Asymmetric synthesis of novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluation of their anti-inflammatory activity |
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| Authors: | Padmanabha V Kattamuri Rebecca Salmonsen Catherine McQuain Sumner Burstein Hao Sun Guigen Li |
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| Institution: | 1. Department of Chemistry and Biochemistry, Texas Tech University, Lubbock, TX 79409, USA;2. Department of Biochemistry and Molecular Pharmacology, University of Massachusetts Medical School, Worcester, MA 01605, USA;3. Institute of Chemistry and Biomedical Sciences, Nanjing University, Nanjing 210093, PR China |
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| Abstract: | AimsTo design and synthesize novel N-(1-phenyl-2,3-dihydroxypropyl)arachidonylamides and evaluate their analgesic and anti-inflammatory potential.Main methodsThe murine macrophage cell line RAW 264.7 has been widely used as a model for inflammatory responses in vitro. Our model consists of cultured monolayers of RAW 264.7 cells in which media concentrations of 15-deoxy-Δ13,14-PGJ2 (PGJ) are measured by ELISA following LPS (10 ng/ml) stimulation and treatment with 0.1, 0.3, 1.0, 3.0 and 10 μM concentrations of the compounds.Key findingsOur data indicate that several of our compounds have the capacity to increase production of PGJ and may also increase the occurrence of programmed cell death (apoptosis).SignificanceThus these agents are potential candidates for the therapy of conditions characterized by ongoing (chronic) inflammation and its associated pain. |
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