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吡唑衍生物通过靶向p38丝裂原活化蛋白激酶和环氧化酶-2改善胶原诱导的关节炎小鼠模型中的滑膜炎症。

Pyrazole derivatives ameliorate synovial inflammation in collagen-induced arthritis mice model via targeting p38 MAPK and COX-2.

作者信息

Abdallah Ahlam M, Naiem Amany H Abdel, Abdelraheim Salama R, Mohafez Omar M, Abdelghany Hend M, Elsayed Sahar A, Gomaa Wafaey, Marey Heba

机构信息

Department of Medical Biochemistry, Faculty of Medicine, Minia University, Minia, 61511, Egypt.

Department of Biochemistry, Faculty of Pharmacy, Al-Azhar University, Assiut Branch, Assiut, 71524, Egypt.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2025 Jan;398(1):819-832. doi: 10.1007/s00210-024-03290-6. Epub 2024 Jul 29.

Abstract

The type II collagen-induced arthritis (CIA) model and human rheumatoid arthritis exhibit similar characteristics. Both diseases involve the production of inflammatory cytokines and other mediators, triggering an inflammatory cascade linked to bone and cartilage damage. Recently, new pyrazole compounds with various pharmacological activities, including antimicrobial, anticancer, anti-inflammatory, and analgesic agents, have been reported. Our aim is to evaluate the therapeutic effectiveness of two newly synthesized pyrazole derivatives, M1E and M1G, in reducing inflammation and oxidative stress in a mouse model of collagen-induced arthritis. Arthritis was induced in DBA/1J mice, and the therapeutic effect of the M1E and M1G is assessed by measuring the arthritic index, quantifying the expression of inflammatory genes such as p38 MAPK, COX-2, IL1β, MMP3, and TNF-α using real-time PCR and analyzing protein expression using western blotting for phosphorylated p38 MAPK and COX-2. Oxidative stress markers and hind paws joint histopathology were also evaluated. Treatment with the two pyrazole derivatives significantly (p < 0.001) improved the arthritic score; downregulated the expression of inflammatory genes p38 MAPK, COX-2, IL1β, MMP3, and TNF-α; and reduced the protein expression of phosphorylated p3  MAPK and COX-2. In addition, both compounds ameliorated oxidative stress by increasing the activities of SOD and reducing the formation of MDA in the paw tissue homogenates. Both M1E and M1G significantly (p < 0.001) improved the pathological features of synovitis. The pyrazole derivatives, M1E and M1G, significantly reduced the arthritic score and the inflammatory cytokine expression, improved synovitis histopathology, and ameliorated oxidative stress in the CIA mice model.

摘要

II型胶原诱导性关节炎(CIA)模型与人类类风湿性关节炎具有相似的特征。这两种疾病都涉及炎性细胞因子和其他介质的产生,引发与骨和软骨损伤相关的炎症级联反应。最近,已报道了具有多种药理活性的新型吡唑化合物,包括抗菌、抗癌、抗炎和镇痛剂。我们的目的是评估两种新合成的吡唑衍生物M1E和M1G在胶原诱导性关节炎小鼠模型中减轻炎症和氧化应激的治疗效果。在DBA/1J小鼠中诱导关节炎,并通过测量关节炎指数、使用实时PCR定量炎性基因如p38 MAPK、COX-2、IL1β、MMP3和TNF-α的表达以及使用蛋白质印迹法分析磷酸化p38 MAPK和COX-2的蛋白表达来评估M1E和M1G的治疗效果。还评估了氧化应激标志物和后爪关节组织病理学。用这两种吡唑衍生物治疗显著(p < 0.001)改善了关节炎评分;下调了炎性基因p38 MAPK、COX-2、IL1β、MMP3和TNF-α的表达;并降低了磷酸化p3 MAPK和COX-2的蛋白表达。此外,两种化合物都通过增加SOD活性和减少爪组织匀浆中MDA的形成来改善氧化应激。M1E和M1G均显著(p < 0.001)改善了滑膜炎的病理特征。吡唑衍生物M1E和M1G显著降低了CIA小鼠模型中的关节炎评分和炎性细胞因子表达,改善了滑膜炎组织病理学,并减轻了氧化应激。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fc76/11787049/97c13c8e9aec/210_2024_3290_Fig1_HTML.jpg

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