• Title/Summary/Keyword: $ER{\beta}$

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Clinical Analysis of Surgical Results and Preoperative Management of Acute Aortic Dissection (급성 대동맥박리증의 수술성적 및 수술전 처치에 대한 임상적 고찰)

  • 현성열;박국양;이재웅;이창하;전양빈;박철현;염석란;신종환;민순식
    • Journal of Chest Surgery
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    • v.35 no.12
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    • pp.876-881
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    • 2002
  • Acute aortic dissection associated with high mortality rate has an extremely poor prognosis if early diagnosis and treatment are not received. Recently, with advanced computed tomography and echocardiography, diagnostic rate is higher and early operation is possible. Therefore preoperative medical therapy at ER(emergency room) lowered the mortality rate. This study was done to analyze the results with preoperative management at ER and operations, retrospectively. Material and Method: A series of 42 patients treated surgically for acute aortic dissections from 1991 to 2001 were included in this study. There were 18 males and 24 females. Mean age was 51.1 years. The admission course through emergency and outpatient department(OPD) was 34 and 8 respectively. Result: 26 patients underwent ascending aorta replacement-7 combined aortic valve replacements, 7 patients underwent descending aorta replacements and 9 patients received Bentall's operation. At emergency department, 20 patients received antihypertensive drugs and $\beta$-receptor blockers and 6 patients died. 22 patients did not receive antihypertensive and $\beta$-receptor block drugs and 10 patients died. There were 16(38%) overall deaths. Conclusion: Early diagnosis at ER or OPD is essential for acute aortic dissection, and it is important to select the most appropriate noninvasive interventions as possible. Therefore, preoperative drug therapy at ER is suggested according the patient conditions.

Organotin Compounds Act as Inhibitor of Transcriptional Activation with Human Estrogen Receptor

  • Cho, Eun-Min;Lee, Haeng-Seog;Moon, Jeong-Suk;Kim, Im-Soon;Sim, Sang-Hyo;Ohta, Akinori
    • Journal of Microbiology and Biotechnology
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    • v.22 no.3
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    • pp.378-384
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    • 2012
  • In aquatic invertebrates, particularly marine gastropods, organotin compounds induce irreversible sexual abnormality in females, which is termed imposex, at very low concentrations. Organotin compounds are agonists for nuclear receptors such as RXRs and $PPAR{\gamma}$. However, the imposex phenomenon has not been reported to act as an antagonist on estrogen receptors in other species, including vertebrates and invertebrates. In order to gain insights into the antagonistic activity of organotin compounds on estrogen receptors (ERs), we examined the inhibitive effect of these compounds on estradiol-dependent ${\beta}$-galactosidase activity using the yeast two-hybrid detection system consisting of a combination of the human estrogen receptor ($hER{\beta}$) ligand-binding domain and the co-activator steroid receptor co-activator-1 (SRC1). Tributyltin-hydroxide (TBT-OH) and triphenyltin-chlorine (TPT-Cl) exhibited an inhibitive effect on $E_2$-dependent transcriptional activity, similar to antagonistic chemicals such as 4-hydroxytamoxifen (OHT) or ICI 182,780, at a very low concentration of $10^{-14}$ M TBT or $10^{-10}$ M TPT, respectively. The yeast growth and transcriptional activity with transcriptional factor GAL4 did not exhibit any effect at the tested concentration of TBT or TPT. Moreover, the yeast two-hybrid system using the interaction between p53 and the T antigen of SV40 large did not describe any effect at the tested concentration of OHT or ICI 182,780. However, the interaction between p53 and T antigen was inhibited at a TBT or TPT concentration of $10^{-9}$ M, respectively. These results indicate that TBT and TPT act as inhibitors of ER-dependent reporter gene transcriptional activation and of the interaction between $hER{\beta}$ LBD and the co-activator SRC1 in the yeast two-hybrid system. Consequently, our data could partly explain the occurrence of organotin compound-induced imposex on the endocrine system of mammals, including humans.

Mitogenic Estrogen Metabolites Alter the Expression of β-estradiol-regulated Proteins Including Heat Shock Proteins in Human MCF-7 Breast Cancer Cells

  • Kim, Seong Hwan;Lee, Su-Ui;Kim, Myung Hee;Kim, Bum Tae;Min, Yong Ki
    • Molecules and Cells
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    • v.20 no.3
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    • pp.378-384
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    • 2005
  • Estrogen metabolites are carcinogenic. The comparative mitogenic activities of $17{\beta}$-estradiol (E2) and four metabolites, 2-hydroxyestradiol (2-OHE2), 4-hydroxyestradiol (4-OHE2), $16{\alpha}$-hydroxyestrone ($16{\alpha}$-OHE1) and 2-methoxyestradiol (2-ME), were determined in estrogen receptor(ER)-positive MCF-7 human breast cancer cells. Each of the E2 metabolites caused proliferation of the MCF-7 cells, but only E2 and $16{\alpha}$-OHE1 induced a greater than 20-fold increases in transcripts of the progesterone receptor (PR) gene, a classical ER-mediated gene. This suggests that the mitogenic action of E2 and $16{\alpha}$-OHE1 could result from their effects on gene expression via the ER. E2 metabolites altered the expression of E2-regulated proteins including heat shock proteins (Hsps). $16{\alpha}$-OHE1 and 2-ME as well as E2 increased levels of Hsp56, Hsp60, $Hsp90{\alpha}$ and Hsp110 transcripts, and the patterns of these inductions resembled that of PR. Hsp56 and Hsp60 protein levels were increased by all the E2 metabolites. Levels of the transcripts of 3 E2-upregulated proteins (XTP3-transactivated protein A, protein disulfide isomerase-associated 4 protein and stathmin 1) and an E2-downregulated protein (aminoacylase 1) were also affected by the E2 metabolites. These results suggest that the altered expression of Hsps (especially Hsp56 and Hsp60) by E2 metabolites such as E2, $16{\alpha}$-OHE1 and 2-ME could be closely linked to their mitogenic action.

Assessment of Adipocyte Differentiation and Maturation-related Gene Expression in the Epididymal Fat of Estrogen Receptor α Knockout (ERαKO) Mouse during Postnatal Development Period

  • Cheon, Yong-Pil;Ko, CheMyong;Lee, Ki-Ho
    • Development and Reproduction
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    • v.24 no.4
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    • pp.287-296
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    • 2020
  • The absence of functional estrogen receptor α (Esr1) results in an overgrowth of the epididymal fat, as observed in estrogen receptor α knockout (ERαKO) mouse. The present research was aimed to evaluate expression of various molecules associated with adipocyte differentiation and maturation in the epididymal fat of ERαKO mouse at several postnatal ages by using quantitative real-time polymerase chain reaction. The highest transcript levels of all molecules were detected at 12 months of postnatal age, except leptin which the mRNA level was increased at 5 months of age and was unchanged until 12 months of age. The expression levels of CCAAT enhancer binding protein (Cebp) alpha, androgen receptor, and lipoprotein lipase were decreased at 5 months of age but increased at about 8 months of age. The mRNA levels of Cebp gamma and sterol regulatory element binding transcription factor 1 remained steady until 8 months of age. Continuous increases of transcript levels during postnatal period were found in Cebp beta, estrogen receptor (ER) beta, fatty acid binding protein 4, and delta like non-canonical Notch ligand 1. The increases of peroxisome proliferator-activated receptor gamma and adiponectin mRNA levels were detected as early as 8 months of age. The levels of fatty acid synthase and resistin transcript at 5 and 8 months of age were lower than that at 2 months of age. These findings show the aberrant expression patterns of genes related to adipocyte differentiation and maturation in the postnatal epididymal fat pad by the disruption of ER alpha function.

Evaluation of Estrogenic Activity of Extract from the Herbal Mixture Cynanchum wilfordii Hemsley, Phlomis umbrosa Turczaninow, and Angelica gigas Nakai

  • Kim, Se Jong;Jin, Sun Woo;Lee, Gi-Ho;Kim, Yong An;Jeong, Hye Gwang
    • Toxicological Research
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    • v.33 no.1
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    • pp.71-77
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    • 2017
  • Hormone replacement therapy (HRT) consists of highly effective prescription medications for treating menopausal symptoms; however, these agents have exhibited side effects including the risk of estrogen-induced carcinogenesis. Therefore, interest in phytotherapy-based materials as a natural source of alternatives to estrogen therapy has increased. However, some of these herbal medicines have been reported to increase the risk of estrogen-induced cancer. Herbal formulations composed of a combination of Cynanchum wilfordii Hemsley (CW), Phlomis umbrosa Turczaninow (PU), and Angelica gigas Nakai (AG) extracts (CPAE) have been used for treating menopausal symptoms. Therefore, in this study, we aimed to examine the safety of CPAE by determining its potential adverse estrogenic activity using the Organization for Economic Cooperation and Development (OECD) test guideline 455 (TG455) in a stably transfected transcriptionally activated human estrogen receptor ${\alpha}$ ($hER{\alpha}$)-HeLa9903 cell model. We found that CPAE did not how any estrogenic activity or stimulate promoters containing estrogen response elements in MCF-7 cells. In addition, CPAE showed no significant selective activity against $hER{\alpha}$ and $hER{\beta}$, non-selective activity against the ER, or effects on ER target gene expression. Furthermore, CPAE did not significantly induce MCF-7 cell proliferation and uterine weight increase in ovariectomized rats. These results demonstrate that CPAE can be used as beneficial herbal drug for prevention and therapeutic intervention of estrogen carcinogenesis in menopausal women.

Potential Therapeutic Targets for the Primary Gallbladder Carcinoma: Estrogen Receptors

  • Zhang, Ling-Qiang;Zhang, Xiu-De;Xu, Jia;Wan, Yong;Qu, Kai;Zhang, Jing-Yao;Wang, Zhi-Xin;Wei, Ji-Chao;Meng, Fan-Di;Tai, Ming-Hui;Zhou, Lei;Liu, Chang
    • Asian Pacific Journal of Cancer Prevention
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    • v.14 no.4
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    • pp.2185-2190
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    • 2013
  • Gallbladder carcinoma, the most frequent malignant neoplasm of the biliary tract system, has always been considered to feature late clinical presentation and diagnosis, limited treatment options and an extremely poor prognosis. In recent years, while the incidence of gallbladder cancer has appeared to be on the increase, the available treatment methods have not greatly improved survival of the affected patients. Thus, exploring new therapeutic targets for this devastating disease is an urgent matter at present. Epidemical studies have demonstrated that the incidence of gallbladder carcinoma exhibits a distinct gender bias, affecting females two to three times more than males, pointing to crucial roles of estrogen. It is well known that estrogen acts on target tissues by binding to estrogen receptors (ERs), which are mainly divided into three subtypes, $ER{\alpha}$, $ER{\beta}$ and $ER{\gamma}$. $ER{\alpha}$ and $ER{\beta}$ appear to have overlapping but also unique even opposite biological effects. As important pathogenic mediators, ERs have been considered to relate to several kinds of tumors. In gallbladder carcinoma tissue, ERs have been shown to be positively expressed, and ERs expression levels are associated with differentiation and prognosis of this cancer. Nevertheless, the exact mechanisms of estrogen inducing growth of gallbladder carcinoma remain poorly understood. On the base of the current investigations, we deduce that estrogen participates in promotion of gallbladder carcinoma by influencing the formation of gallstones, stimulating angiogenesis, and promoting abnormal proliferation. Since ERs mediate the carcinogenic actions of estrogen in gallbladder, and therapy targeting ERs may provide new directions for gallbladder carcinoma. Therefore, it should be stressed that ERs are potential therapeutic targets for gallbladder carcinoma.

17β-estradiol mediated effects on pluripotency transcription factors and differentiation capacity in mesenchymal stem cells derived porcine from newborns as steroid hormones non-functional donors

  • Lee, Won-Jae;Park, Ji-Sung;Lee, HyeonJeong;Lee, Seung-Chan;Lee, Jeong-Hyun;Ock, Sun-A;Rho, Gyu-Jin;Lee, Sung-Lim
    • Journal of Embryo Transfer
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    • v.32 no.3
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    • pp.209-220
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    • 2017
  • The estrogen-mediated effect of mesenchymal stem cells (MSCs) is a highly critical factor for the clinical application of MSCs. However, the present study is conducted on MSCs derived from adult donors, which have different physiological status with steroid hormonal changes. Therefore, we explores the important role of $17{\beta}$-estradiol (E2) in MSCs derived from female and male newborn piglets (NF- and NM-pBMSCs), which are non-sexually matured donors with steroid hormones. The results revealed that in vitro treatment of MSCs with E2 improved cell proliferation, but the rates varied according to the gender of the newborn donors. Following in vitro treatment of newborn MSCs with E2, mRNA levels of Oct3/4 and Sox2 increased in both genders of MSCs and they may be correlated with both estrogen receptor ${\alpha}$ ($ER{\alpha}$) and $ER{\beta}$ in NF-pBMSCs, but NM-pBMSCs were only correlated with $ER{\alpha}$. Moreover, E2-treated NF-pBMSCs decreased in ${\beta}$-galactosidase activity but no influence on NM-pBMSCs. In E2-mediated differentiation capacity, E2 induced an increase in the osteogenic and chondrogenic abilities of both pBMSCs, but adipogenic ability may increased only in NF-pBMSCs. These results demonstrate that E2 could affect both genders of newborn donor-derived MSCs, but the regulatory role of E2 varies depending on gender-dependent characteristics even though the original newborn donors had not been affected by functional steroid hormones.

Study on Estrogenic Activities of Phthalate Esters Using E-screen Assay and Competitive Binding Assay (E-screen Assay 및 상경적 결합반응을 이용한 Phthalate Esters의 내분비계 장애 작용 연구)

  • 한순영;한상국;문현주;김형식;이동하;김소희;김태성;박귀례
    • Toxicological Research
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    • v.16 no.2
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    • pp.141-146
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    • 2000
  • Phthalate esters are used extensively as a plasticizer in the manufacture of plastic products such as PVC bags and medical devices. Recently, phthalate esters have been shown to induce endocrine system mediated responses. However. only a Jew studies have been conducted for estrogenic activity of phthalate esters. In this study estrogenic activities of seven phthalate esters. butyl benzyl phthalate (BBP), di(2-ethylhexyl) phthalate (DEHP), di-n-butylphthalate (DBP), diethylphthalate (DEP), di-n-pentylphthalate (DPP), di-n-propylphthalate (DPrP) and dicyclohexylphthalate (DCHP), were examined in vitro using E-screen assay and competitive binding assay. From the E-screen assay, BBP. DEHP. DBP and DEP showed weak estrogenic activity at the concentration of 5 $\mu\textrm{M}$. The relative proliferative effect (RPE) and the relative proliferative potency (RPP) were 50~70% and 0.01%. respectively, when compared with 500 pM of 17$\beta$-estradiol (E2). In competitive binding assay with the rat uterine estrogen receptor (ER), BBP and DEP showed weak binding potency [(l/$10^4$~1/$10^5$ of E2] while DEHP and DBP scarcely bound to ER. These results suggest that some phthalate esters have weak estrogenic activities in vitro.

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Effect of Bisphenol-A on Vitellogenin Synthesis and Estrogen-Estrogen Receptor Binding Activity in the Primary Hepatocyte Cultures of Rainbow Trout, Oncorhynchus mykiss

  • Hwang Un-Gi;Kang Ju-Chan
    • Fisheries and Aquatic Sciences
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    • v.5 no.4
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    • pp.251-257
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    • 2002
  • Effects of bisphenol-A (BPA) on vitellogenin (VTG) synthesis and estrogen-estrogen receptor $(E_2- ER)$ binding activity were examined in primary hepatocyte cultures of rainbow trout, Oncorhynchus mykiss. Hepatocytes were precultured for 2 days and then $estradiol-17\beta\;(E_2,\;2\times10^{-6}M)\;BPA\;(10^{-5}-10^{-8}M)$ and/or 4-hydroxy-tamoxifen $(4-OHT,\;10^{-6} M)$ were simultaneously added to the incubation medium. Hepatocytes were cultured for 5 more days and then spent medium was analyzed by SDS-PAGE for VTG production. The addition of BPA to the incubation medium had no effect on the viability of hepatocytes in the culture. On the other hand, BPA increased VTG production in a concentration-dependent way and a significant increment occurred at BPA concentrations greater than $10^{-6}$M. Although VTG was increased by the addition of $E_2\;(2\times10^{-6}\;M)\;or\;BPA\;(10^{-5}M)$, its were reduced by a simultaneous 4-OHT $(10^{-6}\;M)$ addition. BPA inhibited $E_2-human$ ER binding activity by $72\%$ at $10^{-5}$ M of BPA. These results suggested that BPA induced VTG synthesis by BPA-ER binding activity in the hepatocyte of rainbow trout.

Beta-spectra for the Radionuclides in Medicine

  • Yi, Chul-Young;Kim, Kyung-Hwa;Park, Kyung-Bae;Han, Hyon-Soo;Jun, Jae-Shik;Chai, Ha-Seok
    • Progress in Medical Physics
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    • v.9 no.1
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    • pp.37-46
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    • 1998
  • Beta-particle energy distributions of the radionuclides in medicine are calculated for the medical physics applications. The radial component solutions of Dirac wave equations are evaluated for a point-nucleus un screened Coulomb potential. The WKB method is employed to correct the screening due to the orbital-electron cloud. Fierz interference terms are ignored. The radionuclides considered are $\^$32/P, $\^$90/Y, $\^$131/I, $\^$166/Ho, $\^$192/Ir, $\^$198/Au, $\^$153/Sm, $\^$169/Er and $\^$188/Re. A total of 9 beta-spectra for the radionuclides, currently in domestic use or potential use in the near future, are calculated with enough accuracy and presented in graphs and tables.

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