PloS one · 2018
LASSBio-1586, an N-acylhydrazone derivative, attenuates nociceptive behavior and the inflammatory response in mice.
СтатьяПоддержка исследования: вне правительства СШАНазвание и аннотация: Перевод в очереди
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Silva Juliane Cabral, Oliveira Júnior Raimundo Gonçalves de, Silva Mariana Gama E, Lavor Érica Martins de, Soares Juliana Mikaelly Dias, Lima-Saraiva Sarah Raquel Gomes de, Diniz Tâmara Coimbra, Mendes Rosemairy Luciane, Alencar Filho Edilson Beserra de, Barreiro Eliezer Jesus de Lacerda, Lima Lídia Moreira, Almeida Jackson Roberto Guedes da Silva
Аннотация
Pain and inflammation are complex clinical conditions that are present in a wide variety of disorders. Most drugs used to treat pain and inflammation have potential side effects, which makes it necessary to search for new sources of bioactive molecules. In this paper, we describe the ability of LASSBio-1586, an N-acylhydrazone derivative, to attenuate nociceptive behavior and the inflammatory response in mice. Antinociceptive activity was evaluated through acetic acid-induced writhing and formalin-induced nociception tests. In these experimental models, LASSBio-1586 significantly (p<0.05) reduced nociceptive behavior. Several methods of acute and chronic inflammation induced by different chemical (carrageenan, histamine, croton oil, arachidonic acid) and physical (cotton pellet) agents were used to evaluate the anti-inflammatory effect of LASSBio-1586. LASSBio-1586 exhibited potent anti-inflammatory activity in all tests (p<0.05). Study of the mechanism of action demonstrated the possible involvement of the nitrergic, serotonergic and histamine signaling pathways. In addition, a molecular docking study was performed, indicating that LASSBio-1586 is able to block the COX-2 enzyme, reducing arachidonic acid metabolism and consequently decreasing the production of prostaglandins, which are important inflammatory mediators. In summary, LASSBio-1586 exhibited relevant antinociceptive and anti-inflammatory potential and acted on several targets, making it a candidate for a new multi-target oral anti-inflammatory drug.
Предметные рубрики MeSH
Acetic AcidAnalgesicsAnimalsAnti-Inflammatory Agents, Non-SteroidalArachidonic AcidCarrageenanCroton OilCyclooxygenase 2Cyclooxygenase 2 InhibitorsDexamethasoneDisease Models, AnimalEdemaFormaldehydeHindlimbHistamineHydrazonesIndomethacinInflammationMaleMiceMolecular Docking SimulationNG-Nitroarginine Methyl EsterNociceptionNociceptive PainOndansetronProstaglandins