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基于白藜芦醇的肉桂酸酯杂化物：合成、表征及抗炎活性

Resveratrol-based cinnamic ester hybrids: synthesis, characterization, and anti-inflammatory activity.

作者信息

Ruan Ban-Feng, Ge Wei-Wei, Cheng Hui-Jie, Xu Hua-Jian, Li Qing-Shan, Liu Xin-Hua

机构信息

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.

出版信息

J Enzyme Inhib Med Chem. 2017 Dec;32(1):1282-1290. doi: 10.1080/14756366.2017.1381090.

DOI:10.1080/14756366.2017.1381090
PMID:29072109
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6009859/
Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/5f5b4b7e7d55/IENZ_A_1381090_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/97d09f6ec804/IENZ_A_1381090_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/f1fbfdec8e31/IENZ_A_1381090_SCH0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/f97b6c0838e5/IENZ_A_1381090_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/4e3fdfcb4d15/IENZ_A_1381090_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/fba34995c932/IENZ_A_1381090_F0004_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/aee7f6a973f1/IENZ_A_1381090_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/5f5b4b7e7d55/IENZ_A_1381090_F0006_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/97d09f6ec804/IENZ_A_1381090_F0001_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/f1fbfdec8e31/IENZ_A_1381090_SCH0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/f97b6c0838e5/IENZ_A_1381090_F0002_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/4e3fdfcb4d15/IENZ_A_1381090_F0003_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/fba34995c932/IENZ_A_1381090_F0004_B.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/aee7f6a973f1/IENZ_A_1381090_F0005_C.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c54a/6009859/5f5b4b7e7d55/IENZ_A_1381090_F0006_C.jpg

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