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使用荧光素酶报告基因测定法,检测双酚S、聚醚砜及其在大鼠肝脏S9组分作用下产生的代谢产物对MVLN细胞的雌激素活性。

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.

作者信息

Kang Jae Soon, Choi Jin-Soo, Kim Woo-Keun, Lee Yong-Ju, Park June-Woo

机构信息

Gyeongnam Department of Environmental Toxicology and Chemistry, Korea Institute of Toxicology, Jin-Ju, Gyeongnam, Republic of Korea.

出版信息

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

DOI:10.1186/1477-7827-12-102
PMID:25371027
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4232735/
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.

摘要

背景

双酚A(BPA)是一种应用于许多工业领域的化学物质,是一种在环境中被发现的潜在内分泌干扰化学物质(EDC)。双酚S(BPS)和聚醚砜(PES)已被提议作为BPA的替代物。在本研究中,评估了17-β-雌二醇(E2)、BPA、BPS、PES及其由大鼠肝脏S9组分形成的代谢产物与人类雌激素受体(ER)结合所诱导的雌激素活性。

方法

我们使用基于MVLN细胞中荧光素酶报告基因检测的体外生物测定法,根据孵育时间(0、20和40分钟)评估17-β-雌二醇(E2)、BPA、BPS、PES(E2:0.001至0.3 nM;BPA、BPS和PES:0.0001至5 μM)及其代谢产物(E2:0.05 μM;BPA、BPS和PES:0.1 mM)的雌激素活性。在对MVLN细胞进行化学处理72小时后,估计细胞活力和诱导的荧光素酶强度,据此评估所测试化学物质的雌激素活性。

结果

在测试浓度下,BPA和BPS诱导了雌激素活性,而PES未显示任何雌激素活性。在代谢产物的体外测定中,BPA代谢产物表现出与BPA相当的雌激素活性,BPS和PES的代谢产物均表现出增加的雌激素活性。

结论

结果表明,BPS和PES的代谢产物具有雌激素潜力,并且在其他EDC评估研究中有必要对这两种化学物质及其代谢产物进行评估。据我们所知,PES及其代谢产物的雌激素活性是首次报道。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/e07c96924679/12958_2014_1271_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/826388636e0f/12958_2014_1271_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/84f084371cb7/12958_2014_1271_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/3b68ebe3e7a3/12958_2014_1271_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/7d41c3b5f727/12958_2014_1271_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/e07c96924679/12958_2014_1271_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/826388636e0f/12958_2014_1271_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/84f084371cb7/12958_2014_1271_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/3b68ebe3e7a3/12958_2014_1271_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/7d41c3b5f727/12958_2014_1271_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eb60/4232735/e07c96924679/12958_2014_1271_Fig5_HTML.jpg

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