Bisphenol AF and Bisphenol B Exert Higher Estrogenic Effects than Bisphenol A via G Protein-Coupled Estrogen Receptor Pathway

Cao, Lin-Ying; Ren, Xiaomin; Li, Chuan-Hai; Zhang, Jing; Qin, Weiping; Yang, Yu; Wan, Bin; Guo, Liang-Hong

doi:10.1021/acs.est.7b03336

Cited by 123 publications

(76 citation statements)

References 40 publications

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“…For example, BPAF was shown to be the most potent xeno‐oestrogen compared to other bisphenols, including BPA, in a ERE transgenic zebrafish strain 73 . In vitro, BPAF exhibited oestrogenic activity, higher than BPA, in a various cell lines assays 29,81 and this higher oestrogenic activity was assigned to the presence of an hydrophobic group in the BPAF structure 29,82 . For all these reasons, the use of BPAF, as a BPA analogue, should be reconsidered and above all because BPAF has become an emerging environmental pollutant 83,84 .…”

Section: Discussionmentioning

confidence: 99%

Impacts of bisphenol A analogues on zebrafish post‐embryonic brain

Coumailleau

Trempont

Pellegrini

et al. 2020

J Neuroendocrinology

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Bisphenol A (BPA) is a widely studied and well‐recognised endocrine‐disrupting chemical, and one of the current issues is its safe replacement by various analogues. Using larva zebrafish as a model, the present study reveals that moderate and chronic exposure to BPA analogues such as bisphenol S, bisphenol F and bisphenol AF may also affect vertebrate neurodevelopment and locomotor activity. Several parameters of embryo‐larval development were investigated, such as mortality, hatching, number of mitotically active cell, as defined by 5‐bromo‐2'‐deoxyuridine incorporation and proliferative cell nuclear antigen labelling, aromatase B protein expression in radial glial cell and locomotor activity. Our results show that exposure to several bisphenol analogues induced an acceleration of embryo hatching rate. At the level of the developing brain, a strong up‐regulation of the oestrogen‐sensitive Aromatase B was also detected in the hypothalamic region. This up‐regulation was not associated with effects on the numbers of mitotically active progenitors nor differentiated neurones in the preoptic area and in the nuclear recessus posterior of the hypothalamus zebrafish larvae. Furthermore, using a high‐throughput video tracking system to monitor locomotor activity in zebrafish larvae, we show that some bisphenol analogues, such as bisphenol AF, significantly reduced locomotor activity following 6 days of exposure. Taken together, our study provides evidence that BPA analogues can also affect the neurobehavioural development of zebrafish.

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Section: Discussionmentioning

confidence: 99%

Impacts of bisphenol A analogues on zebrafish post‐embryonic brain

Coumailleau

Trempont

Pellegrini

et al. 2020

J Neuroendocrinology

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“…Although BPA is partly substituted with bisphenol F (BPF), it has recently been shown in in vitro and in vivo studies that BPF is more estrogenic than BPA [ 58 , 59 , 60 ]. Similarly, bisphenol S and bisphenol B are hormonally active in the same way as BPA or even to a greater extent [ 60 , 61 ]. No such studies were evident in the public domain for the construction sector, although exposure to EDs is likely to occur in those employed in finishing and recovery activities, based on emissions data from materials such as vinyl wall and floor coverings [ 62 , 63 ].…”

Section: Discussion On Eds In Construction and Plastic Industry Tementioning

confidence: 99%

Potential Health Risk of Endocrine Disruptors in Construction Sector and Plastics Industry: A New Paradigm in Occupational Health

Fučić

Galea

Duca

et al. 2018

IJERPH

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Endocrine disruptors (EDs) belong to large and diverse groups of agents that may cause multiple biological effects associated with, for example, hormone imbalance and infertility, chronic diseases such as diabetes, genome damage and cancer. The health risks related with the exposure to EDs are typically underestimated, less well characterized, and not regulated to the same extent as, for example, carcinogens. The increased production and utilization of identified or suspected EDs in many different technological processes raises new challenges with respect to occupational exposure settings and associated health risks. Due to the specific profile of health risk, occupational exposure to EDs demands a new paradigm in health risk assessment, redefinition of exposure assessment, new effects biomarkers for occupational health surveillance and definition of limit values. The construction and plastics industries are among the strongest economic sectors, employing millions of workers globally. They also use large quantities of chemicals that are known or suspected EDs. Focusing on these two industries, this short communication discusses: (a) why occupational exposure to EDs needs a more specific approach to occupational health risk assessments, (b) identifies the current knowledge gaps, and (c) identifies and gives a rationale for a future occupational health paradigm, which will include ED biomarkers as a relevant parameter in occupational health risk assessment, surveillance and exposure prevention.

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“…Since bisphenols are detected in human biological samples ( Yang et al ., 2014 ), BPAF is able to evoke its unwanted effects on breast tissues through interactions with ERβ rather than ERα. Although we mainly focused on the interaction between BPAF and ERβ1 (genomic effects), one of the alternatively spliced transcript variants of the ESR2 gene, to comprehensively understand the biological (toxicological) profiles of BPAF, further studies that consider the involvement of the G protein-coupled estrogen receptor pathway, which has recently been reported to be involved in BPAF-mediated non-genomic estrogenic effects in breast cancer SK-BR-3 cells ( Cao et al ., 2017 ), are needed. Fig.…”

Section: Effects Of An Er β Antagonist On Bpaf-mediated Transcriptionmentioning

confidence: 99%

Bisphenol AF as an activator of human estrogen receptor β1 (ERβ1) in breast cancer cell lines

et al. 2018

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Bisphenol AF (BPAF) is now recognized as one of the replacements for bisphenol A (BPA). Although considerable experimental evidence suggests that BPA is an endocrine-disrupting chemical, the toxicological profile of BPAF has been investigated in less detail than that of BPA, even at the in vitro level. BPAF has been established as an activator of estrogen receptor α (ERα) in many cell lines; however, controversy surrounds its effects on the other isoform, ERβ (i.e., whether it functions as a stimulator). Five human ERβ isoforms have been cloned and characterized. Of these, we focused on the interactions between BPAF and the two isoforms, ERβ1 and ERβ2. We demonstrated that i) BPAF functioned as a stimulator of ERβ1 (and ERα), which is transiently expressed in the two types of human breast cancer cells (MDA-MB-231 and SK-BR-3 cells) (EC values for ERβ: 6.87 nM and 2.58 nM, respectively, and EC values for ERα: 24.7 nM and 181 nM, respectively), ii) the stimulation of ERβ1 by BPAF (1-25 nM) was abrogated by PHTPP (an ERβ selective antagonist), and iii) the expression of ERβ1 and ERβ2 was not modulated by BPAF at nanomolar concentrations up to 25 nM. These results indicate that BPAF activates not only human ERα, but also the ERβ1 isoform in breast cancer cells, and exhibits higher activation potency for ERβ1.

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Bisphenol AF and Bisphenol B Exert Higher Estrogenic Effects than Bisphenol A via G Protein-Coupled Estrogen Receptor Pathway

Cited by 123 publications

References 40 publications

Impacts of bisphenol A analogues on zebrafish post‐embryonic brain

Impacts of bisphenol A analogues on zebrafish post‐embryonic brain

Potential Health Risk of Endocrine Disruptors in Construction Sector and Plastics Industry: A New Paradigm in Occupational Health

Bisphenol AF as an activator of human estrogen receptor β1 (ERβ1) in breast cancer cell lines

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