What question did this study set out to answer?

To determine whether hydroxylated metabolites of the flame-retardant PBDE mixture DE-71 bind to and alter the transcriptional activity of estrogen receptor-alpha (ER-alpha).

May 26, 2008Environmental Health PerspectivesOpen Access

Hydroxylated Metabolites of the Polybrominated Diphenyl Ether Mixture DE-71 Are Weak Estrogen Receptor-α Ligands

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To determine whether hydroxylated metabolites of the flame-retardant PBDE mixture DE-71 bind to and alter the transcriptional activity of estrogen receptor-alpha (ER-alpha).
Assayed estrogenicity via competitive displacement of 3H-estradiol (3H-E2) from recombinant human ER-alpha.
Measured ER-alpha-mediated transcriptional activation using an ERE-luciferase reporter gene assay in cultured cells.
Tested parent DE-71, in vitro rat liver microsomal metabolites of DE-71, and six specific individual hydroxylated PBDE (OH-PBDE) congeners alone and in combination with estradiol.
Parent DE-71 did not displace 3H-E2 from ER-alpha, whereas all six OH-PBDE metabolites displaced 3H-E2, with para-hydroxylated metabolites displaying a 10- to 30-fold higher affinity than ortho-hydroxylated PBDEs.
Metabolized DE-71 induced ERE-luciferase reporter gene activity, and one para-OH-PBDE produced a maximal induction 30% higher than estradiol alone.
Co-treatment of estradiol with DE-71 or specific metabolites yielded additive reporter activation exceeding either compound alone, while two ortho-OH-PBDEs showed antiestrogenic properties.

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Implication

In vitro study demonstrates hydroxylated PBDE metabolites bind ER-alpha and alter gene transcription, suggesting flame retardant endocrine disruption via metabolic activation.

Cite This Study

Mercado-Feliciano et al. (2008) studied this question.

synapsesocial.com/papers/6a9cb6cd48effd99aa57af69 https://doi.org/10.1289/ehp.11343

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Implication

In vitro study demonstrates hydroxylated PBDE metabolites bind ER-alpha and alter gene transcription, suggesting flame retardant endocrine disruption via metabolic activation.

Hydroxylated Metabolites of the Polybrominated Diphenyl Ether Mixture DE-71 Are Weak Estrogen Receptor-α Ligands

Key Points

Discussion

Implication

Cite This Study

Hydroxylated Metabolites of the Polybrominated Diphenyl Ether Mixture DE-71 Are Weak Estrogen Receptor-α Ligands

Key Points

Discussion

Implication

Cite This Study

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