Diarylpentadienone derivatives (curcumin analogues): Synthesis and anti-inflammatory activity

作者：Wang, Zhi Sen; Chen, Liu Zeng; Zhou, Hai Pin; Liu, Xin Hua^*; Chen, Fei Hu^*

来源：Bioorganic & Medicinal Chemistry Letters, 2017, 27(8): 1803-1807.

DOI：10.1016/j.bmcl.2017.02.056

• Synthesis
• Diarylpentadienone
• Anti-inflammatory
• IL-6

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.

• 出版日期2017-4-15
• 单位滁州学院; 安徽医科大学