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基于体外筛选和实验性结肠炎小鼠模型体内评价的溃疡性结肠炎草药配方的制备。

Preparation of Herbal Formulation for Inflammatory Bowel Disease Based on In Vitro Screening and In Vivo Evaluation in a Mouse Model of Experimental Colitis.

机构信息

College of Korean Medicine, Gachon University, Seongnam-si, Gyeonggi-do 13120, Korea.

New Drug Research Team, Kolmar, Korea Co. Ltd., Sandan-gil, Jeonui-myeon, Sejong-si 30003, Korea.

出版信息

Molecules. 2019 Jan 28;24(3):464. doi: 10.3390/molecules24030464.

DOI:10.3390/molecules24030464
PMID:30696085
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6384830/
Abstract

Many medicinal plants have been used traditionally in East Asia for the treatment of gastrointestinal disease and inflammation. The aim of this study was to evaluate the anti-inflammatory activity of 350 extracts (175 water extracts and 175 ethanol extracts) from 71 single plants, 97 mixtures of two plants, and seven formulations based on traditional medicine, to find herbal formulations to treat inflammatory bowel disease (IBD). In the in vitro screening, nitric oxide (NO), tumor necrosis factor (TNF)-α, and interleukin (IL)-6 levels were determined in LPS-treated RAW264.7 cells and the TNF-α induced monocyte-epithelial cell adhesion assay was used for the evaluation of the anti-inflammatory activity of the compounds. Dextran sulfate sodium (DSS)-induced colitis model and 2,4,6-trinitrobenzene sulfonic acid (TNBS)-induced colitis model were used to evaluate the therapeutic effect against IBD of the samples selected from the in vitro screening. KM1608, composed of and Aucklandia lappa, was prepared based on the screening experiments. The oral administration of KM1608 significantly attenuated the severity of colitis symptoms, such as weight loss, diarrhea, and rectal bleeding, in TNBS-induced colitis. In addition, inflammatory mediators, such as myeloperoxidase, TNF-α, and IL-6 levels decreased in the lysate of colon tissues treated with KM1608. Collectively, KM1608 ameliorated colitis through the regulation of inflammatory responses within the colon, which indicated that KM1608 had potential for the treatment of IBD.

摘要

许多药用植物在东亚传统上被用于治疗胃肠道疾病和炎症。本研究旨在评估 71 种单味植物、97 种两味植物混合物和 7 种基于传统医学的配方的 350 种提取物(175 种水提取物和 175 种乙醇提取物)的抗炎活性,以寻找治疗炎症性肠病(IBD)的草药配方。在体外筛选中,测定了 LPS 处理的 RAW264.7 细胞中的一氧化氮(NO)、肿瘤坏死因子(TNF)-α 和白细胞介素(IL)-6 水平,并使用 TNF-α 诱导的单核细胞-上皮细胞黏附试验评估化合物的抗炎活性。葡聚糖硫酸钠(DSS)诱导的结肠炎模型和 2,4,6-三硝基苯磺酸(TNBS)诱导的结肠炎模型用于评估从体外筛选中选择的样品对 IBD 的治疗效果。基于筛选实验,制备了由 和木香组成的 KM1608。KM1608 的口服给药显著减轻了 TNBS 诱导的结肠炎中体重减轻、腹泻和直肠出血等结肠炎症状的严重程度。此外,KM1608 处理的结肠组织裂解物中的炎症介质,如髓过氧化物酶、TNF-α 和 IL-6 水平降低。总之,KM1608 通过调节结肠内的炎症反应改善了结肠炎,表明 KM1608 具有治疗 IBD 的潜力。

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