Ruan Ban-Feng, Ge Wei-Wei, Cheng Hui-Jie, Xu Hua-Jian, Li Qing-Shan, Liu Xin-Hua
a School of Medical Engineering , Hefei University of Technology , Hefei , P. R. China.
b Anhui Province Key Laboratory of Major Autoimmune Diseases, Anhui Institute of Innovative Drugs , School of Pharmacy, Anhui Medical University , Hefei , P. R. China.
J Enzyme Inhib Med Chem. 2017 Dec;32(1):1282-1290. doi: 10.1080/14756366.2017.1381090.
Twenty-three novel resveratrol-based cinnamic ester hybrids were designed and synthesized. All the compounds were evaluated for their anti-inflammatory activity using RAW264.7 cells. Among them, compound D15 was found to be the most potent one in inhibiting NO production in LPS-stimulated RAW264.7 cells. The further study indicated that compound D15 could suppress expression of proteins iNOS, COX-2, p-p65, and p-IκB LPS-induced. Immunofluorescence further revealed compound D15 could reduce activation p65 in nuclei. All the results indicated that the anti-inflammatory activity of title compound may partly due to its inhibitory effect on the NF-κB signaling pathway.
设计并合成了23种基于白藜芦醇的新型肉桂酸酯杂化物。使用RAW264.7细胞评估了所有化合物的抗炎活性。其中，化合物D15被发现是抑制脂多糖刺激的RAW264.7细胞中一氧化氮产生最有效的化合物。进一步的研究表明，化合物D15可以抑制脂多糖诱导的iNOS、COX-2、p-p65和p-IκB蛋白的表达。免疫荧光进一步显示化合物D15可以减少细胞核中p65的激活。所有结果表明，标题化合物的抗炎活性可能部分归因于其对NF-κB信号通路的抑制作用。
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