4.6 Article

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

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出版社

TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2017.1381090

关键词

Resveratrol derivatives; cinnamic ester; antiinflammatory; NF-kappa B signaling pathway; molecular docking

资金

  1. National Natural Science Foundation of China [21602042, 21572003]
  2. Anhui Provincial Natural Science Foundation [1508085MB33]
  3. Fundamental Research Funds for the Central Universities
  4. Key Scientific and Technological Project of Anhui Provincial Tobacco Company [20150551007]

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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-I kappa B 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-kappa B signaling pathway.

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