Discovery of novel sesquistilbene indanone analogues as potent anti-inflammatory agents

  • Eur J Med Chem. 2016 May 4:113:63-74. doi: 10.1016/j.ejmech.2016.02.021.
Mei-Lin Tang  1 ,  Chen Zhong  1 ,  Zheng-Yu Liu  1 ,  Peng Peng  1 ,  Xin-Hua Liu  2 ,  Xun Sun  3
Affiliations
  • 1. Department of Natural Products Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
  • 2. Department of Pharmacology, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China. Electronic address: [email protected].
  • 3. Department of Natural Products Chemistry, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China; Shanghai Key Laboratory of Clinical Geriatric Medicine, 221 West Yanan Road, Shanghai 200040, China. Electronic address: [email protected].
PMID: 26922229 DOI: 10.1016/j.ejmech.2016.02.021
Abstract

To develop novel anti-inflammatory agents with improved pharmaceutical profiles, twenty-eight novel sesquistilbene indanone analogues were synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. Among these compounds, compound 11k was found to be one of the most potent analogues in inhibiting NO production in LPS-stimulated RAW264.7 cells. Furthermore, it could also significantly suppress LPS-induced iNOS and COX-2 expression and NO production through TLR4/JNK/NF-κB signaling pathway in a concentration dependent manner.

Keywords
Anti-inflammatory; Indanone; TLR4/JNK/NF-κB.
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