Hu Kai, He Huan, Yuan Xiaozheng, Du Xinyu, Liu Ronghe, Yang Penglin, Yang Qian, Zhang Yunjie, Qiao Jing
College of Life Sciences, Anhui Medical University, Hefei City, Anhui Province 230032, P.R. China.
School of Mental Health and Psychological Sciences, Anhui Medical University, Hefei City, Anhui Province 230032, P.R. China.
ACS Pharmacol Transl Sci. 2022 Jul 20;5(8):562-572. doi: 10.1021/acsptsci.2c00035. eCollection 2022 Aug 12.
Crohn's disease (CD) is a chronic intestinal disturbance mediated by mucosal immune hyperactivity that is often associated with the formation of stenosis. No reliable solution to stenosis CD exists so far. Therefore, we generated carboxymethyl chitosan oligosaccharide (CMCOS) as a new promising therapy and investigate its efficacy in an improved rat CD model. CMCOS was synthesized by enzymatic hydrolysis, and its biosafety was evaluated in vivo. The rat model of stenosis CD was optimized by an orthogonal experiment of 75 or 100 mg/kg trinitrobenzenesulfonic acid (TNBS) in a 50 or 75% ethanol enema. The therapeutic efficacy of CMCOS on the rat model of stenosis CD was investigated and compared with the commercial drug 5-aminosalicylic acid over a 28 day period of disease progression. The rat model of stenosis CD was well established by intracolonic administration of 75 mg/kg TNBS in 75% ethanol. CMCOS significantly alleviated CD symptoms morphologically, hematologically, and pathologically, promoting functional recovery of intestinal epithelium in a dose-dependent manner. CMCOS reduced infiltrations of inflammatory cells by regulating the IL-17A/PPAR-γ pathway and reduced fibro-proliferation and fibro-degeneration of the colon tissue by downregulating the TGF-β1/WT1 pathway. 75 mg/kg TNBS in a 75% ethanol enema induces a rat model of stenosis CD suitable for preclinical pathology and pharmacological studies. The safety, antifibrosis, and functional repair performance of CMCOS make it a promising candidate for the treatment of stenosis CD.
克罗恩病(CD)是一种由黏膜免疫亢进介导的慢性肠道紊乱疾病,常伴有狭窄形成。目前尚无针对狭窄型CD的可靠解决方案。因此,我们制备了羧甲基壳寡糖(CMCOS)作为一种有前景的新疗法,并在改良的大鼠CD模型中研究其疗效。CMCOS通过酶解合成,并在体内评估其生物安全性。通过在50%或75%乙醇灌肠中使用75或100 mg/kg三硝基苯磺酸(TNBS)进行正交试验,优化了狭窄型CD大鼠模型。在疾病进展的28天内,研究了CMCOS对狭窄型CD大鼠模型的治疗效果,并与市售药物5-氨基水杨酸进行比较。通过在75%乙醇中结肠内给予75 mg/kg TNBS,成功建立了狭窄型CD大鼠模型。CMCOS在形态学、血液学和病理学上显著减轻了CD症状,以剂量依赖的方式促进肠上皮功能恢复。CMCOS通过调节IL-17A/PPAR-γ途径减少炎症细胞浸润,并通过下调TGF-β1/WT1途径减少结肠组织的纤维增生和纤维变性。在75%乙醇灌肠中使用75 mg/kg TNBS可诱导出适用于临床前病理学和药理学研究的狭窄型CD大鼠模型。CMCOS的安全性、抗纤维化和功能修复性能使其成为治疗狭窄型CD的有希望的候选药物。