桔梗皂苷体外抗肿瘤活性研究

Study on anti-tumor activity of saponins from Platycodi Radix in vitro

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。

Objective： To test the inhibitory effects of platyeodin D, Platyeodin D3 and polygalin D on the growth of Bel-7402 hepatocellular careinoma, BGC-823 gastric carcinoma and MCF-7 mammary cancer cell lines in vitro and find out structure-function relationship between antitumor activity and structures of platycodins. Method ： Three saponins were isolated and identified from Playcodi Radix and inhibitory rate of them on tumor cell lines were assayed by using methyl thiazolyl tetrazolium （MTF） method, and then IC50 values were calculated. Result： Three plaeodins possessed stronger inhibitory activities on Bel-7402 hepatocellular carcinoma at the concentration of 20μg/mL, and their inhibitory rates were 87.38 ± 2.17% , 69.81 ± 5.47% and 95.25 ±1.36% respectively. Platycodin D possessed the highest inhibitory rate on three human tumor cell lines （ Bel-7402, BGC-823 and MCF-7 ） and showed dose-dependent relationship, the IC50 values were calculated as 11.70μg/mL, 9. 10μg/ml and 17. 72μg/ml respectively. Conclusion： The result suggested that platycodins presented better anti-tumor activities in vitro, moreover structure-function relationship between anti-tumor activity and structures of platycodins were confirmed. Platyeodin D may be developed one novel anti-tumor compound.