Yang Dong, Zhang Xiling, Zhang Wencun, Rengarajan Thamaraiselvan
Department of Anorectal Surgery, The First People's Hospital of Lianyungang, Lianyungang, China.
Department of Anorectal Surgery, Shaanxi Provincial People's Hospital, Shaanxi, Xi'an, China.
Drug Des Devel Ther. 2018 May 18;12:1303-1310. doi: 10.2147/DDDT.S149307. eCollection 2018.
Colorectal cancer (CRC) is among highest prevailing cancers in the whole world, especially in western countries. For a diverse of reasons, patients prefer naturally occurring dietary substances over synthetic agents to prevent cancer. Vicenin-2 is largely available in a medicinal plant and is an apigenin form, 6,8-di-C-glucoside, which has been reported to have a range of pharmacological values which includes antioxidant, hepatoprotective, anti-inflammatory and anti-cancer. This study was aimed to analyze the anti-proliferative effect of Vicenin-2 on human colon cancer cells via the Wnt/β-catenin signaling inhibition.
MTT assay was used to assess the cell viability at different concentrations and time point. Vicenin-2 at a concentration of 50 µM (IC) decreased the phosphorylated (inactive) glycogen synthase kinase-3β, cyclin D1, and non-p-β-catenin expressions in HT-29 cells, which were evidenced through western blot analysis.
Further, Vincenin-2 reduced the T-cell factor (TCF) / Leukocyte erythroid factor (LEF) reporter activity in HT-29 cells. Vicenin-2 also promoted substantial cell cycle arrest at the GM phase of HT-29 cells, as well induced apoptosis in HT-29 cells, as revealed through flow cytometric analysis. Furthermore, immunoblot analysis showed that Vicenin-2 treatment enhanced the expression of Cytochrome C, Bax and caspase-3 whereas suppressed the Bcl-2 expression.
Together, these results revealed that Vicenin-2 can act as a potent inhibitor of HT-29 cell proliferation and can be used as an agent against CRC.
结直肠癌（CRC）是全球最常见的癌症之一，尤其是在西方国家。由于多种原因，患者更喜欢天然存在的饮食物质而非合成药物来预防癌症。Vicenin-2大量存在于一种药用植物中，是芹菜素的一种形式，即6,8-二-C-葡萄糖苷，据报道具有一系列药理价值，包括抗氧化、保肝、抗炎和抗癌作用。本研究旨在通过抑制Wnt/β-连环蛋白信号通路分析Vicenin-2对人结肠癌细胞的抗增殖作用。
采用MTT法评估不同浓度和时间点的细胞活力。通过蛋白质印迹分析证实，浓度为50μM（IC）的Vicenin-2可降低HT-29细胞中磷酸化（无活性）糖原合酶激酶-3β、细胞周期蛋白D1和非磷酸化β-连环蛋白的表达。
此外，Vincenin-2降低了HT-29细胞中T细胞因子（TCF）/白细胞红系因子（LEF）报告基因的活性。流式细胞术分析显示，Vicenin-2还促使HT-29细胞在G1期大量停滞，并诱导HT-29细胞凋亡。此外，免疫印迹分析表明，Vicenin-2处理可增强细胞色素C、Bax和半胱天冬酶-3的表达，而抑制Bcl-2的表达。
总之，这些结果表明Vicenin-2可作为HT-29细胞增殖的有效抑制剂，并可作为抗结直肠癌的药物。
