The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
In vitro study on the agonistic and antagonistic activities of bisphenol-S and other bisphenol-A congeners and derivatives via nuclear receptors
Open accessAbstract
Bisphenols are a group of chemicals structurally similar to bisphenol-A (BPA) in current use as the primary raw material in the production of polycarbonate and epoxy resins. Some bisphenols are intended to replace BPA in several industrial applications. This is the case of bisphenol-S (BPS), which has an excellent stability at high temperature and resistance to sunlight. Studies on the endocrine properties of BPS have focused on its interaction with human estrogen receptor alpha (hERα), but information on its interaction with other nuclear receptors is scarce. The aim of this study was to investigate interactions of BPS, BPF, BPA and its halogenated derivatives, tetrachlorobisphenol A (TCBPA), and tetrabromobisphenol A (TBBPA), with human estrogen receptors (hERα and hERβ), androgen receptor (hAR), and pregnane X receptor (hPXR), using a panel of in vitro bioassays based on competitive binding to nuclear receptors (NRs), reporter gene expression, and cell proliferation assessment. BPS, BPF, and BPA efficiently activated both ERs, while TCBPA behaved as weak hERα agonist. Unlike BPF and BPA, BPS was more active in the hERβ versus hERα assay. BPF and BPA were full hAR antagonists (BPA>BPF), whereas BPA and BPS were weak hAR agonists. Only BPA, TCBPA, and TBBPA, were hPXR agonists (TCBPA>TBBPA>BPA). These findings provide evidence that BPA congeners and derivatives disrupt multiple NRs and may therefore interfere with the endocrine system. Hence, further research is needed to evaluate the potential endocrine-disrupting activity of putative BPA substitutes.
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Cites
Hormones and endocrine-disrupting chemicals: low-dose effects and nonmonotonic dose responses
Vandenberg, L. N., Colborn, T., Hayes, T. B., Heindel, J. J., Jacobs, D. R., Lee, D.-H., Shioda, T., Soto, A. M., vom Saal, F. S., Welshons, W. V., et al. (2012) · Endocrine Reviews · doi:10.1210/er.2011-1050 · Cited by 3,209
Exposure of the U.S. Population to Bisphenol A and 4- tertiary -Octylphenol: 2003–2004
Calafat, A. M., Ye, X., Wong, L.-Y., Reidy, J. A., & Needham, L. L. (2008) · Environmental Health Perspectives · doi:10.1289/ehp.10753 · Cited by 1,743
Thyroid Hormone Action Is Disrupted by Bisphenol A as an Antagonist
Moriyama, K., Tagami, T., Akamizu, T., Usui, T., Saijo, M., Kanamoto, N., Hataya, Y., Shimatsu, A., Kuzuya, H., & Nakao, K. (2002) · The Journal of Clinical Endocrinology & Metabolism · doi:10.1210/jc.2002-020209 · Cited by 812
Overview of nomenclature of nuclear receptors
Germain, P., Staels, B., Dacquet, C., Spedding, M., & Laudet, V. (2006) · Pharmacological Reviews · doi:10.1124/pr.58.4.2 · Cited by 688 · cited 1×
“NRs are members of the steroid receptor superfamily, a large family of ligand-dependent transcriptional factors (Germain et al., 2006).”
BackgroundDelfosse, V., Grimaldi, M., Pons, J.-L., Boulahtouf, A., le Maire, A., Cavailles, V., Labesse, G., Bourguet, W., & Balaguer, P. (2012) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1203574109 · Cited by 405 · cited 3×
“In this regard, when BPS was tested in HELN cells stably transfected with AF-1 deleted hERs, deletion of the A/B domain in hERβ markedly altered its transactivation potency, indicating that BPS is dependent on AF-1 (Delfosse et al., 2012).”
BackgroundNuclear receptors CAR and PXR: Molecular, functional, and biomedical aspects
di Masi, A., Marinis, E. D., Ascenzi, P., & Marino, M. (2009) · Molecular Aspects of Medicine · doi:10.1016/j.mam.2009.04.002 · Cited by 288
Cited by
Bisphenol Analogues Other Than BPA: Environmental Occurrence, Human Exposure, and Toxicity—A Review
Chen, D., Kannan, K., Tan, H., Zheng, Z., Feng, Y.-L., Wu, Y., & Widelka, M. (2016) · Environmental Science & Technology · doi:10.1021/acs.est.5b05387 · Cited by 1,704
Rochester, J. R., & Bolden, A. L. (2015) · Environmental Health Perspectives · doi:10.1289/ehp.1408989 · Cited by 1,524
Moreman, J., Lee, O., Trznadel, M., David, A., Kudoh, T., & Tyler, C. R. (2017) · Environmental Science & Technology · doi:10.1021/acs.est.7b03283 · Cited by 527
Potential Mechanisms of Bisphenol A (BPA) Contributing to Human Disease
Cimmino, I., Fiory, F., Perruolo, G., Miele, C., Beguinot, F., Formisano, P., & Oriente, F. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21165761 · Cited by 478
Effects of bisphenol A and its analogs on reproductive health: A mini review
Siracusa, J. S., Yin, L., Measel, E., Liang, S., & Yu, X. (2018) · Reproductive Toxicology · doi:10.1016/j.reprotox.2018.06.005 · Cited by 341
Metadata
- Authors
- Molina-Molina, J.-M., Amaya, E., Grimaldi, M., Sáenz, J.-M., Real, M., Fernández, M. F., Balaguer, P., & Olea, N.
- Venue
- Toxicology and Applied Pharmacology
- Publisher
- Elsevier BV
- Published
- 2013-10
- Volume
- 272
- Issue
- 1
- Pages
- 127-136
- ISSN
- 0041-008X (ISSN-L)
- OpenAlex
- W1967655383
- Cited by
- 374
- References
- 6
- FWCI
- 17.26
- Type
- journal article
- Language
- en
- Open access
- green
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- Molina-Molina, J.-M., Amaya, E., Grimaldi, M., Sáenz, J.-M., Real, M., Fernández, M. F., Balaguer, P., & Olea, N. (2013). In vitro study on the agonistic and antagonistic activities of bisphenol-S and other bisphenol-A congeners and derivatives via nuclear receptors. Toxicology and Applied Pharmacology. https://doi.org/10.1016/j.taap.2013.05.015
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