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1 / 1944

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[PMID]: 29253565 [Au] Autor: Lee W; Ko KR; Kim HK; Lim S; Kim S [Ad] Endereço: Department of Biological Sciences, Seoul National University, Seoul 151-742, South Korea; ViroMed Co., Ltd., Seoul 151-747, South Korea. [Ti] Título: Dehydrodiconiferyl alcohol promotes BMP-2-induced osteoblastogenesis through its agonistic effects on estrogen receptor. [So] Source: Biochem Biophys Res Commun;495(3):2242-2248, 2018 01 15. [Is] ISSN: 1090-2104 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Estrogen deficiency results in an imbalance between the levels of bone-resorping osteoclasts and bone-forming osteoblasts, eventually leading to overall bone loss. Dehydrodiconiferyl alcohol (DHCA), a lignan compound originally isolated from Cucurbita moschata, has been shown to bind to estrogen receptor, and indeed exhibits various activities of estrogen, such as anti-inflammatory and anti-oxidative stress effects. In this study, we tested whether synthetic DHCA could affect the BMP-2-induced osteoblastogenesis in vitro. In MC3T3-E1 cells, DHCA promoted BMP-2-induced differentiation of osteoblasts. Consistently, the expression of three osteoblastogenic genes known to be induced by BMP-2, ALP, osteocalcin and OPG, was up-regulated by DHCA treatment. DHCA was also shown to activate the production of RUNX2 by activating Smad1/5/9 and AMPK. Data from transient transfection assays suggested that DHCA might activate the estrogen receptor signaling pathway. Effects of DHCA on BMP-2-induced osteoblastogenesis were reduced when cells were treated with a specific siRNA to ERα or ERß. Taken together, our results suggest that DHCA may be developed as an efficient therapeutic for osteoporosis by regulating osteoblastogenesis through its estrogenic effects. [Mh] Termos MeSH primário: Proteína Morfogenética Óssea 2/metabolismo Moduladores de Receptor Estrogênico/administração & dosagem Estrogênios/metabolismo Osteoblastos/fisiologia Osteogênese/fisiologia Fenóis/administração & dosagem Receptores Estrogênicos/metabolismo [Mh] Termos MeSH secundário: Células 3T3 Animais Diferenciação Celular/efeitos dos fármacos Diferenciação Celular/fisiologia Relação Dose-Resposta a Droga Camundongos Osteoblastos/citologia Osteoblastos/efeitos dos fármacos Osteogênese/efeitos dos fármacos Receptores Estrogênicos/efeitos dos fármacos [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Bmp2 protein, mouse); 0 (Bone Morphogenetic Protein 2); 0 (Estrogen Receptor Modulators); 0 (Estrogens); 0 (Phenols); 0 (Receptors, Estrogen); 4263-87-0 (dehydrodiconiferyl alcohol) [Em] Mês de entrada: 1802 [Cu] Atualização por classe: 180214 [Lr] Data última revisão: 180214 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171219 [St] Status: MEDLINE

2 / 1944

MEDLINE

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[PMID]: 29198894 [Au] Autor: Singla R; Gupta KB; Upadhyay S; Dhiman M; Jaitak V [Ad] Endereço: Centre for Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda, India. [Ti] Título: Design, synthesis and biological evaluation of novel indole-xanthendione hybrids as selective estrogen receptor modulators. [So] Source: Bioorg Med Chem;26(1):266-277, 2018 01 01. [Is] ISSN: 1464-3391 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Ground breaking clinical therapeutic advances in the treatment of breast cancer (BC) is the introduction of selective estrogen receptor modulators (SERMs). We have expeditiously designed and synthesized indole-xanthendione hybrids by coalescing the indole nucleus with xanthendione. All the compounds were first screened for anti-proliferative activity, cytotoxicity and ER-α binding affinity by utilizing ER-α dominant T47D BC cell lines, PBMCs and ER-α competitor assay kit. From this study, two representative compounds 6e and 6f showing most promising activity were advanced for gene expression studies for targeting ER-α. Cell imaging experiment undoubtedly indicate that both the compounds were able to cross cellular bio membrane and accumulate thus instigating cytotoxicity. RT-PCR and Western blotting experiments further strengthened that both compounds altered the expression of mRNA and receptor protein of ER-α, thereby forestalling downstream transactivation and signalling pathway in T47D cells line. Structural investigation from induced fit simulation study suggest that indole moiety of the compounds 6e and 6f helps in the anchoring of the xanthendione moiety in the hydrophobic region of the cavity thus enabling the compound to bind in antagonistic conformation similar to bazedoxifene by extensive hydrogen bonding and Van der Waals forces. All these finding collectively imply that compound 6e and 6f represents a novel potent ER-α antagonist and in the development of SERMs for the management of BC. [Mh] Termos MeSH primário: Antineoplásicos/farmacologia Desenho de Drogas Moduladores de Receptor Estrogênico/farmacologia Receptor alfa de Estrogênio/antagonistas & inibidores Indóis/farmacologia Xantonas/farmacologia [Mh] Termos MeSH secundário: Antineoplásicos/síntese química Antineoplásicos/química Proliferação Celular/efeitos dos fármacos Células Cultivadas Relação Dose-Resposta a Droga Ensaios de Seleção de Medicamentos Antitumorais Moduladores de Receptor Estrogênico/síntese química Moduladores de Receptor Estrogênico/química Receptor alfa de Estrogênio/metabolismo Seres Humanos Indóis/química Estrutura Molecular Relação Estrutura-Atividade Xantonas/química [Pt] Tipo de publicação: JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T [Nm] Nome de substância: 0 (Antineoplastic Agents); 0 (Estrogen Receptor Modulators); 0 (Estrogen Receptor alpha); 0 (Indoles); 0 (Xanthones); 0 (estrogen receptor alpha, human); 8724FJW4M5 (indole) [Em] Mês de entrada: 1801 [Cu] Atualização por classe: 180106 [Lr] Data última revisão: 180106 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171205 [St] Status: MEDLINE

3 / 1944

MEDLINE

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[PMID]: 29031686 [Au] Autor: Alhodhodi A; Alkharobi H; Humphries M; Alkhafaji H; El-Gendy R; Feichtinger G; Speirs V; Beattie J [Ad] Endereço: Department of Oral Biology, Wellcome Trust Brenner Building, St James University Hospital, University of Leeds, UK. [Ti] Título: Oestrogen receptor ß (ERß) regulates osteogenic differentiation of human dental pulp cells. [So] Source: J Steroid Biochem Mol Biol;174:296-302, 2017 Nov. [Is] ISSN: 1879-1220 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Estradiol (E ) has many important actions in the tissues of the oral cavity. Disruption of E metabolism or alterations in systemic E concentrations have been associated with compromised periodontal health. In many instances such changes occur secondarily to the well characterised effects of E on bone physiology -especially maintenance of bone mineral density (BMD). Despite these important epidemiological findings, little is known about the mechanism of action of E in oral tissues or the expression and function of oestrogen receptor (ER) isoforms in these tissues. We have isolated human dental pulp cells (hDPCs), which are able to differentiate towards an osteogenic lineage under appropriate culture conditions. We show that hDPCs express ERα, ERß1, ERß2 and the cell membrane associated G protein-coupled ER (GPR30). Following osteogenic differentiation of hDPCs, ERß1 and ERß2 were up regulated approximately 50-fold while ERα and GPR30 were down regulated, but to a much lesser degree (approximately 2-fold). ERß was characterised as a 59kDa protein following Western blot analysis with validated antibodies and ERß was detected in both nuclear and cytoplasmic cell compartments following immunofluorescence (IF) and immunohistochemical (IHC) analysis of cultured cells. Furthermore isoform specific antibodies detected both ERß1 and ERß2 in DPC cultures and in situ analysis of ERß expression in decalcified tooth/pulp sections identified the odontoblast layer of pulp cells juxtaposed to the tooth enamel as strongly reactive for both ERß isoforms. Finally the use of isoform specific agonists identified ERß as the main receptor responsible for the pro-osteogenic effect of oestrogenic hormones in this tissue. Our data suggest that oestrogens stimulated osteogenic differentiation in hDPCs and that this action is mediated principally through the ERß isoform. These findings may have important consequences for the investigation and treatment of oral and periodontal pathologies which are associated with imbalances in oestrogen concentrations and action. [Mh] Termos MeSH primário: Polpa Dentária/citologia Receptor beta de Estrogênio/metabolismo Osteogênese/fisiologia [Mh] Termos MeSH secundário: Adulto Diferenciação Celular/efeitos dos fármacos Células Cultivadas Moduladores de Receptor Estrogênico/farmacologia Receptor alfa de Estrogênio/genética Receptor alfa de Estrogênio/metabolismo Receptor beta de Estrogênio/genética Estrogênios/farmacologia Feminino Seres Humanos Nitrilos/farmacologia Fenóis/farmacologia Pirazóis/farmacologia Receptores Estrogênicos/genética Receptores Estrogênicos/metabolismo Receptores Acoplados a Proteínas-G/genética Receptores Acoplados a Proteínas-G/metabolismo Adulto Jovem [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (2,3-bis(4-hydroxyphenyl)-propionitrile); 0 (Estrogen Receptor Modulators); 0 (Estrogen Receptor alpha); 0 (Estrogen Receptor beta); 0 (Estrogens); 0 (GPER protein, human); 0 (Nitriles); 0 (Phenols); 0 (Pyrazoles); 0 (Receptors, Estrogen); 0 (Receptors, G-Protein-Coupled); 0 (estrogen receptor alpha, human); 0T83Y6JZPF (1,3,5-tris(4-hydroxyphenyl)-4-propyl-1H-pyrazole) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171113 [Lr] Data última revisão: 171113 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 171017 [St] Status: MEDLINE

4 / 1944

MEDLINE

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[PMID]: 28904064 [Au] Autor: Zhao Y; Laws MJ; Guillen VS; Ziegler Y; Min J; Sharma A; Kim SH; Chu D; Park BH; Oesterreich S; Mao C; Shapiro DJ; Nettles KW; Katzenellenbogen JA; Katzenellenbogen BS [Ad] Endereço: Department of Molecular and Integrative Physiology, University of Illinois at Urbana-Champaign, Urbana, Illinois. [Ti] Título: Structurally Novel Antiestrogens Elicit Differential Responses from Constitutively Active Mutant Estrogen Receptors in Breast Cancer Cells and Tumors. [So] Source: Cancer Res;77(20):5602-5613, 2017 Oct 15. [Is] ISSN: 1538-7445 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: Many estrogen receptor α (ERα)-positive breast cancers develop resistance to endocrine therapy via mutation of ERs whose constitutive activation is associated with shorter patient survival. Because there is now a clinical need for new antiestrogens (AE) against these mutant ERs, we describe here our development and characterization of three chemically novel AEs that effectively suppress proliferation of breast cancer cells and tumors. Our AEs are effective against wild-type and Y537S and D538G ERs, the two most commonly occurring constitutively active ERs. The three new AEs suppressed proliferation and estrogen target gene expression in WT and mutant ER-containing cells and were more effective in D538G than in Y537S cells and tumors. Compared with WT ER, mutants exhibited approximately 10- to 20-fold lower binding affinity for AE and a reduced ability to be blocked in coactivator interaction, likely contributing to their relative resistance to inhibition by AE. Comparisons between mutant ER-containing MCF7 and T47D cells revealed that AE responses were compound, cell-type, and ERα-mutant dependent. These new ligands have favorable pharmacokinetic properties and effectively suppressed growth of WT and mutant ER-expressing tumor xenografts in NOD/SCID-γ mice after oral or subcutaneous administration; D538G tumors were more potently inhibited by AE than Y537S tumors. These studies highlight the differential responsiveness of the mutant ERs to different AEs and make clear the value of having a toolkit of AEs for treatment of endocrine therapy-resistant tumors driven by different constitutively active ERs. . [Mh] Termos MeSH primário: Neoplasias da Mama/tratamento farmacológico Neoplasias da Mama/genética Moduladores de Receptor Estrogênico/farmacologia Receptor alfa de Estrogênio/genética Mutação [Mh] Termos MeSH secundário: Animais Neoplasias da Mama/patologia Diferenciação Celular/efeitos dos fármacos Proliferação Celular/efeitos dos fármacos Moduladores de Receptor Estrogênico/química Receptor alfa de Estrogênio/metabolismo Feminino Seres Humanos Camundongos Camundongos Endogâmicos NOD Camundongos SCID Distribuição Aleatória Relação Estrutura-Atividade Ensaios Antitumorais Modelo de Xenoenxerto [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Estrogen Receptor Modulators); 0 (Estrogen Receptor alpha); 0 (estrogen receptor alpha, human) [Em] Mês de entrada: 1711 [Cu] Atualização por classe: 171108 [Lr] Data última revisão: 171108 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170915 [St] Status: MEDLINE [do] DOI: 10.1158/0008-5472.CAN-17-1265

5 / 1944

MEDLINE

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[PMID]: 28849994 [Au] Autor: Hultman MT; Petersen K; Tollefsen KE [Ad] Endereço: a Norwegian Institute for Water Research (NIVA) , Oslo , Norway. [Ti] Título: Characterizing combined effects of antiestrogenic chemicals on vitellogenin production in rainbow trout (Oncorhynchus mykiss) hepatocytes. [So] Source: J Toxicol Environ Health A;80(16-18):987-1001, 2017. [Is] ISSN: 1528-7394 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Fish are exposed to a complex mixture of endocrine disrupting compounds (EDC), some of which display antiestrogenic activity leading to suppression of estrogen receptor (ER)- mediated reproductive processes. Although the main mode of action (MoA) of these antiestrogens is to directly interfere with natural ligand binding of the ER, several other MoA have been proposed. The aim of the present study was to characterize single and combined antiestrogenic effects of the aryl hydrocarbon receptor (AhR)-agonist ß-naphthoflavone (BNF) and ER-antagonist 4-hydroxytamoxifen (OHT) on vitellogenin (Vtg) protein using primary rainbow trout (Oncorhynchus mykiss) hepatocytes. Supporting transcriptional analysis of ER-responsive genes (estrogen receptor-α (er-α), vitellogenin-1 (vtg-1), eggshell zona radiata protein (zrp)) and AhR-mediated genes (aryl hydrocarbon receptor-2ß, cytochrome p450-1a (cyp1a)) was performed by qPCR to characterize the antiestrogenic influence on ER- and AhR-mediated responses. Data demonstrated that both BNF and OHT significantly reduced 17ß-estradiol (E2)-induced Vtg protein expression in a concentration responsive manner, whereas exposure to a mixture of these produced an additive antiestrogenic effect. The results observed at the protein level were further supported by transcriptional analysis of ER-responsive genes (er-α, vtg-1, zrp), where only E2-induced vtg-1 gene expression was significantly decreased by OHT and the mixture of OHT and BNF. E2-induced er-α and zrp gene expression was not markedly altered. The significant reduction of E2-induced vtg-1 gene expression by OHT suggested that the antiestrogenic effect of this compound may be associated with ER signaling pathway. Specific genes involved in putative AhR-ER cross-talk were also investigated, however none were directly associated with the compound anti-estrogenic MoA. Although the MoA of the single compounds and mixture were not completely characterized, the present study enhanced our knowledge of the combined toxicity mediated by antiestrogens acting through different MoA. [Mh] Termos MeSH primário: Disruptores Endócrinos/toxicidade Moduladores de Receptor Estrogênico/toxicidade Hepatócitos/efeitos dos fármacos Oncorhynchus mykiss/genética Vitelogeninas/biossíntese beta-Naftoflavona/toxicidade [Mh] Termos MeSH secundário: Animais Células Cultivadas Citocromo P-450 CYP1A1/genética Citocromo P-450 CYP1A1/metabolismo Proteínas do Ovo/genética Proteínas do Ovo/metabolismo Estradiol/toxicidade Receptor alfa de Estrogênio/genética Receptor alfa de Estrogênio/metabolismo Hepatócitos/metabolismo Masculino Oncorhynchus mykiss/metabolismo Receptores de Hidrocarboneto Arílico/agonistas Receptores de Hidrocarboneto Arílico/genética Receptores de Hidrocarboneto Arílico/metabolismo Receptores Estrogênicos/antagonistas & inibidores Receptores Estrogênicos/genética Receptores Estrogênicos/metabolismo Transdução de Sinais Tamoxifeno/análogos & derivados Tamoxifeno/toxicidade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Egg Proteins); 0 (Endocrine Disruptors); 0 (Estrogen Receptor Modulators); 0 (Estrogen Receptor alpha); 0 (Receptors, Aryl Hydrocarbon); 0 (Receptors, Estrogen); 0 (Vitellogenins); 0 (zona radiata protein, fish); 094ZI81Y45 (Tamoxifen); 17197F0KYM (afimoxifene); 4TI98Z838E (Estradiol); 6051-87-2 (beta-Naphthoflavone); EC 1.14.14.1 (Cytochrome P-450 CYP1A1) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171031 [Lr] Data última revisão: 171031 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170830 [St] Status: MEDLINE [do] DOI: 10.1080/15287394.2017.1354435

6 / 1944

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[PMID]: 28841614 [Au] Autor: Thomas S; Chen S; Sbitany H; Kwon E; Piper M; Park J; Terranova Barberio M; Pawlowska N; Munster PN [Ad] Endereço: San Francisco, Calif. From the Division of Hematology and Oncology, University of California, San Francisco, Helen Diller Family Comprehensive Cancer Center. [Ti] Título: Autologous Fat Grafting as a Novel Antiestrogen Vehicle for the Treatment of Breast Cancer. [So] Source: Plast Reconstr Surg;140(3):537-544, 2017 Sep. [Is] ISSN: 1529-4242 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: BACKGROUND: Adipose fat transfer is increasingly used for contour corrections of the tumor bed after lumpectomy and breast reconstructions after mastectomy. The lipophilic nature of the fat tissue may render adipocytes an ideal vehicle with which to deliver a high boost of an antiestrogen to the tumor bed to serve as an adjunct systemic hormonal therapy. The authors therefore tested whether adipocytes could safely be loaded with an antiestrogen and allow for release at therapeutic concentrations to treat breast cancer. METHODS: Adipose tissue was collected from patients undergoing autologous fat grafting. The influence of adipose tissue on tumorigenesis was determined both in vitro and in vivo using breast cancer cell lines. Ex vivo, adipose tissue was assessed for its ability to depot fulvestrant and inhibit the growth of breast cancer cell lines. RESULTS: Adipose tissue harvested from patients did not promote breast cancer cell growth in vitro or in an in vivo mouse model. Adipose tissue was successfully loaded with fulvestrant and released at levels sufficient to inhibit estrogen receptor signaling and growth of breast cancer cells. CONCLUSIONS: This work supports the hypothesis that adipose tissue used for autologous fat grafting can serve as a novel method for local drug delivery. As this technique is used to reconstruct a variety of postsurgical defects following cancer resection, this approach for local drug delivery may be an effective alternative in therapeutic settings beyond breast cancer. [Mh] Termos MeSH primário: Tecido Adiposo/transplante Antineoplásicos Hormonais/administração & dosagem Neoplasias da Mama/tratamento farmacológico Neoplasias da Mama/cirurgia Sistemas de Liberação de Medicamentos/métodos Estradiol/análogos & derivados Moduladores de Receptor Estrogênico/administração & dosagem Mamoplastia [Mh] Termos MeSH secundário: Animais Células Cultivadas Quimioterapia Adjuvante/métodos Modelos Animais de Doenças Estradiol/administração & dosagem Feminino Seres Humanos Camundongos Camundongos Nus Transplante Autólogo [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Antineoplastic Agents, Hormonal); 0 (Estrogen Receptor Modulators); 22X328QOC4 (fulvestrant); 4TI98Z838E (Estradiol) [Em] Mês de entrada: 1709 [Cu] Atualização por classe: 170922 [Lr] Data última revisão: 170922 [Sb] Subgrupo de revista: AIM; IM [Da] Data de entrada para processamento: 170826 [St] Status: MEDLINE [do] DOI: 10.1097/PRS.0000000000003579

7 / 1944

MEDLINE

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[PMID]: 28810190 [Au] Autor: Lao K; Wang Y; Chen M; Zhang J; You Q; Xiang H [Ad] Endereço: Institute of Basic and Translational Medicine, and School of Basic Medical Science, Xi'an Medical University, No.1 Xinwang Road, Xi'an, 710021, PR China; Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing, 210009, PR China. [Ti] Título: Design, synthesis and biological evaluation of novel 2-methoxyestradiol analogs as dual selective estrogen receptor modulators (SERMs) and antiangiogenic agents. [So] Source: Eur J Med Chem;139:390-400, 2017 Oct 20. [Is] ISSN: 1768-3254 [Cp] País de publicação: France [La] Idioma: eng [Ab] Resumo: 2-methoxyestradiol is a novel agent showing both anti-angiogenic and vascular disrupting properties. In this study, a series of 11α-substituted 2-methoxyestradiol analogs have been designed and synthesized targeting dual ERα and microtubulin. Biological evaluation was performed on their anti-proliferative activities against 5 different cell lines. The results indicated that most compounds exhibited good activities, in which compound 24c and 30c showed the best activity with low micromolar IC (2.73 µM -7.75 µM) in all cell lines. The investigation of ER affinity showed that the majority of the compounds displayed good activity at the concentration of 50 µM. In further mechanism study, it was observed that 24c and 30c could induce G2/M cell cycle arrest as well as significant anti-estrogenic activity. In CAM assay, compound 24c and 30c presented significantly anti-angiogenesis activity comparable with 2-methoxyestradiol. Overall, based on biological activities data, 24c and 30c can be identified as a potential lead molecule which might be of therapeutic importance for cancer treatment. [Mh] Termos MeSH primário: Inibidores da Angiogênese/farmacologia Desenho de Drogas Estradiol/análogos & derivados Moduladores de Receptor Estrogênico/farmacologia [Mh] Termos MeSH secundário: Inibidores da Angiogênese/síntese química Inibidores da Angiogênese/química Animais Ciclo Celular/efeitos dos fármacos Linhagem Celular Tumoral Proliferação Celular/efeitos dos fármacos Galinhas Membrana Corioalantoide/efeitos dos fármacos Relação Dose-Resposta a Droga Estradiol/síntese química Estradiol/química Estradiol/farmacologia Moduladores de Receptor Estrogênico/síntese química Moduladores de Receptor Estrogênico/química Células Endoteliais da Veia Umbilical Humana/efeitos dos fármacos Seres Humanos Células MCF-7 Estrutura Molecular Receptores Estrogênicos/genética Receptores Estrogênicos/metabolismo Relação Estrutura-Atividade [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Angiogenesis Inhibitors); 0 (Estrogen Receptor Modulators); 0 (Receptors, Estrogen); 4TI98Z838E (Estradiol); 6I2QW73SR5 (2-methoxyestradiol) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171018 [Lr] Data última revisão: 171018 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170816 [St] Status: MEDLINE

8 / 1944

MEDLINE

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[PMID]: 28717100 [Au] Autor: Okazaki H; Takeda S; Matsuo S; Matsumoto M; Furuta E; Kohro-Ikeda E; Aramaki H [Ad] Endereço: Department of Molecular Biology, Daiichi University of Pharmacy. [Ti] Título: Inhibitory modulation of human estrogen receptor α and ß activities by dicyclohexyl phthalate in human breast cancer cell lines. [So] Source: J Toxicol Sci;42(4):417-425, 2017. [Is] ISSN: 1880-3989 [Cp] País de publicação: Japan [La] Idioma: eng [Ab] Resumo: Phthalate esters (PAEs) are man-made compounds that are used widely in industry, and the ubiquitous exposure of humans to PAEs has been reported. Although some PAEs have been suggested to function as xenoestrogens in in vitro systems, such as human estrogen receptors (ERs) expressed in Chinese hamster ovary (CHO)-K1 cells, few studies have attempted to elucidate whether PAEs affect human ERα/ERß-mediated signaling in human breast cancer cells (i.e., combination between human ERs and human cells). Thus, further experiments are needed in order to clarify the activities of PAEs. Among the 9 PAEs (carbon# in the side chains: 2-8) investigated, dibutyl phthalate (DBP), dipentyl phthalate (DPENP), and dicyclohexyl phthalate (DCHP) were found to exhibit strong anti-estrogenic activities in MCF-7 cells (ER-positive) in the presence of 1 nM 17ß-estradiol (E2). Since limited information is currently available on DPENP and DCHP, we herein focused on these two PAEs. Experiments using MDA-MB-231 cells (ER-negative) transfected with human ERα or ERß expression plasmids revealed that DCHP was a markedly stronger anti-estrogenic PAE than DPENP; DCHP inhibited ERα and ERß activities stimulated by 1 nM E2 with IC values of ~5 and 11.2 µM, respectively. Furthermore, DCHP abrogated diarylpropionitrile (DPN)-stimulated ERß activity with an IC value of 5.17 µM, which was approximately 2-fold stronger than that of DPENP (IC = 10 µM). The results of the present study suggest that PAEs (DCHP) function not only as an anti-estrogen for ERα, but also for ERß, at least in human breast cancer cell lines. [Mh] Termos MeSH primário: Neoplasias da Mama/metabolismo Disruptores Endócrinos/toxicidade Moduladores de Receptor Estrogênico Receptor alfa de Estrogênio/metabolismo Receptor beta de Estrogênio/metabolismo Ácidos Ftálicos/toxicidade [Mh] Termos MeSH secundário: Animais Células CHO Linhagem Celular Tumoral Cricetinae Cricetulus Relação Dose-Resposta a Droga Estradiol/farmacologia Receptor alfa de Estrogênio/fisiologia Receptor beta de Estrogênio/fisiologia Feminino Seres Humanos Células MCF-7 Nitrilos/antagonistas & inibidores Ácidos Ftálicos/química Propionatos/antagonistas & inibidores Transdução de Sinais/efeitos dos fármacos [Pt] Tipo de publicação: JOURNAL ARTICLE [Nm] Nome de substância: 0 (Endocrine Disruptors); 0 (Estrogen Receptor Modulators); 0 (Estrogen Receptor alpha); 0 (Estrogen Receptor beta); 0 (Nitriles); 0 (Phthalic Acids); 0 (Propionates); 0 (diarylpropionitrile); 4TI98Z838E (Estradiol); CGD15M7H2N (dicyclohexyl phthalate) [Em] Mês de entrada: 1710 [Cu] Atualização por classe: 171005 [Lr] Data última revisão: 171005 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170719 [St] Status: MEDLINE [do] DOI: 10.2131/jts.42.417

9 / 1944

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[PMID]: 28629994 [Au] Autor: Leblanc DR; Schneider M; Angele P; Vollmer G; Docheva D [Ad] Endereço: Experimental Surgery and Regenerative Medicine, Department of Surgery, Ludwig-Maximilians-University Munich, Germany. [Ti] Título: The effect of estrogen on tendon and ligament metabolism and function. [So] Source: J Steroid Biochem Mol Biol;172:106-116, 2017 Sep. [Is] ISSN: 1879-1220 [Cp] País de publicação: England [La] Idioma: eng [Ab] Resumo: Tendons and ligaments are crucial structures inside the musculoskeletal system. Still many issues in the treatment of tendon diseases and injuries have yet not been resolved sufficiently. In particular, the role of estrogen-like compound (ELC) in tendon biology has received until now little attention in modern research, despite ELC being a well-studied and important factor in the physiology of other parts of the musculoskeletal system. In this review we attempt to summarize the available information on this topic and to determine many open questions in this field. [Mh] Termos MeSH primário: Moduladores de Receptor Estrogênico/farmacologia Ligamentos/efeitos dos fármacos Fitoestrógenos/farmacologia Traumatismos dos Tendões/tratamento farmacológico Tendões/efeitos dos fármacos [Mh] Termos MeSH secundário: Animais Colágeno Tipo I/genética Colágeno Tipo I/metabolismo Receptor alfa de Estrogênio/química Receptor alfa de Estrogênio/genética Receptor alfa de Estrogênio/metabolismo Receptor beta de Estrogênio/química Receptor beta de Estrogênio/genética Receptor beta de Estrogênio/metabolismo Feminino Expressão Gênica/efeitos dos fármacos Terapia de Reposição Hormonal/métodos Seres Humanos Ligamentos/lesões Ligamentos/metabolismo Menopausa/genética Ovariectomia Gravidez Homologia Estrutural de Proteína Traumatismos dos Tendões/genética Traumatismos dos Tendões/metabolismo Traumatismos dos Tendões/patologia Tendões/metabolismo Tendões/patologia [Pt] Tipo de publicação: JOURNAL ARTICLE; REVIEW [Nm] Nome de substância: 0 (Collagen Type I); 0 (Estrogen Receptor Modulators); 0 (Estrogen Receptor alpha); 0 (Estrogen Receptor beta); 0 (Phytoestrogens) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170822 [Lr] Data última revisão: 170822 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170621 [St] Status: MEDLINE

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MEDLINE

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[PMID]: 28602910 [Au] Autor: Pinto PIS; Estêvão MD; Santos S; Andrade A; Power DM [Ad] Endereço: Centre of Marine Sciences (CCMAR), Universidade do Algarve, Campus de Gambelas, 8005-139 Faro, Portugal. Electronic address: ppinto@ualg.pt. [Ti] Título: In vitro screening for estrogenic endocrine disrupting compounds using Mozambique tilapia and sea bass scales. [So] Source: Comp Biochem Physiol C Toxicol Pharmacol;199:106-113, 2017 Sep. [Is] ISSN: 1532-0456 [Cp] País de publicação: United States [La] Idioma: eng [Ab] Resumo: A wide range of estrogenic endocrine disruptors (EDCs) are accumulating in the environment and may disrupt the physiology of aquatic organisms. The effects of EDCs on fish have mainly been assessed using reproductive endpoints and in vivo animal experiments. We used a simple non-invasive assay to evaluate the impact of estrogens and EDCs on sea bass (Dicentrarchus labrax) and tilapia (Oreochromis mossambicus) scales. These were exposed to estradiol (E2), two phytoestrogens and six anthropogenic estrogenic/anti-estrogenic EDCs and activities of enzymes related to mineralized tissue turnover (TRAP, tartrate-resistant acid phosphatase and ALP, alkaline phosphatase) were measured. Semi-quantitative RT-PCR detected the expression of both membrane and nuclear estrogen receptors in the scales of both species, confirming scales as a target for E2 and EDCs through different mechanisms. Changes in TRAP or ALP activities after 30minute and 24h exposure were detected in sea bass and tilapia scales treated with E2 and three EDCs, although compound-, time- and dose-specific responses were observed for the two species. These results support again that the mineralized tissue turnover of fish is regulated by estrogens and reveals that the scales are a mineralized estrogen-responsive tissue that may be affected by some EDCs. The significance of these effects for whole animal physiology needs to be further explored. The in vitro fish scale bioassay is a promising non-invasive screening tool for E2 and EDCs effects, although the low sensitivity of TRAP/ALP quantification limits their utility and indicates that alternative endpoints are required. [Mh] Termos MeSH primário: Bass/fisiologia Disruptores Endócrinos/toxicidade Estrogênios/toxicidade Receptores Estrogênicos/metabolismo Pele/efeitos dos fármacos Tilápia/fisiologia Poluentes Químicos da Água/toxicidade [Mh] Termos MeSH secundário: Fosfatase Alcalina/metabolismo Animais Aquicultura Bass/crescimento & desenvolvimento Membrana Celular/efeitos dos fármacos Membrana Celular/metabolismo Núcleo Celular/efeitos dos fármacos Núcleo Celular/metabolismo Estradiol/toxicidade Moduladores de Receptor Estrogênico/toxicidade Proteínas de Peixes/genética Proteínas de Peixes/metabolismo Masculino Fitoestrógenos/toxicidade Portugal Isoformas de Proteínas/genética Isoformas de Proteínas/metabolismo Receptores Estrogênicos/genética Pele/química Pele/crescimento & desenvolvimento Pele/metabolismo Especificidade da Espécie Fosfatase Ácida Resistente a Tartarato/metabolismo Tilápia/crescimento & desenvolvimento Distribuição Tecidual Testes de Toxicidade Toxicocinética [Pt] Tipo de publicação: COMPARATIVE STUDY; JOURNAL ARTICLE [Nm] Nome de substância: 0 (Endocrine Disruptors); 0 (Estrogen Receptor Modulators); 0 (Estrogens); 0 (Fish Proteins); 0 (Phytoestrogens); 0 (Protein Isoforms); 0 (Receptors, Estrogen); 0 (Water Pollutants, Chemical); 4TI98Z838E (Estradiol); EC 3.1.3.1 (Alkaline Phosphatase); EC 3.1.3.2 (Tartrate-Resistant Acid Phosphatase) [Em] Mês de entrada: 1708 [Cu] Atualização por classe: 170809 [Lr] Data última revisão: 170809 [Sb] Subgrupo de revista: IM [Da] Data de entrada para processamento: 170613 [St] Status: MEDLINE

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