Balkrishna Acharya, Singh Rani, Gohel Vivek, Arora Sagar, Dev Rishabh, Bhattacharya Kunal, Varshney Anurag
Drug Discovery and Development Division, Patanjali Research Institute, Uttarakhand, Haridwar 249 405, India.
Department of Allied and Applied Sciences, University of Patanjali, Patanjali Yog Peeth, Uttarakhand, Haridwar 249 405, India.
Pharmaceuticals (Basel). 2022 Dec 31;16(1):63. doi: 10.3390/ph16010063.
Ulcerative colitis (UC) is an inflammatory bowel disease that affects the patients' colorectal area culminating in an inflamed 'leaky gut.' The majority of UC treatments only provide temporary respite leading to its relapse. Therefore, this study investigated the efficacy of the enteric-coated 'Cologrit' (EC) tablet in alleviating UC-like inflammation. Cologrit is formulated using polyherbal extracts that have anti-inflammatory qualities according to ancient Ayurveda scriptures. Phytochemical profiling revealed the presence of gallic acid, rutin, ellagic acid, and imperatorin in Cologrit formulation. Cologrit treatment decreased inflammation in LPS-induced transformed THP-1 macrophages, and TNF-α-stimulated human colorectal (HT-29) cells through the modulation of NFκB activity, IL-6 production, and NFκB, IL-1β, IL-8, and CXCL5 mRNA expression levels. Cologrit also lessened human monocytic (U937) cell adhesion to HT29 cells. Methacrylic acid-ethylacrylate copolymer-coating of the enteric Cologrit tablets (EC) supported their dissolution, and the release of phytochemicals in the small intestine pH 7.0 environment in a simulated gastrointestinal digestion model. Small intestine EC digestae effectively abridged dextran sodium sulfate (2.5% /)-induced cell viability loss and oxidative stress in human colon epithelial Caco-2 cells. In conclusion, the enteric-coated Cologrit tablets demonstrated good small intestine-specific phytochemical delivery capability, and decreased UC-like inflammation, and oxidative stress through the regulation of TNF-α/NFκB/IL6 signaling axis.
溃疡性结肠炎（UC）是一种炎症性肠病，会影响患者的结肠直肠区域，最终导致肠道发炎并出现“肠漏”。大多数UC治疗方法只能提供暂时缓解，导致病情复发。因此，本研究调查了肠溶包衣的“Cologrit”（EC）片在减轻UC样炎症方面的疗效。根据古代阿育吠陀经文，Cologrit是使用具有抗炎特性的多种草药提取物配制而成。植物化学分析表明，Cologrit制剂中存在没食子酸、芦丁、鞣花酸和欧前胡素。Cologrit治疗通过调节NFκB活性、IL-6产生以及NFκB、IL-1β、IL-8和CXCL5 mRNA表达水平，降低了LPS诱导的转化THP-1巨噬细胞和TNF-α刺激的人结肠直肠（HT-29）细胞中的炎症。Cologrit还减少了人单核细胞（U937）细胞与HT29细胞的粘附。肠溶Cologrit片（EC）的甲基丙烯酸-丙烯酸乙酯共聚物包衣有助于其溶解，并在模拟胃肠道消化模型中在小肠pH 7.0环境中释放植物化学物质。小肠EC消化物有效减轻了葡聚糖硫酸钠（2.5%/）诱导的人结肠上皮Caco-2细胞的细胞活力丧失和氧化应激。总之，肠溶包衣的Cologrit片表现出良好的小肠特异性植物化学物质递送能力，并通过调节TNF-α/NFκB/IL6信号轴降低了UC样炎症和氧化应激。
