Perindopril alleviates inflammation via Cyclooxygenase inhibition: a bioinformatics, in vitro and in vivo evaluation
Background and Objective: Perindopril (PER), an angiotensin-converting enzyme (ACE) inhibitor with anti-apoptotic, antioxidant and anti-inflammatory characteristics, has long been used to treat cardiovascular illnesses. In this study, the enzyme inhibitory activity of PER against Cyclooxygenase-1 (C...
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| Main Authors: | , , , , , , , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
2023
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| In: |
International journal of pharmacology
Year: 2023, Volume: 19, Issue: 3, Pages: 428-438 |
| ISSN: | 1812-5700 |
| DOI: | 10.3923/ijp.2023.428.438 |
| Online Access: | Verlag, kostenfrei, Volltext: https://doi.org/10.3923/ijp.2023.428.438 Verlag, kostenfrei, Volltext: https://www.scialert.net/abstract/?doi=ijp.2023.428.438 
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| Author Notes: | Mahmoud El Sebaei, Mohamed Karam Zabady, Ibrahim Ghonim, Abdulrahman Taha Hereba, Ahmed Meligy Abdelghany, Sabry Mohamed El-Bahr, Mohamed Mahmoud Salem Gaballa and Mahmoud Kandeel |
| Summary: | Background and Objective: Perindopril (PER), an angiotensin-converting enzyme (ACE) inhibitor with anti-apoptotic, antioxidant and anti-inflammatory characteristics, has long been used to treat cardiovascular illnesses. In this study, the enzyme inhibitory activity of PER against Cyclooxygenase-1 (COX-1) and Cyclooxygenase-2 (COX-2) was determined. Materials and Methods: The PERʼs anti-inflammatory actions were estimated by in vitro COX-1 and COX-2 inhibition assays, the in vivo rat model of carrageenan-induced paw edema, histopathological examination, molecular modeling, docking and molecular dynamics studies. The data were analyzed using the Analysis of Variance (ANOVA) Test. Results: The PER IC50 values for COX-1 and COX-2 were calculated to be 8.3 and 0.1 µM, respectively, showing that PER has an 85.5-fold higher affinity for COX-2 than for COX-1. The PER was found to be a moderate inflammation suppressor in rat paw assay, comparable to celecoxib and indomethacin. Docking and molecular dynamics (MD) simulation supported the stable binding of PER with COX-2. Conclusion: Current findings revealed that PER can be used for local acute inflammation and utilized as a substitute for other topical anti-inflammatory medicines, particularly those containing steroids. |
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| Item Description: | Gesehen am 09.09.2024 |
| Physical Description: | Online Resource |
| ISSN: | 1812-5700 |
| DOI: | 10.3923/ijp.2023.428.438 |