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目的:研究桔梗皂苷D(platycodin D),桔梗皂苷D3(platycodin D3),远志皂苷D(polygalin D)对人肝癌Bel-7402、胃癌BGC-823、乳腺癌MCF-7细胞株的体外增殖的抑制作用及构效关系。方法:利用常规柱色谱与制备高效液相色谱相结合从桔梗根中分离得到3种单体皂苷,采用甲基噻唑基四唑(MTT)比色法检测桔梗皂苷对3种肿瘤细胞株的抑制率,计算IC50值。结果:在质量浓度为20μg/ml时,3种皂苷均对人肝癌Bel-7402细胞株的增殖有较强的抑制活性,质量浓度为20μg/ml时,抑制率分别为87.38±2.17%,69.81±5.47%,95.25±1.36%。桔梗皂苷D对人肝癌Bel-7402、胃癌BGC-823、乳腺癌MCF-7细胞株的增殖抑制最强,且呈剂量依赖关系,IC50值分别为11.70μg/mL、9.10μg/mL、17.72μg/mL。结论:桔梗皂苷具有良好的体外抗肿瘤活性,体外抗肿瘤活性与皂苷结构存在明显的构效关系,桔梗皂苷D有望成为抗肿瘤备选化合物。
AIM: To investigate the inhibitory effects of platycodin D, platycodin D3 and polygalin D on the proliferation of human hepatocellular carcinoma Bel-7402, gastric cancer BGC-823 and breast cancer MCF-7 cells in vitro Role and structure-activity relationship. METHODS: Three kinds of monomeric saponins were isolated from the root of Campanulaceae by conventional column chromatography and preparative high performance liquid chromatography (HPLC). Methyl thiazolyl tetrazolium (MTT) colorimetry was used to detect the inhibitory effect of platycodin on three tumor cell lines Rate, calculate IC50 value. Results: All of the three saponins inhibited the proliferation of Bel-7402 human hepatocellular carcinoma cell line at the concentration of 20μg / ml. The inhibitory rates of the three saponins were 87.38 ± 2.17%, 69.81 ± 5.47%, 95.25 ± 1.36%. The inhibitory effect of platycodin D on human hepatocellular carcinoma Bel-7402, gastric cancer BGC-823 and breast cancer MCF-7 cell lines was the strongest and its IC50 values were 11.70μg / mL, 9.10μg / mL and 17.72μg / mL. CONCLUSION: Platycodin has good antitumor activity in vitro. Antitumor activity in vitro has obvious structure-activity relationship with the structure of saponin. Platycodin D is expected to become an anti-tumor candidate compound.