雷公藤治疗乳腺癌主要活性成分筛选及分子机制探讨

Mechanism and main active ingredients of Radix Et Rhizoma Tripterygii Wilfordii for breast cancer

目的基于网络药理学筛选雷公藤治疗乳腺癌主要活性成分并初步探讨分子机制。方法利用TCMSP平台获取雷公藤活性成分及作用靶点信息,检索GeneCard数据库筛选雷公藤治疗乳腺癌潜在靶标,将两者进行匹配获得雷公藤治疗乳腺癌核心成分及靶点基因。应用Cytoscape3.6.0、AutoDock Vina等软件,构建活性成分-靶点网络图,进行靶点基因富集分析,完成核心靶标与成分的分子对接。利用CCK8及qPCR等方法验证核心单体成分对乳腺癌细胞及治疗靶点的作用。结果筛选获得雷公藤治疗乳腺癌有效成分7种,核心治疗靶点25个。其中最优成分为雷公藤红素,其对乳腺癌细胞具有明显抑制作用且显著降低核心治疗靶点的mRNA表达。结论雷公藤通过多靶点发挥治疗乳腺癌作用,其中雷公藤红素是其核心药用成分。

Aim To explore the main active ingredients of Tripterygium wilfordii and the mechanism in treat-ment of breast cancer based on network pharmacology.Methods The active components and targets of Tripterygii Wilfordii were searched by TCMSP.GeneCard database was used to screen the potential targets of Tripterygii Wilfordii in treatment of breast cancer.The two were matched to obtain the core components and targets of Tripterygii Wilfordii.Cytoscape3.6.0 and AutoDock Vina were used to draw the drug-target network diagram,and GO enrichment analysis,KEGG pathway enrichment analysis,and molecular docking between the core target and the components were carried out.CCK8 and qPCR were used to verify the effect of optimal core component tripterine on breast cancer cells.Results Seven kinds of active anti-breast cancer components and twenty-five core therapeutic targets of Tripterygii Wilfordii were obtained.Tripterine,which significantly inhibited the growth of breast cancer cells,was the most valuable component of Tripterygii Wilfordii for breast cancer.QPCR results showed that tripterine decreased the expression of core therapeutic targets.Conclusions The effectiveness of Tripterygii Wilfordii has multiple pathways,and tripterine may play an important role in treatment of breast cancer.