Evaluation of the Inhibitory Effects of Pyridylpyrazole Derivatives on LPS-Induced PGE<sub>2</sub> Productions and Nitric Oxide in Murine RAW 264.7 Macrophages
A series of thirteen triarylpyrazole analogs were investigated as inhibitors of lipopolysaccharide (LPS)-induced prostaglandin E<sub>2</sub> (PGE<sub>2</sub>) and nitric oxide (NO) production in RAW 264.7 macrophages. The target compounds <b>1a</b>–<b>m</...
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| Main Authors: | , , , , , , , , |
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| Format: | article |
| Language: | EN |
| Published: |
MDPI AG
2021
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| Subjects: | |
| Online Access: | https://doaj.org/article/f9d0f03beb1344b18df4f2d77a158151 |
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| Summary: | A series of thirteen triarylpyrazole analogs were investigated as inhibitors of lipopolysaccharide (LPS)-induced prostaglandin E<sub>2</sub> (PGE<sub>2</sub>) and nitric oxide (NO) production in RAW 264.7 macrophages. The target compounds <b>1a</b>–<b>m</b> have first been assessed for cytotoxicity against RAW 264.7 macrophages to determine their non-cytotoxic concentration(s) for anti-inflammatory testing to make sure that the inhibition of PGE<sub>2</sub> and NO production would not be caused by cytotoxicity. It was found that compounds <b>1f</b> and <b>1m</b> were the most potent PGE<sub>2</sub> inhibitors with IC<sub>50</sub> values of 7.1 and 1.1 μM, respectively. In addition, these compounds also showed inhibitory effects of 11.6% and 37.19% on LPS-induced NO production, respectively. The western blots analysis of COX-2 and iNOS showed that the PGE<sub>2</sub> and NO inhibitory effect of compound <b>1m</b> are attributed to inhibition of COX-2 and iNOS protein expression through inactivation of p38. |
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