{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,14]],"date-time":"2026-07-14T05:23:42Z","timestamp":1784006622788,"version":"3.55.0"},"reference-count":28,"publisher":"Frontiers Media SA","license":[{"start":{"date-parts":[[2024,10,29]],"date-time":"2024-10-29T00:00:00Z","timestamp":1730160000000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":["frontiersin.org"],"crossmark-restriction":true},"short-container-title":["Front. Pharmacol."],"abstract":"<jats:p>A series of <jats:italic>para<\/jats:italic>-quinone methide derivatives were evaluated their anti-inflammatory activity. Through the screening of the lipopolysaccharide (LPS)-induced inflammatory cell model in Raw264.7 cells, it was found that the inhibitory activity of <jats:italic>meta<\/jats:italic>-substituted derivatives on NO production was superior to that of <jats:italic>ortho<\/jats:italic>- and <jats:italic>para<\/jats:italic>-substituted derivatives. Among them, in the inflammatory cell model, the <jats:italic>meta<\/jats:italic>-trifluoromethyl substituted <jats:italic>para<\/jats:italic>-quinone methide derivative <jats:bold>1i<\/jats:bold> had the best activity in inhibiting LPS-induced excess generation of NO. And <jats:bold>1i<\/jats:bold> could effectively inhibit the increase of ROS in inflammatory cells, the expression of iNOS related to the production of NO, and the expressions of inflammation related initiating protein TLR4, pro-inflammatory cytokines IL-6 and TNF-\u03b1, inflammasome NLRP3 and Caspase1. In the dextran sulfate sodium (DSS)-induced ulcerative colitis (UC) mouse model, the active derivative <jats:bold>1i<\/jats:bold> could inhibit DSS-induced colon shortening, and reverse DSS-induced pathological changes in colon tissue, such as inflammatory infiltration, structural destruction and crypt disappearance. <jats:bold>1i<\/jats:bold> could effectively inhibit oxidative stress, inflammation and apoptosis in UC mice. Moreover, through the determination of serum biochemical indicators, tissue pathologies and tissue organ indexes, <jats:bold>1i<\/jats:bold> could effectively reverse the damage to mouse liver and kidney caused by DSS, playing a protective role in liver and kidney of mice. In summary, <jats:bold>1i<\/jats:bold> was an effective anti-inflammatory reagent and could be developed as a potential drug for anti-UC.<\/jats:p>","DOI":"10.3389\/fphar.2024.1474678","type":"journal-article","created":{"date-parts":[[2024,10,29]],"date-time":"2024-10-29T04:51:26Z","timestamp":1730177486000},"update-policy":"https:\/\/doi.org\/10.3389\/crossmark-policy","source":"Crossref","is-referenced-by-count":5,"title":["Anti-inflammatory effects of para-quinone methide derivatives on ulcerative colitis"],"prefix":"10.3389","volume":"15","author":[{"given":"Yue","family":"Qiu","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xin","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xu","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiaotong","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xuekun","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jie","family":"Yang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Guoyun","family":"Liu","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1965","published-online":{"date-parts":[[2024,10,29]]},"reference":[{"key":"B1","doi-asserted-by":"publisher","first-page":"1341","DOI":"10.1016\/s0278-5846(01)00192-0","article-title":"Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer\u2019s disease","volume":"25","author":"Allison","year":"2001","journal-title":"Prog. 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