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Molecular Pharmacology

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Research ArticleArticle

The Green Tea Polyphenol (−)-Epigallocatechin-3-Gallate Blocks Nuclear Factor-κB Activation by Inhibiting IκB Kinase Activity in the Intestinal Epithelial Cell Line IEC-6

Fajun Yang, Helieh S. Oz, Shirish Barve, Willem J. S. de Villiers, Craig J. McClain and Gary W. Varilek
Molecular Pharmacology September 2001, 60 (3) 528-533;
Fajun Yang
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Helieh S. Oz
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Shirish Barve
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Willem J. S. de Villiers
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Craig J. McClain
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Gary W. Varilek
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Abstract

The IκB kinase complex (IKK) mediates activation of the transcription factor nuclear factor-κB (NF-κB). We previously showed that green tea polyphenols inhibited endotoxin-mediated tumor necrosis factor-α (TNFα) production by blocking NF-κB activation. In this study, we evaluated whether green tea polyphenols inhibit NF-κB by blocking IKK activity. We assessed IKK activity by detecting changes in phosphorylation of an IκBα-glutathioneS-transferase (GST) fusion protein. IEC-6 cells pretreated with an extract of green tea polyphenols (GrTPs; 0–0.4 mg/ml) had diminished TNFα-induced IKK and NF-κB activity. Of the various GrTPs, (−)-epigallocatechin-3-gallate (EGCG) was the most potent inhibitor. We next examined whether EGCG inhibited activated IKK. In cytosolic extracts of TNFα-stimulated cells, EGCG inhibited phosphorylation of IκBα-GST (IC50 > 18 μM) consistent with inhibition of IKK activity. Using other polyphenols, we showed that the gallate group was essential for inhibition, and antioxidants were ineffective in blocking activated IKK. Importantly, EGCG decreased IKK activity in cytosolic extracts of NIK transiently transfected cells. This latter finding showed that our findings were not related to nonspecific kinase activity. In conclusion, EGCG is an effective inhibitor of IKK activity. This may explain, at least in part, some of the reported anti-inflammatory and anticancer effects of green tea.

Footnotes

  • This work was supported by National Institutes of Health Grants KO8-DK02401-01A, MO1-RR02602, IPO1-NS31220-01A1, and RO1-AA010762 and by the Veterans Administration.

  • Abbreviations:
    EC
    epicatechin
    EGC
    (−)-epigallocatechin
    ECG
    (−)-epicatechin-3-gallate
    EGCG
    (−)-epigallocatechin-3-gallate
    TNF
    tumor necrosis factor
    LPS
    lipopolysaccharide
    NF-κB
    nuclear factor-κB
    IKK
    IκB kinase
    PDTC
    pyrrolidinedithiocarbamate
    NAC
    N-acetyl cysteine
    GrTP
    green tea polyphenols
    GST
    glutathione S-transferase
    EMSA
    electrophoretic mobility shift assay
    CINC
    cytokine-induced neutrophil chemoattractant
    NIK
    NF-κB-inducing kinase
    • Received May 10, 2001.
    • Accepted May 21, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 60 (3)
Molecular Pharmacology
Vol. 60, Issue 3
1 Sep 2001
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Research ArticleArticle

The Green Tea Polyphenol (−)-Epigallocatechin-3-Gallate Blocks Nuclear Factor-κB Activation by Inhibiting IκB Kinase Activity in the Intestinal Epithelial Cell Line IEC-6

Fajun Yang, Helieh S. Oz, Shirish Barve, Willem J. S. de Villiers, Craig J. McClain and Gary W. Varilek
Molecular Pharmacology September 1, 2001, 60 (3) 528-533;

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Research ArticleArticle

The Green Tea Polyphenol (−)-Epigallocatechin-3-Gallate Blocks Nuclear Factor-κB Activation by Inhibiting IκB Kinase Activity in the Intestinal Epithelial Cell Line IEC-6

Fajun Yang, Helieh S. Oz, Shirish Barve, Willem J. S. de Villiers, Craig J. McClain and Gary W. Varilek
Molecular Pharmacology September 1, 2001, 60 (3) 528-533;
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