• Title/Summary/Keyword: Estrogen receptor agonist

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Effects of Short-Term Treatment with Estrogen Receptor Agonist on Morphological Changes in Reproductive Organs of Adult Male Mice

  • Choi, Hayana;Mo, Yun Jeong;Lee, Mi-Kyung;Choe, Eun Sang;Yee, Sung Tae;Cho, Hyun Wook
    • Applied Microscopy
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    • v.46 no.4
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    • pp.193-200
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    • 2016
  • Male reproductive organs are strongly affected by estrogen signaling mediated via the estrogen receptor. In this study, propyl pyrazole triol (PPT), an estrogen receptor alpha agonist, was subcutaneously injected in adult male mice every 2 days for a total duration of 8, 16, or 24 days. Histological changes in the reproductive organs, including the testes, efferent ductules, and epididymides, were observed. The weight of the reproductive organs decreased in the PPT group. In addition, the diameter of the seminiferous tubules decreased in the PPT group compared with the control group. The epithelial cell height decreased in the initial segment of the epididymis, whereas the luminal diameter increased in the efferent ductules of the PPT group. PPT induced irregular morphology of stereocilia in the luminal region of the initial segment. Therefore, PPT treatment at high concentrations had inhibitory effects in the reproductive organs of adult male mice. These findings suggest that short-term treatment with estrogen receptor agonist causes histological changes in the testes, efferent ductules, and epididymis, which are similar to those caused by estrogen receptor antagonist treatment. Therefore, the estrogen receptor may have functional roles in male reproductive organs, implying that treatment with an estrogen receptor agonist can affect male fertility.

Estrogen Receptor Alpha Agonist Propyl Pyrazole Triol Causes Alterations of the Morphology and Function of the Mouse Male Reproductive System

  • Lee, Eun-Jung;Cho, Hyun-Wook
    • Animal cells and systems
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    • v.13 no.2
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    • pp.205-212
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    • 2009
  • Known as a female hormone, estrogen, performs important functions, and the activities of the hormone are mediated via the estrogen receptor. The principal objective of the present study was to assess the effects of a estrogen receptor agonist in male reproductive organs. In this study, the estrogen receptor alpha agonist, PPT, was injected subcutaneously into adult male mice. The effects of PPT on the murine reproductive system were histologically assessed at 3,5, and 8 weeks after treatment. In the treatment group, reductions were observed in the weight of the body, testis and epididymis. Microscopic examination revealed a reduction in seminiferous tubular diameter in the testis, and epithelial cell height in the epididymis during the experiment. 8 weeks after treatment, spermatogenesis was not detected, nor was the lumen of the seminiferous tubules. In the fertility test, 1 week after PPT injection, the fertilizing ability of males was decreased, and on the 2nd and 3rd weeks, complete infertility was observed. In conclusion, the injection of high concentrations of PPT into adult males induced physiological changes, including infertility, and also induced morphological changes, including a reduction in the height of epithelial cells within the reproductive system.

Effects of Alternate Treatment of Estrogen Receptor Antagonist and Agonist on Morphology of Male Reproductive Organs of Adult Mice

  • Choi, Hayana;Seong, Chi Nam;Park, Mi Suk;Cho, Hyun Wook
    • Applied Microscopy
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    • v.43 no.3
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    • pp.103-109
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    • 2013
  • ICI 182,780 (ICI) is known as an estrogen receptor antagonist, whereas propyl pyrazole triol (PPT) is an estrogen receptor agonist. In this study, ICI or ICI added with PPT was injected into adult male mice. Body and reproductive organ weights were reduced in the ICI added with PPT group compared to the control group. Further, the ICI and ICI added with PPT groups both showed increases in luminal areas of the seminiferous tubules of the testis, whereas cell heights of efferent ductules and the initial segment of the epididymis were reduced. Sperm count in the caudal epididymis was reduced in the ICI and ICI added with PPT groups. These results show that reproductive tissues were more deeply affected in the ICI added with PPT group. We also demonstrated that treatment with ICI resulted in histological changes in the testis, efferent ductule, and epididymis. Further, alternate treatment with ICI and PPT induced abnormalities in reproductive organs. These results indicate that a high concentration of PPT together with ICI may cause histological abnormalities instead of histological restoration in reproductive organs.

Ginsenoside-Rb1 Acts as a Weak Estrogen Receptor Agonist Independent of Ligand Binding.

  • Park, Wan-Kyu;Jungyoon Cho;Lee, Young-Joo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.114-114
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    • 2003
  • Ginseng is a medicinal herb widely used in Asian countries, and its pharmacological effects has been demonstrated in various systems such as cardiovascular, central nervous, and endocrine systems. Its effects are mainly attributed to the ginsenosides. We hypothesize that a component of Panax ginseng, ginsenoside-Rbl, acts by binding to estrogen receptor. We have investigated the estrogenic activity of ginsenoside-Rbl in a transient transfection system using estrogen receptors ${\alpha}$ or ${\beta}$ with estrogen -responsive luciferase plasmids in COS monkey kidney cells. Ginsenoside-Rbl activated both estrogen receptors ${\alpha}$ and ${\beta}$ in a dose-dependent manner (0.5 -100 M ). Activation was inhibited by the specific estrogen receptor antagonist ICI 182,780, indicating that the estrogenic effect of ginsenoside-Rbl is estrogen receptor dependent. Next, we evaluated the ability of ginsenoside-Rbl to induce estrogen-responsive progesterone receptor gene by semi-quantitative RT-PCR assays. MCF-7 cells treated with l7${\beta}$-estradiol or ginsenoside- Rb1 exhibited an increased expression of progesterone receptor mRNA. However, ginsenoside-Rbl failed to displace the specific binding of [3H]17${\beta}$-estradiol to estrogen receptor in MCF-7 cells as examined by whole cell ligand binding assays, suggesting that there is no direct interaction of ginsenoside-Rbl with estrogen receptor. Our results indicate that estrogen-like activity of ginsenoside-Rbl is independent of direct estrogen receptor association.

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Effects of Estrogen Receptor $\alpha$-Selective Agonist Propyl Pyrazole Triol on the Morphology of Accessory Genital Glands of Male Mouse (수컷 생쥐 부속 생식샘의 형태에 미치는 에스트로겐 수용체 $\alpha$의 선택적 효능제 propyl pyrazole triol의 영향)

  • Han, Ji-Yeon;Cho, Hyun-Wook
    • Applied Microscopy
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    • v.39 no.1
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    • pp.17-25
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    • 2009
  • This study investigated that exposure of male mice to estrogen receptor $\alpha$-selective agonist, 4,4',4"-(4-propyl-[1H]-pyrazole-1,3,5-triyl)tris-phenol (PPT) induce morphological changes of accessory genital glands. The male reproductive organs were fixed and processed for light microscopy. The PPT induced decreases of ventral prostates, seminal vesicles and preputial glands weights with experimental time. The glandular lumen of ventral prostate was atrophied compared with control group. Type of epithelial tissues in the prostate was changed from simple columnar epithelium to stratified cuboidal or squamous epithelium. Treated group with the agonist showed that increased connective tissue underlying epithelium in the prostate and seminal vesicle. Especially, the glandular lumen of the seminal vesicle was contracted when PPT-treated animals were compared with control group. Secretion cells of preputial gland were smaller than that of control group. On week 8, PPT treatment caused decrease of epithelial cell height lining the lumen of preputial gland. These results provide information useful in researching the physiological function of estrogen mediated by estrogen receptor $\alpha$ in male accessory genital gland.

Endocrinic Effects of Toxaphene and Chlordane in Human Hepatoma Cell (HepG2 Cell) Transfected with Estrogen Receptor and Luciferase Reporter Gene (에스트로겐 수용체 및 Luciferase 리포터 유전자 도입 사람 간 종양세포(HepG2 Cell)에서 Toxaphene과 Chlordane의 내분비 독성)

  • Kim Kyeong-Bae;Jung Ji-Won;Yang Se-Ran;Kang Kyung-Sun;Lee Yong-Soon
    • Toxicological Research
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    • v.20 no.3
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    • pp.205-211
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    • 2004
  • Concern that some chemicals in our environment may affect human health by disrupt-ing normal endocrine function has prompted a research on interactions of environmental contaminants with steroid hormone receptor. Toxaphene and chlordane are among the 12 persistent organic pollutants identified by the United Nations Environment Programme as requiring urgent attention. We compared the estrogenic activity of two organochlorine pesticides, toxaphene and chlordane, at estrogen receptor a (ER$\alpha$) and estrogen receptor $\beta$ (ER$\beta$). Human hepatoma cells (HepG2) were transiently transfected with rat ER$\alpha$ or ER$\beta$ plus an estrogen-responsive complement C3-luciferase (C3-Luc) reporter gene. After transfection, cells were treated with various concentrations of toxaphene and chlordane to investigate agonism or antagonism of these chemicals. Both toxaphene and chlordane were potent agonists in HepG2 cells for ER$\alpha$. In contrast, these chemicals had a minimal agonist activity with ER$\beta$ and almost abolished 17$\beta$-estradiol-induced ER$\beta$-mediated activity. Therefore, toxaphene and chlordane behaved as an ER$\alpha$ agonist and an ER$\beta$ antagonist with estrogen-responsive reporter plasmid C3-Luc, and exposure to these organochlorine pesticides could have a crictical effect on normal endocrine function.