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
| Autor: | Qing Yan Sun, Bing Yang Chen, Hui-Zi Jin, Weidong Zhang, Lei Shan, Shan Xiang Liu, Hua Wu Zeng |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Lipopolysaccharides
Models Molecular Lipopolysaccharide Stereochemistry Clinical Biochemistry Pharmaceutical Science Crystallography X-Ray Nitric Oxide 010402 general chemistry Inhibitory postsynaptic potential 01 natural sciences Biochemistry Nitric oxide Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Animals Structure–activity relationship Cytotoxic T cell No production Cytotoxicity Molecular Biology Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Truxillic acid Macrophages Organic Chemistry 3. Good health 0104 chemical sciences chemistry Molecular Medicine Cyclobutanes |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 23:2207-2211 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2013.01.091 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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