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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.

Kang JS, Choi JS, Kim WK, Lee YJ, Park JW - Reprod. Biol. Endocrinol. (2014)

Bottom Line: BPA and BPS induced estrogenic activity whereas PES did not show any estrogenic activity in the concentrations tested.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.

View Article: PubMed Central - PubMed

Affiliation: Gyeongnam Department of Environmental Toxicology and Chemistry, Korea Institute of Toxicology, Jin-Ju, Gyeongnam, Republic of Korea. jwpark@kitox.re.kr.

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.

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Related in: MedlinePlus

The luciferase activity of BPA, BPS and PES according to the exposure concentrations. The activity ratio was measured by compare to the luciferase activity of the highest concentration (E2max). Data represent the mean ± SD were statistically analyzed by ANOVA followed by the Least Significant Difference (LSD) test (p <0.05). All tests were performed in triplicate.
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Fig2: The luciferase activity of BPA, BPS and PES according to the exposure concentrations. The activity ratio was measured by compare to the luciferase activity of the highest concentration (E2max). Data represent the mean ± SD were statistically analyzed by ANOVA followed by the Least Significant Difference (LSD) test (p <0.05). All tests were performed in triplicate.

Mentions: From the several concentrations of E2, BPA, BPS and PES, the luciferase activities (RLU, relative light unit) were obtained and were calculated for REP against the maximum luciferase activity of 0.3 nM E2, which was the maximum tested concentration of E2 (E2max). In the highest concentration (5 μM) of BPA, BPS and PES, the death cell (in BPA and BPS) and chemical aggregation (in PES) were observed, thus the result in this concentration was excluded to calculate REP. The relationship of E2 was determined by comparing to E2max using the REP values (see Additional file 1: Figure S1), from which each EC20, EC50 and EC80 value was estimated (Table 1). The estrogenic activity of BPA increased by a dose–response manner statistically and that of BPS also was shown the increasing tendency although there was little of statistical difference (Figure 2). No estrogenic activity was observed at two low concentrations (1 and 0.1 nM) of BPA and BPS. PES showed no estrogenic activity in all of the concentration ranges tested (data was not shown). In the highest concentration of both BPA and BPS (0.5 μM), 48.8% REP of BPA and 19.2% REP of BPS were shown, respectively (Figure 2 and Table 2). By comparing these values to the respective EC values of E2, REP20, REP50 and REP80 of both BPA and BPS were estimated, and were summarized in Table 2. The REP50 of BPA and BPS was 4.25 × 10−5 and 4.09 × 10−9, respectively, and REP20–80 was 2.17 × 10−4 to 8.32 × 10−6 and 2.25 × 10−6 to 7.41 × 10−12, respectively.Table 1


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.

Kang JS, Choi JS, Kim WK, Lee YJ, Park JW - Reprod. Biol. Endocrinol. (2014)

The luciferase activity of BPA, BPS and PES according to the exposure concentrations. The activity ratio was measured by compare to the luciferase activity of the highest concentration (E2max). Data represent the mean ± SD were statistically analyzed by ANOVA followed by the Least Significant Difference (LSD) test (p <0.05). All tests were performed in triplicate.
© Copyright Policy - open-access
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4232735&req=5

Fig2: The luciferase activity of BPA, BPS and PES according to the exposure concentrations. The activity ratio was measured by compare to the luciferase activity of the highest concentration (E2max). Data represent the mean ± SD were statistically analyzed by ANOVA followed by the Least Significant Difference (LSD) test (p <0.05). All tests were performed in triplicate.
Mentions: From the several concentrations of E2, BPA, BPS and PES, the luciferase activities (RLU, relative light unit) were obtained and were calculated for REP against the maximum luciferase activity of 0.3 nM E2, which was the maximum tested concentration of E2 (E2max). In the highest concentration (5 μM) of BPA, BPS and PES, the death cell (in BPA and BPS) and chemical aggregation (in PES) were observed, thus the result in this concentration was excluded to calculate REP. The relationship of E2 was determined by comparing to E2max using the REP values (see Additional file 1: Figure S1), from which each EC20, EC50 and EC80 value was estimated (Table 1). The estrogenic activity of BPA increased by a dose–response manner statistically and that of BPS also was shown the increasing tendency although there was little of statistical difference (Figure 2). No estrogenic activity was observed at two low concentrations (1 and 0.1 nM) of BPA and BPS. PES showed no estrogenic activity in all of the concentration ranges tested (data was not shown). In the highest concentration of both BPA and BPS (0.5 μM), 48.8% REP of BPA and 19.2% REP of BPS were shown, respectively (Figure 2 and Table 2). By comparing these values to the respective EC values of E2, REP20, REP50 and REP80 of both BPA and BPS were estimated, and were summarized in Table 2. The REP50 of BPA and BPS was 4.25 × 10−5 and 4.09 × 10−9, respectively, and REP20–80 was 2.17 × 10−4 to 8.32 × 10−6 and 2.25 × 10−6 to 7.41 × 10−12, respectively.Table 1

Bottom Line: BPA and BPS induced estrogenic activity whereas PES did not show any estrogenic activity in the concentrations tested.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.

View Article: PubMed Central - PubMed

Affiliation: Gyeongnam Department of Environmental Toxicology and Chemistry, Korea Institute of Toxicology, Jin-Ju, Gyeongnam, Republic of Korea. jwpark@kitox.re.kr.

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.

Show MeSH
Related in: MedlinePlus