The aim of this study was to synthesise the novel di-tert-butylphenol compound, 5-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-thioxo-dihydropyrimidine-4,6(1H, 5H)-dione (LQFM218), and evaluate the potential anti-nociceptive and anti-inflammatory activities in acute (mice) models in vivo. The compound was tested on acute models of pain such as acetic acid-induced abdominal writhing, formalin-induced nociception and carrageenan-induced mechanical hyperalgesia. The anti-inflammatory activity was observed in paw oedema, carrageenan-induced pleurisy tests and inflammatory mediator quantification. Key findings: oral treatment with the LQFM218 (50, 100 or 200 mg/kg) reduced abdominal writhing (18.8%, 31.6% and 48.3%). The dose intermediate (100 mg/kg) reduced the nociception in the second phase of the formalin test (61.4%), and also showed anti-hyperalgic activity in carrageenan-induced mechanical hyperalgesia (until 42.3%). In acute inflammation models, the treatment of mice LQFM218 (100 mg/kg) reduced the paw oedema all the time (33.8%, 42.6%, 37.4% and 36%) and in pleurisy test reduced: polymorphonuclear cell migration (35.4%), myeloperoxidase activity (52.2%) and the levels of inflammatory mediators such as PGE₂ (23.0%), TNF-α (67.6%) and IL-1β (53.4%). The present study showed that LQFM218 effectively reduced the nociception and inflammation in different models, and its mechanism might be related to the reduction of PGE₂ and pro-inflammatory cytokines. These findings show LQFM218 as a potential anti-inflammatory drug.

这项研究的目的是合成新型的二叔丁基苯酚化合物5-（3,5-二叔丁基-4-羟基亚苄基）-2-硫代-二氢嘧啶-4,6（1H，5H）- Dione（LQFM218），并评估体内急性（小鼠）模型中潜在的抗伤害性和抗炎活性。在急性疼痛模型上测试了该化合物，例如乙酸引起的腹部扭动，福尔马林引起的伤害感受和角叉菜胶引起的机械性痛觉过敏。在爪水肿，角叉菜胶诱发的胸膜炎试验和炎症介质定量观察到抗炎活性。主要发现：口服LQFM218（50、100或200 mg / kg）可以减轻腹部扭伤（18.8％，31.6％和48.3％）。中间剂量（100 mg / kg）在福尔马林试验的第二阶段降低了伤害感受（61.4％），并且在角叉菜胶诱导的机械性痛觉过敏中也显示出抗痛觉过敏的活性（直至42.3％）。在急性炎症模型中，小鼠LQFM218（100 mg / kg）的治疗始终减轻爪水肿（33.8％，42.6％，37.4％和36％），而在胸膜炎试验中减轻：多形核细胞迁移（35.4％），₂（23.0％），TNF-α（67.6％）和IL-1β（53.4％）。本研究表明，LQFM218能有效减轻不同模型的伤害感受和炎症反应，其机制可能与降低PGE ₂和促炎细胞因子有关。这些发现表明LQFM218是一种潜在的抗炎药。