 μg&;#8226;mL-1、23 μg&;#8226;mL-1；3和6次之，在100 μg&;#8226;mL-1浓度下增殖抑制率分别为26.1 %和31.3 %。化合物5和6在无细胞毒的浓度下对 ECV304 细胞的缺氧损伤有保护作用。结论 化合物1~8系首次从该植物分离得到，其中1~3、5和6为该植物生物活性成分的首例报道。

Chemical constituents of Dillenia kerrii and their activities on antitumor and anti-hypoxia in vitro

Aim To investigate chemical constituents of Dillenia kerrii and evaluate their antitumor and anti-hypoxia activities. Methods Chemical constituents were isolated by combination of various column and thin-layer chromatography and the compounds obtained were identified by spectroscopic methods. The anti-tumor and anti-hypoxia activities were assayed by the MTT method using K562 and anoxic ECV304 cells respectively. Results Compounds 1-8 were isolated from the fruits of Dillenia kerrii and they were identified as betulinic acid (1), betulinol (2), lupeol (3), β-sitosterol (4), gallic acid (5), ethyl gallate (6), protocatechuic acid (7) and protocatechuic acid methyl ester (8), respectively. Compounds 1-3, 5 and 6 inhibited the proliferation of K562 cells with IC50 values of 31 μg&;#8226;mL-1 (1), 29 μg&;#8226;mL-1 (2) and 23 μg&;#8226;mL-1 (5), and inhibition rates of 26.1 % (3) and 31.3 % (6) at 100 μg&;#8226;mL-1, respectively. Compounds 5 and 6 also showed the anti-hypoxia effect at the concentration (50 μg&;#8226;mL-1) with no cytotoxicity on anoxic ECV304 cells. Conclusions Compounds 1-8 were isolated from Dillenia kerrii for the first time. Compounds 1-3, 5 and 6 provide the first example of bioactive constituents of D. kerrii.