Endocrine disrupting activities of the flavonoid nutraceuticals luteolin and quercetin

Horm Cancer. 2013 Oct;4(5):293-300. doi: 10.1007/s12672-013-0150-1. Epub 2013 Jul 9.

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Breast Neoplasms / drug therapy
  • Cell Line, Tumor
  • Dietary Supplements*
  • Endocrine Disruptors / adverse effects
  • Endocrine Disruptors / chemistry
  • Endocrine Disruptors / pharmacology*
  • Female
  • Humans
  • Luteolin / adverse effects
  • Luteolin / chemistry
  • Luteolin / pharmacology*
  • Models, Molecular
  • Quercetin / adverse effects
  • Quercetin / pharmacology*
  • Receptors, Progesterone / chemistry
  • Receptors, Progesterone / metabolism

Substances

  • Endocrine Disruptors
  • Receptors, Progesterone
  • Quercetin
  • Luteolin