Estrogenic potency of bisphenol S, polyethersulfone and their metabolites generated by the rat liver S9 fractions on a MVLN cell using a luciferase reporter gene assay

Reprod Biol Endocrinol. 2014 Nov 4:12:102. doi: 10.1186/1477-7827-12-102.

Abstract

Background: Bisphenol A (BPA) is an applied chemical that is used in many industrial fields and is a potential endocrine disruption chemical (EDC) that is found in the environment. Bisphenol S (BPS) and polyethersulfone (PES) have been suggested as putative BPA alternatives. In this study, the estrogenic potency induced by the binding of 17-beta-estradiol (E2), BPA, BPS, PES and their metabolites formed by the rat liver S9 fraction to the human estrogen receptor (ER) was estimated.

Methods: We used an in vitro bioassay based on the luciferase reporter assay in MVLN cells to evaluate the estrogenic activity of 17-beta-estradiol (E2), BPA, BPS, PES (E2: 0.001 to 0.3 nM; BPA, BPS and PES: 0.0001 to 5 microM) and their metabolites (E2: 0.05 microM; BPA, BPS and PES: 0.1 mM) according to incubation times (0, 20 and 40 min). After chemical treatment to MVLN cells for 72 hrs, and the cell viability and luciferase intensity induced were estimated, from which the estrogenic activity of the chemicals tested was evaluated.

Results: BPA and BPS induced estrogenic activity whereas PES did not show any estrogenic activity in the concentrations tested. In an in vitro assay of metabolites, BPA metabolites displayed comparable estrogenic activity with BPA and metabolites of both BPS and PES showed increasing estrogenic activity.

Conclusions: The results suggest that the metabolites of BPS and PES have estrogenic potential and the need for the assessment of both chemicals and their metabolites in other EDC evaluation studies. The estrogenic potency of PES and its metabolites is the first report in our best knowledge.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biotransformation
  • Cell Survival / drug effects
  • Endocrine Disruptors / metabolism
  • Endocrine Disruptors / pharmacology*
  • Estrogens / metabolism
  • Estrogens / pharmacology*
  • Gene Expression Regulation, Neoplastic / drug effects
  • Genes, Reporter / drug effects
  • Humans
  • Kinetics
  • Luciferases, Firefly / genetics
  • Luciferases, Firefly / metabolism
  • MCF-7 Cells
  • Microsomes, Liver / metabolism*
  • Phenols / metabolism
  • Phenols / pharmacology*
  • Polymers / metabolism
  • Polymers / pharmacology*
  • Rats
  • Receptors, Estrogen / chemistry
  • Receptors, Estrogen / metabolism
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Response Elements / drug effects*
  • Sulfones / metabolism
  • Sulfones / pharmacology*
  • Toxicokinetics

Substances

  • Endocrine Disruptors
  • Estrogens
  • Phenols
  • Polymers
  • Receptors, Estrogen
  • Recombinant Proteins
  • Sulfones
  • polyether sulfone
  • bis(4-hydroxyphenyl)sulfone
  • Luciferases, Firefly