The biologic activity of selenoestrogens

1982 ◽  
Vol 60 (2) ◽  
pp. 152-156 ◽  
Author(s):  
G. Longcope ◽  
T. Arunachalam ◽  
E. Caspi
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Uterine Weight ◽  
Binding Properties ◽  
Active Compounds ◽  
Relative Binding ◽  
Biologic Activity ◽  
Differential Imaging

For differential imaging of mammary tumors with estrogen receptors and without estrogen receptors we required γ-emitting estrogen analogues. In this paper we report on the binding properties of 7α-, 16α-, and 17α-methylselenoestrogens and 17α-phenylselenoestrogens relative to the binding properties of estradiol.The selenium-containing estrogens retained the ability to displace [3H]estradiol from the estrogen receptor of rabbit uterine cytosol, although in most instances the displacement was small (3–7% compared to estradiol).The most active compounds were 16α-phenylselenoestrone, 16α-methylselenoestradiol, and 17α-methylselenomethyl-estradiol which had relative binding of 23, 27, and 31%, respectively, compared with that of estradiol.16α-Methylselenoestradiol was able to translocate the estrogen cytosol receptor to the nucleus, in vitro, but was not able to increase the uterine weight when administered to mice in vivo.

scholarly journals Sexually Dimorphic Effect of Genistein on Hypothalamic Neuronal Differentiation in Vitro

2019 ◽  
Vol 20 (10) ◽  
pp. 2465 ◽  
Author(s):  
Marilena Marraudino ◽  
Alice Farinetti ◽  
Maria-Angeles Arevalo ◽  
Stefano Gotti ◽  
GianCarlo Panzica ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Sex Differences ◽  
Estrogen Receptors ◽  
Estrogen Receptor Α ◽  
Neuronal Cultures ◽  
Sexually Dimorphic ◽  
Hypothalamic Neurons ◽  
Estrogen Receptor Antagonists

Developmental actions of estradiol in the hypothalamus are well characterized. This hormone generates sex differences in the development of hypothalamic neuronal circuits controlling neuroendocrine events, feeding, growth, reproduction and behavior. In vitro, estradiol promotes sexually dimorphic effects on hypothalamic neuritogenesis. Previous studies have shown that developmental actions of the phytoestrogen genistein result in permanent sexually dimorphic effects in some behaviors and neural circuits in vivo. In the present study, we have explored if genistein, like estradiol, affects neuritogenesis in primary hypothalamic neurons and investigated the estrogen receptors implicated in this action. Hypothalamic neuronal cultures, obtained from male or female embryonic day 14 (E14) CD1 mice, were treated with genistein (0.1 µM, 0.5 µM or 1 µM) or vehicle. Under basal conditions, female neurons had longer primary neurites, higher number of secondary neurites and higher neuritic arborization compared to male neurons. The treatment with genistein increased neuritic arborization and the number of primary neurites and decreased the number of secondary neurites in female neurons, but not in male neurons. In contrast, genistein resulted in a significant increase in primary neuritic length in male neurons, but not in female neurons. The use of selective estrogen receptor antagonists suggests that estrogen receptor α, estrogen receptor β and G-protein-coupled estrogen receptors are involved in the neuritogenic action of genistein. In summary, these findings indicate that genistein exerts sexually dimorphic actions on the development of hypothalamic neurons, altering the normal pattern of sex differences in neuritogenesis.

scholarly journals 2-Phenylacetamide Isolated from the Seeds of Lepidium apetalum and Its Estrogen-Like Effects In Vitro and In Vivo

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2293 ◽  
Author(s):  
Mengnan Zeng ◽  
Meng Li ◽  
Miao Li ◽  
Beibei Zhang ◽  
Benke Li ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Inductive Effect ◽  
Uterine Weight ◽  
Immature Female ◽  
Main Compound ◽  
Material Basis ◽  
Weight Test ◽  
Mcf 7

The aim of this study was to investigate the estrogen-like effects of 2-phenylacetamide (PA), which is the main compound isolated from the seeds of Lepidium apetalum Willd (LA). Results showed that LA and PA could promote the proliferation of MCF-7 cells. The mouse uterine weight test showed that, LA and PA could increase the uterus index of immature female mice, and the levels of luteinizing hormone (LH) and estrogen (E2). LA could increase the expression of ERα and ERβ, while PA could increase the expression of ERα, ERβ and GPR30 in the uterus and MCF-7 cells. In addition, co-incubation of the estrogen receptor blocker with LA or PA abolished the inductive effect of the proliferation. PA has estrogenic activities and was the material basis of LA that played the estrogenic effect. LA and PA might be used for the treatment of perimenopause syndrome in a novel application.

Calycosin promotes proliferation of estrogen receptor-positive cells via estrogen receptors and ERK1/2 activation in vitro and in vivo

2011 ◽  
Vol 308 (2) ◽  
pp. 144-151 ◽  
Author(s):  
Jian Chen ◽  
Litao Liu ◽  
Ruanling Hou ◽  
Zhenjun Shao ◽  
Yiying Wu ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Estrogen Receptors ◽  
Estrogen Receptor Positive

Effect of triiodothyronine administration on estrogen receptor contents in peripuberal Sertoli cells

1996 ◽  
Vol 134 (5) ◽  
pp. 633-638 ◽  
Author(s):  
ML Panno ◽  
D Sisci ◽  
M Salerno ◽  
M Lanzino ◽  
L Mauro ◽  
...  
Keyword(s):  
Estrogen Receptor ◽  
Thyroid Hormone ◽  
Estrogen Receptors ◽  
Sertoli Cells ◽  
Androgen Metabolism ◽  
Testicular Steroids ◽  
In Vivo Administration

Panno ML, Sisci D, Salerno M, Lanzino M, Mauro L, Morrone EG, Pezzi V, Palmero S. Fugassa E, Andò S. Effect of triiodothyronine administration on estrogen receptor contents in peripuberal Sertoli cells. Eur J Endocrinol 1996:134:633–8. ISSN 0804–4643 The effects of thyroid hormone on androgen metabolism in peripuberal Sertoli cells through the inhibition of estradiol production have been reported previously. It was our intention to investigate further the possible role of thyroid hormone on the interaction between testicular steroids and Sertoli cells by analyzing the effects of triiodothyronine (T3) on estrogen receptor content in 2-, 3- and 4week-old euthyroid rats. Triiodothyronine treatment (3 μg/100 body wt per day) given during the last week prior to sacrifice resulted in reduced testicular growth in 2-week-old animals. Sertoli cells from all groups were cultured initially under basal conditions for the first 24 h and subsequently in the presence of testosterone and/or T3 for the additional 24 h. The in vitro addition of T3 induced a decrease of estrogen receptors (ERs) in 2- and 3-week-old animals that appeared more pronounced especially in the presence of T3 and testosterone. When T3 was tested in vivo we noticed that the decrease of ER content was even greater in all three groups under the in vitro influence of both T3 and testosterone. In 3-week-old animals a simultaneous assay of ERs in both nuclear and cytoplasmic compartments was performed. The ER concentrations in the nucleus were closely related to those of the cytoplasm. The in vivo administration of T3 was responsible for a greater decrease of ERs in the nucleus than in the cytosol. On the basis of these results, and in agreement with our previous data, we speculate that the effect of T3 in the maturational events of Sertoli cells could involve both estradiol production and ER content. Sebastiano Andò Cattedra di Fisiopatologia Endocrina, Dipartimento di Biologia Cellulare, Università della Calabria, 87030 Arcavacata di Rende, Cosenza, Italy

In vivo and in vitro phosphorylation of the human estrogen receptor

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

scholarly journals The treatment effects of flaxseed-derived secoisolariciresinol diglycoside and its metabolite enterolactone on benign prostatic hyperplasia involve the G protein-coupled estrogen receptor 1

2016 ◽  
Vol 41 (12) ◽  
pp. 1303-1310 ◽  
Author(s):  
Guan-Yu Ren ◽  
Chun-Yang Chen ◽  
Wei-Guo Chen ◽  
Ya Huang ◽  
Li-Qiang Qin ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Estrogen Receptor ◽  
Benign Prostatic Hyperplasia ◽  
G Protein ◽  
Therapeutic Potential ◽  
Prostatic Hyperplasia ◽  
Docking Simulations ◽  
G Protein Coupled

Secoisolariciresinol diglucoside (SDG), a lignan extracted from flaxseed, has been shown to suppress benign prostatic hyperplasia (BPH). However, little is known about the mechanistic basis for its anti-BPH activity. The present study showed that enterolactone (ENL), the mammalian metabolite of SDG, shared the similar binding site of G1 on a new type of membranous estrogen receptor, G-protein-coupled estrogen eceptor 1 (GPER), by docking simulations method. ENL and G1 (the specific agonist of GPER) inhibited the proliferation of human prostate stromal cell line WPMY-1 as shown by MTT assay and arrested cell cycle at the G0/G1 phase, which was displayed by propidium iodide staining following flow cytometer examination. Silencing GPER by short interfering RNA attenuated the inhibitory effect of ENL on WPMY-1 cells. The therapeutic potential of SDG in the treatment of BPH was confirmed in a testosterone propionate-induced BPH rat model. SDG significantly reduced the enlargement of the rat prostate and the number of papillary projections of prostatic alveolus and thickness of the pseudostratified epithelial and stromal cells when comparing with the model group. Mechanistic studies showed that SDG and ENL increased the expression of GPER both in vitro and in vivo. Furthermore, ENL-induced cell cycle arrest may be mediated by the activation of GPER/ERK pathway and subsequent upregulation of p53 and p21 and downregulation of cyclin D1. This work, in tandem with previous studies, will enhance our knowledge regarding the mechanism(s) of dietary phytochemicals on BPH prevention and ultimately expand the scope of adopting alternative approaches in BPH treatment.

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