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Hop bitter acids efficiently block inflammation independent of GRα, PPARα, or PPARγ

Marjan Van Cleemput UGent, Arne Heyerick UGent, Claude Libert UGent, Katrien Swerts UGent, Jan Philippé UGent, Denis De Keukeleire UGent, Guy Haegeman UGent and Karolien De Bosscher UGent (2009) MOLECULAR NUTRITION & FOOD RESEARCH. 53(9). p.1143-1155
abstract
Hop (Humulus lupulus L.) is an essential ingredient of beer, where it provides the typical bitter taste, but is also applied in traditional folk medicine for sedative and antibacterial purposes. In this study, we demonstrate and compare the anti-inflammatory effect of various classes of hop bitter acids (HBA), including alpha-acids (AA), beta-acids (BA), and iso-alpha-acids (IAA), in fibroblasts, which are important players in the inflammatory response. All three studied classes of HBA blocked the turner necrosis factor alpha (TNF)-induced production of the cytokine IL6, and inhibited the transactivation of the pro-inflammatory transcription factors nuclear factor kappa B (NF-kappa B), activator protein-I (AP-1), and cAMP-response element-binding protein (CREB). In this respect, the six-membered ring compounds AA and BA showed equal potency, whereas the five-membered ring compounds, IAA, were effective only when used at higher concentrations. Furthermore, with regard to the mechanism of NF-kappa B suppression, we excluded a possible role for glucocorticoid receptor alpha (GR alpha), peroxisome proliferators-activated receptor alpha/gamma (PPAR alpha or PPAR gamma), nuclear receptors (NRs) that are also known to inhibit inflammation by directly interfering with the activity of pro-inflammatory transcription factors. Interestingly, combining hop acids and selective agonists for GR alpha, PPAR alpha, or PPAR gamma resulted in additive inhibition of NF-kappa B activity after TNF treatment, which may open up new avenues for combinatorial anti-inflammatory strategies with fewer side effects. Finally, systemic administration of HBA efficiently inhibited acute local inflammation in vivo.
Please use this url to cite or link to this publication:
author
organization
alternative title
Hop bitter acids efficiently block inflammation independent of GR alpha, PPAR alpha, or PPAR gamma
year
type
journalArticle (original)
publication status
published
subject
keyword
ANTIINFLAMMATORY COMPOUNDS, NF-KAPPA-B, MOLECULAR-MECHANISMS, HUMULUS-LUPULUS L., PLANT-ORIGIN, GENE-REGULATION, GLUCOCORTICOID-RECEPTOR, NUCLEAR RECEPTORS, PROLIFERATOR-ACTIVATED RECEPTORS, CROSS-TALK
journal title
MOLECULAR NUTRITION & FOOD RESEARCH
Mol. Nutr. Food Res.
volume
53
issue
9
pages
1143 - 1155
Web of Science type
Article
Web of Science id
000270329600008
JCR category
FOOD SCIENCE & TECHNOLOGY
JCR impact factor
4.356 (2009)
JCR rank
1/117 (2009)
JCR quartile
1 (2009)
ISSN
1613-4125
DOI
10.1002/mnfr.200800493
language
English
UGent publication?
yes
classification
A1
copyright statement
I have transferred the copyright for this publication to the publisher
id
874006
handle
http://hdl.handle.net/1854/LU-874006
date created
2010-02-22 15:53:52
date last changed
2012-06-26 14:31:55
@article{874006,
  abstract     = {Hop (Humulus lupulus L.) is an essential ingredient of beer, where it provides the typical bitter taste, but is also applied in traditional folk medicine for sedative and antibacterial purposes. In this study, we demonstrate and compare the anti-inflammatory effect of various classes of hop bitter acids (HBA), including alpha-acids (AA), beta-acids (BA), and iso-alpha-acids (IAA), in fibroblasts, which are important players in the inflammatory response. All three studied classes of HBA blocked the turner necrosis factor alpha (TNF)-induced production of the cytokine IL6, and inhibited the transactivation of the pro-inflammatory transcription factors nuclear factor kappa B (NF-kappa B), activator protein-I (AP-1), and cAMP-response element-binding protein (CREB). In this respect, the six-membered ring compounds AA and BA showed equal potency, whereas the five-membered ring compounds, IAA, were effective only when used at higher concentrations. Furthermore, with regard to the mechanism of NF-kappa B suppression, we excluded a possible role for glucocorticoid receptor alpha (GR alpha), peroxisome proliferators-activated receptor alpha/gamma (PPAR alpha or PPAR gamma), nuclear receptors (NRs) that are also known to inhibit inflammation by directly interfering with the activity of pro-inflammatory transcription factors. Interestingly, combining hop acids and selective agonists for GR alpha, PPAR alpha, or PPAR gamma resulted in additive inhibition of NF-kappa B activity after TNF treatment, which may open up new avenues for combinatorial anti-inflammatory strategies with fewer side effects. Finally, systemic administration of HBA efficiently inhibited acute local inflammation in vivo.},
  author       = {Van Cleemput, Marjan and Heyerick, Arne and Libert, Claude and Swerts, Katrien and Philipp{\'e}, Jan and De Keukeleire, Denis and Haegeman, Guy and De Bosscher, Karolien},
  issn         = {1613-4125},
  journal      = {MOLECULAR NUTRITION \& FOOD RESEARCH},
  keyword      = {ANTIINFLAMMATORY COMPOUNDS,NF-KAPPA-B,MOLECULAR-MECHANISMS,HUMULUS-LUPULUS L.,PLANT-ORIGIN,GENE-REGULATION,GLUCOCORTICOID-RECEPTOR,NUCLEAR RECEPTORS,PROLIFERATOR-ACTIVATED RECEPTORS,CROSS-TALK},
  language     = {eng},
  number       = {9},
  pages        = {1143--1155},
  title        = {Hop bitter acids efficiently block inflammation independent of GR\ensuremath{\alpha}, PPAR\ensuremath{\alpha}, or PPAR\ensuremath{\gamma}},
  url          = {http://dx.doi.org/10.1002/mnfr.200800493},
  volume       = {53},
  year         = {2009},
}

Chicago
Van Cleemput, Marjan, Arne Heyerick, Claude Libert, Katrien Swerts, Jan Philippé, Denis De Keukeleire, Guy Haegeman, and Karolien De Bosscher. 2009. “Hop Bitter Acids Efficiently Block Inflammation Independent of GRα, PPARα, or PPARγ.” Molecular Nutrition & Food Research 53 (9): 1143–1155.
APA
Van Cleemput, M., Heyerick, A., Libert, C., Swerts, K., Philippé, J., De Keukeleire, D., Haegeman, G., et al. (2009). Hop bitter acids efficiently block inflammation independent of GRα, PPARα, or PPARγ. MOLECULAR NUTRITION & FOOD RESEARCH, 53(9), 1143–1155.
Vancouver
1.
Van Cleemput M, Heyerick A, Libert C, Swerts K, Philippé J, De Keukeleire D, et al. Hop bitter acids efficiently block inflammation independent of GRα, PPARα, or PPARγ. MOLECULAR NUTRITION & FOOD RESEARCH. 2009;53(9):1143–55.
MLA
Van Cleemput, Marjan, Arne Heyerick, Claude Libert, et al. “Hop Bitter Acids Efficiently Block Inflammation Independent of GRα, PPARα, or PPARγ.” MOLECULAR NUTRITION & FOOD RESEARCH 53.9 (2009): 1143–1155. Print.