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

Iranian Journal of Pharmaceutical Research

关键词: Sinapic acid;    inflammation;    Nuclear factor-kappa B;    Interleukin;   

DOI  :  

学科分类：社会科学、人文和艺术（综合）

来源: Shaheed Beheshti Medical University * School of Pharmacy

【 摘 要 】

Transcription factor NF-κB and relevant cytokines IL-6 and IL-8 play a pivotal role in thepathogenesis of inflammation. Sinapic acid is a natural product and was demonstrated to possessanti-inflammatory activity. In this paper, we synthesized a series of sinapic acid derivativesand evaluated their anti-inflammatory effects. The result suggested that all of the targetscompounds 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 displayedstronger anti-inflammatory activities than their precursor sinapic acid. Especially, compounds7g 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 referencedrug dexamethasone.

【 授权许可】

CC BY