Anti-inflammatory and antinociceptive activity profile of a new lead compound – LQFM219

Galvão, Gustavo Mota; Florentino, Iziara Ferreira; Sanz Lobón, Germán; Vaz, Boniek Gontijo; Liao, Luciano Morais; Sabino, José Ricardo; Cardoso, Cariina Sofia; Silva, Daiany Priscilla Bueno da; Costa, Elson Alves; Silva, Andreia Luiza Pereira; Silva, Artur Christian Garcia da; Valadares, Marize Campos; Leite, Jacqueline Alves; Gil, Eric de Souza; Menegatti, Ricardo

Anti-inflammatory and antinociceptive activity profile of a new lead compound – LQFM219

Data

2020

Autores

Galvão, Gustavo Mota

Florentino, Iziara Ferreira

Cardoso, Cariina Sofia

Silva, Daiany Priscilla Bueno da

Costa, Elson Alves

Silva, Andreia Luiza Pereira

Resumo

LQFM219 is a molecule designed from celecoxibe (COX-2 inhibitor) and darbufelone (inhibitor of COX-2 and 5-LOX) lead compounds through a molecular hybridisation strategy. Therefore, this work aimed to investigate the antinociceptive and anti-inflammatory activities of this new hybrid compound. The acute oral systemic toxicity of LQFM219 was evaluated via the neutral red uptake assay. Acetic acid-induced abdominal writhing and CFA-induced mechanical hyperalgesia were performed to evaluate the antinociceptive activity, and the anti-oedematogenic activity was studied by CFA-induced paw oedema and croton oil-induced ear oedema. Moreover, the acute anti-inflammatory activity was determined by carrageenan-induced pleurisy. In addition, cell migration, myeloperoxidase enzyme activity, and TNF-α and IL-1β levels were determined in pleural exudate. Moreover, a redox assay was conducted using electroanalytical and DPPH methods. The results demonstrated that LQFM219 was classified as GHS category 4, and it showed better free radical scavenger activity compared to BHT. Besides, LQFM219 decreased the number of writhings induced by acetic acid and the response to the mechanical stimulus in the CFA-induced mechanical hyperalgesia test. Furthermore, LQFM219 reduced oedema formation, cell migration, and IL-1β and TNF-α levels in the pleural cavity and inhibited myeloperoxidase enzyme activity. Thus, our study provides that the new pyrazole derivative, LQFM219, demonstrated low toxicity, antinociceptive and anti-inflammatory potential in vitro and in vivo.

Citação

GALVÃO, Gustavo M. et al. Anti-inflammatory and antinociceptive activity profile of a new lead compound - LQFM289. International Immunopharmacology, Amsterdam, v. 88, e106893, 2020. DOI: 10.1016/j.intimp.2020.106893. Disponível em: https://www.sciencedirect.com/science/article/abs/pii/S1567576920323493?via%3Dihub. Acesso em: 28 jun. 2023.