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Anti‐Inflammatory Activities of Melatonin Derivatives in Lipopolysaccharide‐Stimulated RAW 264.7 Cells and Antinociceptive Effects in Mice
Author(s) -
Phiphatwatcharaded Chawapon,
ToparkNgarm Acharawan,
Puthongking Ploenthip,
Mahakunakorn Pramote
Publication year - 2014
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21177
Subject(s) - melatonin , nociception , nitric oxide , lipopolysaccharide , chemistry , pharmacology , analgesic , potency , endocrinology , in vitro , biochemistry , medicine , receptor , organic chemistry
Preclinical ResearchThis study describes the anti‐inflammatory activities of two semisynthesized melatonin ( MT ) derivatives, benzoyl‐melatonin ( BMT ) and acetyl‐melatonin ( AMT ), on the production of pro‐inflammatory mediators in lipopolysaccharide ( LPS )‐stimulated macrophage cells ( RAW 264.7) and their antinociceptive effects in mice. The MT derivatives inhibited production of nitric oxide NO and prostaglandin E 2 in LPS ‐stimulated RAW 264.7 cells in a dose‐dependent manner with IC 50 values lower than those of MT . BMT produced increased tail flick latency time, decreased number of writhes, and reduced nociceptive response in mice when compared with AMT and MT . BMT and AMT had enhanced anti‐inflammatory effects in LPS ‐stimulated RAW 264.7 compared with MT . However, in mouse studies BMT exhibited the highest potency as an anti‐inflammatory agent and was longer‐acting as an antinociceptive compound compared with AMT or MT , suggesting that BMT has potential as an anti‐inflammatory and analgesic compound.