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G protein‐coupled receptor 39 plays an anti‐inflammatory role by enhancing IL‐10 production from macrophages under inflammatory conditions

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ABSTRACT The possible role of G protein‐coupled receptor 39 (GPR39) in inflammation was examined in macrophages. Gpr39 expression increased in thioglycollate‐induced peritoneal macrophages. TC‐G 1008, a G protein‐coupled receptor 39… Click to show full abstract

ABSTRACT The possible role of G protein‐coupled receptor 39 (GPR39) in inflammation was examined in macrophages. Gpr39 expression increased in thioglycollate‐induced peritoneal macrophages. TC‐G 1008, a G protein‐coupled receptor 39 agonist, enhanced interleukin (IL)‐10 production from thioglycollate‐induced peritoneal macrophages stimulated with lipopolysaccharide (LPS) in vitro. In addition, the oral administration of TC‐G 1008 enhanced serum IL‐10 concentrations in an LPS‐induced murine model of sepsis. The ablation of G protein‐coupled receptor 39 significantly reduced IL‐10 production by TC‐G 1008 in thioglycollate‐induced peritoneal macrophages stimulated with LPS and in the LPS‐induced murine model of sepsis. Moreover, the oral administration of TC‐G 1008 significantly improved the survival rate in the LPS‐induced murine model of sepsis. Taken together, our data suggest that G protein‐coupled receptor 39 exhibits an anti‐inflammatory activity by enhancing IL‐10 production from macrophages.

Keywords: protein coupled; coupled receptor; production; anti inflammatory

Journal Title: European Journal of Pharmacology
Year Published: 2018

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