Activity Anti-Inflammatory and in silico Study of New Thiazolidinedione Derivatives
Laudelina R. de Magalhães, Iane Bezerra Vasconcelos Alves, Everaldo dos Santos, Vinícius Barros Ribeiro da Silva, Luiz Carlos Apolinário da Silva, Anekécia Lauro da Silva, Leidiane Carla Lira de Oliveira, Anne Cecília Nascimento da Cruz, Bruno Iraquitan Miranda da Silva, Lúcia Fernanda C. da Costa Leite, Marcelo Hernani Zaldini, Ivan da Rocha Pitta, Teresinha Gonçalves da Silva, Maria do Carmo Alves de Lima
Journal of Pharmaceutical Research International · pp. 1739–1752 · Published 12 Jul 2014
10.9734/BJPR/2014/11294Abstract
Aims: Evaluation of the anti-inflammatory properties of new thiazolidine-2,4-diones derivatives. Study Design: Study the effects of new thiazolidine-2,4-diones derivatives on the inflammatory process. Place and Duration of Study: Departamento de Antibióticos, Universidade Federal de Pernambuco (UFPE), between June 2011 and July 2012. Methodology: Compounds thiazolidine-2,4-diones were tested for anti-inflammatory activity by air pouch model. Swiss albino mice were used for the study. Air cavities were produced by subcutaneous injection of 2.5 mL of sterile air into the intrascapular area of the back. An additional 2.5 mL of air was injected into the cavity every 3 days to keep the space open. Seven days after the initial air injection, 1 mL of a 1% solution of carrageenan dissolved in saline was injected directly into the pouch to produce an inflammatory response. The compounds thiazolidine-2,4-diones and standard piroxicam were tested at doses of 3 mg/kg body weight. The total number of polymorphonuclear leukocytes (PMNL) was counted using an improved. Results: The results support the use of these derivatives in inflammatory process. Among the compounds tested the ones that showed a greater effect in inhibiting the migration of neutrophils were the 3a, 3b, 3c, 3d and 3e. The anti-inflammatory effects showed by 3a-j were promising, probably due to the duality of action on PPAR alpha and gamma. Conclusion: In conclusion, this study has shown that the thiazolidine derivatives do possess significant anti-inflammatory effects in laboratory animals. The exact mechanism and the bioactive principles responsible for these actions remain to be explained.
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