• Title/Summary/Keyword: estrogen activity

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Influences of Testosterone and Estrogen on the Contractile Sensitivity to Oxytocics, the Cholinesterase activity and Electrolytes of the Uterine Muscle of Rabbits (Testosterone 및 Estrogen 투여(投與)가 자궁수축약(子宮收縮藥)의 적출자궁(摘出子宮) 수축성(收縮性)에 미치는 영향(影響)과 자궁근내(子宮筋內) Cholinesterase 활성도(活性度) 및 전해질(電解質)에 미치는 효과(?果))

  • Koo, Hee-Soo;Kong, Wha-Soon;Kim, Soon-Yeung;Song, Hyun-Sub;Lee, Jeung-Ja
    • The Korean Journal of Pharmacology
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    • v.6 no.1
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    • pp.45-55
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    • 1970
  • It is well known that the uterine contractility is affected by sexual hormone. In this experiment, the authors attempted to study the influences of testosterone and estrogen or the uterine contractility to oxytocics. The contractile sensitivity of the excised uterine muscle of non-castrated and castrated rabbits with testosterone and estrogen 24 hours before experiment is observed respectively. And the cholinesterase activity and electrolytes (Na, K, Ca and Mg) in the uterine muscle are measured in order to study the relationship with contractile sensitivity and those changes. The results obtained were summarized as follows: 1. The contractile effect of spareng on the excised uterine muscle of non-castrated rabbits pretreated with estrogen was markedly increased in small dose, but that of rabbits pretreated with testosterone was significantly increased in large dose, comparing with that of the control group. In castrated rabbits, the contractile sensitivity of the uterine muscle to spareng was significantly increased by pretreatment with estrogen in large dose but it was markedly decreased by pretreatment with testosterone in small dose. 2. The contractile effect of quinine on the excised uterine muscle of non-castrated rabbits pretreated with estrogen was significantly decreased but that of castrated rabbits pretreated with both estrogen and testosterone were markedly increased comparing with that of the control group. 3. The cholinesterase activity in the uterine muscle of non-castrated rabbits was significantly increased by pretreatment with small dose of estrogen or large dose of testosterone, but that of castrated rabbits was markedly decreased by pretreatment with large dose of estrogen. 4. Na and K contents in the uterine muscle of non-castrated rabbits were markedly increased by pretreatment with both estrogen and testosterone, but that of castrated rabbits was significantly increased by pretreatment with small dose of estrogen. 5. Ca content in uterine muscle of non-castrated rabbits was significantly decreased by pretreatment with both large dose of estrogen and testosterone but increased by pretreatment of testosterone. In castrated rabbits, Ca content was significantly decreased by pretreatment with both estrogen and testosterone. 6. Mg content in the uterine muscle of non-castrated rabbits was markedly increased by pretreatment with estrogen and small dose of testosterone, but that of castrated rabbits was significantly decreased by pretreatment with both large dose of estrogen and testosterone.

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In Vitro Effects of Female Sex Hormones on Collagenase Activity of Gingival Fibroblast and Periodontal Ligament Fibroblast (여성 호르몬의 변화가 치은 섬유아세포와 치주인대세포의 교원질 분해 효소의 활성에 미치는 영향)

  • Sin, Ji-Yearn;Lee, Chul-Woo;Han, Soo-Boo
    • Journal of Periodontal and Implant Science
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    • v.29 no.1
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    • pp.31-40
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    • 1999
  • Many factors may affect periodontal changes during the physiologic conditions of woman(e.g. puberty, menstrual cycle, pregnancy, menopause). Recently many research has focused on the immunological changes of host, but the exact mechanism is not clear. Collagen is a major constituent of periodontium, and collagenase specifically digests the collagen and plays a role in destruction of periodontal tissue. So, I suppose that it participates with the cytokines in the inflammation of gingiva and vascular response during the changes of female sex hormones. Because there are some evidences of the existence of the receptors of estrogen and progesterone in the gingiva, it may be a target tissue of female sex hormones. In this experiment, gingival fibroblast and periodontal ligament cell were cultured in the presence of various concentrations of estrogen or progesterone corresponding to the menstrual cycle and pregnancy. Collagenase activity of the supernatant of culture media was determined by Spectrophotometric collagenase assay. The enzyme activity was calculated by the % decrease of the coated collagen. 1. The estrogen at both concentrations had no effect on the activity of collagenase of the gingival fibroblast. 2. The progesterone had some effect on the collagenase activity of the gingival fibroblast at low and high concentration of menstrual cycle, and elevated the enzyme activity at all range of pregnancy concentrations. 3. In periodontal ligament cells, estrogen elevated the enzyme activity at the early pregnancy concentration and progesterone elevated at the concentration just before menstruation. In this experiment, pregesterone elevated the collagenase activity of gingival fibroblast and periodontal ligament cells. But the mechanism of the up-regulation of the enzyme activity was not confirmed. The more experiments of direct effect of progesterone on gingival at the molecular level(e.g. northern blot analysis) can reveal the exact mechanism.

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Estrogen Receptor-α Mediates the Effects of Estradiol on Telomerase Activity in Human Mesenchymal Stem Cells

  • Cha, Young;Kwon, Su Jin;Seol, Wongi;Park, Kyung-Soon
    • Molecules and Cells
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    • v.26 no.5
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    • pp.454-458
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    • 2008
  • Sex steroid hormone receptors play a central role in modulating telomerase activity, especially in cancer cells. However, information on the regulation of steroid hormone receptors and their distinct functions on telomerase activity within the mesenchymal stem cell are largely unavailable due to low telomerase activity in the cell. In this study, the effects of estrogen ($E_2$) treatment and function of estrogen receptor alpha ($ER{\alpha}$) and estrogen receptor beta ($ER{\beta}$) on telomerase activity were investigated in human mesenchymal stem cells (hMSCs). Telomerase activity and mRNA expression of the catalytic subunit of telomerase (hTERT) were upregulated by treatment of the cells with $E_2$. The protein concentration of $ER{\alpha}$ was also increased by $E_2$ treatment, and enhancement of $ER{\alpha}$ accumulation in the nucleus was clearly detected with immunocytochemistry. When $ER{\alpha}$ expression was reduced by siRNA transfection into hMSCs, the effect of $E_2$ on the induction of hTERT expression and telomerase activity was diminished. In contrast, the transient overexpression of $ER{\alpha}$ increased the effect of $E_2$ on the expression of hTERT mRNA. These findings indicate that the activation of hTERT expression and telomerase activity by $E_2$ in hMSCs depends on $ER{\alpha}$, but not on $ER{\beta}$.

Effects of Dioscorea batatas on Estrogen-deficient Osteoporosis (Estrogen 결핍성(缺乏性) 골다공증(骨多孔症)에 미치는 산약(山藥) 추출물(抽出物)의 영향(影響))

  • Hwang Gwi-Seo;Lee Dae-Young
    • Journal of Society of Preventive Korean Medicine
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    • v.7 no.1
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    • pp.55-66
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    • 2003
  • Osteoporosis is characterized by bone loss and mobidity with osteoporotic fracture. This study was performed to evaluate the effect of on the bone mass and its related factors in estrogen-deficient animal model. The model rats of osteoporsis showed a significant decrease in bone density, bone ash density, calcium content of femur bone. At the 14th day after ovariectomy-surgery, rats were administered with DBE, extract of Dioscorea batatas, per orally, and continued for 10 weeks. And osteoporosis related parameters were determined to investigate the effect of DBE. Osteoporetic rats showed lower serum estrogen level, higher body weight than normal rats, and showed atrophy of uterine horns. DBE showed inhibitory effect on bone loss in osteoporetic condition, and reduced the increase of ALP activity and osteocalcin level in serum, and reduced the increase of OH-proline level in urine. But, DBE had no effect on cell proliferation and ALP activity in rat calvarial cell culture.

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Basic Study on Estrogen-like Activity of Herbal Medicine (한약재의 에스트로겐 유사 활성에 대한 기초 연구)

  • Son, Bo-Gil;Lee, Hee-Yoon;Bae, Ju-Eun;Yoon, Young-Jin
    • The Journal of Korean Obstetrics and Gynecology
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    • v.31 no.4
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    • pp.54-72
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    • 2018
  • Objectives: The aim of this review is to investigate studies on Estrogen-like activity and to contribute to the utilization of herbal medicines including phytoestrogens. Methods: Electric searches were performed with Pubmed from 2013 to June 2018, for the words, 'herb and estrogen', 'traditional Chinese medicine and estrogen', 'Oriental medicine and estrogen', and 'Korean medicine and estrogen'. 49 papers are investigated and classified into 'in vitro', 'in vivo' and 'in vivo and in vitro' experimental studies. Results: 1. In vitro experimental studies have shown that estrogen-like effects of the components extracted from Rhei Radix et Rhizoma, Rubi Fructus, Sparganii Rhizoma, Epimedii Herba, Spatholobi Caulis, Evodiae fructus, Curcumae longae Radix, Ginseng Radix, Bupleuri Radix, Astragali Radix, Salviae Miltiorrhizae Radix, Puerariae Radix, Scutellariae Radix are present. 2. In vivo experimental studies have shown that estrogen-like effects of the components extracted from Phytolaccae Radix, Ligustri Lucidi Fructus, Alismatis Rhizoma, Notoginseng Radix, Puerariae Radix, Ginseng Radix, Cyperi Rhizoma, Cistanchis Herba, Cynomorii Herba, Granati fructus, Astragali Radix, Rehmanniae Radix Crudus, Epimedii Herba, Polygalae Radix, Artemisiae Annuae Herba are present. 3. In vitro and in vivo experimental studies have shown that estrogen-like effects of the components extracted from Cirsii Herba, Dioscoreae Rhizoma, Salviae Miltiorrhizae Radix, Cynomorii Herba, Cinnamomi cortex, Drynariae Rhizoma, Psoraleae Semen, Schisandrae Fructus, Epimedii Herba, Astragali Radix are present. Conclusions: Future studies will require additional research on numerous herbal medicines used in clinical practice.

Antioxidant, Anti-inflammatory, Anti-obesity and Estrogen-like Activities of Soybean Pod Extracts (콩깍지 추출물의 항산화·항염·항비만 및 에스트로겐 유사활성 평가)

  • Jung, Eun-Suk;Kim, Haeng-Ran;Hwang, Yu-Jin;Jang, Kyeong-A;Seo, Mi-Kyung;Chu, Han-na
    • Journal of the Korean Society of Food Culture
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    • v.36 no.6
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    • pp.649-660
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    • 2021
  • In this study, soybean pods of 45 soybean landraces (or varieties) were classified as yellow (19 samples), black (23 samples), or black in green (3 samples) based on soybean seed coat color. Total polyphenol and flavonoid contents were measured, and antioxidant, anti-inflammatory, anti-obesity, and estrogen-like activities were assessed. Total polyphenol and flavonoid content ranges were 24.13-108.03 mg GAE/g and 3.31-72.02 mg CE/g, respectively, and were highest in the black group followed by the yellow group and were least in the black in green group, while ABTS and DPPH activities followed the order black in green > black > yellow. Estrogen-like and estrogen receptor-α activity ranges were 29.06-35.58 pg/mL and 7.05-10.13 pg/mL and were followed the order yellow > black > black in green and black in green > yellow > black, respectively. Nitric oxide (NO) inhibitory and UCP-1 activities followed the same order as estrogen receptor-α activities. Our findings suggest that soybean pods are excellent sources of antioxidants and high-quality functional materials.

Aluminium and Cadmium Interfere with the Estrogen Receptor Level in the Primary Culture of Hepatocytes in the Rainbow Trout Oncorhynchus mykiss

  • Hwang Un-Gi
    • Fisheries and Aquatic Sciences
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    • v.4 no.4
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    • pp.180-185
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    • 2001
  • Al and Cd-induced inhibition of vitellogenin (VTG) production was examined at the estrogen receptor (ER) level in rainbow trout Oncorhynchus mykiss hepatocytes. The binding of $[^3H]$ $estradiol-17\beta\;(E_2)$ to hepatocytes reached a plateau 3 days after addition of $E_2\;(2\times\;10^{-6} M)$to the medium. The binding activity was linearly reduced with the increased concentrations $(-10^{-5}\;M)$ of 4-hydroxy-tamoxifen (4-OHT) and specific binding linearly increased with the increased doses of $[^3H]\;E_2$, indicating that the radioligand bound to ER. Al $(-10^{-4}\;M)$and Cd $(10^{-6}\;M)$ as well as 4-OHT $(10^{-6}\;M)$ significantly reduced the $[^3H]\;E_2$-binding activity by $30­40\%$, while they completely inhibited VTG production. Al and Cd had no effect on $E_2-human$ $ER\alpha$ binding activity at any concentrations used $(-10^5\;nM\;each)$. These results suggested that Al and Cd inhibited VTG production in part by interfereing with the ER level. Inhibitory effects of these metals on the $E_z-dependent$ upregulation of ER activity are also discussed.

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Repression of $PPAR{\gamma}$ Activity on Adipogenesis by $17{\beta}$-estradiol in Differentiated 3T3-L1 Cell

  • Yoon, Mi-Chung;Jeong, Sun-Hyo
    • Biomedical Science Letters
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    • v.15 no.3
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    • pp.179-185
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    • 2009
  • In our previous report, we showed that $PPAR{\gamma}$ does not influence adipogenesis in females with functioning ovaries, indicating that $PPAR{\gamma}$ activity on adipogenesis is associated with sex-related factors. Among the sex-related factors, estrogen has been recognized as a major factor in inhibiting adiposgenesis in females. Thus, we hypothensized that $17{\beta}$-estradiol (E) inhibits 3T3-L1 cell adipogenesis by preventing $PPAR{\gamma}$ activity. E decreased triglyceirde accumulation in differentiated 3T3-L1 cells compared with control group. E also decreased the expression of $PPAR{\gamma}$ mRNA as well as $PPAR{\gamma}$ dependent adipocyte-specific genes, such as adipocyte fatty acid binding protein and tumor necrosis factor $\alpha$. In addition, E not only decreased luciferase reporter activity by $PPAR{\gamma}$, but also transfection of estrogen receptor $\alpha$ ($ER{\alpha}$) or $ER{\beta}$ led to decreases in $PPAR{\gamma}$ reporter gene activation. Moreover, E-activated ERs significantly decreased the luciferase reporter gene activation induced by $PPAR{\gamma}$ transfection, suggesting that estrogen-activated ERs inhibit $PPAR{\gamma}$-dependent transactivation. Accordingly, our results demonstrate that E inhibits the action of $PPAR{\gamma}$ on adipogenesis through E activated ER, providing evidence that lack of estrogen may potentiate $PPAR{\gamma}$ action on adipogenesis.

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Loss of estrogen responsiveness under hypoxia occurs through hypoxia inducible factor-l induced proteasome-dependent down regulation of estrogen receptor

  • Cho, Jung-Yoon;Kim, Duk-Kyung;Lee, Young-Joo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 2003.11a
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    • pp.70-70
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    • 2003
  • Estrogen receptor is a ligand-activated transcription factor. Its action depends on the receptor, its ligand, and its coactivator proteins. As a consequence, the concentration of the receptor is a major component that governs the magnitude of the estrogen response. Despite the extensive knowledge on mechanism of estrogen receptor action, regulation of estrogen receptor itself is not very well understood. Estrogen receptor is known to be downregulated under hypoxia leading to inhibition of estrogen receptor mediated transcription activation. We have studied mechanism of loss of estrogen responsiveness under hypoxia. We found that Hif-l${\alpha}$, a major transcription factor regulating hypoxic response, inhibited transcription of estrogen response element driven luciferase gene by expression of HIF-l${\alpha}$/vp16 construct designed to contain transcription activity under normoxia. This loss of estrogen responsiveness appears to be the result of ER${\alpha}$ downregulation. ER${\alpha}$was downregulated at the levels of ligand-biding and protein within l2-24h, and the response was blocked by the proteasome inhibitor MG132, protein synthesis inhibitor cyclohexamide, and tyrosine kinase inhibitor Genistein. These results demonstrate that Hif-l${\alpha}$ downregulates ER${\alpha}$ by proteasome dependent pathway.

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Estrogen, Androgen, and Retinoic Acid Hormone Activity of Ginseng Total Saponin (인삼 총 사포닌의 에스트로젠, 안드로젠, 레티노익산 호르몬 수용체에 대한 활성)

  • Ji, Sang-Mi;Lee, Young-Joo
    • Journal of Ginseng Research
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    • v.27 no.3
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    • pp.93-97
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    • 2003
  • Alternative or complementary medicine plays an important role in health care system. Ginseng, being one of the most popular oriental herbs, is believed to contain various steroid hormone activity. Ginseng has been demonstrated pharmacological effect in the cardiovascular, endocrine, central nervous, and immune system. Our objective was to study that total saponin might mediate some of their actions by binding to the steroid hormone receptor, as they share many of the actions of steroid hormone in various physiological system. Using total saponin from Panax Ginseng, we have studied the possibility of total saponin being a potential estrogen receptor, androgen receptor, and retinoic acid receptor ligand. Total saponin activated the transcription of both the estrogen and androgen responsive luciferase reporter plasmids at a concentration of 100$\mu\textrm{g}$/ml in COS cells transiently transfected with the corresponding receptor and hormone responsive receptor plasmids. And total saponin caused a concentration-dependent stimulation of estrogen receptor. Total saponin increased the expression of estrogen responsive c-fos proto-oncogene at the protein level in MCF7 cells at 24 h treatment as examined by Western analysis. The c-fos induction was used as a specific marker of estrogen responsiveness. This activation was inhibited by the specific estrogen receptor antagonist, ICI 182,780. However, total saponin failed to activate the retinoic acid receptor in COS cells transiently transfected with the corresponding receptor and retinoic acid responsive reporter plasmids. These results show that total saponin is capable of activating estrogen and androgen receptors.