2. Academic Validation
  3. Inhibitory effect of 4,4'-dihydroxy-α-truxillic acid derivatives on NO production in lipopolysaccharide-induced RAW 264.7 macrophages and exploration of structure-activity relationships

Inhibitory effect of 4,4'-dihydroxy-α-truxillic acid derivatives on NO production in lipopolysaccharide-induced RAW 264.7 macrophages and exploration of structure-activity relationships

  • Bioorg Med Chem Lett. 2013 Apr 1;23(7):2207-11. doi: 10.1016/j.bmcl.2013.01.091.
Shan Xiang Liu 1,  Hui Zi Jin,  Lei Shan,  Hua Wu Zeng,  Bing Yang Chen,  Qing Yan Sun,  Wei Dong Zhang
Affiliations

Affiliation

  • 1 School of Pharmacy, Shanghai Jiao Tong University, MinHang DongChuan Rd800, Shanghai 200240, PR China.
PMID: 23454014 DOI: 10.1016/j.bmcl.2013.01.091
Abstract

The inhibitory activity of 4,4'-dihydroxy-α-truxillic acid and its derivatives (5-1a-5-35a) on nitric oxide (NO) release was evaluated in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. Compounds 5-3a, 5-4a, 5-5a, 5-10a, 5-24a, 5-26a and 5-30a exhibited significant inhibitory effects on NO production, with IC50 values of 19.8, 21.1, 16.4, 17.5, 20.8, 22.6 and 17.6 μM, respectively. Their cytotoxicities were also estimated using a CCK-8 assay. Among them, compound 5-10a showed no cytotoxic effect on cells up to a concentration of 50 μM. The structure-activity relationships of the compounds are also discussed.

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