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ORIGINAL RESEARCH article

Front. Pharmacol.
Sec. Experimental Pharmacology and Drug Discovery
Volume 15 - 2024 | doi: 10.3389/fphar.2024.1474678

Anti-inflammatory effects of para-quinone methide derivatives on ulcerative colitis

Provisionally accepted
Yue Qiu Yue Qiu *Xin Li Xin Li *Xu Zhang Xu Zhang *Xiaotong Wang Xiaotong Wang *Xuekun Wang Xuekun Wang *Jie Yang Jie Yang *Guoyun Liu Guoyun Liu *
  • Liaocheng University, Liaocheng, China

The final, formatted version of the article will be published soon.

    A series of para-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 meta-substituted derivatives on NO production was superior to that of ortho- and para-substituted derivatives. Among them, in the inflammatory cell model, the meta-trifluoromethyl substituted para-quinone methide derivative 1i had the best activity in inhibiting LPS-induced excess generation of NO. And 1i 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-, inflammasome NLRP3 and Caspase1. In the dextran sulfate sodium (DSS)-induced ulcerative colitis (UC) mouse model, the active derivative 1i could inhibit DSS-induced colon shortening, and reverse DSS-induced pathological changes in colon tissue, such as inflammatory infiltration, structural destruction and crypt disappearance. 1i 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, 1i 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, 1i was an effective anti-inflammatory reagent and could be developed as a potential drug for anti-UC.

    Keywords: anti-inflammatory, ulcerative colitis, para-quinone methides, Oxidative Stress, Apoptosis

    Received: 02 Aug 2024; Accepted: 18 Oct 2024.

    Copyright: © 2024 Qiu, Li, Zhang, Wang, Wang, Yang and Liu. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

    * Correspondence:
    Yue Qiu, Liaocheng University, Liaocheng, China
    Xin Li, Liaocheng University, Liaocheng, China
    Xu Zhang, Liaocheng University, Liaocheng, China
    Xiaotong Wang, Liaocheng University, Liaocheng, China
    Xuekun Wang, Liaocheng University, Liaocheng, China
    Jie Yang, Liaocheng University, Liaocheng, China
    Guoyun Liu, Liaocheng University, Liaocheng, China

    Disclaimer: All claims expressed in this article are solely those of the authors and do not necessarily represent those of their affiliated organizations, or those of the publisher, the editors and the reviewers. Any product that may be evaluated in this article or claim that may be made by its manufacturer is not guaranteed or endorsed by the publisher.