Document Detail


Investigation of nuclear factor-κB inhibitors and interleukin-10 as regulators of inflammatory signalling in human adipocytes.
MedLine Citation:
PMID:  20846165     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The poor prognosis of obesity is now known to involve a proinflammatory state associated with elevated circulating levels of cytokines and with macrophage infiltration of adipose tissue. In particular, Toll-like receptor (TLR)-4-driven adipose inflammation has been implicated recently in obesity and the development of diabetes. Adipocytes are now recognized as an important source of cytokine and chemokine production, including interleukin (IL)-6 and monocyte chemotractant protein (MCP)-1, and this appears to be a key step in the development of the obesity-associated inflammatory state. Interventions targeted at adipocyte inflammation may therefore form novel therapies to treat or prevent medical complications of obesity. We set out to explore whether anti-inflammatory interventions which are effective in conventional immune cells would operate on primary human cultures of in-vitro differentiated adipocytes. IL-10 was ineffective against TLR-4-induced cytokine secretion due to lack of IL-10 receptor on human adipocytes, in contrast to the widely used murine 3T3-L1 adipocyte model, which is known to respond to IL-10. Adenoviral delivery of an IL-10 receptor construct to the cells restored IL-10 responsiveness as assessed by signal transducer and activator of transcription-3 (STAT-3) phosphorylation. However, the small molecule nuclear factor (NF)-κB inhibitors 2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide (TPCA)-1 and carbobenzoxyl-Ile-Glu(O-t-butyl)-Ala-leucinal (PSI) as well as adenovirally delivered dominant negative inhibitor of IkappaB kinase 2 (IKK2) and wild-type IκBα were effective inhibitors of TLR-4-driven IL-6 and MCP-1 induction. These data identify a central role for canonical NF-κB signalling in adipocyte cytokine induction and indicate that small molecule inhibitors of NF-κB may form the basis of future treatments for obesity-related conditions where adipocyte inflammatory signalling is implicated.
Authors:
J J O Turner; K M Foxwell; R Kanji; C Brenner; S Wood; B M J Foxwell; M Feldmann
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-09-15
Journal Detail:
Title:  Clinical and experimental immunology     Volume:  162     ISSN:  1365-2249     ISO Abbreviation:  Clin. Exp. Immunol.     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2010-11-12     Completed Date:  2011-03-08     Revised Date:  2011-12-21    
Medline Journal Info:
Nlm Unique ID:  0057202     Medline TA:  Clin Exp Immunol     Country:  England    
Other Details:
Languages:  eng     Pagination:  487-93     Citation Subset:  IM    
Copyright Information:
© 2010 Authors. Clinical and Experimental Immunology © 2010 British Society for Immunology.
Affiliation:
Kennedy Institute of Rheumatology, Charing Cross Hospital, London, UK. jeremy.turner@nnuh.nhs.uk
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MeSH Terms
Descriptor/Qualifier:
Adipocytes / drug effects,  immunology,  metabolism*,  pathology
Amides / pharmacology
Cells, Cultured
Chemokine CCL2 / biosynthesis,  genetics,  secretion
Humans
Inflammation*
Interleukin-10 / immunology,  metabolism
Interleukin-6 / biosynthesis,  genetics,  secretion
NF-kappa B / antagonists & inhibitors,  immunology,  metabolism*
Obesity / drug therapy,  immunology*
Receptors, Interleukin-10 / genetics,  immunology,  metabolism*
STAT3 Transcription Factor / genetics,  metabolism
Thiophenes / pharmacology
Toll-Like Receptor 4 / immunology,  metabolism
Transgenes / genetics
Grant Support
ID/Acronym/Agency:
072643/Z/03/Z//Wellcome Trust; G7811974//Medical Research Council; //Arthritis Research UK
Chemical
Reg. No./Substance:
0/2-((aminocarbonyl)amino)-5-(4-fluorophenyl)-3-thiophenecarboxamide; 0/Amides; 0/CCL2 protein, human; 0/Chemokine CCL2; 0/Interleukin-6; 0/NF-kappa B; 0/Receptors, Interleukin-10; 0/STAT3 Transcription Factor; 0/TLR4 protein, human; 0/Thiophenes; 0/Toll-Like Receptor 4; 130068-27-8/Interleukin-10

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