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Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation

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 thei...

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Autores principales: Zhang, Qiongyu, Hu, Jun-Xiao, Kui, Xu, Liu, Chao, Zhou, Hui, Jiang, Xiaoxin, Zeng, Leping
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Shaheed Beheshti University of Medical Sciences 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5843302/
https://www.ncbi.nlm.nih.gov/pubmed/29552049
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author Zhang, Qiongyu
Hu, Jun-Xiao
Kui, Xu
Liu, Chao
Zhou, Hui
Jiang, Xiaoxin
Zeng, Leping
author_facet Zhang, Qiongyu
Hu, Jun-Xiao
Kui, Xu
Liu, Chao
Zhou, Hui
Jiang, Xiaoxin
Zeng, Leping
author_sort Zhang, Qiongyu
collection PubMed
description 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.
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spelling pubmed-58433022018-03-16 Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation Zhang, Qiongyu Hu, Jun-Xiao Kui, Xu Liu, Chao Zhou, Hui Jiang, Xiaoxin Zeng, Leping Iran J Pharm Res Original Article 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. Shaheed Beheshti University of Medical Sciences 2017 /pmc/articles/PMC5843302/ /pubmed/29552049 Text en © 2017 by School of Pharmacy,Shaheed Beheshti University of Medical Sciences and Health Services This is an Open Access article distributed under the terms of the Creative Commons Attribution License, (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Original Article
Zhang, Qiongyu
Hu, Jun-Xiao
Kui, Xu
Liu, Chao
Zhou, Hui
Jiang, Xiaoxin
Zeng, Leping
Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation
title Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation
title_full Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation
title_fullStr Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation
title_full_unstemmed Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation
title_short Sinapic Acid Derivatives as Potential Anti-Inflammatory Agents: Synthesis and Biological Evaluation
title_sort sinapic acid derivatives as potential anti-inflammatory agents: synthesis and biological evaluation
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5843302/
https://www.ncbi.nlm.nih.gov/pubmed/29552049
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