Original Paper

Hormones and Cancer

, Volume 4, Issue 5, pp 293-300

Endocrine Disrupting Activities of the Flavonoid Nutraceuticals Luteolin and Quercetin

  • Steven K. NordeenAffiliated withDepartment of Pathology, University of Colorado School of Medicine Email author 
  • , Betty J. BonaAffiliated withDepartment of Pathology, University of Colorado School of Medicine
  • , David N. JonesAffiliated withDepartment of Pharmacology, University of Colorado School of Medicine
  • , James R. LambertAffiliated withDepartment of Pathology, University of Colorado School of Medicine
  • , Twila A. JacksonAffiliated withDepartment of Obstetrics and Gynecology, University of Colorado School of Medicine

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Abstract

Dietary plant flavonoids have been proposed to contribute to cancer prevention, neuroprotection, and cardiovascular health through their anti-oxidant, anti-inflammatory, pro-apoptotic, and antiproliferative activities. As a consequence, flavonoid supplements are aggressively marketed by the nutraceutical industry for many purposes, including pediatric applications, despite inadequate understanding of their value and drawbacks. We show that two flavonoids, luteolin and quercetin, are promiscuous endocrine disruptors. These flavonoids display progesterone antagonist activity beneficial in a breast cancer model but deleterious in an endometrial cancer model. Concurrently, luteolin possesses potent estrogen agonist activity while quercetin is considerably less effective. These results highlight the promise and peril of flavonoid nutraceuticals and suggest caution in supplementation beyond levels attained in a healthy, plant-rich diet.