2. Academic Validation
  3. Synthesis and biological evaluation of curcumin derivatives containing NSAIDs for their anti-inflammatory activity

Synthesis and biological evaluation of curcumin derivatives containing NSAIDs for their anti-inflammatory activity

  • Bioorg Med Chem Lett. 2015 Aug 1;25(15):3044-51. doi: 10.1016/j.bmcl.2015.04.077.
Wenfeng Liu 1,  Yonlian Li 2,  Yuan Yue 1,  Kun Zhang 3,  Qian Chen 1,  Huaqian Wang 1,  Yujing Lu 1,  Mou-Tuan Huang 4,  Xi Zheng 5,  Zhiyun Du 6
Affiliations

Affiliations

  • 1 Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China.
  • 2 Guangdong Industry Technical College, Guangzhou 510300, China.
  • 3 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.
  • 4 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.
  • 5 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: [email protected].
  • 6 Laboratory of Natural Medicinal Chemistry & Green Chemistry, Faculty of Light Industry and Chemical Engineering, Guangdong University of Technology, Guangzhou 510006, China. Electronic address: [email protected].
PMID: 26048786 DOI: 10.1016/j.bmcl.2015.04.077
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.

Keywords

Anti-inflammatory; Curcumin; NSAIDs; TPA.

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