title: Design and Discovery of Some Novel Chalcones as Antioxidant and Anti-Inflammatory Agents via Attenuating NF-κB.
abstract: Concerning the role of antioxidant and anti-inflammatory agents for hepatic fibrosis patients, the current study deals with the development of novel chalcone derivatives 5a-i via efficient synthetic methodology in a two-step reaction involving Claisen-Schmidt condensation. The obtained target analogs were screened for in vitro antioxidant activity by various methods (H2 O2 , DPPH, ferrous reducing power, and nitric oxide), where they exhibit considerable radical scavenging activity. These compounds were also evaluated for inhibitory potency against NF-κB activation induced by LPS for the determination of their anti-inflammatory activity. The inhibition values indicate that the entire set of compounds efficiently inhibits the NF-κB activation provoked by LPS. Among the series, compound 5i was identified as the most potent inhibitor of NF-κB, with a relative NF-κB activity of 1.12 ± 0.53. It also inhibits various inflammatory mediators, such as TNF-α, IL-1β, IL-6, and PGE2 .
authors.affiliation: Department of Hepatobiliary Surgery, Affiliated Hospital of Logistics University of PAPF, Tianjin, P. R. China.
authors.forename: Jun
authors.initials: J
authors.lastname: Chu
authors.affiliation: Department of Hepatobiliary Surgery, Affiliated Hospital of Logistics University of PAPF, Tianjin, P. R. China.
authors.forename: Chun-Liang
authors.initials: CL
authors.lastname: Guo
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015232:Dinoprostone / Q000378:metabolism; D016166:Free Radical Scavengers / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D053583:Interleukin-1beta / Q000378:metabolism; D015850:Interleukin-6 / Q000378:metabolism; D008070:Lipopolysaccharides / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D062105:Molecular Docking Simulation; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D047188:Chalcones; D016166:Free Radical Scavengers; D053583:Interleukin-1beta; D015850:Interleukin-6; D008070:Lipopolysaccharides; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D015232:Dinoprostone
keywords: Anti-inflammatory; Antioxidant; Chalcones; Hepatic fibrosis