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肝细胞肝癌是恶性程度很高的肿瘤,其恶性增殖是临床治疗失败的原因之一。寻找能有效的抑制肝癌细胞增殖的药物,是肝癌治疗的一条重要途径。体外抗肿瘤活性筛选结果表明,天然产物Dalbinol能浓度依赖性的显著抑制肝癌细胞SMMC-7721增殖;初步的机制研究发现Dalbinol能够降低Dvl-2/3和GSK-3β(p S9)的表达水平,从而抑制Wnt/β-catenin通路的过度激活,下调β-catenin靶蛋白c-Myc和Survivin的表达。此外,Dalbinol也能抑制β-catenin的上游一个重要的调节蛋白Fox M1的表达。综上所述,本研究发现了Dalbinol在肝癌中的抗肿瘤效果,初步阐明了其抑制肝癌增殖的分子机制,可能为肝细胞肝癌的临床治疗提供更有效的候选药物和相关的理论基础。
Hepatocellular carcinoma is a highly malignant tumor whose malignant proliferation is one of the reasons for the failure of clinical treatment. Looking for drugs that can effectively inhibit the proliferation of liver cancer cells is an important way for the treatment of liver cancer. In vitro antitumor activity screening results showed that the natural product Dalbinol can significantly inhibit the proliferation of hepatocellular carcinoma SMMC-7721 in a concentration-dependent manner; preliminary study found that Dalbinol can reduce the expression of Dvl-2/3 and GSK-3β (p S9) Thus inhibiting the over-activation of Wnt / β-catenin pathway and down-regulating the expression of c-Myc and Survivin. In addition, Daltinol also inhibits the expression of Fox M1, an important regulatory protein upstream of β-catenin. In conclusion, the present study found that antitumor effect of Dalbinol in hepatocellular carcinoma and preliminary elucidation of its molecular mechanism of inhibiting the proliferation of hepatocellular carcinoma may provide more effective drug candidates and related theoretical basis for the clinical treatment of hepatocellular carcinoma.