Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 32, Issue 1, Pages 1282-1290Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2017.1381090
Keywords
Resveratrol derivatives; cinnamic ester; antiinflammatory; NF-kappa B signaling pathway; molecular docking
Funding
- National Natural Science Foundation of China [21602042, 21572003]
- Anhui Provincial Natural Science Foundation [1508085MB33]
- Fundamental Research Funds for the Central Universities
- 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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