Anti-inflammatory effect of a new piperazine derivative: (4-methylpiperazin-1-yl)(1-phenyl-1H-pyrazol-4-yl)methanone

Batista, Daniel da Costa; Silva, Daiany Priscilla Bueno da; Florentino, Iziara Ferreira; Cardoso, Carina Sofia; Gonçalves, Merita Pereira; Valadares, Marize Campos; Liao, Luciano Morais; Sanz Lobón, Germán; Vaz, Boniek Gontijo; Costa, Elson Alves; Menegatti, Ricardo

Anti-inflammatory effect of a new piperazine derivative: (4-methylpiperazin-1-yl)(1-phenyl-1H-pyrazol-4-yl)methanone

Data

2017

Autores

Batista, Daniel da Costa

Silva, Daiany Priscilla Bueno da

Florentino, Iziara Ferreira

Cardoso, Carina Sofia

Gonçalves, Merita Pereira

Valadares, Marize Campos

Resumo

Aims This study investigates the anti-nociceptive and anti-inflammatory effects of new piperazine compound (LQFM182) as well as the toxicity acute in vitro. Main methods To evaluate the anti-nociceptive activity, the acetic acid-induced abdominal writhing test, tail flick test and formalin-induced pain test were used. The anti-inflammatory activity was evaluated using the models of paw oedema and pleurisy induced by carrageenan and some inflammatory parameters were evaluated, including cell migration, myeloperoxidase enzyme activity and the levels of TNF-α and IL-1β cytokines in pleural exudate. The acute oral systemic toxicity of LQFM182 in mice was evaluated through the neutral red uptake (nru) assay. Key findings LQFM182 (50, 100 or 200 mg/kg, p.o.) decreased the number of writhings induced by acetic acid in a dose-dependent manner, and an intermediate dose (100 mg/kg, p.o.) reduced the paw licking time of animals in the second phase of the formalin test. Furthermore, LQFM182 (100 mg/kg, p.o.) reduced oedema formation at all hours of the paw oedema induced by carrageenan test and in pleurisy test reduced cell migration from the reduction of polymorphonuclear cells, myeloperoxidase enzyme activity and the levels of pro-inflammatory cytokines IL-1β and TNF-α. Therefore, it was classified in GHS category 300 < LD50 < 2000 mg/kg.

Palavras-chave

Anti-inflammatory, N-arylheterocycles, IL-1β, TNF-α

Citação

BATISTA, Daniel C. et al. Anti-inflammatory effect of a new piperazine derivative: (4-methylpiperazin-1-yl)(1-phenyl-1H-pyrazol-4-yl)methanone. Inflammopharmacology, London, v. 26, p. 217-226, 2018. DOI: 10.1007/s10787-017-0390-8. Disponível em: https://link.springer.com/article/10.1007/s10787-017-0390-8. Acesso em: 28 jun. 2023.