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U.S. Department of Health and Human Services

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Food Chem Toxicol 2017 Aug;106(Pt A):193-201

Metabolism and pharmacokinetics of zearalenone following oral and intravenous administration in juvenile female pigs.

Fleck SC, Churchwell MI, Doerge DR


Zearalenone (ZEN) is a well-studied mycotoxin whose potent estrogenic properties have been used by international regulatory bodies to set health-based guidance values for ZEN exposure in grain-based foods from changes in hormonally responsive tissues of juvenile female pigs. The role of metabolism in determining estrogenic responses in vivo is a major uncertainty in inter-species extrapolation to humans and in assessing the potential for added susceptibility in sensitive subpopulations. This study evaluated the metabolism of ZEN and pharmacokinetics in approximately 2 month-old female pigs using oral and intravenous dosing. The absolute bioavailability (AUCoral/AUCIV) of receptor-active ZEN aglycone was 1.8 +/- 0.80%, consistent with extensive pre-systemic Phase II conjugation. Reductive metabolism to alpha-zearalenol (alpha-ZEL) was extensive, with smaller amounts of beta-ZEL. When combined with its higher binding affinity, relative to ZEN and beta-ZEL, alpha- ZEL was the predominant contributor to total estrogen receptor ligand activity ( approximately 90%) after oral dosing with ZEN. The apparent similarities of reductive and Phase II conjugation metabolism of ZEN between pigs and humans supports the use of juvenile female pigs as a sensitive model for risk assessments of estrogenic effects from dietary ZEN.

Category: Journal Article
PubMed ID: #28552786 DOI: 10.1016/j.fct.2017.05.048
Includes FDA Authors from Scientific Area(s): Toxicological Research
Entry Created: 2017-06-04 Entry Last Modified: 2017-07-30