槲皮素抑制人肝癌细胞HepG2的体内外活性研究

In vivo and in vitro anticancer activity of quercetin against human liver cancer HepG2 Cells

目的系统评价槲皮素(Qu)体内外干预HepG2人肝癌细胞增殖效果。方法使用MTT法检测不同浓度Qu在不同作用时间对HepG2细胞的体外抑制活性;采用裸鼠移植瘤实验,评价腹腔注射Qu对HepG2人肝癌裸鼠移植瘤生长的抑制作用;使用TUNEL法检测凋亡指数。结果Qu作用HepG2细胞24、48和72h的IC50分别为110.50,63.73和46.38μmol/L;12.5,25和50mg/kg的Qu都能显著抑制裸鼠皮下移植瘤的生长,且呈浓度依赖性;其中50mg/kg的Qu对人肝癌HepG2细胞裸鼠皮下肿瘤模型的抑瘤率为46.65%,差异有统计学意义(P<0.05),相对肿瘤增殖率为46.68%。同时Qu还会导致约20.17%的体内肿瘤细胞发生凋亡,且几乎无毒性,表现出良好的抑瘤效果。结论Qu能较为显著的抑制体内外HepG2肝癌细胞的增殖并会导致其发生凋亡,且由于极低的毒性及在自然界的广泛分布,使Qu成为新型抗肝癌药物开发的重要资源。

Objective To evaluate the anticancer effect of quercetin(Qu)against HepG2 cells in vitro and in vivo.Methods MTT assay was used to evaluate the anticancer activity of Qu against HepG2 cells in vitro,and nude mice xenograft model was employed to study the in vivo antitumor activity with intraperitoneal injection of Qu.TUNEL assay was used to test the apoptosis index of the tumor issue.Results The IC 50 values of Qu against HepG2 in vitro with experimental time of 24,48 and 72 h were 110.50,63.73 and 46.38 μmol/L,respectively.All three concentrations of Qu(12.5,25 and 50 mg/kg)could inhibit the growth of subcutaneous xenografts in Balb/C mice in a concentration-dependent manner.Among them,the tumor inhibition rate of Qu with concentration of 50 mg/kg was 46.65%,which had statistically significant effect(P<0.05),and the relative proliferation rate was 46.68%.Meanwhile,nearly 20% of tumor cell apoptosis and no toxicity were observed,suggesting a good inhibitory effect of Qu against liver cancer.Conclusion Qu can significantly inhibit the proliferation of HepG2 cells in vitro and in vivo and cause tumor cells apoptosis.Due to the low toxicity and widespread distribution in nature,Qu is an important resources for developing novel anti-hepatocarcinoma drugs.