Xanthohumol from Hop (Humulus lupulus L.) Is an Efficient Inhibitor of Monocyte Chemoattractant Protein-1 and Tumor Necrosis Factor-a Release in LPS-Stimulated RAW 264.7 Mouse Macrophages and U937 Human Monocytes

E. Lupinacci, J. Meijerink, J.P. Vincken, B. Gabriele, H. Gruppen, R.F. Witkamp

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Abstract

Activated macrophages in adipose tissue play a major role in the chronic inflammatory process that has been linked to the complications of overweight and obesity. The hop plant (Humulus lupulus L.) has been described to possess both anti-inflammatory and antidiabetic effects. In the present study, the chemical composition of a hop crude extract (HCE) was investigated by ultrahigh-performance liquid chromatography (UHPLC). Next, HCE and various fractions obtained by preparative HPLC were tested for their ability to inhibit production of two pro-inflammatory cytokines, monocyte chemoattractant protein-1 (MCP-1, CCL2) and tumor necrosis factor-a (TNF-a), which play crucial roles in the complications of obesity. The hop chalcone xanthohumol was found to be the most potent inhibitor of both cytokines in LPS-activated RAW 264.7 mouse macrophages and U937 human monocytes. Moreover, other constituents, namely, iso-a-acids, in combination with the ß-acid hulupone, showed a moderate but selective inhibitory activity only on MCP-1 release. These findings underscore the potential health effects of hop and support further optimization, selection, and use of this plant.
Original languageEnglish
Pages (from-to)7274-7281
JournalJournal of Agricultural and Food Chemistry
Volume57
Issue number16
DOIs
Publication statusPublished - 2009

Fingerprint

Humulus lupulus
Humulus
Chemokine CCL2
Macrophages
hops
Complex Mixtures
monocytes
tumor necrosis factor-alpha
Monocytes
macrophages
Tumor Necrosis Factor-alpha
Cytokines
Chalcone
Acids
Liquid chromatography
mice
Hypoglycemic Agents
1-methylcyclopropene
Anti-Inflammatory Agents
Health

Keywords

  • ionization mass-spectrometry
  • activated-receptor-alpha
  • nf-kappa-b
  • adipose-tissue
  • insulin-resistance
  • liquid-chromatography
  • leukemia-cells
  • obese subjects
  • acids
  • beer

Cite this

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title = "Xanthohumol from Hop (Humulus lupulus L.) Is an Efficient Inhibitor of Monocyte Chemoattractant Protein-1 and Tumor Necrosis Factor-a Release in LPS-Stimulated RAW 264.7 Mouse Macrophages and U937 Human Monocytes",
abstract = "Activated macrophages in adipose tissue play a major role in the chronic inflammatory process that has been linked to the complications of overweight and obesity. The hop plant (Humulus lupulus L.) has been described to possess both anti-inflammatory and antidiabetic effects. In the present study, the chemical composition of a hop crude extract (HCE) was investigated by ultrahigh-performance liquid chromatography (UHPLC). Next, HCE and various fractions obtained by preparative HPLC were tested for their ability to inhibit production of two pro-inflammatory cytokines, monocyte chemoattractant protein-1 (MCP-1, CCL2) and tumor necrosis factor-a (TNF-a), which play crucial roles in the complications of obesity. The hop chalcone xanthohumol was found to be the most potent inhibitor of both cytokines in LPS-activated RAW 264.7 mouse macrophages and U937 human monocytes. Moreover, other constituents, namely, iso-a-acids, in combination with the {\ss}-acid hulupone, showed a moderate but selective inhibitory activity only on MCP-1 release. These findings underscore the potential health effects of hop and support further optimization, selection, and use of this plant.",
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author = "E. Lupinacci and J. Meijerink and J.P. Vincken and B. Gabriele and H. Gruppen and R.F. Witkamp",
year = "2009",
doi = "10.1021/jf901244k",
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journal = "Journal of Agricultural and Food Chemistry",
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publisher = "American Chemical Society",
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TY - JOUR

T1 - Xanthohumol from Hop (Humulus lupulus L.) Is an Efficient Inhibitor of Monocyte Chemoattractant Protein-1 and Tumor Necrosis Factor-a Release in LPS-Stimulated RAW 264.7 Mouse Macrophages and U937 Human Monocytes

AU - Lupinacci, E.

AU - Meijerink, J.

AU - Vincken, J.P.

AU - Gabriele, B.

AU - Gruppen, H.

AU - Witkamp, R.F.

PY - 2009

Y1 - 2009

N2 - Activated macrophages in adipose tissue play a major role in the chronic inflammatory process that has been linked to the complications of overweight and obesity. The hop plant (Humulus lupulus L.) has been described to possess both anti-inflammatory and antidiabetic effects. In the present study, the chemical composition of a hop crude extract (HCE) was investigated by ultrahigh-performance liquid chromatography (UHPLC). Next, HCE and various fractions obtained by preparative HPLC were tested for their ability to inhibit production of two pro-inflammatory cytokines, monocyte chemoattractant protein-1 (MCP-1, CCL2) and tumor necrosis factor-a (TNF-a), which play crucial roles in the complications of obesity. The hop chalcone xanthohumol was found to be the most potent inhibitor of both cytokines in LPS-activated RAW 264.7 mouse macrophages and U937 human monocytes. Moreover, other constituents, namely, iso-a-acids, in combination with the ß-acid hulupone, showed a moderate but selective inhibitory activity only on MCP-1 release. These findings underscore the potential health effects of hop and support further optimization, selection, and use of this plant.

AB - Activated macrophages in adipose tissue play a major role in the chronic inflammatory process that has been linked to the complications of overweight and obesity. The hop plant (Humulus lupulus L.) has been described to possess both anti-inflammatory and antidiabetic effects. In the present study, the chemical composition of a hop crude extract (HCE) was investigated by ultrahigh-performance liquid chromatography (UHPLC). Next, HCE and various fractions obtained by preparative HPLC were tested for their ability to inhibit production of two pro-inflammatory cytokines, monocyte chemoattractant protein-1 (MCP-1, CCL2) and tumor necrosis factor-a (TNF-a), which play crucial roles in the complications of obesity. The hop chalcone xanthohumol was found to be the most potent inhibitor of both cytokines in LPS-activated RAW 264.7 mouse macrophages and U937 human monocytes. Moreover, other constituents, namely, iso-a-acids, in combination with the ß-acid hulupone, showed a moderate but selective inhibitory activity only on MCP-1 release. These findings underscore the potential health effects of hop and support further optimization, selection, and use of this plant.

KW - ionization mass-spectrometry

KW - activated-receptor-alpha

KW - nf-kappa-b

KW - adipose-tissue

KW - insulin-resistance

KW - liquid-chromatography

KW - leukemia-cells

KW - obese subjects

KW - acids

KW - beer

U2 - 10.1021/jf901244k

DO - 10.1021/jf901244k

M3 - Article

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