Activity Anti-Inflammatory and in silico Study of New Thiazolidinedione Derivatives
Laudelina R. de Magalhães
Department of Chemistry, Universidade Católica de Pernambuco, 50050-90, PE, 16, Brazil.
Iane Bezerra Vasconcelos Alves
Department of Chemistry Fundamental, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
Everaldo dos Santos
Department of Chemistry Fundamental, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
Vinícius Barros Ribeiro da Silva
Department of Pharmaceutical Sciences, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil
Luiz Carlos Apolinário da Silva
Department of Antibiotics, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
Anekécia Lauro da Silva
Department of Antibiotics, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
Leidiane Carla Lira de Oliveira
Department of Antibiotics, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
Anne Cecília Nascimento da Cruz
Department of Antibiotics, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
Bruno Iraquitan Miranda da Silva
Department of Antibiotics, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
Lúcia Fernanda C. da Costa Leite
Department of Chemistry, Universidade Católica de Pernambuco, 50050-90, PE, 16, Brazil.
Marcelo Hernani Zaldini
Department of Pharmaceutical Sciences, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
Ivan da Rocha Pitta
Department of Chemistry, Universidade Católica de Pernambuco, 50050-90, PE, 16, Brazil.
Teresinha Gonçalves da Silva
Department of Chemistry, Universidade Católica de Pernambuco, 50050-90, PE, 16, Brazil.
Maria do Carmo Alves de Lima *
Department of Antibiotics, Universidade Federal de Pernambuco (UFPE), Recife 50670-901, PE, Brazil.
*Author to whom correspondence should be addressed.
Abstract
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.
Keywords: Thiazolidinedione, molecular modeling, anti-inflammatory properties