title: Diarylpentadienone derivatives (curcumin analogues): Synthesis and anti-inflammatory activity.
abstract: A series of new (2E,4E)-1-(substitutedphenyl)-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-α release in cell RAW 264.7 stimulated with LPS. Compound 3i showed the highest anti-inflammatory activity on decreasing IL-6 and TNF-α. 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-κB signaling pathway.
authors.affiliation: School of Pharmacy, Anhui Medical University, Hefei 230032, PR China.
authors.forename: Zhi Sen
authors.initials: ZS
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Anhui Medical University, Hefei 230032, PR China.
authors.forename: Liu Zeng
authors.initials: LZ
authors.lastname: Chen
authors.affiliation: School of Material Science Chemical Engineering, ChuZhou University, ChuZhou 239000, PR China.
authors.forename: Hai Pin
authors.initials: HP
authors.lastname: Zhou
authors.affiliation: School of Pharmacy, Anhui Medical University, Hefei 230032, PR China; School of Material Science Chemical Engineering, ChuZhou University, ChuZhou 239000, PR China. Electronic address: xhliuhx@163.com.
authors.forename: Xin Hua
authors.initials: XH
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Anhui Medical University, Hefei 230032, PR China. Electronic address: fhchen@soho.com.
authors.forename: Fei Hu
authors.initials: FH
authors.lastname: Chen
mesh_terms: D000466:Alkadienes / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000737:chemistry* / Q000494:pharmacology*; D003474:Curcumin / Q000031:analogs & derivatives* / Q000494:pharmacology*; D015850:Interleukin-6 / Q000276:immunology; D008070:Lipopolysaccharides / Q000276:immunology; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D008958:Models, Molecular; D000067996:RAW 264.7 Cells; D014409:Tumor Necrosis Factor-alpha / Q000276:immunology
chemical_list: D000466:Alkadienes; D000893:Anti-Inflammatory Agents; D015850:Interleukin-6; D008070:Lipopolysaccharides; D014409:Tumor Necrosis Factor-alpha; D003474:Curcumin
keywords: Anti-inflammatory; Diarylpentadienone; IL-6; Synthesis