Identification of the pregnancy hormone relaxin as glucocorticoid receptor agonist THOMAS DSCHIETZIG 1 , CORNELIA BARTSCH, VERENA STANGL, GERT BAUMANN and KARL STANGL Medizinische Klinik m. S. Kardiologie, Angiologie, Pulmologie, Charité Berlin, Berlin, Germany 1 Correspondence: Charité Berlin, Campus Mitte, Medizinische Klinik m. S. Kardiologie, Angiologie und Pulmologie, Schumannstr. 20/21, Berlin 10117, Germany. E-mail: thomas.dschietzig@t-online.de <h3>SPECIFIC AIMS</h3> The insulin-like peptide relaxin is a central hormone of pregnancy, but it also produces anti-fibrotic, myocardial, renal, central nervous, and vascular effects. Recently, two G protein-coupled receptors, LGR7 and LGR8, have been identified as relaxin receptors. Prompted by reports on immunoregulatory effects of relaxin, we investigated possible interactions with human glucocorticoid receptor (GR). <h3>PRINCIPAL FINDINGS</h3> <h3>1. Relaxin blunts endotoxin-induced production of inflammatory cytokines by THP-1 cells in a GR-dependent manner</h3> We analyzed the immunomodulatory properties of relaxin in THP-1 cells differentiated into macrophages. Endotoxin evoked a marked increase in secretion of IL-1, IL-6, and TNF-α over 8, 24, and 48 h. Relaxin suppressed stimulated secretion of all cytokines—an effect that plateaued between 5 and 10 nmol/L, showed an estimated IC 50 of 0.8 nmol/L, and weakened at higher concentrations, although it was still present at 100 nmol/L. At maximum, stimulated IL-1,
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Identification of the pregnancy hormone relaxin as glucocorticoid receptor agonist
DSCHIETZIG, THOMAS; BARTSCH, CORNELIA; STANGL, VERENA; BAUMANN, GERT; STANGL, KARL
Follow The FASEB Journal
, Volume 18 (13): 1536
Fed of American Socs for Experimental Biology – Oct 1, 2004
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