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

Document Type: Research article

Authors

1 Department of Basic Medical Science, Yongzhou Vocational Technical College, Yong Zhou 425100, PR China

2 Department of Anatomy and Neurobiology, Biology Postdoctoral Workstation, Basic School of Medicine Central South University, Changsha, Hunan, 410013, China

3 Tumor Hospital Xiangya School of Medicine of Central South University, Changsha, Hunan, 410013, China

4 The First Affiliated Hospital, University of South China, Hengyang, Hunan, 421001, China

5 Department of Anatomy and Neurobiology, Biology Postdoctoral Workstation, Basic School of Medicine Central South University, Changsha, Hunan, 410013, China

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.

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