五柱五桠果的化学成分及其体外抗肿瘤抗缺氧活性

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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。 Objective To study the chemical constituents and anti-hypoxic activity of five-pillar pods. Methods The chemical constituents were separated by various chromatographic techniques. The structures were identified by physicochemical properties and spectral data. The antitumor activity was tested by MTT assay. Results Betulinic acid (1), Betulin (2), Lupinol (3), sitosterol (4), Gallic acid (5), Gallic acid ethyl ester (6) Protocatechuic acid (7), protocatechuic acid methyl ester (8). Compounds 1, 2, 3, 5 and 6 had inhibitory activity against proliferation of K562 cells, with strong effects of 1, 2 and 5, with IC50 of 31 μg.mL-1, 29 μg.mL-1, and 23 μg.mL-1, respectively. At 3 and 6 times, the inhibition rate of proliferation at the concentration of 100 μg·mL-1 was 26.1% and 31.3%, respectively. Compounds 5 and 6 have protective effects against hypoxic injury of ECV304 cells at cytotoxic concentrations. Conclusion Compounds 1-8 were isolated from the plant for the first time. Among them, 1, 2, 3, 5 and 6 were the first reported examples of the bioactive components of the plant.
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