Comparison of the Hershberger assay and androgen receptor binding assay of twelve chemicals

Yamasaki, Kanji; Sawaki, Masakuni; Noda, Shoji; Muroi, Takako; Takakura, Saori; Mitoma, Hideo; Sakamoto, Satoko; Nakai, Makoto; Yakabe, Yoshikuni

doi:10.1016/j.tox.2003.09.012

Cited by 33 publications

(17 citation statements)

References 26 publications

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“…Such effect is thought to be associated with its estrogenic effect, because tamoxifen, a triphenylethylene derivative, is an antagonist of estrogen receptors (Yamasaki et al 2004;Kim et al 2007;Ghisari and BonefeldJørgensen 2009). However, in our study, tamoxifen (1 lM) was not found to reverse DEHP-mediated inhibition of I K(erg) .…”

Section: Discussionmentioning

confidence: 99%

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The inhibition by di(2-ethylhexyl)-phthalate of erg-mediated K+ current in pituitary tumor (GH3) cells

Yang

Yeh

et al. 2012

Arch Toxicol

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DEHP (bis(2-ethylhexyl)-phthalate) known to be an endocrine-disrupting chemical is a widely used phthalate. Little information regarding the effects of phthalate esters on ion currents is available. In this study, the effects of DEHP and other phthalate esters (DBEP: di(2-butoxyethyl)-phthalate and DMGP: di(2-methylglycol)-phthalate) on ion currents were investigated in pituitary GH₃ cells. Hyperpolarization-elicited K⁺ currents in GH3 cells bathed in high-K⁺, Ca²⁺-free solution were examined to evaluate the effects of DEHP, DBEP, and DMGP on the ether-a`-go-go-related-gene (erg) K⁺ current (IK(erg)). Addition of DEHP to GH₃ cells suppressed the amplitude of IK(erg) in a concentration-dependent manner with an IC₅₀ value of 16.3 μM. With a two-pulse protocol, addition of DEHP shifted the activation curve of IK(erg) to a depolarized potential by approximately 10 mV with no change in the rate of IK(erg) deactivation. This compound did not have any effects on delayed rectifier K⁺ current in GH₃ cells, while 4-aminopyridine-3-methanol (100 μM) suppressed this current significantly. DBEP (30 μM) had little or no effect on IK(erg), while DMGP (30 μM) slightly reduced it. In inside-out configuration, DEHP (30 μM) applied to the bath slightly reduced the activity of large-conductance Ca²⁺-activated K⁺ channels. DEHP (30 μM) increased the frequency of spontaneous action potentials (APs); however, this compound at the same concentration had no effect on AP firing in KCNH2 siRNA-transfected GH₃ cells. The effects described herein can contribute to their actions on functional activity of endocrine or neuroendocrine cells if similar results are found in vivo.

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Section: Discussionmentioning

confidence: 99%

“…DEHP was demonstrated to suppress tamoxifen-induced apoptosis possibly linked to its estrogenic effects in pituitary GH 3 cells (Yamasaki et al 2004;Kim et al 2007). This compound was noted to exert an agedependent influence on the pituitary-adrenocortical axis in vivo (Supornsilchai et al 2007).…”

Section: Introductionmentioning

confidence: 99%

The inhibition by di(2-ethylhexyl)-phthalate of erg-mediated K+ current in pituitary tumor (GH3) cells

Yang

Yeh

et al. 2012

Arch Toxicol

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show abstract

“…The fact that we did not find changes in saline ingestion after spironolactone treatment suggests that changes in body fluids were not a significant factor. It also should be noted that, in addition to blocking GR, RU-486 has anti-progesterone effects (Truss et al, 1994), while spironolactone has anti-androgen effects (Yamasaki et al, 2004). As reflex ovulators, prairie voles do not experience cyclic fluctuations in progesterone and functional corpora lutea are not observed until at least 10 h after mating (Carter et al, 1989).…”

Section: Gr Blockade and Pair Bondingmentioning

confidence: 99%

Glucocorticoid receptor involvement in pair bonding in female prairie voles: The effects of acute blockade and interactions with central dopamine reward systems

Curtis

Wang

2005

Neuroscience

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“…The experimental methods for determining xenoestrogens summarized by the Organisation for Economic Co-operation and Development (OECD), include methods such as the yeast-based assay (Routledge and Sumpter, 1997), E-Screen (Soto et al, 1995), the MCF-7 cells proliferation test (Gierthy et al, 2003), the rat uterotrophic assay (Kanno et al, 2001) and the Hershberger assay (Yamasaki et al, 2004). However, the number of exhaustive virtual chemicals is much bigger than the number of estrogenic chemicals that we could test.…”

Section: Introductionmentioning

confidence: 99%

Docking and QSAR study on the binding interactions between polycyclic aromatic hydrocarbons and estrogen receptor

et al. 2012

Ecotoxicology and Environmental Safety

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Comparison of the Hershberger assay and androgen receptor binding assay of twelve chemicals

Cited by 33 publications

References 26 publications

The inhibition by di(2-ethylhexyl)-phthalate of erg-mediated K+ current in pituitary tumor (GH3) cells

The inhibition by di(2-ethylhexyl)-phthalate of erg-mediated K+ current in pituitary tumor (GH3) cells

Glucocorticoid receptor involvement in pair bonding in female prairie voles: The effects of acute blockade and interactions with central dopamine reward systems

Docking and QSAR study on the binding interactions between polycyclic aromatic hydrocarbons and estrogen receptor

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