1Department of Basic Medical Science, Yongzhou Vocational Technical College, Yong Zhou 425100, PR China
2Department of Anatomy and Neurobiology, Biology Postdoctoral Workstation, Basic School of Medicine Central South University, Changsha, Hunan, 410013, China
3Tumor Hospital Xiangya School of Medicine of Central South University, Changsha, Hunan, 410013, China
4The First Affiliated Hospital, University of South China, Hengyang, Hunan, 421001, China
5Department 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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