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Effect of flavonoids and vitamin E on cyclooxygenase-2 (COX-2) transcription

Karen A O'Leary1, Sonia de Pascual-Teresa, Sonia de Pascual-Tereasa

  • 1Institute of Food Research, Norwich Research Park, Colney, Norwich NR4 7UA, UK.

Mutation Research
|July 1, 2004
PubMed

Insights

Flavonoids like quercetin can reduce cyclooxygenase-2 (COX-2) mRNA expression and inhibit its activity, potentially offering anti-cancer benefits. Vitamin E derivatives inhibit COX-2 activity post-transcriptionally.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Cyclooxygenase-2 (COX-2) produces prostaglandin E2, crucial in inflammation, cancer, and cardiovascular disease.
  • Flavonoids are known to inhibit COX-2 activity, but their role in transcriptional regulation is also significant.
  • Understanding COX-2 regulation is vital for developing therapeutic strategies against inflammatory diseases and cancer.

Purpose of the Study:

  • To review the literature on flavonoid-mediated transcriptional regulation of COX-2.
  • To investigate the effects of quercetin conjugates and Vitamin E (tocopherols) on COX-2 expression and activity.
  • To elucidate the mechanisms by which these compounds modulate COX-2.

Main Methods:

  • Review of existing literature on flavonoids and COX-2 transcription.
  • Experimental analysis of quercetin, quercetin conjugates, and tocopherols in colon cancer (Caco2) cells.
  • Measurement of COX-2 mRNA expression and COX-2 activity.

Main Results:

  • Quercetin, quercetin 3-glucuronide, quercetin 3'-sulfate, and 3'methylquercetin 3-glucuronide reduced COX-2 mRNA expression in Caco2 cells.
  • Quercetin and quercetin 3'-sulfate inhibited COX-2 activity, while quercetin 3-glucuronide and 3'methylquercetin 3-glucuronide did not.
  • Tocopherols inhibited COX-2 activity post-transcriptionally without affecting mRNA levels, unlike quercetin and its conjugates which impacted both transcription and activity.

Conclusions:

  • Quercetin and certain quercetin conjugates modulate both COX-2 transcription and activity.
  • Tocopherols primarily inhibit COX-2 activity post-transcriptionally.
  • Flavonoid-induced modulation of COX-2 transcription represents a potential mechanism in anti-carcinogenesis.

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