Literature DB >> 11211928

Characterization of chenodeoxycholic acid as an endogenous antagonist of the G-coupled formyl peptide receptors.

X Chen1, D Yang, W Shen, H F Dong, J M Wang, J J Oppenheim, M Z Howard.   

Abstract

OBJECTIVE AND
DESIGN: To demonstrate the role of bile acids in immune modulation we examined the ability of select bile acids to inhibit leukocyte migration and chemoattractant receptor function. MATERIALS: To elucidate this mechanism, we employed primary human monocytes, neutrophils and cell lines transfected to express either the high affinity fMLP receptor (FPR) or the low affinity fMLP receptor like 1 (FPRL1). TREATMENT: Cells were treated with chenodeoxycholic acid (CDCA) and related bile acids in a 0-400 micromolar range.
METHOD: Cell viability, chemotaxis and calcium flux analysis were preformed.
RESULTS: We observed that pathophysiological levels (< or = 150 micromolar) of CDCA competitively inhibited 3H-fMLP binding to human monocytes, FPR and FPRL1 transfected cells. Additionally, CDCA reduced both the chemotactic and calcium flux responses induced by fMLP or "W" peptide. Further, CDCA inhibited anti-FPR antibody binding to monocytes.
CONCLUSIONS: CDCA selectively inhibited human leukocyte chemotaxis and calcium flux induced by fMLP, but not other chemoattractants, suggesting a mechanism for inhibition of inflammation and suppression of innate immune response.

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Year:  2000        PMID: 11211928     DOI: 10.1007/s000110050656

Source DB:  PubMed          Journal:  Inflamm Res        ISSN: 1023-3830            Impact factor:   4.575


  16 in total

1.  Pharmacophore model for bile acids recognition by the FPR receptor.

Authors:  Cristina Ferrari; Antonio Macchiarulo; Gabriele Costantino; Roberto Pellicciari
Journal:  J Comput Aided Mol Des       Date:  2006-09-14       Impact factor: 3.686

Review 2.  Development of small molecule non-peptide formyl peptide receptor (FPR) ligands and molecular modeling of their recognition.

Authors:  I A Schepetkin; A I Khlebnikov; M P Giovannoni; L N Kirpotina; A Cilibrizzi; M T Quinn
Journal:  Curr Med Chem       Date:  2014       Impact factor: 4.530

3.  The mechanism underlying the contractile effect of a chemotactic peptide, formyl-Met-Leu-Phe on the guinea-pig Taenia coli.

Authors:  Hiroshi Kawata; Katsuya Hirano; Junji Nishimura; Chiharu Kubo; Hideo Kanaide
Journal:  Br J Pharmacol       Date:  2005-06       Impact factor: 8.739

Review 4.  The bile acid membrane receptor TGR5 as an emerging target in metabolism and inflammation.

Authors:  Thijs W H Pols; Lilia G Noriega; Mitsunori Nomura; Johan Auwerx; Kristina Schoonjans
Journal:  J Hepatol       Date:  2010-12-09       Impact factor: 25.083

5.  Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors.

Authors:  Igor A Schepetkin; Liliya N Kirpotina; Andrei I Khlebnikov; Mark A Jutila; Mark T Quinn
Journal:  Mol Pharmacol       Date:  2010-10-13       Impact factor: 4.436

6.  Contributions of bile acids to gastrointestinal physiology as receptor agonists and modifiers of ion channels.

Authors:  Stephen J Keely; Andreacarola Urso; Alexandr V Ilyaskin; Christoph Korbmacher; Nigel W Bunnett; Daniel P Poole; Simona E Carbone
Journal:  Am J Physiol Gastrointest Liver Physiol       Date:  2021-11-10       Impact factor: 4.052

Review 7.  Antagonism of human formyl peptide receptor 1 with natural compounds and their synthetic derivatives.

Authors:  Igor A Schepetkin; Andrei I Khlebnikov; Liliya N Kirpotina; Mark T Quinn
Journal:  Int Immunopharmacol       Date:  2015-09-15       Impact factor: 4.932

Review 8.  International Union of Basic and Clinical Pharmacology. LXXIII. Nomenclature for the formyl peptide receptor (FPR) family.

Authors:  Richard D Ye; François Boulay; Ji Ming Wang; Claes Dahlgren; Craig Gerard; Marc Parmentier; Charles N Serhan; Philip M Murphy
Journal:  Pharmacol Rev       Date:  2009-06-04       Impact factor: 25.468

Review 9.  Bile Acids Activated Receptors in Inflammatory Bowel Disease.

Authors:  Michele Biagioli; Silvia Marchianò; Adriana Carino; Cristina Di Giorgio; Luca Santucci; Eleonora Distrutti; Stefano Fiorucci
Journal:  Cells       Date:  2021-05-21       Impact factor: 6.600

Review 10.  The Gut Microbiota as a Therapeutic Target in IBD and Metabolic Disease: A Role for the Bile Acid Receptors FXR and TGR5.

Authors:  Annemarie Baars; Annemarie Oosting; Jan Knol; Johan Garssen; Jeroen van Bergenhenegouwen
Journal:  Microorganisms       Date:  2015-10-10
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