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Pesquisa : D04.210.500.668.651.693.762 [Categoria DeCS]
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[PMID]:28972919
[Au] Autor:Liang YQ; Huang GY; Lin Z; Li J; Yang JW; Zhong LY; Ying GG
[Ad] Endereço:Faculty of Chemistry and Environmental Science, Guangdong Ocean University, Zhanjiang, 524088, PR China. Electronic address: liangyanqiu11@126.com.
[Ti] Título:Reproductive effects of synthetic progestin norgestrel in zebrafish (Danio rerio).
[So] Source:Chemosphere;190:17-24, 2018 Jan.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The aim of this study was to assess the adverse effects of synthetic progestin norgestrel (NGT) on the reproduction of zebrafish by measuring the egg production, histology and transcriptional expression profiles along the hypothalamic-pituitary-gonadal (HPG) axis in adult zebrafish. After a pre-exposure period of 7 days, adult zebrafish were exposed to 6, 29 and 69 ng L NGT for 21 days. The results showed that exposure to 69 ng L NGT led to a significant up-regulation of follicle stimulating hormone, beta polypeptide (fshb), luteinizing hormone, beta polypeptide (lhb), progesterone receptor (pgr), estrogen receptor 1 (esr1) and androgen receptor (ar) genes in the brains, as well as significant up-regulation of hydroxysteroid 20-beta dehydrogenase (hsd20b) and hydroxysteroid 11-beta dehydrogenase 2 (hsd11b2) genes and down-regulation of 11-beta-hydroxylase (cyp11b) gene in the ovaries of females. In the testes of males, an overall down-regulation of steroidogenic acute regulatory protein (star), cytochrome P450-mediated side-chain cleavage enzyme (cyp11a1), cyp11b, hsd20b, hydroxysteroid 17-beta dehydrogenase type 3 (hsd17b3), hsd11b2 and ar genes were observed following exposure to different treatments of NGT. These transcriptional alterations imply that NGT could exhibit the potent progestogenic and androgenic activities in zebrafish. Egg production as well as histology in the ovaries and testes was not affected by NGT. Taken together, the overall results demonstrated that NGT could significantly affect transcriptional expression levels of genes related to HPG axis in zebrafish, and whether that change translates to additional physiological effects is needed further research.
[Mh] Termos MeSH primário: Regulação da Expressão Gênica/efeitos dos fármacos
Norgestrel/farmacologia
Reprodução/efeitos dos fármacos
Peixe-Zebra/fisiologia
[Mh] Termos MeSH secundário: Animais
Anticoncepcionais Orais Sintéticos/farmacologia
Feminino
Gonadotropinas Hipofisárias/genética
Hormônios Hipotalâmicos/genética
Masculino
Norgestrel/metabolismo
Progestinas/fisiologia
Receptores de Progesterona/genética
Peixe-Zebra/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Contraceptives, Oral, Synthetic); 0 (Gonadotropins, Pituitary); 0 (Hypothalamic Hormones); 0 (Progestins); 0 (Receptors, Progesterone); 3J8Q1747Z2 (Norgestrel)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171004
[St] Status:MEDLINE


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[PMID]:28732067
[Au] Autor:Hasegawa S; Matsui T; Hane Y; Abe J; Hatahira H; Motooka Y; Sasaoka S; Fukuda A; Naganuma M; Hirade K; Takahashi Y; Kinosada Y; Nakamura M
[Ad] Endereço:Laboratory of Drug Informatics, Gifu Pharmaceutical University, Gifu, Japan.
[Ti] Título:Thromboembolic adverse event study of combined estrogen-progestin preparations using Japanese Adverse Drug Event Report database.
[So] Source:PLoS One;12(7):e0182045, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Combined estrogen-progestin preparations (CEPs) are associated with thromboembolic (TE) side effects. The aim of this study was to evaluate the incidence of TE using the Japanese Adverse Drug Event Report (JADER) database. Adverse events recorded from April 2004 to November 2014 in the JADER database were obtained from the Pharmaceuticals and Medical Devices Agency (PMDA) website (www.pmda.go.jp). We calculated the reporting odds ratios (RORs) of suspected CEPs, analyzed the time-to-onset profile, and assessed the hazard type using Weibull shape parameter (WSP). Furthermore, we used the applied association rule mining technique to discover undetected relationships such as the possible risk factors. The total number of reported cases in the JADER contained was 338,224. The RORs (95% confidential interval, CI) of drospirenone combined with ethinyl estradiol (EE, Dro-EE), norethisterone with EE (Ne-EE), levonorgestrel with EE (Lev-EE), desogestrel with EE (Des-EE), and norgestrel with EE (Nor-EE) were 56.2 (44.3-71.4), 29.1 (23.5-35.9), 42.9 (32.3-57.0), 44.7 (32.7-61.1), and 38.6 (26.3-56.7), respectively. The medians (25%-75%) of the time-to-onset of Dro-EE, Ne-EE, Lev-EE, Des-EE, and Nor-EE were 150.0 (75.3-314.0), 128.0 (27.0-279.0), 204.0 (44.0-660.0), 142.0 (41.3-344.0), and 16.5 (8.8-32.0) days, respectively. The 95% CIs of the WSP-ß for Ne-EE, Lev-EE, and Nor-EE were lower and excluded 1. Association rule mining indicated that patients with anemia had a potential risk of developing a TE when using CEPs. Our results suggest that it is important to monitor patients administered CEP for TE. Careful observation is recommended, especially for those using Nor-EE, and this information may be useful for efficient therapeutic planning.
[Mh] Termos MeSH primário: Efeitos Colaterais e Reações Adversas Relacionados a Medicamentos/genética
Estrogênios/administração & dosagem
Estrogênios/efeitos adversos
Progestinas/administração & dosagem
Progestinas/efeitos adversos
Tromboembolia/induzido quimicamente
[Mh] Termos MeSH secundário: Adolescente
Adulto
Sistemas de Notificação de Reações Adversas a Medicamentos
Androstenos/administração & dosagem
Androstenos/efeitos adversos
Criança
Anticoncepcionais Orais Combinados/administração & dosagem
Anticoncepcionais Orais Combinados/efeitos adversos
Bases de Dados Factuais
Desogestrel/administração & dosagem
Desogestrel/efeitos adversos
Etinilestradiol/administração & dosagem
Etinilestradiol/efeitos adversos
Feminino
Seres Humanos
Japão
Levanogestrel/administração & dosagem
Levanogestrel/efeitos adversos
Masculino
Meia-Idade
Noretindrona/administração & dosagem
Noretindrona/efeitos adversos
Norgestrel/administração & dosagem
Norgestrel/efeitos adversos
Razão de Chances
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Androstenes); 0 (Contraceptives, Oral, Combined); 0 (Estrogens); 0 (Progestins); 3J8Q1747Z2 (Norgestrel); 423D2T571U (Ethinyl Estradiol); 5W7SIA7YZW (Levonorgestrel); 81K9V7M3A3 (Desogestrel); N295J34A25 (drospirenone); T18F433X4S (Norethindrone)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170722
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0182045


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[PMID]:28219785
[Au] Autor:Liang YQ; Huang GY; Zhao JL; Shi WJ; Hu LX; Tian F; Liu SS; Jiang YX; Ying GG
[Ad] Endereço:State Key Laboratory of Organic Geochemistry, CAS Research Centre of PRD Environmental Pollution and Control, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences, Guangzhou 510640, PR China; College of Chemistry and Environment, Guangdong Ocean University, Zhanjiang 524088, PR China.
[Ti] Título:Transcriptional alterations induced by binary mixtures of ethinylestradiol and norgestrel during the early development of zebrafish (Danio rerio).
[So] Source:Comp Biochem Physiol C Toxicol Pharmacol;195:60-67, 2017 May.
[Is] ISSN:1532-0456
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Synthetic estrogens and progestins are commonly used in human and veterinary medicine. After use, they reach aquatic environments via discharge of wastewaters from human and animals, thus posing potential risks to organisms. So far, very little is known about their combined effects in aquatic organisms. The aim of this study was to investigate the effects of binary mixtures of ethinylestradiol (EE2) and norgestrel (NGT) on embryonic zebrafish (Danio rerio) by measuring transcriptional alterations. Zebrafish embryos were exposed to EE2 and NGT alone or in combination at concentrations between 36 and 5513ngL for 96h post-fertilization (hpf). The results showed that most of gene transcriptions of hypothalamic-pituitary-gonadal axis (e.g., Pgr, Mprα, Esr1, Esr2a, Vtg1, Ar, Cyp11b, Star, Gnrh3 and Fshb) and circadian rhythm signaling (e.g., Cry1a, Cry2a, Cry2b, Per3, Arntl1b, Arntl2, Clock1a, Cry3 and Cry4) displayed most pronounced alterations in the mixtures as compared to single EE2 and NGT exposures. This finding suggests exposure to the binary mixtures of EE2 and NGT produced significantly enhanced effects in fish as compared to single chemical exposures, and their coexistence could have significant environmental implications.
[Mh] Termos MeSH primário: Etinilestradiol/farmacologia
Perfilação da Expressão Gênica/métodos
Regulação da Expressão Gênica no Desenvolvimento/efeitos dos fármacos
Norgestrel/farmacologia
Peixe-Zebra/genética
[Mh] Termos MeSH secundário: Análise de Variância
Animais
Relação Dose-Resposta a Droga
Sinergismo Farmacológico
Estrogênios/farmacologia
Feminino
Masculino
Reação em Cadeia da Polimerase Via Transcriptase Reversa
Fatores de Tempo
Peixe-Zebra/embriologia
Proteínas de Peixe-Zebra/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Estrogens); 0 (Zebrafish Proteins); 3J8Q1747Z2 (Norgestrel); 423D2T571U (Ethinyl Estradiol)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170330
[Lr] Data última revisão:
170330
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170222
[St] Status:MEDLINE


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[PMID]:27475035
[Au] Autor:Edelman AB; Cherala G; Li H; Pau F; Blithe DL; Jensen JT
[Ad] Endereço:Department of Obstetrics & Gynecology, Oregon Health & Science University, Portland, OR; Oregon National Primate Research Center, Beaverton, OR. Electronic address: edelmana@ohsu.edu.
[Ti] Título:Levonorgestrel butanoate intramuscular injection does not reliably suppress ovulation for 90 days in obese and normal-BMI women: a pilot study.
[So] Source:Contraception;95(1):55-58, 2017 Jan.
[Is] ISSN:1879-0518
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: We performed a pilot evaluation of a new formulation of levonorgestrel butanoate (LB) designed to be a long-acting injectable (6 months) contraceptive to determine pharmacodynamic end points in normal-body mass index (BMI) and obese women. STUDY DESIGN: Obese (BMI ≥30 kg/m ) and normal-BMI, otherwise healthy, women received a single intramuscular injection of LB after ovulation was confirmed in a baseline cycle. The primary outcome was return of ovulation in days. RESULTS: A total of 14 women enrolled and completed the study [normal BMI n=9, median BMI 22.7kg/m (range 19.4-25.8); obese n=5, median BMI 35.7kg/m (30.1-39.2)]. The first 6 subjects (normal BMI=4/9, obese BMI=2/5) received 40 mg of LB, and the remaining 8 received 20 mg. All women except one returned to ovulation prior to 6 months. Return to ovulation occurred earlier in the obese group; 3/5 obese and 0/9 normal BMI subjects returned to ovulation within 90 days (p=.03). No serious adverse events were reported during the study. CONCLUSION: Return to ovulation was earlier than 6 months in both BMI groups but more so in the obese BMI group. IMPLICATIONS: Since return of ovulation was earlier than expected for this LB injectable formulation, additional steps are needed to develop a preparation suitable as a longer-lasting product.
[Mh] Termos MeSH primário: Anticoncepcionais Femininos/farmacocinética
Norgestrel/análogos & derivados
Obesidade/sangue
Ovulação/efeitos dos fármacos
[Mh] Termos MeSH secundário: Adulto
Índice de Massa Corporal
Peso Corporal/efeitos dos fármacos
Anticoncepcionais Femininos/administração & dosagem
Feminino
Seres Humanos
Injeções Intramusculares
Estimativa de Kaplan-Meier
Norgestrel/administração & dosagem
Norgestrel/farmacocinética
Oregon
Projetos Piloto
Estudos Prospectivos
Fatores de Tempo
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Contraceptive Agents, Female); 0 (levonorgestrel butanoate); 3J8Q1747Z2 (Norgestrel)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160801
[St] Status:MEDLINE


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[PMID]:27814376
[Au] Autor:Roche SL; Wyse-Jackson AC; Gómez-Vicente V; Lax P; Ruiz-Lopez AM; Byrne AM; Cuenca N; Cotter TG
[Ad] Endereço:Cell Development and Disease Laboratory, Biochemistry Department, Biosciences Institute, University College Cork, Cork, Ireland.
[Ti] Título:Progesterone Attenuates Microglial-Driven Retinal Degeneration and Stimulates Protective Fractalkine-CX3CR1 Signaling.
[So] Source:PLoS One;11(11):e0165197, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Retinitis pigmentosa (RP) is a degenerative disease leading to photoreceptor cell loss. Mouse models of RP, such as the rd10 mouse (B6.CXBl-Pde6brd10/J), have enhanced our understanding of the disease, allowing for development of potential therapeutics. In 2011, our group first demonstrated that the synthetic progesterone analogue 'Norgestrel' is neuroprotective in two mouse models of retinal degeneration, including the rd10 mouse. We have since elucidated several mechanisms by which Norgestrel protects stressed photoreceptors, such as upregulating growth factors. This study consequently aimed to further characterize Norgestrel's neuroprotective effects. Specifically, we sought to investigate the role that microglia might play; for microglial-derived inflammation has been shown to potentiate neurodegeneration. Dams of post-natal day (P) 10 rd10 pups were given a Norgestrel-supplemented diet (80mg/kg). Upon weaning, pups remained on Norgestrel. Tissue was harvested from P15-P50 rd10 mice on control or Norgestrel-supplemented diet. Norgestrel-diet administration provided significant retinal protection out to P40 in rd10 mice. Alterations in microglial activity coincided with significant protection, implicating microglial changes in Norgestrel-induced neuroprotection. Utilizing primary cultures of retinal microglia and 661W photoreceptor-like cells, we show that rd10 microglia drive neuronal cell death. We reveal a novel role of Norgestrel, acting directly on microglia to reduce pro-inflammatory activation and prevent neuronal cell death. Norgestrel effectively suppresses cytokine, chemokine and danger-associated molecular pattern molecule (DAMP) expression in the rd10 retina. Remarkably, Norgestrel upregulates fractalkine-CX3CR1 signaling 1 000-fold at the RNA level, in the rd10 mouse. Fractalkine-CX3CR1 signaling has been shown to protect neurons by regulating retinal microglial activation and migration. Ultimately, these results present Norgestrel as a promising treatment for RP, with dual actions as a neuroprotective and anti-inflammatory agent in the retina.
[Mh] Termos MeSH primário: Quimiocina CX3CL1/metabolismo
Microglia/metabolismo
Fármacos Neuroprotetores/metabolismo
Progesterona/metabolismo
Receptores de Quimiocinas/metabolismo
Degeneração Retiniana/metabolismo
Transdução de Sinais/fisiologia
[Mh] Termos MeSH secundário: Animais
Receptor 1 de Quimiocina CX3C
Linhagem Celular
Estimulantes do Sistema Nervoso Central/metabolismo
Modelos Animais de Doenças
Feminino
Masculino
Camundongos
Camundongos Endogâmicos C57BL
Norgestrel/metabolismo
Células Fotorreceptoras de Vertebrados/metabolismo
Retina/metabolismo
Retinite Pigmentosa/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (CX3C Chemokine Receptor 1); 0 (Central Nervous System Stimulants); 0 (Chemokine CX3CL1); 0 (Cx3cl1 protein, mouse); 0 (Cx3cr1 protein, mouse); 0 (Neuroprotective Agents); 0 (Receptors, Chemokine); 3J8Q1747Z2 (Norgestrel); 4G7DS2Q64Y (Progesterone)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161105
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0165197


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[PMID]:27763693
[Au] Autor:Wyse-Jackson AC; Roche SL; Ruiz-Lopez AM; Moloney JN; Byrne AM; Cotter TG
[Ad] Endereço:Cell Development and Disease Laboratory, Biochemistry Department, Bioscience Research Institute, University College Cork, Western Road, Cork, Ireland.
[Ti] Título:Progesterone analogue protects stressed photoreceptors via bFGF-mediated calcium influx.
[So] Source:Eur J Neurosci;44(12):3067-3079, 2016 Dec.
[Is] ISSN:1460-9568
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Retinitis pigmentosa (RP) is a degenerative retinal disease leading to photoreceptor cell loss. In 2011, our group identified the synthetic progesterone 'Norgestrel' as a potential treatment for RP. Subsequent research showed Norgestrel to work through progesterone receptor membrane component 1 (PGRMC1) activation and upregulation of neuroprotective basic fibroblast growth factor (bFGF). Using trophic factor deprivation of 661W photoreceptor-like cells, we aimed to further elucidate the mechanism leading to Norgestrel-induced neuroprotection. In the present manuscript, we show by flow cytometry and live-cell immunofluorescence that Norgestrel induces an increase in cytosolic calcium in both healthy and stressed 661Ws over 24 h. Specific PGRMC1 inhibition by AG205 (1 µm) showed this rise to be PGRMC1-dependent, primarily utilizing calcium from extracellular sources, for blockade of L-type calcium channels by verapamil (50 µm) prevented a Norgestrel-induced calcium influx in stressed cells. Calcium influx was also shown to be bFGF-dependent, for siRNA knock down of bFGF prevented Norgestrel-PGRMC1 induced changes in cytosolic calcium. Notably, we demonstrate PGRMC1-activation is necessary for Norgestrel-induced bFGF upregulation. We propose that Norgestrel protects through the following pathway: binding to and activating PGRMC1 expressed on the surface of photoreceptor cells, PGRMC1 activation drives bFGF upregulation and subsequent calcium influx. Importantly, raised intracellular calcium is critical to Norgestrel's protective efficacy, for extracellular calcium chelation by EGTA abrogates the protective effects of Norgestrel on stressed 661W cells in vitro.
[Mh] Termos MeSH primário: Sinalização do Cálcio/efeitos dos fármacos
Fator 2 de Crescimento de Fibroblastos/metabolismo
Norgestrel/administração & dosagem
Células Fotorreceptoras/efeitos dos fármacos
Células Fotorreceptoras/metabolismo
Progesterona/análogos & derivados
Estresse Fisiológico/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Linhagem Celular
Proteínas de Membrana/metabolismo
Camundongos
Progesterona/administração & dosagem
Receptores de Progesterona/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Membrane Proteins); 0 (PGRMC1 protein, mouse); 0 (Receptors, Progesterone); 103107-01-3 (Fibroblast Growth Factor 2); 3J8Q1747Z2 (Norgestrel); 4G7DS2Q64Y (Progesterone)
[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:161021
[St] Status:MEDLINE
[do] DOI:10.1111/ejn.13445


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[PMID]:27174800
[Au] Autor:Tamura K; Naraba H; Hara T; Nakamura K; Yoshie M; Kogo H; Tachikawa E
[Ad] Endereço:Department of Endocrine and Neural Pharmacology, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan. Electronic address: hiro@toyaku.ac.jp.
[Ti] Título:A positive feedback loop between progesterone and microsomal prostaglandin E synthase-1-mediated PGE2 promotes production of both in mouse granulosa cells.
[So] Source:Prostaglandins Other Lipid Mediat;123:56-62, 2016 03.
[Is] ISSN:1098-8823
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Microsomal prostaglandin E synthase-1 (mPGES-1) is primarily expressed in granulosa cells (GCs) in the preovulatory follicle. Both prostaglandin E2 (PGE2) and progesterone (P4) are implicated in various reproductive functions. Here, we demonstrate that mPges-1 may be a direct downstream target gene of the P4 receptor and P4-stimulated PGE2 secretion can stimulate P4 production in a newly generated mouse GC line (GtsT). Treatment of GtsT cells with a P4 receptor agonist, norgestrel, markedly increased mPGES-1 expression detected by RT-PCR analysis. PGE2 secretion measured by an enzyme-linked immunosorbent assay was enhanced by P4 treatment. Luciferase assays revealed that the proximal promoter region of the mPges-1 gene was responsible for the effects of P4 treatment. Conversely, PGE2 treatment stimulated P4 secretion, which coordinated with mRNA expression of steroidogenic acute regulatory protein. Taken together, P4 may regulate mPGES-1 expression to increase PGE2 secretion and in turn P4 production. An autocrine loop between P4 and PGE2 might function to maintain the increased levels of both in GCs.
[Mh] Termos MeSH primário: Dinoprostona/secreção
Retroalimentação Fisiológica
Células da Granulosa/metabolismo
Progesterona/metabolismo
Prostaglandina-E Sintases/genética
Receptores de Progesterona/genética
[Mh] Termos MeSH secundário: Animais
Comunicação Autócrina
Dinoprostona/farmacologia
Feminino
Regulação da Expressão Gênica
Genes Reporter
Células da Granulosa/citologia
Células da Granulosa/efeitos dos fármacos
Luciferases/genética
Luciferases/metabolismo
Camundongos
Microssomos/metabolismo
Norgestrel/farmacologia
Cultura Primária de Células
Progesterona/farmacologia
Regiões Promotoras Genéticas
Prostaglandina-E Sintases/metabolismo
Receptores de Progesterona/agonistas
Receptores de Progesterona/metabolismo
Transdução de Sinais
Acetato de Tetradecanoilforbol/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Receptors, Progesterone); 3J8Q1747Z2 (Norgestrel); 4G7DS2Q64Y (Progesterone); EC 1.13.12.- (Luciferases); EC 5.3.99.3 (Prostaglandin-E Synthases); EC 5.3.99.3 (Ptges protein, mouse); K7Q1JQR04M (Dinoprostone); NI40JAQ945 (Tetradecanoylphorbol Acetate)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170418
[Lr] Data última revisão:
170418
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160514
[St] Status:MEDLINE


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[PMID]:27081297
[Au] Autor:Byrne AM; Roche SL; Ruiz-Lopez AM; Jackson AC; Cotter TG
[Ad] Endereço:Cell Development and Disease Laboratory, Biochemistry Department, Biosciences Institute, University College Cork, Cork, Ireland.
[Ti] Título:The synthetic progestin norgestrel acts to increase LIF levels in the rd10 mouse model of retinitis pigmentosa.
[So] Source:Mol Vis;22:264-74, 2016.
[Is] ISSN:1090-0535
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Retinal degenerative conditions affect thousands of people worldwide. Retinitis pigmentosa (RP) is among the most common, but it is currently incurable. It is characterized by the progressive death of photoreceptor cells, eventually leading to blindness. Neurotrophic factors play an important role in such retinopathies, and much research has been performed on their use as treatments. Our group previously demonstrated the ability of the synthetic progestin norgestrel to rescue photoreceptors from cell death, the mechanism of which is believed to include upregulation of the neurotrophic factor basic fibroblast growth factor (bFGF). The objective of the present study was to investigate whether the protection provided by norgestrel is likely to be mediated by other neurotrophins. METHODS: The 661W photoreceptor cells and retinal explants from P30 to P40 wild-type (wt) C57BL/6 mice were treated with norgestrel over time. Homozygous rd10/rd10 mice that mimic the human form of RP were fed either a control or a norgestrel-containing diet. Changes in neurotrophic factor expression in response to norgestrel were detected with real-time PCR, western blotting, or immunofluorescence staining. Using specific siRNA, leukemia inhibitory factor (Lif) expression was knocked down in 661W photoreceptor cells that were stressed by serum starvation. Cells were treated with norgestrel followed by measurement of cell viability with (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) (MTS) assay. RESULTS: LIF, a potent neuroprotective cytokine, was found to be upregulated in response to norgestrel in vitro and in vivo. Upregulation of LIF in degenerating rd10 retinas coincided with preservation of the photoreceptor layer. We also found LIF was necessary for the norgestrel-mediated rescue of stressed photoreceptor cells from cell death in vitro. CONCLUSIONS: LIF was upregulated in response to norgestrel in all models studied and is necessary for the protective effects of norgestrel in vitro. The increase in LIF expression in rd10 mice undergoing retinal degeneration was concurrent with rescue of the photoreceptor cell layer. These results highlight the ability of norgestrel to induce prosurvival molecules in the compromised retina, underlining norgestrel's potential as a viable drug for treatment of RP.
[Mh] Termos MeSH primário: Anticoncepcionais Orais Sintéticos/farmacologia
Modelos Animais de Doenças
Regulação da Expressão Gênica/fisiologia
Fator Inibidor de Leucemia/genética
Norgestrel/farmacologia
Retinite Pigmentosa/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Western Blotting
Sobrevivência Celular
Células Cultivadas
Anticoncepcionais Orais Sintéticos/síntese química
Dieta
Técnica Indireta de Fluorescência para Anticorpo
Fator Inibidor de Leucemia/metabolismo
Camundongos
Camundongos Endogâmicos C57BL
Norgestrel/síntese química
Células Fotorreceptoras de Vertebrados/efeitos dos fármacos
Células Fotorreceptoras de Vertebrados/metabolismo
Células Fotorreceptoras de Vertebrados/patologia
RNA Mensageiro/genética
RNA Interferente Pequeno/genética
Reação em Cadeia da Polimerase em Tempo Real
Retinite Pigmentosa/genética
Retinite Pigmentosa/metabolismo
Transfecção
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Contraceptives, Oral, Synthetic); 0 (Leukemia Inhibitory Factor); 0 (Lif protein, mouse); 0 (RNA, Messenger); 0 (RNA, Small Interfering); 3J8Q1747Z2 (Norgestrel)
[Em] Mês de entrada:1611
[Cu] Atualização por classe:161230
[Lr] Data última revisão:
161230
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160416
[St] Status:MEDLINE


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[PMID]:27018506
[Au] Autor:Abdallah IA; Hammell DC; Hassan HE; Stinchcomb AL
[Ad] Endereço:Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD, United States; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Misr International University, Cairo, Egypt.
[Ti] Título:Norelgestromin/ethinyl estradiol intravenous infusion formulation optimization, stability and compatibility testing: A case study to overcome polysorbate 80 interference in chromatographic analysis.
[So] Source:J Pharm Biomed Anal;125:145-53, 2016 Jun 05.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Norelgestromin/ethinyl estradiol is a progestin/estrogen combination hormonal contraceptive indicated for the prevention of pregnancy in women. The very poor solubility and wettability of these drugs, along with their high potency (adsorption issues), give rise to difficulties in designing intravenous (IV) formulations to assess absolute bioavailability of products containing both drugs. The purpose of this study was to develop an IV formulation, evaluate its stability under different conditions and evaluate its compatibility with IV sets for potential use in absolute bioavailability studies in humans. Also, a selective high-performance liquid chromatography (HPLC) method for quantification of ethinyl estradiol and norelgestromin in polysorbate 80 matrix was developed and validated. Norelgestromin/ethinyl estradiol IV solution was prepared using sterile water for injection with 2.5% ethanol and 2.5% polysorbate 80 as a cosolvent/surfactant system to obtain a final drug solution of 25µg ethinyl estradiol and 252µg norelgestromin from a concentrated stock drug solution. The stabilities of the concentrated stock and IV solutions were assessed after storing them in the refrigerator (3.7±0.6°C) and at room temperature (19.5±0.5°C), respectively. Additional studies were conducted to examine the stability of the IV solution using an Alarias(®) low sorbing IV administration set with and without an inline filter. The solution was allowed to drip at 1mL/min over a 60min period. Samples were obtained at the beginning, middle and end of the 60min duration. The chemical stability was evaluated for up to 10 days. Norelgestromin and ethinyl estradiol concentration, purity, and degradant levels were determined using the HPLC method. The norelgestromin/ethinyl estradiol IV formulation met the chemical stability criteria when tested on day 1 through day 9 (216h). Norelgestromin concentrations assayed in stock and IV solutions were in the range of 90.0-98.5% and 90.9-98.8% after 9 days, respectively. As for ethinyl estradiol, the assayed concentrations were in the range of 91.8-100.9% and 92.7-100.8% for the stock and IV solutions, respectively. The administration set was found to be compatible with both drugs; the assayed concentrations were in the range of 99.2-100.3% for norelgestromin and 96.3-102.7% for ethinyl estradiol, but the inline filter showed some adsorption of ethinyl estradiol; where the assayed concentrations were in the range of 98.1-99.8% for norelgestromin and 95.9-97.4% for ethinyl estradiol. The present study provided evidence supporting the suitability of an intravenous formulation for norelgestromin/ethinyl estradiol using ethanol/polysorbate 80 as a cosolvent/surfactant system. Both IV and concentrated stock solutions when stored at room temperature and refrigeration, respectively, were found to be chemically stable up to 9 days. These results indicated that this formulation is chemically stable and can be used over the time period tested. This IV formulation can be used to evaluate the absolute bioavailability of products containing norelgestromin and ethinyl estradiol provided that microbial testing of the IV formulation is performed.
[Mh] Termos MeSH primário: Cromatografia Líquida de Alta Pressão/métodos
Etinilestradiol/química
Norgestrel/análogos & derivados
[Mh] Termos MeSH secundário: Infusões Intravenosas
Limite de Detecção
Norgestrel/química
Oximas/química
Reprodutibilidade dos Testes
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Oximes); 3J8Q1747Z2 (Norgestrel); 423D2T571U (Ethinyl Estradiol); R0TAY3X631 (norelgestromin)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160329
[St] Status:MEDLINE


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[PMID]:26992536
[Au] Autor:Hordge LN; McDaniel KL; Jones DD; Fakayode SO
[Ad] Endereço:Department of Chemistry, North Carolina A&T State University, Greensboro, NC 27411, USA.
[Ti] Título:Simultaneous determination of estrogens (ethinylestradiol and norgestimate) concentrations in human and bovine serum albumin by use of fluorescence spectroscopy and multivariate regression analysis.
[So] Source:Talanta;152:401-9, 2016 May 15.
[Is] ISSN:1873-3573
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The endocrine disruption property of estrogens necessitates the immediate need for effective monitoring and development of analytical protocols for their analyses in biological and human specimens. This study explores the first combined utility of a steady-state fluorescence spectroscopy and multivariate partial-least-square (PLS) regression analysis for the simultaneous determination of two estrogens (17α-ethinylestradiol (EE) and norgestimate (NOR)) concentrations in bovine serum albumin (BSA) and human serum albumin (HSA) samples. The influence of EE and NOR concentrations and temperature on the emission spectra of EE-HSA EE-BSA, NOR-HSA, and NOR-BSA complexes was also investigated. The binding of EE with HSA and BSA resulted in increase in emission characteristics of HSA and BSA and a significant blue spectra shift. In contrast, the interaction of NOR with HSA and BSA quenched the emission characteristics of HSA and BSA. The observed emission spectral shifts preclude the effective use of traditional univariate regression analysis of fluorescent data for the determination of EE and NOR concentrations in HSA and BSA samples. Multivariate partial-least-squares (PLS) regression analysis was utilized to correlate the changes in emission spectra with EE and NOR concentrations in HSA and BSA samples. The figures-of-merit of the developed PLS regression models were excellent, with limits of detection as low as 1.6×10(-8) M for EE and 2.4×10(-7) M for NOR and good linearity (R(2)>0.994985). The PLS models correctly predicted EE and NOR concentrations in independent validation HSA and BSA samples with a root-mean-square-percent-relative-error (RMS%RE) of less than 6.0% at physiological condition. On the contrary, the use of univariate regression resulted in poor predictions of EE and NOR in HSA and BSA samples, with RMS%RE larger than 40% at physiological conditions. High accuracy, low sensitivity, simplicity, low-cost with no prior analyte extraction or separation required makes this method promising, compelling, and attractive alternative for the rapid determination of estrogen concentrations in biomedical and biological specimens, pharmaceuticals, or environmental samples.
[Mh] Termos MeSH primário: Estrogênios/análise
Etinilestradiol/análise
Norgestrel/análogos & derivados
Soroalbumina Bovina/química
Espectrometria de Fluorescência/métodos
[Mh] Termos MeSH secundário: Animais
Bovinos
Estrogênios/química
Etinilestradiol/química
Seres Humanos
Análise dos Mínimos Quadrados
Análise Multivariada
Norgestrel/análise
Norgestrel/química
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Estrogens); 27432CM55Q (Serum Albumin, Bovine); 3J8Q1747Z2 (Norgestrel); 423D2T571U (Ethinyl Estradiol); C291HFX4DY (norgestimate)
[Em] Mês de entrada:1612
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160320
[St] Status:MEDLINE



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