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目的研究甲基丙烯酰紫草素(MA)在体内外的抗肿瘤作用,并探讨其作用机制。方法用MTT法和生长曲线法研究不同浓度的MA对SGC-7901细胞的生长抑制作用;应用S180荷瘤小鼠模型进行其体内抗瘤实验;免疫组化法检测凋亡相关蛋白NF-κB p50的表达。结果MA对SGC-7901细胞具有抑制作用,且呈明显的量效和时效关系,其IC50=14.12±1.83mg.L-1;0.375、0.750、1.500 mg.kg-1的MA对小鼠移植性肉瘤S180的抑制率分别为25.00%、41.20%、61.11%,呈剂量依赖性;随着MA浓度的增大,NF-κB p50蛋白的表达下调。结论MA具有较好的体内外抗肿瘤作用,可能与诱导细胞凋亡和抑制NF-κB p50的活性有关。
Objective To study the antitumor effect of methacryl shikonin (MA) in vitro and in vivo and to explore its mechanism. Methods MTT and growth curve were used to study the effects of different concentrations of MA on the growth of SGC-7901 cells. S180 tumor-bearing mice model was used to test the antitumor activity in vivo. Immunohistochemistry was used to detect the expression of apoptosis-related protein NF-κB p50 expression. Results MA had inhibitory effect on SGC-7901 cells, and showed a significant dose-effect and time-dependent relationship. The IC50 was 14.12 ± 1.83 mg.L-1; 0.375, 0.750 and 1.500 mg.kg-1 The inhibitory rates of sarcoma S180 were 25.00%, 41.20% and 61.11%, respectively, in a dose-dependent manner. With the increase of MA concentration, the expression of NF-κB p50 protein was down-regulated. Conclusion MA has good antitumor activity in vitro and in vivo, which may be related to the induction of apoptosis and the inhibition of NF-κB p50 activity.