Investigation of anti-inflammatory potential of 5-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-thioxodihydropyrimidine-4,6 (1H,5H)-dione compound
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2020
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The aim of this study was to synthesise the novel di-tert-butylphenol compound, 5-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-thioxo-dihydropyrimidine-4,6(1H, 5H)-dione (LQFM218), and evaluate the potential antinociceptive and anti-inflammatory activities in acute (mice) models in vivo. The compound was tested on
acute models of pain such as acetic acid-induced abdominal writhing, formalin-induced nociception and
carrageenan-induced mechanical hyperalgesia. The anti-inflammatory activity was observed in paw oedema,
carrageenan-induced pleurisy tests and inflammatory mediator quantification. Key findings: oral treatment with
the LQFM218 (50, 100 or 200 mg/kg) reduced abdominal writhing (18.8%, 31.6% and 48.3%). The dose intermediate (100 mg/kg) reduced the nociception in the second phase of the formalin test (61.4%), and also
showed anti-hyperalgic activity in carrageenan-induced mechanical hyperalgesia (until 42.3%). In acute
inflammation models, the treatment of mice LQFM218 (100 mg/kg) reduced the paw oedema all the time
(33.8%, 42.6%, 37.4% and 36%) and in pleurisy test reduced: polymorphonuclear cell migration (35.4%),
myeloperoxidase activity (52.2%) and the levels of inflammatory mediators such as PGE2 (23.0%), TNF-α
(67.6%) and IL-1β (53.4%). The present study showed that LQFM218 effectively reduced the nociception and
inflammation in different models, and its mechanism might be related to the reduction of PGE2 and proinflammatory cytokines. These findings show LQFM218 as a potential anti-inflammatory drug.
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Oedema, Inflammation, Non-steroidal anti-inflammatory drugs, Pain
Citação
ALMEIDA, Dionys de S. et al. Investigation of anti-inflammatory potential of 5-(3,5-di-tert-butyl-4-hydroxybenzylidene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione compound. European Journal of Pharmacology, Amsterdam, v. 886, e173388, 2020.
DOI: 10.1016/j.ejphar.2020.173388. Disponível em: https://www.sciencedirect.com/science/article/pii/S0014299920304805?via%3Dihub. Acesso em: 21 jun. 2023.