Colorectal cancer (CRC) is a common malignancy with high mortality and poor prognosis. Diacerein (DIA) is an anti-inflammatory used for treatment of osteoarthritis. We delineated some underlying molecular mechanisms of DIA’s anti-carcinogenic effect in CRC using in vivo and in vitro models. Human Caco-2 cells were treated with DIA followed by MTT and Annexin V assays and CRC was experimentally induced using 1,2-dimethylhydrazine. DIA (50 mg/kg/day, orally) was administrated for 8 weeks. The MTT assay confirmed cytotoxic effect of DIA in vitro and Annexin V confirmed its apoptotic effect. DIA resulted in regression of tumour lesions with reduced colonic TLR4, NF-κB and TNF-α protein levels and down-regulated VEGF expression, confirming anti-angiogenic impact. DIA triggered caspase-3 expression and regulated Wnt/β-Catenin pathway, by apparently interrupting the IL-6/STAT3/ lncRNA HOTAIR axis. In conclusion, DIA disrupted IL-6/STAT3/ lncRNA HOTAIR axis which could offer an effective therapeutic strategy for the management of CRC.

结直肠癌（CRC）是一种常见的恶性肿瘤，死亡率高，预后差。双醋瑞因 (DIA) 是一种用于治疗骨关节炎的抗炎药。我们使用体内和体外模型描述了 DIA 在 CRC 中的抗癌作用的一些潜在分子机制。用 DIA 处理人 Caco-2 细胞，然后进行 MTT 和膜联蛋白 V 测定，并使用 1,2-二甲基肼实验性诱导 CRC。DIA（50 mg/kg/天，口服）给药 8 周。MTT 测定证实了 DIA 在体外的细胞毒性作用，而 Annexin V 证实了其凋亡作用。DIA 导致肿瘤病变消退，结肠 TLR4、NF-κB 和 TNF-α 蛋白水平降低，VEGF 表达下调，证实了抗血管生成作用。DIA 触发 caspase-3 表达并调节 Wnt/β-Catenin 通路，通过明显中断 IL-6/STAT3/lncRNA HOTAIR 轴。总之，DIA 破坏了 IL-6/STAT3/lncRNA HOTAIR 轴，可为 CRC 的管理提供有效的治疗策略。