Author/Authors :
Zhang, Qiongyu Department of Basic Medical Science - Yongzhou Vocational Technical College, Yong Zhou 425100, PR China , Hu, Jun-Xiao Department of Basic Medical Science - Yongzhou Vocational Technical College, Yong Zhou 425100, PR China , Kui, Xu Department of Basic Medical Science - Yongzhou Vocational Technical College, Yong Zhou 425100, PR China , Liu, Chao Department of Anatomy and Neurobiology - Biology Postdoctoral Workstation - Basic School of Medicine Central South University, Changsha, Hunan, 410013, China , Zhou, Hui Tumor Hospital Xiangya School of Medicine of Central South University, Changsha, Hunan, 410013, China , Jiang, Xiaoxin Department of Anatomy and Neurobiology - Biology Postdoctoral Workstation - Basic School of Medicine Central South University, Changsha, Hunan, 410013, China , Zeng, Leping 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.
Keywords :
Interleukin , Nuclear factor-kappa B , Inflammation , Sinapic acid
