Anti-inflammatory Effects of Novel Thiazolidinone Derivatives as Bioactive Heterocycles on RAW264.7 Cells
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...
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| Format: | Article |
| Language: | English |
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Tehran University of Medical Sciences
2017-02-01
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| Series: | Iranian Journal of Allergy, Asthma and Immunology |
| Subjects: | |
| Online Access: | https://ijaai.tums.ac.ir/index.php/ijaai/article/view/907 |
| _version_ | 1819058661438259200 |
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| author | Hossein Ghafoori Mehrnaz Rezaei Asadollah Mohammadi |
| author_facet | Hossein Ghafoori Mehrnaz Rezaei Asadollah Mohammadi |
| author_sort | Hossein Ghafoori |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-21T13:58:45Z |
| format | Article |
| id | doaj.art-e17e5511cc1040e385adc247c6809665 |
| institution | Directory Open Access Journal |
| issn | 1735-1502 1735-5249 |
| language | English |
| last_indexed | 2024-12-21T13:58:45Z |
| publishDate | 2017-02-01 |
| publisher | Tehran University of Medical Sciences |
| record_format | Article |
| series | Iranian Journal of Allergy, Asthma and Immunology |
| spelling | doaj.art-e17e5511cc1040e385adc247c68096652022-12-21T19:01:27ZengTehran University of Medical SciencesIranian Journal of Allergy, Asthma and Immunology1735-15021735-52492017-02-01161907Anti-inflammatory Effects of Novel Thiazolidinone Derivatives as Bioactive Heterocycles on RAW264.7 CellsHossein Ghafoori0Mehrnaz Rezaei1Asadollah Mohammadi2Department of Biology, University of Guilan, Rasht, IranDepartment of Biology, University of Guilan, University Campus 2, Rasht, IranDepartment of Chemistry, University of Guilan, Rasht, IranThe 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/907Anti-inflammatory effectsCOX-2iNOSNF-κB (p65)Thiazolidinone |
| spellingShingle | Hossein Ghafoori Mehrnaz Rezaei Asadollah Mohammadi Anti-inflammatory Effects of Novel Thiazolidinone Derivatives as Bioactive Heterocycles on RAW264.7 Cells Iranian Journal of Allergy, Asthma and Immunology Anti-inflammatory effects COX-2 iNOS NF-κB (p65) Thiazolidinone |
| title | Anti-inflammatory Effects of Novel Thiazolidinone Derivatives as Bioactive Heterocycles on RAW264.7 Cells |
| title_full | Anti-inflammatory Effects of Novel Thiazolidinone Derivatives as Bioactive Heterocycles on RAW264.7 Cells |
| title_fullStr | Anti-inflammatory Effects of Novel Thiazolidinone Derivatives as Bioactive Heterocycles on RAW264.7 Cells |
| title_full_unstemmed | Anti-inflammatory Effects of Novel Thiazolidinone Derivatives as Bioactive Heterocycles on RAW264.7 Cells |
| title_short | Anti-inflammatory Effects of Novel Thiazolidinone Derivatives as Bioactive Heterocycles on RAW264.7 Cells |
| title_sort | anti inflammatory effects of novel thiazolidinone derivatives as bioactive heterocycles on raw264 7 cells |
| topic | Anti-inflammatory effects COX-2 iNOS NF-κB (p65) Thiazolidinone |
| url | https://ijaai.tums.ac.ir/index.php/ijaai/article/view/907 |
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