title: Synthesis and biological evaluation of curcumin derivatives containing NSAIDs for their anti-inflammatory activity.
abstract: Oral administration of nonsteroidal anti-inflammatory drugs (NSAIDs) was frequently associated with serious adverse effects. Inspired by curcumin-a naturally traditional Chinese medicine, a series of curcumin derivatives containing NSAIDs, used for transdermal application, were synthesized and screened for their anti-inflammatory activities in vitro and in vivo. Compared with curcumin and parent NSAID (salicylic acid and salsalate), topical application of A11 and B13 onto mouse ear edema, prior to TPA treatment markedly suppressed the expression of IL-1β, IL-6 and TNF-α, respectively. Mechanistically, A11 and B13 blocked the phosphorylation of IκBα and suppressed the activation of p65 and IκBα. It was found that A11 and B13 may be potent anti-inflammatory agents for the treatment of inflammatory diseases.
authors.affiliation: Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China.
authors.forename: Wenfeng
authors.initials: W
authors.lastname: Liu
authors.affiliation: Guangdong Industry Technical College, Guangzhou 510300, China.
authors.forename: Yonlian
authors.initials: Y
authors.lastname: Li
authors.affiliation: Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China.
authors.forename: Yuan
authors.initials: Y
authors.lastname: Yue
authors.affiliation: Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China; Wuyi University, Jiangmen 529020, China.
authors.forename: Kun
authors.initials: K
authors.lastname: Zhang
authors.affiliation: Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Chen
authors.affiliation: Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China.
authors.forename: Huaqian
authors.initials: H
authors.lastname: Wang
authors.affiliation: Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China.
authors.forename: Yujing
authors.initials: Y
authors.lastname: Lu
authors.affiliation: Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA.
authors.forename: Mou-Tuan
authors.initials: MT
authors.lastname: Huang
authors.affiliation: Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China; Susan Lehman Cullman Laboratory for Cancer Research, Department of Chemical Biology, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA. Electronic address: xizheng@pharmacy.rutgers.edu.
authors.forename: Xi
authors.initials: X
authors.lastname: Zheng
authors.affiliation: Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China. Electronic address: zhiyundu@foxmail.com.
authors.forename: Zhiyun
authors.initials: Z
authors.lastname: Du
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use*; D003474:Curcumin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000627:therapeutic use*; D004423:Ear / Q000473:pathology; D004487:Edema / Q000188:drug therapy* / Q000276:immunology / Q000473:pathology; D007249:Inflammation / Q000188:drug therapy* / Q000276:immunology / Q000473:pathology; D053583:Interleukin-1beta / Q000032:analysis / Q000276:immunology; D015850:Interleukin-6 / Q000032:analysis / Q000276:immunology; D051379:Mice; D016328:NF-kappa B / Q000032:analysis / Q000276:immunology; D014409:Tumor Necrosis Factor-alpha / Q000032:analysis / Q000276:immunology
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D053583:Interleukin-1beta; D015850:Interleukin-6; D016328:NF-kappa B; D014409:Tumor Necrosis Factor-alpha; D003474:Curcumin
keywords: Anti-inflammatory; Curcumin; NSAIDs; TPA