Anti-inflammatory, Antiarthritic and Antinociceptive Activities of 3,5-Disubstituted Thiazolidine Derivatives
Diana Jussara do N. Malta
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
Larissa Cardoso C. Araújo *
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
Aline S.G Carrazoni
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
Fernanda Virginia B. Mota
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
Sandra Cabral da Silva
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
Maria Andrea de S. Carmino
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
Maria do Carmo A. Lima
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
Ivan da Rocha Pitta
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
Teresinha Gonçalves da Silva
Bioassay Laboratory for Drug Screening, Department of Antibiotics, Federal University of Pernambuco (UFPe), PE, Brazil.
*Author to whom correspondence should be addressed.
Abstract
Aims: The aim of this study was to investigate the anti-inflammatory, antiarthritic and antinociceptive effects of two thiazolidinedione derivatives: 3-(2-bromo-benzyl)-5-(4-methylsufonyl-benzylidene)-thiazolidine-2,4-dione (LPSF/GQ-125) and 3-(2,6-difluoro-benzyl)-5-(4-methylsufonyl-benzylidene)-thiazolidine-2,4-dione (LPSF/GQ-192).
Study Design: Study the effects of thiazolidinedione derivatives on the inflammatory process.
Place and Duration of Study: Department of Antibiotics of the Federal University of Pernambuco, Brazil, between March 2010 and February 2012.
Methodology: The carrageenan-induced air pouch in mice was performed and cytokine levels (TNF-α and IL-1β) were determined. Arthritis was induced in female wistar rats by complete Freund's adjuvant (CFA). To determine the antinociceptive activity, acetic acid-induced nociception and hot plate tests in mice were utilized.
Results: Treatment with the compounds reduced leukocyte migration and the release of both TNF-α and IL-1β in the air pouch. Both LPSF/GQ-125 and LPSF/GQ-192 reduced the CFA-induced paw edema and the nociception induced by acetic acid; the hot plate test, however, showed no antinociceptive activity when compared to the control group.
Conclusion: These results indicate that LPSF/GQ-125 and LPSF/GQ-192 exhibit promising anti-inflammatory, antinociceptive and antiarthritic activities related to their ability to inhibit TNF-α and IL-1β production as well as reduction of leukocyte migration.
Keywords: Thiazolidinones, inflammation, air-pouch, cytokines, arthritis