Anti-inflammatory, Antiarthritic and Antinociceptive Activities of 3,5-Disubstituted Thiazolidine Derivatives

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.