Tehran University of Medical Sciences Iranian Journal of Allergy, Asthma and Immunology 1735-1502 16 1 2017 02 25 28 38 EN Hossein Ghafoori Department of Biology, University of Guilan, Rasht, Iran Mehrnaz Rezaei Department of Biology, University of Guilan, University Campus 2, Rasht, Iran Asadollah Mohammadi Department of Chemistry, University of Guilan, Rasht, Iran 2016 05 04 2016 09 04 The inhibition of the inducible nitric oxide synthase (iNOS), cyclooxygenase 2 (COX-2) and nuclear factor-κB (NF-κB) production are research targets of attract in the field of anti-inflammatory drug development. Therefore, this study was designed to investigate the anti-inflammatory effects of novel thiazolidinone derivatives using a cellular model of lipopolysaccharide (LPS)-stimulated murine macrophage RAW 264.7. In the present study, five new derivatives (A to E) of thiazolidinone were synthesized and screened for anti-inflammatory activities. Cell viability of LPS-stimulated RAW 264.7 macrophages clearly decreased in >55 μg/mL of synthesized A-E compounds especially in the presence of C; therefore, up to 50 μg/mL of compounds were selected for the subsequent analysis. A majority of these compounds showed significant inhibition on the production of NO in LPS-stimulated macrophages in a dose-dependent manner. Compounds B and D (10-50 μg/mL) significantly inhibited LPS-induced NF-κB (p65) production in a dose-dependent manner. The effects of B and D on iNOS and COX-2 mRNA and protein expression in LPS-stimulated RAW 264.7 cells were detected by real time-PCR and western blot. B derivative significantly suppressed the iNOS and COX-2 mRNA level and as well as protein expression. Taken together, these results reveal that compound B as new thiazolidinone derivative decreased expression of the inflammatory-related signals (NO, iNOS and COX-2) through regulation of NF-κB; hence, this compound could be suggested as a novel therapeutic strategy for inflammation-associated disorders. https://ijaai.tums.ac.ir/index.php/ijaai/article/view/907 https://ijaai.tums.ac.ir/index.php/ijaai/article/download/907/705