Anti-inflammatory and antinociceptive effects, and safety toxicological profile of a new paracetamol analog, LQFM291

In the scope of a research program with the goal of developing treatments for inflammatory diseases, the pharmacological evaluation of LQFM291, designed by molecular hybridization from butylated hydroxytoluene and paracetamol, was described. The antioxidant profile of LQFM291 was evaluated by electr...

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Veröffentlicht in:Inflammopharmacology 2023-10, Vol.31 (5), p.2451-2465
Hauptverfasser: Turones, Larissa Córdova, Machado, Lucas S., Vaz, Boniek G., de Almeida R. Oliveira, Gerlon, da Silva Moreira, Lorrane Kelle, Almeida, Dionys de Souza, Martins, Aline Nazareth, Fajemiroye, James Oluwagbamigbe, Martins, José Luís R., Ghedini, Paulo César, Campos, Hericles Mesquita, dos Santos, Fernanda Cristina A., da Silva, Cinthia Rio Branco, Lião, Luciano M., Gil, Eric de Souza, Costa, Elson Alves, Menegatti, Ricardo
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Sprache:eng
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Zusammenfassung:In the scope of a research program with the goal of developing treatments for inflammatory diseases, the pharmacological evaluation of LQFM291, designed by molecular hybridization from butylated hydroxytoluene and paracetamol, was described. The antioxidant profile of LQFM291 was evaluated by electrochemical measurement. Also, acute or repeated treatments with equimolar doses to paracetamol were used to evaluate the antinociceptive and/or anti-inflammatory activities of LQFM291 in animal models. The toxicologic potential of LQFM291 was also evaluated and compared to paracetamol through biochemical and histopathological analysis after the repeated treatment schedule. As a result of the acute treatment, paracetamol showed a similar antinociceptive effect in formalin test compared to LQFM291. Whereas, after the repeated treatment, when carrageenan-induced hyperalgesia and edema tests were performed, paracetamol showed a delayed antinociceptive and anti-inflammatory effect compared to LQFM291. Furthermore, as other advantages the LQFM291 showed a high redox capacity, a gastroprotective activity and a safety pharmacological profile without any liver or kidney damage. These effects can be related to the prevention of oxidative stress by reduction of protein and lipid peroxidation in gastric tissue, maintenance of glutathione levels in hepatic homogenate, and a systemic reduction of pro-inflammatory cytokine levels, which may characterize the LQFM291 as a more viable and effective alternative to relief pain and inflammatory signs in patients with chronic disorders. Graphical Abstract
ISSN:0925-4692
1568-5608
DOI:10.1007/s10787-023-01324-8