Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation
| Author | Qiongyu Zhang | en |
| Author | Jun-Xiao Hu | en |
| Author | Xu Kui | en |
| Author | Chao Liu | en |
| Author | Hui Zhou | en |
| Author | Xiaoxin Jiang | en |
| Author | Leping Zeng | en |
| Issued Date | 2017-10-31 | en |
| Abstract | Transcription factor NF-κB and relevant cytokines IL-6 and IL-8 play a pivotal role in the pathogenesis of inflammation. Sinapic acid is a natural product and was demonstrated to possess anti-inflammatory activity. In this paper, we synthesized a series of sinapic acid derivatives and evaluated their anti-inflammatory effects. The result suggested that all of the targets compounds 7a-j inhibit NF-κB activation and decrease IL-6 and IL-8 expression in BEAS-2B cells. By our biological assays, we found that all of the prepared compounds displayed stronger anti-inflammatory activities than their precursor sinapic acid. Especially, compounds 7g and 7i, with electron-drawing groups (nitro and fluoro moieties) in the benzimidazole ring, exhibited remarkable anti-inflammation activity, which was even stronger than the reference drug dexamethasone. | en |
| DOI | https://doi.org/10.22037/ijpr.2017.2137 | en |
| Keyword | Sinapic acid | en |
| Keyword | Inflammation | en |
| Keyword | Nuclear factor-kappa B | en |
| Keyword | Interleukin | en |
| Publisher | Brieflands | en |
| Title | Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation | en |
| Type | Original Article | en |
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