Characterization of Estrogenic and Androgenic Activities for Bisphenol A-like Chemicals (BPs): In Vitro Estrogen and Androgen Receptors Transcriptional Activation, Gene Regulation, and Binding Profiles.
Level 5 - mechanism / opinion, no new human data
In vitro bench research and molecular modeling without human or animal subjects
PubMed 31388671 · doi:10.1093/toxsci/kfz173
What was done
Researchers evaluated the endocrine-disrupting potential of 22 bisphenol A-like chemicals (BPs) using in vitro cell models. They assessed transcriptional activation, gene regulation, and binding profiles to determine whether these chemicals induce or inhibit estrogen receptor (ERα and ERβ) and androgen receptor (AR) activity, supplemented by molecular modeling analysis.
What was found
Twelve BPs (BPA, BPAF, BPZ, BPC, TMBPA, BPS, BPE, 4,4-BPF, BPAP, BPB, TCBPA, and PHBB) induced ERα and/or ERβ activity. Most of these ER-active compounds also functioned as AR antagonists, with the exceptions of BPS, TCBPA, and PHBB. Three chemicals acted as ER antagonists: BPP selectively inhibited ERβ activity, while BPS-MPE and 2,4-BPS selectively inhibited ERα activity. None of the 22 tested BPs induced AR agonist activity. No quantitative numerical values (e.g., EC50 or IC50 concentrations) were reported in the abstract.
Why it matters
Many industrial substitutes used to replace bisphenol A display similar or dual estrogenic and anti-androgenic activity in vitro, suggesting structural replacements may carry comparable endocrine-disrupting hazards.
Limits
The study is limited to in vitro cell systems and computational molecular modeling; it does not evaluate in vivo metabolism, tissue bioaccumulation, pharmacokinetics, or physiological endpoints in living organisms. Quantitative potency metrics and effect concentrations are omitted from the abstract.
Cited by
- supports Endocrine-disrupting chemicals interact directly with estrogen and androgen receptors, acting as anti-androgens or anti-estrogens by occupying receptor binding sites.