Alternative methods in vitro for screening of endocrine disruptors

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11120%2F16%3A43913086" target="_blank" >RIV/00216208:11120/16:43913086 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/75010330:_____/16:00011663

Výsledek na webu

—

DOI - Digital Object Identifier

—

Jazyk výsledku

angličtina

Název v původním jazyce

Alternative methods in vitro for screening of endocrine disruptors

Popis výsledku v původním jazyce

The aim of this study was to compare in silico data with results obtained in two alternative in vitro methods; and to investigate the potential endocrine activity of bisphenol A analogues. This article contributes to recent findings and brings up-to-date information on development of EU legislation and in vitro testing methods of endocrine disruption. In silico approach based on the OECD QSAR Toolbox was used for prediction of potential ligands of human estrogen receptor α. Estrogen Receptor Transactivation in vitro Assay to Detect Estrogen Receptor Agonists and Antagonists (OECD TG 455/457) using the VM7Luc4E2 (formerly designated BG1Luc4E2) cell line was performed for measurement of transactivation activity of the tested substances. Commercially available yeast-based microplate assay (XenoScreen YES/YAS, Xenometrix, Switzerland) for detection of compounds with estrogenic and androgenic agonistic/antagonistic activity was used as a comparative test to estrogen receptor transactivation assay (OECD TG 455/457) and for screening of the agonistic/antagonistic potential of human estrogen receptor and agonistic/antagonistic activity of tested compounds on human androgen receptor. The study showed good correlation between the two in vitro assays and significant correlation with in silico data. All tested substances were identified as agonists for human estrogen receptor α by methods in silico and in vitro, four substances showed a potentially higher estrogenic activity comparing to bisphenol A, two substances were identified as very weak antagonists of human androgen receptor and one compound showed a potential of agonistic activity to human androgen receptor. The study contributes to recent findings and brings new in silico and in vitro data of bisphenol A analogues, revealing that these analogous substances should be further tested as they may show similar or higher activity in vivo comparing to bisphenol A, which has been recently legislatively regulated.

Název v anglickém jazyce

Alternative methods in vitro for screening of endocrine disruptors

Popis výsledku anglicky

The aim of this study was to compare in silico data with results obtained in two alternative in vitro methods; and to investigate the potential endocrine activity of bisphenol A analogues. This article contributes to recent findings and brings up-to-date information on development of EU legislation and in vitro testing methods of endocrine disruption. In silico approach based on the OECD QSAR Toolbox was used for prediction of potential ligands of human estrogen receptor α. Estrogen Receptor Transactivation in vitro Assay to Detect Estrogen Receptor Agonists and Antagonists (OECD TG 455/457) using the VM7Luc4E2 (formerly designated BG1Luc4E2) cell line was performed for measurement of transactivation activity of the tested substances. Commercially available yeast-based microplate assay (XenoScreen YES/YAS, Xenometrix, Switzerland) for detection of compounds with estrogenic and androgenic agonistic/antagonistic activity was used as a comparative test to estrogen receptor transactivation assay (OECD TG 455/457) and for screening of the agonistic/antagonistic potential of human estrogen receptor and agonistic/antagonistic activity of tested compounds on human androgen receptor. The study showed good correlation between the two in vitro assays and significant correlation with in silico data. All tested substances were identified as agonists for human estrogen receptor α by methods in silico and in vitro, four substances showed a potentially higher estrogenic activity comparing to bisphenol A, two substances were identified as very weak antagonists of human androgen receptor and one compound showed a potential of agonistic activity to human androgen receptor. The study contributes to recent findings and brings new in silico and in vitro data of bisphenol A analogues, revealing that these analogous substances should be further tested as they may show similar or higher activity in vivo comparing to bisphenol A, which has been recently legislatively regulated.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30202 - Endocrinology and metabolism (including diabetes, hormones)

Projekt

—

Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2016

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Neuroendocrinology Letters

ISSN

0172-780X

e-ISSN

2354-4716

Svazek periodika

37

Číslo periodika v rámci svazku

Suppl. 1

Stát vydavatele periodika

SE - Švédské království

Počet stran výsledku

9

Strana od-do

123-131

Kód UT WoS článku

000406112100019

EID výsledku v databázi Scopus

2-s2.0-85018801008