五柱五桠果的化学成分及其体外抗肿瘤抗缺氧活性

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

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、2、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31μg.mL^-1、29μg.mL^-1、23μg.mL^-1;3和6次之,在100μg·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、2、3、5和6为该植物生物活性成分的首例报道。

Aim To investigate chemical constituents of Dillenia kerrii and evaluate their antitumor and antihypoxia activities. Methods Chemical constituents were isolated by combination of various column and thinlayer chromatography and the compounds obtained were identified by spectroscopic methods. The antitumor 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 1,2,3,5 and 6 inhibited the proliferation of K562 cells with IC50 values of 31 μg·mL^- 1 （ 1 ）, 29μg·mL^- 1 （2） and 23μg·mL^- 1 （ 5 ）, and inhibition rates of 26. 1% （3） and 31.3% （6） at 100μg·mL^- 1,respectively. Compounds 5 and 6 also showed the anti-hypoxia effect at the concentration （50μg·mL^- 1） with no cytotoxicity on anoxic ECV304 cells. Conclusion Compounds 1 - 8 were isolated from Dillenia kerrii for the first time. Compounds 1,2,3,5 and 6 provide the first example of bioactive constituents of D. kerrii.