Institute of Pathology, Ruhr-University Bochum, D-44789, Germany.
Carcinogenesis. 2012 Mar;33(3):637-43. doi: 10.1093/carcin/bgr306. Epub 2011 Dec 22.
Surveillance colonoscopy is an important strategy for prevention of colorectal cancer. 5-aminosalicylate (ASA) (mesalazine) is discussed as a chemopreventive agent as it reduces the cancer risk in ulcerative colitis patients. The current study analyses the effect of 5-ASA on Wnt/β-catenin signaling in vitro and in vivo in colon epithelial cells. The effect of 5-ASA was determined using a β-catenin/T-cell factor (TCF)-reporter assay and by western blotting in cultured colon cancer cells. Formalin fixed paraffin embedded material from 227 polyps removed from a subgroup of 56 patients, who participated in a randomized placebo-controlled 3-year prevention trial with 5-ASA was evaluated according to histomorphological characteristics and expression of β-catenin and target genes Cox2, cyclin D1 and E-cadherin as well as ornithine decarboxylase (ODC). Patients were grouped into a low-risk and a high-risk group according to the number of adenomas at initial colonoscopy. ß-catenin/TCF signaling activity was significantly reduced by 5-ASA treatment possibly through a reduction in ß-catenin levels. Moreover, 5-ASA significantly reduced ß-catenin levels and nuclear localization in patients' adenomas. In addition, 5-ASA also significantly changed expression of the downstream targets Cox2, cyclin D1 and E-cadherin, correlating with ß-catenin status. Moreover, 5-ASA significantly reduced levels of ODC in vivo. Expression of p53 was unaltered by the 5-ASA treatment. Our study shows a significant in vitro and long-term in vivo effect of 5-ASA on ß-catenin signaling as a key signaling pathway in the development of colorectal adenoma. Therefore, we suggest the use of 5-ASA as a promising drug for prevention of sporadic colorectal carcinoma.
结肠镜监测是预防结直肠癌的重要策略。5-氨基水杨酸(ASA)(美沙拉嗪)被认为是一种化学预防剂,因为它可以降低溃疡性结肠炎患者的癌症风险。本研究分析了 5-ASA 在体外和体内对结肠上皮细胞中 Wnt/β-catenin 信号通路的影响。通过β-catenin/T 细胞因子(TCF)-报告基因测定和培养的结肠癌细胞中的 Western blot 测定,确定了 5-ASA 的作用。根据组织形态学特征以及β-连环蛋白和靶基因 Cox2、cyclin D1 和 E-钙粘蛋白以及鸟氨酸脱羧酶(ODC)的表达,对来自 56 名参加了为期 3 年的 5-ASA 随机安慰剂对照预防试验的 56 名患者中切除的 227 个息肉的福尔马林固定石蜡包埋材料进行了评估。根据初次结肠镜检查时腺瘤的数量,将患者分为低风险组和高风险组。5-ASA 治疗可显著降低β-catenin/TCF 信号活性,可能是通过降低β-catenin 水平实现的。此外,5-ASA 还可显著降低患者腺瘤中β-catenin 的水平和核定位。此外,5-ASA 还可显著改变下游靶基因 Cox2、cyclin D1 和 E-钙粘蛋白的表达,与β-catenin 状态相关。此外,5-ASA 还可显著降低体内 ODC 的水平。5-ASA 治疗对 p53 的表达没有影响。本研究表明,5-ASA 对β-catenin 信号具有显著的体外和长期体内作用,β-catenin 信号是结直肠腺瘤发生的关键信号通路。因此,我们建议将 5-ASA 用作预防散发性结直肠癌的有前途的药物。