Base de dados : MEDLINE
Pesquisa : D04.210.500.155.580.064.580 [Categoria DeCS]
Referências encontradas : 85 [refinar]
Mostrando: 1 .. 10   no formato [Detalhado]

página 1 de 9 ir para página                      

  1 / 85 MEDLINE  
              next record last record
seleciona
para imprimir
Fotocópia
PubMed Central Texto completo
Texto completo
[PMID]:26592202
[Au] Autor:Okuyama-Dobashi K; Kasai H; Tanaka T; Yamashita A; Yasumoto J; Chen W; Okamoto T; Maekawa S; Watashi K; Wakita T; Ryo A; Suzuki T; Matsuura Y; Enomoto N; Moriishi K
[Ad] Endereço:Department of Microbiology, Faculty of Medicine, University of Yamanashi, Japan.
[Ti] Título:Hepatitis B virus efficiently infects non-adherent hepatoma cells via human sodium taurocholate cotransporting polypeptide.
[So] Source:Sci Rep;5:17047, 2015 Nov 23.
[Is] ISSN:2045-2322
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Sodium taurocholate cotransporting polypeptide (NTCP) has been reported as a functional receptor for hepatitis B virus (HBV) infection. However, HBV could not efficiently infect HepG2 cells expressing NTCP (NTCP-HepG2 cells) under adherent monolayer-cell conditions. In this study, NTCP was mainly detected in the basolateral membrane region, but not the apical site, of monolayer NTCP-HepG2 cells. We hypothesized that non-adherent cell conditions of infection would enhance HBV infectivity. Non-adherent NTCP-HepG2 cells were prepared by treatment with trypsin and EDTA, which did not degrade NTCP in the membrane fraction. HBV successfully infected NTCP-HepG2 cells at a viral dose 10 times lower in non-adherent phase than in adherent phase. Efficient infection of non-adherent NTCP-HepG2 cells with blood-borne or cell-culture-derived HBV was observed and was remarkably impaired in the presence of the myristoylated preS1 peptide. HBV could also efficiently infect HepaRG cells under non-adherent cell conditions. We screened several compounds using our culture system and identified proscillaridin A as a potent anti-HBV agent with an IC50 value of 7.2 nM. In conclusion, non-adherent host cell conditions of infection augmented HBV infectivity in an NTCP-dependent manner, thus providing a novel strategy to identify anti-HBV drugs and investigate the mechanism of HBV infection.
[Mh] Termos MeSH primário: Antivirais/farmacologia
Transportadores de Ânions Orgânicos Dependentes de Sódio/genética
Proscilaridina/farmacologia
Receptores Virais/genética
Simportadores/genética
Internalização do Vírus/efeitos dos fármacos
[Mh] Termos MeSH secundário: Bufanolídeos/farmacologia
Adesão Celular
Digitoxina/farmacologia
Digoxina/farmacologia
Expressão Gênica
Células Hep G2
Vírus da Hepatite B/efeitos dos fármacos
Vírus da Hepatite B/fisiologia
Ensaios de Triagem em Larga Escala
Seres Humanos
Transportadores de Ânions Orgânicos Dependentes de Sódio/antagonistas & inibidores
Transportadores de Ânions Orgânicos Dependentes de Sódio/metabolismo
Ftalazinas/farmacologia
Receptores Virais/antagonistas & inibidores
Receptores Virais/metabolismo
Sinvastatina/farmacologia
Estrofantinas/farmacologia
Simportadores/antagonistas & inibidores
Simportadores/metabolismo
Transgenes
Proteínas do Envelope Viral/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Bufanolides); 0 (L protein, hepatitis B virus); 0 (Organic Anion Transporters, Sodium-Dependent); 0 (Phthalazines); 0 (Receptors, Virus); 0 (Strophanthins); 0 (Symporters); 0 (Viral Envelope Proteins); 145420-23-1 (sodium-bile acid cotransporter); 73K4184T59 (Digoxin); AGG2FN16EV (Simvastatin); E90NZP2L9U (Digitoxin); JY264VIR1Y (convallatoxin); KC6BL281EN (Proscillaridin); U549S98QLW (bufalin); ZQI909440X (azelastine)
[Em] Mês de entrada:1609
[Cu] Atualização por classe:151128
[Lr] Data última revisão:
151128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:151124
[St] Status:MEDLINE
[do] DOI:10.1038/srep17047


  2 / 85 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
PubMed Central Texto completo
[PMID]:25400117
[Au] Autor:Denicolaï E; Baeza-Kallee N; Tchoghandjian A; Carré M; Colin C; Jiglaire CJ; Mercurio S; Beclin C; Figarella-Branger D
[Ad] Endereço:Inserm, Aix-Marseille Université, CRO2 UMR_S 911, Marseille, 13385, France.
[Ti] Título:Proscillaridin A is cytotoxic for glioblastoma cell lines and controls tumor xenograft growth in vivo.
[So] Source:Oncotarget;5(21):10934-48, 2014 Nov 15.
[Is] ISSN:1949-2553
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Glioblastoma is the most frequent primary brain tumor in adults. Because of molecular and cellular heterogeneity, high proliferation rate and significant invasive ability, prognosis of patients is poor. Recent therapeutic advances increased median overall survival but tumor recurrence remains inevitable. In this context, we used a high throughput screening approach to bring out novel compounds with anti-proliferative and anti-migratory properties for glioblastoma treatment. Screening of the Prestwick chemical library® of 1120 molecules identified proscillaridin A, a cardiac glycoside inhibitor of the Na(+)/K(+) ATPase pump, with most significant effects on glioblastoma cell lines. In vitro effects of proscillaridin A were evaluated on GBM6 and GBM9 stem-like cell lines and on U87-MG and U251-MG cell lines. We showed that proscillaridin A displayed cytotoxic properties, triggered cell death, induced G2/M phase blockade in all the glioblastoma cell lines and impaired GBM stem self-renewal capacity even at low concentrations. Heterotopic and orthotopic xenotransplantations were used to confirm in vivo anticancer effects of proscillaridin A that both controls xenograft growth and improves mice survival. Altogether, results suggest that proscillaridin A is a promising candidate as cancer therapies in glioblastoma. This sustains previous reports showing that cardiac glycosides act as anticancer drugs in other cancers.
[Mh] Termos MeSH primário: Neoplasias Encefálicas/patologia
Proliferação Celular/efeitos dos fármacos
Inibidores Enzimáticos/farmacologia
Glioblastoma/patologia
Proscilaridina/farmacologia
[Mh] Termos MeSH secundário: Adulto
Animais
Apoptose/efeitos dos fármacos
Western Blotting
Neoplasias Encefálicas/tratamento farmacológico
Neoplasias Encefálicas/mortalidade
Ciclo Celular/efeitos dos fármacos
Movimento Celular/efeitos dos fármacos
Feminino
Perfilação da Expressão Gênica
Glioblastoma/tratamento farmacológico
Glioblastoma/mortalidade
Ensaios de Triagem em Larga Escala
Seres Humanos
Técnicas Imunoenzimáticas
Camundongos
Camundongos Nus
RNA Mensageiro/genética
Reação em Cadeia da Polimerase em Tempo Real
Reação em Cadeia da Polimerase Via Transcriptase Reversa
Taxa de Sobrevida
Células Tumorais Cultivadas
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (RNA, Messenger); KC6BL281EN (Proscillaridin)
[Em] Mês de entrada:1508
[Cu] Atualização por classe:170220
[Lr] Data última revisão:
170220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:141118
[St] Status:MEDLINE


  3 / 85 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:23228916
[Au] Autor:El-Seedi HR; Burman R; Mansour A; Turki Z; Boulos L; Gullbo J; Göransson U
[Ad] Endereço:Division of Pharmacognosy, Department of Medicinal Chemistry, Uppsala University, Biomedical Centre, Box 574, 751 23 Uppsala, Sweden. hesham.el-seedi@fkog.uu.se
[Ti] Título:The traditional medical uses and cytotoxic activities of sixty-one Egyptian plants: discovery of an active cardiac glycoside from Urginea maritima.
[So] Source:J Ethnopharmacol;145(3):746-57, 2013 Feb 13.
[Is] ISSN:1872-7573
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:ETHNOPHARMACOLOGICAL RELEVANCE: Medicinal plants from the Sinai desert are widely used in traditional Bedouin medicine to treat a range of conditions including, cancers, and may thus be useful sources of novel anti-tumor compounds. Information on plants used in this way was obtained through collaboration with Bedouin herbalists. AIM OF THE STUDY: To document the traditional uses of 61 species from 29 families of Egyptian medicinal plants and to investigate their biological activity using a cytotoxicity assay. MATERIAL AND METHODS: MeOH extracts of the 61 plant species investigated were dissolved in 10% DMSO and their cytotoxic activity was evaluated. The extracts were tested in duplicate on three separate occasions at three different concentrations (1, 10 and 100µg/ml) against human lymphoma U-937 GTB. The most active extract was subjected to bioassay-guided fractionation using HPLC and LC/ESI-MS to isolate and identify its active components. RESULTS AND DISCUSSION: The most potent extracts were those from Asclepias sinaica, Urginea maritima, Nerium oleander and Catharanthus roseus, followed by those from Cichorium endivia, Pulicaria undulate and Melia azedarach. Literature reports indicate that several of these plants produce cardiac glycosides. Bioassay-guided fractionation of alcoholic U. maritima extracts led to the isolation of a bioactive bufadienolide that was subsequently shown to be proscillaridin A, as determined by 1D and 2D NMR spectroscopy. This result demonstrates the value of plants used in traditional medicine as sources of medicinally interesting cytotoxic compounds.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Drimia
Extratos Vegetais/farmacologia
Plantas Medicinais
Proscilaridina/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/isolamento & purificação
Sobrevivência Celular/efeitos dos fármacos
Egito
Seres Humanos
Medicina Tradicional
Proscilaridina/isolamento & purificação
Células U937
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Plant Extracts); KC6BL281EN (Proscillaridin)
[Em] Mês de entrada:1307
[Cu] Atualização por classe:161125
[Lr] Data última revisão:
161125
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:121212
[St] Status:MEDLINE


  4 / 85 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
[PMID]:21229879
[Au] Autor:Winnicka K; Bielawska A; Bielawski K
[Ad] Endereço:Department of Pharmaceutical Technology, Medical University of Bialystok, Kilinskiego 1, 15-089 Bialystok, Poland. kwin@umwb.edu.pl
[Ti] Título:Inhibition of DNA topoisomerases I and II by G3 PAMAM-NH2 dendrimer-modified digoxin and proscillaridin A conjugates in a cell free system.
[So] Source:Acta Pol Pharm;67(6):630-4, 2010 Nov-Dec.
[Is] ISSN:0001-6837
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:Two modified glycosides--digoxin and proscillaridin A conjugated to a generation 3 of polyamidoamine dendrimer (G3 PAMAM-NH2) were evaluated as DNA topoisomerase II inhibitors. The ability of these compounds (PAMAM-Dig and PAMAM-Prosc) to inhibit topoisomerase I and II activity was quantified by measuring the action on supercoiled DNA substrate as a function of increasing concentration of the test compounds by the use of agarose gel electrophoresis. The obtained results suggest that a conjugation of the modified glycosides with G3 PAMAM-NH2 significantly improved the ability of the parent compounds to an inhibition of DNA topoisomerases.
[Mh] Termos MeSH primário: DNA Topoisomerases Tipo I
Proteínas de Ligação a DNA/antagonistas & inibidores
Dendrímeros/farmacologia
Digoxina/farmacologia
Proscilaridina/farmacologia
Inibidores da Topoisomerase/farmacologia
[Mh] Termos MeSH secundário: Antígenos de Neoplasias/química
Antígenos de Neoplasias/metabolismo
DNA Topoisomerases Tipo I/química
DNA Topoisomerases Tipo I/metabolismo
DNA Topoisomerases Tipo II/química
DNA Topoisomerases Tipo II/metabolismo
DNA Super-Helicoidal/metabolismo
Proteínas de Ligação a DNA/química
Proteínas de Ligação a DNA/metabolismo
Dendrímeros/química
Digoxina/química
Relação Dose-Resposta a Droga
Eletroforese em Gel de Ágar
Seres Humanos
Estrutura Molecular
Proscilaridina/química
Relação Estrutura-Atividade
Inibidores da Topoisomerase/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antigens, Neoplasm); 0 (DNA, Superhelical); 0 (DNA-Binding Proteins); 0 (Dendrimers); 0 (G3 PAMAM-NH2 dendrimer-modified digoxin); 0 (G3 PAMAM-NH2 dendrimer-modified proscillaridin A); 0 (Topoisomerase Inhibitors); 73K4184T59 (Digoxin); EC 5.99.1.2 (DNA Topoisomerases, Type I); EC 5.99.1.2 (TOP1 protein, human); EC 5.99.1.3 (DNA Topoisomerases, Type II); KC6BL281EN (Proscillaridin)
[Em] Mês de entrada:1102
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:110115
[St] Status:MEDLINE


  5 / 85 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
[PMID]:20508299
[Au] Autor:Winnicka K; Bielawski K; Bielawska A
[Ad] Endereço:Department of Pharmaceutical Technology, Medical University of Bialystok, Kilinskiego 1, PL 15-089 Bialystok, Poland. kwin@umwb.edu.pl
[Ti] Título:Synthesis and cytotoxic activity of G3 PAMAM-NH(2) dendrimer-modified digoxin and proscillaridin A conjugates in breast cancer cells.
[So] Source:Pharmacol Rep;62(2):414-23, 2010 Mar-Apr.
[Is] ISSN:1734-1140
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:The objective of this study was to determine the cytotoxicity, antiproliferative activity, and apoptosis induction activity of two modified glycosides - digoxin and proscillaridin A - conjugated to a generation 3 polyamidoamine dendrimer (G3 PAMAM-NH(2)) in human breast cancer cells. The results suggest that conjugation with the G3 PAMAM-NH(2) dendrimer enhances the cytotoxicity of modified digoxin and proscillaridin Aboth in MCF-7 and in MDA-MB-231 breast cancer cells. Additionally, the conjugate-induced apoptosis was significantly greater than apoptosis evoked by free modified digoxin and proscillaridin A.
[Mh] Termos MeSH primário: Antineoplásicos/síntese química
Neoplasias da Mama/tratamento farmacológico
Dendrímeros/síntese química
Digoxina/análogos & derivados
Proscilaridina/análogos & derivados
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Neoplasias da Mama/patologia
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Dendrímeros/farmacologia
Digoxina/farmacologia
Feminino
Seres Humanos
Proscilaridina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Dendrimers); 0 (PAMAM Starburst); 73K4184T59 (Digoxin); KC6BL281EN (Proscillaridin)
[Em] Mês de entrada:1009
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100529
[St] Status:MEDLINE


  6 / 85 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:20140806
[Au] Autor:Winnicka K; Bielawski K; Bielawska A; Miltyk W
[Ad] Endereço:Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Bialystok, 15-222 Bialystok, Poland. kwin@umwb.edu.pl
[Ti] Título:Dual effects of ouabain, digoxin and proscillaridin A on the regulation of apoptosis in human fibroblasts.
[So] Source:Nat Prod Res;24(3):274-85, 2010 Feb.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:In this study, we looked at the effect of ouabain, digoxin and proscillaridin A on human fibroblasts. These data show that low concentrations of ouabain, digoxin and proscillaridin A can activate proliferation of human fibroblasts, suggesting that the Na+, K+-adenosine triphosphatase complex may act as a transducing receptor. It was shown that 30 nM ouabain, digoxin and proscillaridin A stimulated an antiapoptotic action by the increase in the level of phosphorylated extracellular signal-regulated kinases (P-ERK 1/2). Ouabain, digoxin and proscillaridin A only at the relatively high concentration of 300 nM increased intracellular Ca2+ concentration, activated caspase-3 and induced apoptosis in human fibroblasts. In terms of reduction in cell viability, antiproliferative and apoptotic activity, these cardiac glycosides rank in the order proscillaridin A >digoxin >ouabain.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Digoxina/farmacologia
Fibroblastos/efeitos dos fármacos
Ouabaína/farmacologia
Proscilaridina/farmacologia
[Mh] Termos MeSH secundário: Relação Dose-Resposta a Droga
Ativação Enzimática
Seres Humanos
Quinases de Proteína Quinase Ativadas por Mitógeno/metabolismo
Transdução de Sinais
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
5ACL011P69 (Ouabain); 73K4184T59 (Digoxin); EC 2.7.12.2 (Mitogen-Activated Protein Kinase Kinases); KC6BL281EN (Proscillaridin)
[Em] Mês de entrada:1005
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100209
[St] Status:MEDLINE
[do] DOI:10.1080/14786410902991878


  7 / 85 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
Texto completo
[PMID]:19894733
[Au] Autor:Felth J; Rickardson L; Rosén J; Wickström M; Fryknäs M; Lindskog M; Bohlin L; Gullbo J
[Ad] Endereço:Division of Pharmacognosy, Department of Medicinal Chemistry, Biomedical Center, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden. jenny.felth@fkog.uu.se
[Ti] Título:Cytotoxic effects of cardiac glycosides in colon cancer cells, alone and in combination with standard chemotherapeutic drugs.
[So] Source:J Nat Prod;72(11):1969-74, 2009 Nov.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Cardiac glycosides have been reported to exhibit cytotoxic activity against several different cancer types, but studies against colorectal cancer are lacking. In a screening procedure aimed at identifying natural products with activity against colon cancer, several cardiac glycosides were shown to be of interest, and five of these were further evaluated in different colorectal cancer cell lines and primary cells from patients. Convallatoxin (1), oleandrin (4), and proscillaridin A (5) were identified as the most potent compounds (submicromolar IC50 values), and digitoxin (2) and digoxin (3), which are used in cardiac disease, exhibited somewhat lower activity (IC50 values 0.27-4.1 microM). Selected cardiac glycosides were tested in combination with four clinically relevant cytotoxic drugs (5-fluorouracil, oxaliplatin, cisplatin, irinotecan). The combination of 2 and oxaliplatin exhibited synergism including the otherwise highly drug-resistant HT29 cell line. A ChemGPS-NP application comparing modes of action of anticancer drugs identified cardiac glycosides as a separate cluster. These findings demonstrate that such substances may exhibit significant activity against colorectal cancer cell lines, by mechanisms disparate from currently used anticancer drugs, but at concentrations generally considered not achievable in patient plasma.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
[Mh] Termos MeSH secundário: Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia
Camptotecina/análogos & derivados
Camptotecina/farmacologia
Cardenolídeos/sangue
Cardenolídeos/química
Cardenolídeos/farmacologia
Neoplasias do Colo/tratamento farmacológico
Digitoxina/sangue
Digitoxina/química
Digitoxina/farmacologia
Digoxina/sangue
Digoxina/química
Digoxina/farmacologia
Ensaios de Seleção de Medicamentos Antitumorais
Células HT29
Seres Humanos
NF-kappa B/efeitos dos fármacos
Proscilaridina/sangue
Proscilaridina/química
Proscilaridina/farmacologia
Estrofantinas/sangue
Estrofantinas/química
Estrofantinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Cardenolides); 0 (NF-kappa B); 0 (Strophanthins); 73K4184T59 (Digoxin); 7673326042 (irinotecan); E90NZP2L9U (Digitoxin); II95UDU7I4 (oleandrin); JY264VIR1Y (convallatoxin); KC6BL281EN (Proscillaridin); XT3Z54Z28A (Camptothecin)
[Em] Mês de entrada:0912
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:091110
[St] Status:MEDLINE
[do] DOI:10.1021/np900210m


  8 / 85 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
[PMID]:18520043
[Au] Autor:Winnicka K; Bielawski K; Bielawska A; Surazynski A
[Ad] Endereço:Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Bialystok, Kilinskiego, Bialystok, Poland. kwin@amb.edu.pl
[Ti] Título:Antiproliferative activity of derivatives of ouabain, digoxin and proscillaridin A in human MCF-7 and MDA-MB-231 breast cancer cells.
[So] Source:Biol Pharm Bull;31(6):1131-40, 2008 Jun.
[Is] ISSN:0918-6158
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Three derivatives of ouabain, digoxin and proscillaridin A containing the carboxylic group instead of the lactone moiety were synthesized and examined for cytotoxicity in human breast cancer cells. Evaluation of the cytotoxicity of these compounds employing an MTT assay and inhibition of [3H]thymidine incorporation into DNA in both MCF-7 and MDA-MB-231 breast cancer cells demonstrated that compound 3, the most active of the series, proved to be only slightly less potent than proscillaridin A. We evaluated the effects of these compounds 1-3 on change in intracellular Ca2+, appearance of apoptosis, inhibition of DNA topoisomerase I and II, and the activity of caspase-3 in breast cancer cells. These studies indicate that the increase in potency for 3 may be related, in part, to an activation of caspase-3, increasing free calcium concentration and topoisomerase II inhibition. All these data emphasize the potential usefulness of these derivatives of cardiac glycosides as anticancer agents.
[Mh] Termos MeSH primário: Proliferação Celular/efeitos dos fármacos
Digoxina/farmacologia
Inibidores Enzimáticos/farmacologia
Ouabaína/farmacologia
Proscilaridina/farmacologia
[Mh] Termos MeSH secundário: Western Blotting
Cálcio/metabolismo
Cálcio/farmacologia
Sequência de Carboidratos
Caspase 3/metabolismo
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
DNA de Neoplasias/biossíntese
Eletroforese em Gel de Poliacrilamida
Feminino
Citometria de Fluxo
Seres Humanos
Imunoprecipitação
Indicadores e Reagentes
Microscopia de Fluorescência
Dados de Sequência Molecular
Inibidores da Topoisomerase I
Inibidores da Topoisomerase II
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (DNA, Neoplasm); 0 (Enzyme Inhibitors); 0 (Indicators and Reagents); 0 (Topoisomerase I Inhibitors); 0 (Topoisomerase II Inhibitors); 5ACL011P69 (Ouabain); 73K4184T59 (Digoxin); EC 3.4.22.- (Caspase 3); KC6BL281EN (Proscillaridin); SY7Q814VUP (Calcium)
[Em] Mês de entrada:0806
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080604
[St] Status:MEDLINE


  9 / 85 MEDLINE  
              first record previous record next record last record
seleciona
para imprimir
Fotocópia
[PMID]:18038900
[Au] Autor:Winnicka K; Bielawski K; Bielawska A; Miltyk W
[Ad] Endereço:Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University in Bialystok, Kilinskiego 1, 15-089 Bialystok, Poland. kwin@amb.edu.pl
[Ti] Título:Apoptosis-mediated cytotoxicity of ouabain, digoxin and proscillaridin A in the estrogen independent MDA-MB-231 breast cancer cells.
[So] Source:Arch Pharm Res;30(10):1216-24, 2007 Oct.
[Is] ISSN:0253-6269
[Cp] País de publicação:Korea (South)
[La] Idioma:eng
[Ab] Resumo:We examined the effects of three cardiac glycosides, ouabain, digoxin and proscillaridin A, on the proliferation of estrogen independent MDA-MB-231 breast cancer cells. In terms of reduction in cell viability, the compounds rank for both 24 h and 48 h of incubation in MDA-MB-231 cells in the order proscillaridin A > digoxin > ouabain. Digoxin for 24 h and 48 h of incubation in MDA-MB-231 cells proved to be only slightly more potent than ouabain, with IC50 values of 122 +/- 2 and 70 +/- 2 nM, respectively, compared to 150 +/- 2 and 90 +/- 2 nM for ouabain. In contrast, proscillaridin A, was much more active and showed a high level of cytotoxic potency, IC50 51 +/- 2 and 15 +/- 2 nM for 24 h and 48 h of incubation, respectively. The concentrations of digoxin, ouabain and proscillaridin A needed to inhibit [3H]thymidine incorporation into DNA by 50% (IC50) in MDA-MB-231 cells for 24 h of incubation were found to be 124 +/- 2 nM, 142 +/- 2 nM, and 48 +/- 2 nM, respectively. In the present study, we demonstrated that ouabain, digoxin, and proscillaridin A induce apoptosis in MDA-MB-231 cells by increasing free calcium concentration and by activating caspase-3.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/farmacologia
Apoptose/efeitos dos fármacos
Neoplasias da Mama/patologia
Digoxina/farmacologia
Ouabaína/farmacologia
Proscilaridina/farmacologia
[Mh] Termos MeSH secundário: Neoplasias da Mama/enzimologia
Neoplasias da Mama/metabolismo
Cálcio/metabolismo
Caspase 3/metabolismo
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Ativação Enzimática
Feminino
Seres Humanos
Concentração Inibidora 50
Fatores de Tempo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents, Phytogenic); 5ACL011P69 (Ouabain); 73K4184T59 (Digoxin); EC 3.4.22.- (Caspase 3); KC6BL281EN (Proscillaridin); SY7Q814VUP (Calcium)
[Em] Mês de entrada:0712
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:071128
[St] Status:MEDLINE


  10 / 85 MEDLINE  
              first record previous record
seleciona
para imprimir
Fotocópia
[PMID]:16819197
[Au] Autor:Bielawski K; Winnicka K; Bielawska A
[Ad] Endereço:Department of Medicinal Chemistry and Drug Technology, Medical University of Bialystok, Poland. kbiel@amb.edu.pl
[Ti] Título:Inhibition of DNA topoisomerases I and II, and growth inhibition of breast cancer MCF-7 cells by ouabain, digoxin and proscillaridin A.
[So] Source:Biol Pharm Bull;29(7):1493-7, 2006 Jul.
[Is] ISSN:0918-6158
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:We evaluated the cytotoxicity and underlying mechanisms of cardiac glycosides, including digoxin, ouabain and proscillaridin A, on the proliferation of breast cancer MCF-7 cells. In terms of inhibition of cell proliferation of MCF-7 cells, the compounds rank in the order proscillaridin A>digoxin>ouabain. While both digoxin and ouabain inhibited topoisomerase II catalytic activity at nanomolar concentrations (100 nM), neither agent inhibited topoisomerase I catalytic activity even at concentrations as high as 100 microM. On the other hand, proscillaridin A was a potent poison of topoisomerase I and II activity at nanomolar drug concentrations (30 nM, 100 nM, respectively), suggesting that this agent may produce its cytotoxic activity by targeting both enzymes simultaneously. These studies suggest that the stabilization of DNA-topoisomerase II complexes is closely linked to the mechanism of digoxin, ouabain and proscillaridin A cytotoxicity. The potential DNA-binding properties of the cardiac glycosides have been assessed by measuring the displacement of ethidium bromide from calf thymus DNA. These results indicate that digoxin, ouabain and proscillaridin A neither intercalate nor interact with the minor groove of DNA.
[Mh] Termos MeSH primário: Sobrevivência Celular/efeitos dos fármacos
Digoxina/farmacologia
Inibidores Enzimáticos/farmacologia
Ouabaína/farmacologia
Proscilaridina/farmacologia
Inibidores da Topoisomerase I
Inibidores da Topoisomerase II
[Mh] Termos MeSH secundário: Neoplasias da Mama
Linhagem Celular Tumoral
Digoxina/química
Relação Dose-Resposta a Droga
Feminino
Seres Humanos
Cinética
Modelos Moleculares
Ouabaína/química
Proscilaridina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Enzyme Inhibitors); 0 (Topoisomerase I Inhibitors); 0 (Topoisomerase II Inhibitors); 5ACL011P69 (Ouabain); 73K4184T59 (Digoxin); KC6BL281EN (Proscillaridin)
[Em] Mês de entrada:0609
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:060705
[St] Status:MEDLINE



página 1 de 9 ir para página                      
   


Refinar a pesquisa
  Base de dados : MEDLINE Formulário avançado   

    Pesquisar no campo  
1  
2
3
 
           



Search engine: iAH v2.6 powered by WWWISIS

BIREME/OPAS/OMS - Centro Latino-Americano e do Caribe de Informação em Ciências da Saúde