scholarly journals Estrogenic Effects of Fluorotelomer Alcohols for Human Estrogen Receptor Isoforms α and β in Vitro

2007 ◽  
Vol 30 (7) ◽  
pp. 1358-1359 ◽  
Author(s):  
Hiroshi Ishibashi ◽  
Haruna Ishida ◽  
Munekazu Matsuoka ◽  
Nobuaki Tominaga ◽  
Koji Arizono
2015 ◽  
Vol 308 (6) ◽  
pp. F522-F534 ◽  
Author(s):  
Dara Burris ◽  
Rose Webster ◽  
Sulaiman Sheriff ◽  
Rashma Faroqui ◽  
Moshe Levi ◽  
...  

We have previously demonstrated that estrogen (E2) downregulates phosphate transporter NaPi-IIa and causes phosphaturia and hypophosphatemia in ovariectomized rats. In the present study, we examined whether E2directly targets NaPi-IIa in the proximal tubule (PT) and studied the respective roles of estrogen receptor isoforms (ERα and ERβ) in the downregulation of NaPi-IIa using both in vivo and an in vitro expression systems. We found that estrogen specifically downregulates NaPi-IIa but not NaPi-IIc or Pit2 in the kidney cortex. Proximal tubules incubated in a “shake” suspension with E2for 24 h exhibited a dose-dependent decrease in NaPi-IIa protein abundance. Results from OVX rats treated with specific agonists for either ERα [4,4′,4″;-(4-propyl-[1 H]-pyrazole-1,3,5-triyl) trisphenol, PPT] or ERβ [4,4′,4″-(4-propyl-[1 H]-pyrazole-1,3,5-triyl) trisphenol, DPN] or both (PPT + DPN), indicated that only the latter caused a sharp downregulation of NaPi-IIa, along with significant phosphaturia and hypophosphatemia. Lastly, heterologous expression studies demonstrated that estrogen downregulated NaPi-IIa only in U20S cells expressing both ERα and ERβ, but not in cells expressing either receptor alone. In conclusion, these studies demonstrate that rat PT cells express both ERα and ERβ and that E2induces phosphaturia by directly and specifically targeting NaPi-IIa in the PT cells. This effect is mediated via a mechanism involving coactivation of both ERα and ERβ, which likely form a functional heterodimer complex in the rat kidney proximal tubule.


1995 ◽  
Vol 52 (2) ◽  
pp. 159-171 ◽  
Author(s):  
Steven F. Arnold ◽  
John D. Obourn ◽  
Matthew R. Yudt ◽  
Timothy H. Carter ◽  
Angelo C. Notides

2007 ◽  
Vol 39 (3) ◽  
pp. A16-A17
Author(s):  
A. Castellaneta ◽  
N. De Tullio ◽  
F. Gagliardi ◽  
M. Margiotta ◽  
S. Tanzi ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1558 ◽  
Author(s):  
Kim ◽  
Park ◽  
Kim ◽  
Kim

Endocrine active compounds with structural similarities to natural hormones such as 17β-estradiol (E2) and androgen are suspected to affect the human endocrine system by inducing hormone-dependent effects. This study aimed to detect the (anti-)estrogenic and (anti-)androgenic activities of mono-(2-ethylhexyl) phthalate (MEHP) by yeast estrogen/androgen bioassay (YES/YAS). In addition, the mechanism and uptake of MEHP to receptors during agonistic and antagonistic activities were investigated through the activation signal recovery test and chromatographic analysis using liquid chromatography and tandem mass spectrometry (LC-MS/MS). Estrogenic and androgenic activities of MEHP were not observed. However, MEHP exhibited anti-estrogenic (IC50 = 125 μM) and anti-androgenic effects (IC50 = 736 μM). It was confirmed that these inhibitory effects of MEHP were caused by receptor-mediated activity of the estrogen receptor and non-receptor-mediated activity of the androgen receptor in an activation signal recovery test. When IC50 concentrations of anti-estrogenic and androgenic activity of MEHP were exposed to yeast cells, the uptake concentration observed was 0.0562 ± 0.0252 μM and 0.143 ± 0.0486 μM by LC-MS/MS analysis.


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