In vivo effects of a selected thiourea derivative 1-(2-chlorobenzoyl)-3-(2,3-dichlorophenyl) against nociception, inflammation and gastric ulcerogenicity: Biochemical, histopathological and in silico approaches - 27/04/24
Abstract |
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.
Le texte complet de cet article est disponible en PDF.Highlights |
• | A selected synthetic compound, 1-(2-chlorobenzoyl)-3-(2,3-dichlorophenyl) thiourea, was tested in vivo and in silico. |
• | 1-(2-chlorobenzoyl)-3-(2,3-dichlorophenyl) thiourea significantly inhibited chemically and thermally induced nociceptive pain. |
• | The results of the ulcerogenic study suggest that the test compound has a much lower propensity to induce gastric ulcers. |
• | Docking studies indicated noteworthy interactions between the test compound and target receptors. |
• | The test compound may possess therapeutic effectiveness in treating pain and inflammation without inducing ulcerogenicity. |
Abbreviations : BSA, COX, GABA, GI, MOE, NaOH, NSAIDs, PDB, PTZ, RMSD, SAIDs, TCA
Keywords : 1-(2-chlorobenzoyl)-3-(2,3-dichlorophenyl) thiourea, Inflammation, Nociception, NSAIDs, Ulcer
Plan
Vol 174
Article 116544- mai 2024 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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