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Information Journal Paper

Title

Computational and pharmacological investigation of novel 1, 5-diaryl-1, 4-pentadien-3-one derivatives for analgesic, antiinflammatory and anticancer potential

Pages

  72-79

Abstract

 Objective(s): The novel 1, 5-diaryl-1, 4-pentadien-3-one derivatives were studied for Analgesic, antiinflammatory and Anticancer potential to establish their role in pain, inflammatory disorders and cancer. Materials and Methods: Two 1, 5-diaryl-1, 4-pentadien-3-one derivatives: (1E, 4E)-5-(4-fluoro phenyl)-1-(4-methoxyphenyl)-2-methylpenta-1, 4-dien-3-one (A2K2A17) and (1E, 4E)-5-(4-nitrophenyl)-1-(4-nitrophenyl)-2-ethylhexa-1, 4-dien-3-one (A11K3A11) were synthesized and characterized via 1H NMR and 13C NMR techniques. Molecular docking, Anti-inflammatory, Analgesic and Anticancer activities were performed using Auto Doc Vina, carrageenan mediated paw edema and formalin induced chronic inflammation, acetic acid induced writhings and hotplate assay and brine-shrimp lethality assay. Results: A2K2A17 and A11K3A11 showed high computational affinities (binding energy >-9. 0 Kcal/ mol) against COX-1, kappa receptor and braf kinase domain. A2K2A17 and A11K3A11 exhibited moderate docking affinities (binding energy >-8. 0 Kcal/mol) against COX-2, human capsaicin receptor, tumor necrosis factor, lipoxygenase, colony stimulating factor, delta receptor, cyclin dependent protein kinase-2, mitogen activated kinase, mu receptor and kit kinase domain. A2K2A17 and A11K3A11 possess low docking affinities (binding energy >-7. 0 Kcal/mol) against purinoceptor, plateletsderived growth Factor-1 and vascular-endothelial growth factor. In Analgesic activity, A2K2A17 (1-30 mg/kg) and A11K3A11 (1-10 mg/kg) decreased acetic acid induced writhes and prolonged the latency time (P<0. 01, P<0. 001 vs saline group) respectively. A2K2A17 (10-30 mg/kg) and A11K3A11 (1-10 mg/kg) reduced carrageenan as well as formalin mediated edema (P<0. 01, P<0. 001). A2K2A17 found effective for cytotoxicity assay with LC50 value 1. 5 μ g/ml. Conclusion: The in silico, in vitro and in vivo studies on A2K2A17 and A11K3A11 reports their computational binding affinities against targets as well as the Analgesic, Anti-inflammatory and the Anticancer effects.

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    Cite

    APA: Copy

    Tariq, Muhammad Sheraz, Khan, Arif ullah, Minhas, Amber Mahmood, Filho, Edson Rodrigues, Din, Zia ud, & Khan, Aslam. (2019). Computational and pharmacological investigation of novel 1, 5-diaryl-1, 4-pentadien-3-one derivatives for analgesic, antiinflammatory and anticancer potential. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 22(1), 72-79. SID. https://sid.ir/paper/721783/en

    Vancouver: Copy

    Tariq Muhammad Sheraz, Khan Arif ullah, Minhas Amber Mahmood, Filho Edson Rodrigues, Din Zia ud, Khan Aslam. Computational and pharmacological investigation of novel 1, 5-diaryl-1, 4-pentadien-3-one derivatives for analgesic, antiinflammatory and anticancer potential. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES[Internet]. 2019;22(1):72-79. Available from: https://sid.ir/paper/721783/en

    IEEE: Copy

    Muhammad Sheraz Tariq, Arif ullah Khan, Amber Mahmood Minhas, Edson Rodrigues Filho, Zia ud Din, and Aslam Khan, “Computational and pharmacological investigation of novel 1, 5-diaryl-1, 4-pentadien-3-one derivatives for analgesic, antiinflammatory and anticancer potential,” IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, vol. 22, no. 1, pp. 72–79, 2019, [Online]. Available: https://sid.ir/paper/721783/en

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