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Therapeutic potential of isobavachalcone, a natural flavonoid, in murine experimental colitis by inhibiting NF-κB p65
Zhou, Yishan1; Zhong, Bingling2; Min, Xiangjing1; Hou, Ying2; Lin, Ligen2,3; Wu, Qin1; Shi, Jingshan1; Chen, Xiuping2,3
2021-10-01
Source PublicationPhytotherapy Research
ISSN0951-418X
Volume35Issue:10Pages:5861-5870
Abstract

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

KeywordInflammation Isobavachalcone Nf-κb P65 Ulcerative Colitis
DOI10.1002/ptr.7246
URLView the original
Indexed BySCIE
Language英語English
WOS Research AreaPharmacology & Pharmacy
WOS SubjectChemistry, Medicinal ; Pharmacology & Pharmacy
WOS IDWOS:000688268600001
Scopus ID2-s2.0-85113393900
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Cited Times [WOS]:5   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Corresponding AuthorChen, Xiuping
Affiliation1.Key Lab for Pharmacology of Ministry of Education, Department of Pharmacology, Zunyi Medical University, Zunyi, China
2.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao
3.Department of Pharmaceutical Sciences, Faculty of Health Sciences, University of Macau, Macao
Corresponding Author AffilicationInstitute of Chinese Medical Sciences;  Faculty of Health Sciences
Recommended Citation
GB/T 7714
Zhou, Yishan,Zhong, Bingling,Min, Xiangjing,et al. Therapeutic potential of isobavachalcone, a natural flavonoid, in murine experimental colitis by inhibiting NF-κB p65[J]. Phytotherapy Research,2021,35(10):5861-5870.
APA Zhou, Yishan,Zhong, Bingling,Min, Xiangjing,Hou, Ying,Lin, Ligen,Wu, Qin,Shi, Jingshan,&Chen, Xiuping.(2021).Therapeutic potential of isobavachalcone, a natural flavonoid, in murine experimental colitis by inhibiting NF-κB p65.Phytotherapy Research,35(10),5861-5870.
MLA Zhou, Yishan,et al."Therapeutic potential of isobavachalcone, a natural flavonoid, in murine experimental colitis by inhibiting NF-κB p65".Phytotherapy Research 35.10(2021):5861-5870.
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