• Title/Summary/Keyword: estrogen activity

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Anticancer activity of steroid hormones (Steroid hormone의 제암작용)

  • 한덕용
    • YAKHAK HOEJI
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    • v.17 no.2
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    • pp.92-102
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    • 1973
  • Hormone이 암발생과 밀접한 관계가 있음은 이미 1935년대에 밝혀진 바 있다. 즉 lacassagne은 estrogen이 토끼 자궁벽의 fibromyomatous transformation에 영향을 준다고 하였다. Nelson는 guinea-pig를 시험동물로 해서 estrogen을 장기투여한 결과 uterine fibroids가 수발됨을 확인한 이래, 유발됨을 확인한 이래, 이러한 hormone이 암발생의 장기요인이 됨으리 밝히게 되었다. 이러한 업적은 Lipschutz에 의해 더욱 수식되었다. 이러한 업적의 결과가 여러편의 종설로 발표되었다. 즉 Lacassagne, Zuckerman, Burrows등, Gardner는 각기 종설을 발표하여 이를 확증하기에 이르렀다. 한편 각개 hormone, 그중에서도 sex-hormone의 opposite action은 Steinach등 및 Sand에 의해 밝혀졌고 거세백서에 estrogen을 투여했을때 유기되는 vaginal mucosa의 epidermization이 testosterone의 투여에 의해 급속히 소진됨을 Currier 일파가 증명하였고 estrogen에 의해 유발된 웅백서 부속성선의 조직변성이 androgen의 동시투여의 소실됨이 homone에 의해 유발된 neoplastic에 대해 유효하리하는 것은 백명한 일이고 이러한 사실은 현재 실시로 허다히 이용되고 있는 것이다.

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Estrogen, Body Weight, and Appetite

  • Bond, Eleanor F.;Deechakawan, Wimon;Chung, Shih-Chi
    • Perspectives in Nursing Science
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    • v.2 no.1
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    • pp.92-104
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    • 2005
  • Obesity rates are increasing worldwide, associated with excess acute and chronic disease risk. In most countries, obesity rates among women exceed rates in men, particularly during the post menopausal years. Many factors affect body weight and appetite, including age, metabolic rate, physical activity level, stress, cultural factors, socioeconomic status, health status and health literacy, diet composition, attitudes, and beliefs. Gender affects appetite and body weight indirectly by altering factors contributing to food choice. However, there is emerging evidence that gender affects appetite and body weight directly, altering the physiological control systems regulating appetite. The follicular menstrual cycle phase (estrogen-rich) is associated with relative suppression of appetite. Lower estrogen levels are associated with increased food intake, body weight gain, and altered body fat distribution in humans and animals. This paper reviews the linkages between estrogen and appetite regulation. While relationships among appetite, body weight, and gender-linked hormones are complex, research elucidating these interrelationships could lead to development of gender-specific treatment approaches for obesity and appetite dysregulation.

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Effective Chemopreventive Activity of Genistein against Human Breast Cancer Cells

  • Shon, Yun-Hee;Park, Sun-Dong;Nam, Kyung-Soo
    • BMB Reports
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    • v.39 no.4
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    • pp.448-451
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    • 2006
  • Chemopreventive and cytotoxic effect of genistein against human breast cancer cell lines was investigated. Genistein inhibited cell proliferation in estrogen receptor-positive (MCF-7) and estrogen receptor-negative (MDA-MB-231) human breast carcinoma cell lines. Cytochrome P450 (CYP) 1A1-mediated ethoxyresorufin O-deethylase (EROD) activity was inhibited by genistein in a concentrationdependent manner. Genistein significantly inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced cyclooxy-genase-2 activity and protein expression at the concentrations of 10 (p < 0.05), 25 (p < 0.05) and 50 mM (p < 0.01). In addition, ornithine decarboxylase (ODC) activity was reduced to 53.8 % of the control after 6 h treatment with 50 mM genistein in MCF-7 breast cancer cells. These results suggest that genistein could be of therapeutic value in preventing human breast cancer.

Breast Cancer Chemopreventive Activity of Polysaccharides from Starfish In Vitro

  • Nam Kyung-Soo;Kim Cheorl-Ho;Shon Yun-Hee
    • Journal of Microbiology and Biotechnology
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    • v.16 no.9
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    • pp.1405-1409
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    • 2006
  • Polysaccharides from the starfish Asterina pectinifera were assessed in vitro for their chemopreventive potential in human breast cancer. The polysaccharides from A. pectinifera inhibited cell proliferation in the estrogen receptor-positive (MCF-7) and estrogen receptor-negative (MDA-MB-231) human breast carcinoma cell lines. In addition, the polysaccharides were found to be an inhibitor of cytochrome P450 1A1-mediated ethoxyresorufin O-deethylase activity, and caused a dose-dependent inhibition of aromatase activity in microsomes isolated from a human placenta. There was a significant reduction in the ornithine decarboxylase activity to 30.7% of the control in the polysaccharide-treated MCF-7 breast cancer cells. Therefore, the polysaccharides from A. pectinifera merit further investigation with respect to breast cancer chemoprevention.

In vitro Screening of Medicinal Plants with Estrogen Receptor Modulation Activity (생약의 여성호르몬 수용체 조절 활성 검색)

  • Lee, Chang-Min;Kang, Se-Chan;Oh, Joa-Sub;Choi, Han;Li, Xue-Mei;Lee, Jae-Hyun;Lee, Mi-Hyun;Choung, Eui-Su;Kawk, Joung-Hwan;Zee, Ok-Pyo
    • Korean Journal of Pharmacognosy
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    • v.37 no.1 s.144
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    • pp.21-27
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    • 2006
  • Yeast based estrogenicity assay is the simplest and useful for the assay and the discovery of novel estrogenic substances in natural specimens, The estrogen receptor(ER) modulation activity of 50% EtOH extracts of 101 traditional medicinal herbs was assessed using a recombinant yeast assay system with both a human estrogen receptor expression plasmid and a receptor plasmid. Among them, 14 species proved to be active. Pureariae Flos (flower of Puerraria thunbergiana BENTH.) had the highest estrogenic relative potency$(7.75{\times}10^{-3})$ $(EC_{50}=9.39\;{\mu}g/ml)$. The $EC_{50}$ value of $17{\beta}-estradiol$ used as the positive control was $0.073\;{\mu}g/ml)$ (Relative Potency=1.00). There results demonstrated that some of the traditional medical herb may be useful in the therapy of estrogen replacement.

TERT mRNA Expression is Up-Regulated in MCF-7 Cells and a Mouse Mammary Organ Culture (MMOC) System by Endosulfan Treatment

  • Je Kang Hoon;Kim Ki Nam;Nam Kung Woo;Cho Myung Haing;Mar Woong Chon
    • Archives of Pharmacal Research
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    • v.28 no.3
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    • pp.351-357
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    • 2005
  • Endosulfan is one of the organochlorine pesticides, which are well-known endocrine disruptors (EDs), and it acts as an estrogen agonist. Estrogen is a group of hormones that play an important role in mammary gland function and are implicated in mammary carcinogenesis. In the present study, we studied the effects of endosulfan on nodule like alveolar lesion (NLAL) formation in mouse mammary gland development using a mouse mammary gland organ culture (MMOC) system. Although endosulfan-treated mammary glands did not form NLALs, more alveolar buds were formed in this group than in the negative control (vehicle-treated) group. In addition, telomerase reverse transcriptase (TERT) mRNA expression levels were increased in endosulfan-treated mammary glands in a dose-dependent manner. Telomerase can be activated by estrogen, therefore, we examined the effects of endosulfan on telomerase activity, and found that the telomerase activity in estrogen receptor-positive MCF-7 cells was up-regulated by endosulfan treatment. Moreover, this activation was accompanied by the up­regulation of the TERT mRNA expression. Also, transient expression assays using CAT reporter plasm ids containing various fragments of the TERT promoter showed that this imperfect palindromic estrogen-responsive element is almost certainly responsible for the transcriptional activation by endosulfan. These results may help elucidate the endocrine disrupting mechanism of endosulfan.

Estrogenic and Antiestrogenic Insecticides in MCF7-BUS Cell Line (피레스로이드계 살충제의 MCF7-BUS세포에 대한 에스트로겐 및 항에스트로겐 효과)

  • 오승민;정규혁
    • YAKHAK HOEJI
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    • v.45 no.6
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    • pp.694-700
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    • 2001
  • Synthetic pyrethroids are analysis of a natural chemical moiety, pyrethrin derived from the pyrethrum plant Chrysanthemum. The natural pyrethrin structure has been modified to be highly lipophilic and photostable, creating an effective pesticide and resulting in an increased presence in the environment. Worldwide, they are commonly used insecticides against ticks, mites, mosquitoes, and as treatment for human head lice and scabies. Therefore, human exposure to their compounds in extensive. Several studies on the effects of pyrethroids on thyroid hormone regulation, estrogen and androgen function have been reported and yet little has been done try assess their potential hormonal activities. Among humans, a pyrethroid compound was suggested to be the causal agent for gynecomastia in a group of Haitian men. The reports suggest that some pyrethroid compounds are capable of disrupting endocrine function. Therefore, we examined estrogenic/antiestrogenic potential of three pyrethroid insecticides, that is permethrin, allethrin and fenvalerate in human breast cancer cell and action mechanism mediated by the estrogen receptor. Fenvalerate showed weak estrogenic activity but aallethrin and permethrin showed no effect. In combination with high levels (10$^{-10}$ M, 10$^{-11}$ M) of 17$\beta$-estradiol and three synthetic pyrethroids inhibited cert proliferations in MCF7-BUS cell by 17$\beta$-estradiol. Whereas, fenvalerate increased cell proliferative activity at lower level of estradiol (10$^{-12}$ M, 10$^{-13}$ M). The relative affinities to the estrogen receptor were observed by allethrin and permethrin treatment, but not by fenvalerate. These results indicated that some of pyrethroid insecticides may modulate estrogen functions in human breast cancer cell. The action mechanisms of estrogen receptor mediated antiestrogenicity by allethrin and permethrin were postulated.

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Transcriptional Activity of an Estrogen Receptor β Subtype in the Medaka Oryzias dancena

  • Maeng, Sejung;Yoon, Sung Woo;Kim, Eun Jeong;Nam, Yoon Kwon;Sohn, Young Chang
    • Development and Reproduction
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    • v.23 no.4
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    • pp.333-344
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    • 2019
  • In vertebrate reproductive system, estrogen receptor (ER) plays a pivotal role in mediation of estrogenic signaling pathways. In the present study, we report the cDNA cloning, expression analysis, and transcriptional activity of ERβ1 subtype from medaka Oryzias dancena. The deduced O. dancena ERβ1 (odERβ1; 519 amino acids) contained six characteristic A/B to E/F domains with very short activation function 2 region (called AF2). A phylogenetic analysis indicated that odERβ1 was highly conserved among teleost ERβ1 subgroup. A conventional RT-PCR revealed that the odERβ1 transcripts were widely distributed in the multiple tissues, the ovary, brain, gill, intestine, kidney, and muscle. Further, the relatively higher odERβ1 expressions in the ovary and brain were clearly reproduced in RT-qPCR assay. When HA-fused odERβ1 expression vector was transfected into HEK293 cells, an immunoreactivity for odERβ1 was mainly detected in the nucleus part. Finally, an estrogen responsive element driven luciferase reporter assays demonstrated that the transcriptional activity of odERβ1 significantly increased by estradiol-17β (E2) in a dose dependent manner (p<0.05). However, fold-activation of odERβ1 in the presence of E2 was markedly weak, when it compared with those of O. latipes ERβ1. Taken together, these data suggest that odERβ1 represents a functional variant of teleost ERβ subtype and provides a basic tool allowing future studies examining the function of F domain of ERβ1 subtype and expanding our knowledge of ERβ evolution.

Estrogenic Activity of Sanguiin H-6 through Activation of Estrogen Receptor α Coactivator-binding Site

  • Trinh, Tuy An;Park, Eun-Ji;Lee, Dahae;Song, Ji Hoon;Lee, Hye Lim;Kim, Ki Hyun;Kim, Younghoon;Jung, Kiwon;Kang, Ki Sung;Yoo, Jeong-Eun
    • Natural Product Sciences
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    • v.25 no.1
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    • pp.28-33
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    • 2019
  • A popular approach for the study of estrogen receptor ${\alpha}$ inhibition is to investigate the protein-protein interaction between the estrogen receptor (ER) and the coactivator surface. In our study, we investigated phytochemicals from Rubus coreanus that were able to disrupt $ER{\alpha}$ and coactivator interaction with an $ER{\alpha}$ antagonist. The E-screen assay and molecular docking analysis were performed to evaluate the effects of the estrogenic activity of R. coreanus extract and its constituents on the MCF-7 human breast cancer cell line. At $100{\mu}g/mL$, R. coreanus extract significantly stimulated cell proliferation ($574.57{\pm}8.56%$). Sanguiin H6, which was isolated from R. coreanus, demonstrated the strongest affinity for the $ER{\alpha}$ coactivator-binding site in molecular docking analysis, with a binding energy of -250.149. The initial results of the study indicated that sanguiin H6 contributed to the estrogenic activity of R. coreanus through the activation of the $ER{\alpha}$ coactivator-binding site.

Verification of Estrogenic Activities in Ethanol Extracts of Oriental Herbal Medicines using In vitro Detection System (In vitro 검출시스템을 이용한 한약재 추출물로부터의 에스트로겐 활성의 검증)

  • Lee Sang Hyeon
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.17 no.4
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    • pp.1054-1058
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    • 2003
  • In order to evaluate the direct effect of estrogenic compounds in oriental herbal medicines, the estrogenic activity was measured using an in vitro detection system. For this system, human breast cancer cell line MCF7 was transfected using an estrogen responsive CAT reporter plasmid. Estrogenic activities of Platycodi radix, Astragali radix and Glycyrrhizae radix were evaluated using this system. Estrogenic activity of a 500 ㎍/ml ethanol extract of Platycodi radix was as same as that of a 10/sup -8/ M standard solution (17β-estradiol) and activity of a 50 ㎍/ml ethanol extract was between those of a 10/sup -8/ M and a 10/sup -9/ M standard solutions. In addition, estrogenic activity of a 50 ㎍/ml ethanol extract of Platycodi radix was as same as that of a 10/sup -10/ M standard solution. The same activity patterns were observed in the system which was treated by Astragali radix or Glycyrrhizae radix extracts. The most effective activity was observed in a system which was treated by Platycodi radix extract, but the least activity was observed by Glycyrrhizae radix extract. In this result, it was confirmed that Platycodi radix, Astragali radix and Glycyrrhizae radix extracts possess estrogenic compounds.