title: Endocrine disrupting activities of the flavonoid nutraceuticals luteolin and quercetin.
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.
authors.affiliation: Department of Pathology, University of Colorado School of Medicine, Aurora, CO 80045, USA. steve.nordeen@ucdenver.edu
authors.forename: Steven K
authors.initials: SK
authors.lastname: Nordeen
authors.forename: Betty J
authors.initials: BJ
authors.lastname: Bona
authors.forename: David N
authors.initials: DN
authors.lastname: Jones
authors.forename: James R
authors.initials: JR
authors.lastname: Lambert
authors.forename: Twila A
authors.initials: TA
authors.lastname: Jackson
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy; D045744:Cell Line, Tumor; D019587:Dietary Supplements; D052244:Endocrine Disruptors / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D006801:Humans; D047311:Luteolin / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D011794:Quercetin / Q000009:adverse effects / Q000494:pharmacology*; D011980:Receptors, Progesterone / Q000737:chemistry / Q000378:metabolism
chemical_list: D052244:Endocrine Disruptors; D011980:Receptors, Progesterone; D011794:Quercetin; D047311:Luteolin