title: (E)-1-(4-ethoxyphenyl)-3-(4-nitrophenyl)-prop-2-en-1-one suppresses LPS-induced inflammatory response through inhibition of NF-κB signaling pathway.
abstract: Flavonoids are a class of compounds that exist in nature with the structure of 2-phenyl-chromone. In Chinese traditional medicine, herbal drugs containing flavonoids are widely used for the treatment of inflammation, cardiovascular disease, tumor and so on. In this study, we investigated the anti-inflammatory effect and related mechanisms of a novel synthetic flavonoid, (E)-1-(4-ethoxyphenyl)-3-(4-nitrophenyl)-prop-2-en-1-one (ETH) in lipopolysaccharide (LPS) stimulated macrophages. Our results showed that ETH inhibited LPS-induced TNF-α and IL-6 release in a dose-dependent manner, and decreased TNF-α, IL-1β, IL-6 and iNOS mRNA production. LPS-induced expression of cyclooxygenase-2 (COX-2) was also significantly attenuated by ETH. Pretreatment with ETH reduced the I-κBα phosphorylation, p65 nuclear translocation as well as NF-κB-dependent transcriptional activity. In addition, ETH exhibited a significant protection against LPS-induced inflammatory mortality in mice. Taken together, these findings suggest that ETH can inhibit LPS-induced inflammation via suppressing NF-κB signaling pathway, indicating that ETH may be a potential anti-inflammatory agent.
authors.affiliation: Department of Pharmacology and Toxicology, School of Pharmaceutical Sciences, Sun Yat-sen University, PR China.
authors.forename: Jian
authors.initials: J
authors.lastname: Xu
authors.forename: Yan-Yan
authors.initials: YY
authors.lastname: Jia
authors.forename: Shao-Rui
authors.initials: SR
authors.lastname: Chen
authors.forename: Jian-Tao
authors.initials: JT
authors.lastname: Ye
authors.forename: Xian-Zhang
authors.initials: XZ
authors.lastname: Bu
authors.forename: Yun
authors.initials: Y
authors.lastname: Hu
authors.forename: Yun-Zi
authors.initials: YZ
authors.lastname: Ma
authors.forename: Jin-Lei
authors.initials: JL
authors.lastname: Guo
authors.forename: Pei-Qing
authors.initials: PQ
authors.lastname: Liu
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000494:pharmacology*; D015153:Blotting, Western; D018929:Cell Culture Techniques; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000737:chemistry / Q000494:pharmacology*; D005786:Gene Expression Regulation / Q000187:drug effects*; D053583:Interleukin-1beta / Q000235:genetics; D015850:Interleukin-6 / Q000235:genetics; D008070:Lipopolysaccharides / Q000633:toxicity*; D008264:Macrophages / Q000187:drug effects / Q000276:immunology; D008297:Male; D008516:Medicine, Chinese Traditional; D051379:Mice; D008810:Mice, Inbred C57BL; D008813:Mice, Inbred ICR; D015394:Molecular Structure; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D052247:Nitric Oxide Synthase Type II / Q000235:genetics; D021381:Protein Transport; D060888:Real-Time Polymerase Chain Reaction; D012772:Shock, Septic / Q000517:prevention & control; D015398:Signal Transduction / Q000187:drug effects*; D016019:Survival Analysis; D014409:Tumor Necrosis Factor-alpha / Q000235:genetics
chemical_list: C583916:1-(4-ethoxyphenyl)-3-(4-nitrophenyl)-prop-2-en-1-one; D000894:Anti-Inflammatory Agents, Non-Steroidal; D047188:Chalcones; D005419:Flavonoids; D053583:Interleukin-1beta; D015850:Interleukin-6; D008070:Lipopolysaccharides; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; C482199:lipopolysaccharide, E coli O55-B5; D052247:Nitric Oxide Synthase Type II; C496317:Nos2 protein, mouse