Therapeutic potential of isobavachalcone, a natural flavonoid, in murine experimental colitis by inhibiting NF‐κB p65

• DOI: 10.1002/ptr.7246
• Publication Date: 2021-08-26T05:27:46Z
• Authors: Yishan Zhou; Bingling Zhong; Xiangjing Min; Ying Hou; Ligen Lin; Qin Wu; Jingshan Shi; Xiuping Chen
• Keywords: Flavonoids; 0301 basic medicine; Dextran Sulfate; NF-kappa B; Colitis; 3. Good health; Molecular Docking Simulation; Mice; 03 medical and health sciences; Chalcones; Animals; Cytokines; Colitis, Ulcerative; Signal Transduction

The incidence of ulcerative colitis (UC), one the two types inflammatory bowel disease, is increasing in many countries. Various natural products have been demonstrated with therapeutic potentials for UC. Herein, effects and mechanisms isobavachalcone (IBC), a chalcone, were evaluated dextran sulfate sodium (DSS)-induced mice lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. results that IBC treatment significantly improved clinical symptoms, assessed by disease activity index (DAI) scores histological changes colon. levels myeloperoxidase (MPO), TNF-α, IL-6, IL-1β, prostaglandin E2 (PGE2) colon tissues suppressed IBC. upregulation inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), NF-κB p65 reversed as well. Furthermore, inhibited LPS-triggered secretion nitrite, nuclear translocation p65, cells. luciferase reporter assay indicated transcription toll-like receptor 4 (TLR4). Molecular docking showed binding pocket was adjacent to Ser276 p65-p50 heterodimer could form H-bond Thr191. Collectively, these ameliorated possibly through inhibition p65.