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Screening Active Constituents for Anti-Ulcerative Colitis: In silico, In vitro and In vivo ˗ Taking Turkish galls for example

Abstract

Turkish galls has been reported to exhibit beneficial remedy effects in ulcerative colitis (UC). However, the active constituents of Turkish galls for the treatment of UC remain vague. The purpose of this study is to screen anti-inflammatory active constituents and clarify its associated molecular mechanisms. Here, systems pharmacology was introduced to predict relationship between constituents and corresponding targets as well as pathways. In addition, mass spectrometry guided preparative chromatography technique was inducted for preparing constituents to compare the anti-inflammatory activities and the therapeutic efficacy of UC. In silico, active constituents exhibited a beneficial effect on UC might through hitting on multiple targets and regulating multiple pathways, meanwhile these targets were mainly involved in NF-κB pathway which was selected to verify. In vitro, 5 categories of constituents were screened out as active constituents by comparing the cytotoxicity and detecting the level of the pro-inflammatory factors of 9 category constituents. In vivo, dextran sulfate sodium (DSS)-induced UC was significantly ameliorated in active constituents-fed mice. The results indicated that active fraction including methyl gallate, digallic acid and di-O-galloyl-β-D-glucose, tri-O-galloyl-β-D-glucose was considered as the major contribution for the treatment of UC. Moreover, active fraction could also inhibit the phosphorylation level of IKKβ, thereby inhibiting the downstream of NF-κB signaling pathway. The approach developed in this work not merely clarified the anti-inflammation effect of Turkish galls but also provided a beneficial reference for the discovery of material basis and functional mechanism of herbal medicine.

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Supplementary files

Publication details

The article was received on 19 Jul 2018, accepted on 09 Sep 2018 and first published on 12 Sep 2018


Article type: Paper
DOI: 10.1039/C8FO01439F
Citation: Food Funct., 2018, Accepted Manuscript
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    Screening Active Constituents for Anti-Ulcerative Colitis: In silico, In vitro and In vivo ˗ Taking Turkish galls for example

    B. Han, J. Zang, S. Ma, C. Wang, G. Guo, L. Zhou, X. Tian, M. Lv and J. Zhang, Food Funct., 2018, Accepted Manuscript , DOI: 10.1039/C8FO01439F

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