Activity Anti-Inflammatory and in silico Study of New Thiazolidinedione Derivatives.
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Date
2014-07
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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 compoundsthiazolidine-2,4-diones and standard piroxicam
were tested at doses of 3 mg/kg body weight. The total number of polymorphonuclear
leukocytes (PMNL) was countedusing 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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Keywords
Thiazolidinedione, molecular modeling, anti-inflammatory properties
Citation
Magalhães Laudelina R de, Alves Iane Bezerra Vasconcelos, Santos Everaldo dos, Silva Vinícius Barros Ribeiro da, Silva Luiz Carlos Apolinário da, Silva Anekécia Lauro da, Oliveira Leidiane Carla Lira de, Cruz Anne Cecília Nascimento da, Silva Bruno Iraquitan Miranda da, Leite Lúcia Fernanda C da Costa, Zaldini Marcelo Hernani, Pitta Ivan da Rocha, Silva Teresinha Gonçalves da, Lima Maria do Carmo Alves de. Activity Anti-Inflammatory and in silico Study of New Thiazolidinedione Derivatives. British Journal of Pharmaceutical Research. 2014 July; 4(14): 1739-1752.