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The ionic liquid 1-octyl-3-methylimidazolium (M8OI) is an activator of the human estrogen receptor alpha

Lookup NU author(s): Dr Alistair Leitch, Anne Lakey, will Hotham, Emerita Professor Loranne Agius, Professor George Kass, Professor Peter Blain, Professor Matthew Wright

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Abstract

Recent environmental sampling around a landfill site in the UK demonstrated that unidentified xenoestrogens were present at higher levels than control sites; that these xenoestrogens were capable of super-activating (resisting ligand-dependent antagonism) the murine variant 2 ERβ and that the ionic liquid 1-octyl-3-methylimidazolium chloride (M8OI) was present in some samples. To determine whether M8OI was a contributor to the xenoestrogen pool in the soils, activation of human estrogen receptors by M8OI was examined. M8OI activated the human ERα in MCF7 cells in a dose-response manner. These effects were inhibited by the ER antagonist ICI182780; occurred in the absence of any metabolism of M8OI and were confirmed on examination of ER-dependent induction of trefoil factor 1 mRNA in MCF7 cells. M8OI also super-activated the murine variant 2 ERβ in a murine hepatopancreatobiliary cell line. The human ERβ was not activated by M8OI when expressed in HEK293 cells. These data demonstrate that M8OI is a xenoestrogen capable of activating the human ERα and super-activating the murine variant 2 ERβ.

Publication metadata

Author(s): Leitch AC, Lakey AF, Hotham WE, Agius L, Kass GE, Blain PG, Wright MC

Publication type: Article

Publication status: Published

Journal: Biochemical and Biophysical Research Communications

Year: 2018

Volume: 503

Issue: 3

Pages: 2167-2178

Print publication date: 10/09/2018

Online publication date: 04/08/2018

Acceptance date: 10/08/2018

Date deposited: 10/08/2018

ISSN (print): 0006-291X

ISSN (electronic): 1090-2104

Publisher: Elsevier Inc.

URL: https://doi.org/10.1016/j.bbrc.2018.08.008

DOI: 10.1016/j.bbrc.2018.08.008

PubMed id: 30086880

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