本研究旨在研究合成治疗剂更好地管理疼痛和炎症的潜力,表现出最小到不存在的溃疡效应。通过小鼠伤害性感受和抗炎活性模型系统评估1-(2-氯苯甲酰基)-3-(2,3-二氯苯基)硫脲的作用。此外,使用NSAID诱导的幽门结扎模型评估大鼠的溃疡形成潜能,其次是组织病理学和生化分析。测试是在八组白化病大鼠上进行的,包括I组(生理盐水),II组和III组(阿司匹林®剂量为100mg/kg和150mg/kg,分别),IV和V组(吲哚美辛的剂量为100mg/kg和150mg/kg,分别),和第六组,VII,和VIII(15mg/kg的铅化合物,30mg/kg和45mg/kg剂量,分别)。此外,进行分子对接分析以预测潜在的分子靶位点相互作用.结果表明,铅化合物,以15、30和45mg/kg的剂量给药,显著减少了化学和热诱发的伤害性疼痛,与阿司匹林®和曲马多观察到的水平一致。该化合物还有效抑制角叉菜胶诱导的爪水肿模型中的炎症反应。至于致溃疡的作用,与阿司匹林®和吲哚美辛组相比,化合物组没有明显的变化,显示溃疡评分大幅增加,总酸度,游离酸度,和胃液量,胃液pH值下降。总之,这些发现表明我们的测试化合物表现出有效的抗伤害感受,抗炎特性,缺乏致溃疡作用。
The current study was designed to investigate the potential of a synthetic therapeutic agent for better management of pain and inflammation, exhibiting minimal to non-existent ulcerogenic effects. The effect of 1-(2-chlorobenzoyl)-3-(2,3-dichlorophenyl) thiourea was assessed through model systems of
nociception and anti-inflammatory activities in mice. In addition, the ulcerogenic potential was evaluated in rats using the NSAID-induced pyloric ligation model, followed by histopathological and biochemical analysis. The test was conducted on eight groups of albino rats, comprising of group I (normal saline), groups II and III (aspirin® at doses of 100 mg/kg and 150 mg/kg, respectively), groups IV and V (indomethacin at doses of 100 mg/kg and 150 mg/kg, respectively), and groups VI, VII, and VIII (lead-compound at 15 mg/kg, 30 mg/kg and 45 mg/kg doses, respectively). Furthermore, molecular docking analyses were performed to predict potential molecular target site interactions. The results showed that the lead-compound, administered at doses of 15, 30, and 45 mg/kg, yielded significant reductions in chemically and thermally induced nociceptive pain, aligning with the levels observed for aspirin® and tramadol. The compound also effectively suppressed inflammatory response in the carrageenan-induced paw edema model. As for the ulcerogenic effects, the compound groups displayed no considerable alterations compared to the aspirin® and indomethacin groups, which displayed substantial increases in ulcer scores, total acidity, free acidity, and gastric juice volume, and a decrease in gastric juice pH. In conclusion, these findings suggest that our test compound exhibits potent antinociceptive, anti-inflammatory properties and is devoid of ulcerogenic effects.