2. Academic Validation
  3. Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents

Rational design, synthesis, and pharmacological properties of pyranochalcone derivatives as potent anti-inflammatory agents

  • Eur J Med Chem. 2012 Aug:54:272-80. doi: 10.1016/j.ejmech.2012.05.005.
Fei Peng 1,  Guangcheng Wang,  Xiuxia Li,  Dong Cao,  Zhuang Yang,  Liang Ma,  Haoyu Ye,  Xiaolin Liang,  Yan Ran,  Jinying Chen,  Jingxiang Qiu,  Caifeng Xie,  Chongyang Deng,  Mingli Xiang,  Aihua Peng,  Yuquan Wei,  Lijuan Chen
Affiliations

Affiliation

  • 1 State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Keyuan Road 4, Gaopeng Street, Chengdu 610041, China.
PMID: 22633833 DOI: 10.1016/j.ejmech.2012.05.005
Abstract

24 derivatives (5a-x) derived from natural pyranochalcones (I and II) were designed and evaluated for their inhibitory potency on the production of nitric oxide (NO) in LPS-stimulated RAW264.7 cells. Among them, four compounds (5b, 5d, 5f, and 5h) exhibited more potent inhibitory effects on iNOS activity and iNOS-mediated NO production than a positive control indomethacin. Furthermore, 5b could significantly suppress the progression of carrageenan-induced hind paw edema compared to indomethacin at a dosage of 10 mg/kg/day, and dose-dependently ameliorated the development of adjuvant-induced arthritis (AIA) validated by arthritic scores and H&E staining of joints. In addition, docking study confirmed that 5b was an iNOS Inhibitor with binding to the active site of murine iNOS.

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