Diarylpentadienone derivatives (curcumin analogues): Synthesis and anti-inflammatory activity
Diarylpentadienone derivatives (curcumin analogues): Synthesis and anti-inflammatory activity
复制标题
二芳基戊二烯酮衍生物（姜黄素类似物）：合成和抗炎活性
DOI：
10.1016/j.bmcl.2017.02.056
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发表时间：
2017-04-15
影响因子：
2.7
通讯作者：
Chen, Fei Hu
中科院分区：
文献类型：
--
作者：
Wang, Zhi Sen;Chen, Liu Zeng;Chen, Fei Hu
A series of new (2E,4E)-1-(substitutedpheny1)-5-(substitutedphenyl)penta-2,4-dien-1-one derivatives were designed and synthesized. Compounds 3i, 3k were determined by X-ray. All of the compounds have been screened for their anti-inflammatory activity characterized by evaluating their inhibition against LPS-induced IL-6 and TNF-alpha release in cell RAW 264.7 stimulated with LPS. Compound 3i showed the highest anti-inflammatory activity on decreasing IL-6 and TNF-alpha. The further study showed that title compound 3i inhibited expression of proteins p-p65, iNOS, COX-2 LPS-induced. Immunofluorescence also revealed compound 3i could lightly reduce activation p65 in nuclei. These results indicate that compound 3i anti-inflammatory role may partly due to its inhibitory effect on the NF-kappa Beta signaling pathway. (C) 2017 Elsevier Ltd. All rights reserved.
