title: 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.
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.
authors: School of Pharmacy, Shanghai Jiao Tong University, MinHang DongChuan Rd800, Shanghai 200240, PR China.
authors: Shan Xiang
authors: SX
authors: Liu
authors: Hui Zi
authors: HZ
authors: Jin
authors: Lei
authors: L
authors: Shan
authors: Hua Wu
authors: HW
authors: Zeng
authors: Bing Yang
authors: BY
authors: Chen
authors: Qing Yan
authors: QY
authors: Sun
authors: Wei Dong
authors: WD
authors: Zhang
mesh_terms: D000818:Animals; D018360:Crystallography, X-Ray; D003503:Cyclobutanes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D008070:Lipopolysaccharides / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects*; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D009569:Nitric Oxide / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D013329:Structure-Activity Relationship
chemical_list: C510228:4,4'-dihydroxy-alpha-truxillic acid; D003503:Cyclobutanes; D008070:Lipopolysaccharides; D009569:Nitric Oxide