Colorectal cancer (CRC) is one of the most common malignant tumours in the world. Recent reports have revealed natural products displayed inhibition on colon cancer potential by suppressing transforming growth factor-β/Smads induced epidermal-mesenchymal transition (EMT). In this article, 12 kinds of natural berberine analogues were screened for their effects on the inhibition of the colon cancer cells, the results showed that demethyleneberberine (DM-BBR) exhibited an interesting and potential effect on inducing the apoptosis of HCT-116 cells with drug concentrations of 6, 12 and 18 μM. Particularly, DM-BBR reversed the EMT process by inhibiting the expression of p-Smad2 and p-Smad3 in the transforming growth factor-β/Smads signal pathway, up-regulated pro-apoptotic protein cleaved caspase-9, and blocked cell cycle at the S phase and increasing the expression of cyclin proteins P27 and P21. Taken together, these findings suggested that DM-BBR could promote apoptosis and suppress TGF-β/Smads induced EMT in the colon cancer cells HCT-116.

中文翻译：

---

去甲小檗碱促进细胞凋亡并抑制结肠癌细胞 HCT-116 中 TGF-β/Smads 诱导的 EMT

结直肠癌（CRC）是世界上最常见的恶性肿瘤之一。最近的报告显示，天然产物通过抑制转化生长因子-β/Smads 诱导的表皮间充质转化 (EMT) 来抑制结肠癌的可能性。在本文中，筛选了 12 种天然小檗碱类似物对结肠癌细胞的抑制作用，结果表明，去甲小檗碱 (DM-BBR) 在诱导 HCT-116 细胞凋亡方面表现出有趣和潜在的作用。药物浓度为 6、12 和 18 μM。特别是DM-BBR通过抑制转化生长因子-β/Smads信号通路中p-Smad2和p-Smad3的表达，上调促凋亡蛋白裂解的caspase-9，逆转EMT过程，并在 S 期阻断细胞周期并增加细胞周期蛋白 P27 和 P21 的表达。总之，这些发现表明 DM-BBR 可以促进结肠癌细胞 HCT-116 中的细胞凋亡并抑制 TGF-β/Smads 诱导的 EMT。