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[PMID]:28388523
[Au] Autor:Wang R; Zhang X; Chen C; Chen G; Sarabia C; Zhang Q; Zheng S; Wang G; Chen QH
[Ad] Endereço:Department of Chemistry, California State University, Fresno, 2555 E. San Ramon Avenue, M/S SB70, Fresno, CA 93740, USA.
[Ti] Título:Structure-activity relationship studies of 1,7-diheteroarylhepta-1,4,6-trien-3-ones with two different terminal rings in prostate epithelial cell models.
[So] Source:Eur J Med Chem;133:208-226, 2017 Jun 16.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:To systematically investigate the structure-activity relationships of 1,7-diheteroarylhepta-1,4,6-trien-3-ones in three human prostate cancer cell models and one human prostate non-neoplastic epithelial cell model, thirty five 1,7-diarylhepta-1,4,6-trien-3-ones with different terminal heteroaromatic rings have been designed for evaluation of their anti-proliferative potency in vitro. These target compounds have been successfully synthesized through two sequential Horner-Wadsworth-Emmons reactions starting from the appropriate aldehydes and tetraethyl (2-oxopropane-1,3-diyl)bis(phosphonate). Their anti-proliferative potency against PC-3, DU-145 and LNCaP human prostate cancer cell lines can be significantly enhanced by the manipulation of the terminal heteroaromatic rings, further demonstrating the utility of 1,7-diarylhepta-1,4,6-trien-3-one as a potential scaffold for the development of anti-prostate cancer agents. The optimal analog 40 is 82-, 67-, and 39-fold more potent than curcumin toward the three prostate cancer cell lines, respectively. The experimental data also reveal that the trienones with two different terminal aromatic rings possess greater potency toward three prostate cancer cell lines, but also have greater capability of suppressing the proliferation of PWR-1E benign human prostate epithelial cells, as compared to the corresponding counterparts with two identical terminal rings and curcumin. The terminal aromatic rings also affect the cell apoptosis perturbation.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Hidrocarbonetos Aromáticos/química
Hidrocarbonetos Aromáticos/farmacologia
Neoplasias da Próstata/tratamento farmacológico
Trientina/química
Trientina/farmacologia
[Mh] Termos MeSH secundário: Apoptose/efeitos dos fármacos
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Masculino
Próstata/efeitos dos fármacos
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Hydrocarbons, Aromatic); SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170913
[Lr] Data última revisão:
170913
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170408
[St] Status:MEDLINE


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[PMID]:28280522
[Au] Autor:Wang L; Luo X; Li C; Huang Y; Xu P; Lloyd-Davies LH; Delplancke T; Peng C; Gao R; Qi H; Tong C; Baker P
[Ad] Endereço:Department of Reproduction Health and Infertility, The First Affiliated Hospital of Chongqing Medical University, Chongqing 400016, China; Department of Obstetrics and Gynecology, The First Affiliated Hospital of Chongqing Medical University, Chongqing 400016, China; Canada-China-New Zealand Joint L
[Ti] Título:Triethylenetetramine Synergizes with Pharmacologic Ascorbic Acid in Hydrogen Peroxide Mediated Selective Toxicity to Breast Cancer Cell.
[So] Source:Oxid Med Cell Longev;2017:3481710, 2017.
[Is] ISSN:1942-0994
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Breast cancer is characterized by overexpression of superoxide dismutase (SOD) and downregulation of catalase and more resistance to hydrogen peroxide (H O ) than normal cells. Thus, relatively high H O promotes breast cancer cell growth and proliferation. However, excessive intracellular H O leads to death of breast cancer cells. In cancer cells, high level ascorbic acid (Asc) is able to be autoxidized and thus provides an electron to oxygen to generate H O . In the present study, we demonstrated that triethylenetetramine (TETA) enhances Asc autoxidation and thus elevates H O production in MCF-7 cells. Furthermore, Asc/TETA combination significantly impaired cancer cell viability, while having much milder effects on normal cells, indicating Asc/TETA could be a promising therapy for breast cancer. Moreover, SOD1 and N-acetyl-L-cysteine failed to improve MCF-7 cells viability in the presence of Asc/TETA, while catalase significantly inhibited the cytotoxicity of Asc/TETA to breast cancer cells, strongly suggesting that the selective cytotoxicity of Asc/TETA to cancer cells is H O -dependent. In addition, Asc/TETA induces RAS/ERK downregulation in breast cancer cells. Animal studies confirmed that Asc/TETA effectively suppressed tumor growth in vivo. In conclusion, TETA synergizes pharmacologic Asc autoxidation and H O overproduction in breast cancer cells, which suppresses RAS/ERK pathway and results in apoptosis.
[Mh] Termos MeSH primário: Apoptose/efeitos dos fármacos
Ácido Ascórbico/farmacologia
Neoplasias da Mama/patologia
Peróxido de Hidrogênio/toxicidade
Trientina/farmacologia
[Mh] Termos MeSH secundário: Animais
Neoplasias da Mama/enzimologia
Carcinogênese/efeitos dos fármacos
Carcinogênese/patologia
Modelos Animais de Doenças
Sinergismo Farmacológico
MAP Quinases Reguladas por Sinal Extracelular/metabolismo
Feminino
Seres Humanos
Células MCF-7
Camundongos
Oxirredução
Transdução de Sinais/efeitos dos fármacos
Superóxido Dismutase/metabolismo
Superóxidos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
11062-77-4 (Superoxides); BBX060AN9V (Hydrogen Peroxide); EC 1.15.1.1 (Superoxide Dismutase); EC 2.7.11.24 (Extracellular Signal-Regulated MAP Kinases); PQ6CK8PD0R (Ascorbic Acid); SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170320
[Lr] Data última revisão:
170320
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170311
[St] Status:MEDLINE
[do] DOI:10.1155/2017/3481710


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[PMID]:27613237
[Au] Autor:Yin JM; Sun LB; Zheng JS; Wang XX; Chen DX; Li N
[Ad] Endereço:Beijing Youan Hospital, Capital Medical University, No. 8, Xitoutiao, Youanmenwai, Fengtai District, Beijing, China.
[Ti] Título:Copper chelation by trientine dihydrochloride inhibits liver RFA-induced inflammatory responses in vivo.
[So] Source:Inflamm Res;65(12):1009-1020, 2016 Dec.
[Is] ISSN:1420-908X
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: Hepatocellular carcinoma (HCC) is the fifth most common cancer and the third most common cause of cancer-related death worldwide. Radiofrequency ablation (RFA) is currently performed widely for managing HCC. RFA treatment causes damage around the ablation. Trientine dihydrochloride has been used to reduce the copper in liver. METHODS: The rats were treated with trientine dihydrochloride for 5 days before liver RFA. Liver function, copper concentration, inflammation biomarkers and MDA, SOD were analyzed after RFA treatment for 2 h, 2 and 5 days. RESULTS: The results indicated that trientine dihydrochloride reduced the copper in plasma and liver tissue significantly. And trientine dihydrochloride significantly inhibited RFA-induced inflammatory gene expression in liver. Similar inhibitory effects of trientine dihydrochloride were observed on ROS-induced malondialdehyde production in liver tissues. CONCLUSION: These results suggest that pre-treatment with the selective copper chelator trientine dihydrochloride can inhibit inflammatory response effectively during and after liver RFA in vivo. Chelation of copper to a lower level before liver RFA may be a novel strategy to prevent or ameliorate inflammatory responses in liver induced by RFA and to protect the parenchyma tissues in liver during and after RFA in HCC patients.
[Mh] Termos MeSH primário: Anti-Inflamatórios/uso terapêutico
Ablação por Cateter
Quelantes/uso terapêutico
Cobre/metabolismo
Fígado/efeitos dos fármacos
Trientina/uso terapêutico
[Mh] Termos MeSH secundário: Alanina Transaminase/sangue
Animais
Anti-Inflamatórios/farmacologia
Aspartato Aminotransferases/sangue
Quelantes/farmacologia
Cobre/sangue
Citocinas/sangue
Citocinas/metabolismo
Fígado/metabolismo
Fígado/patologia
Fígado/cirurgia
Masculino
Malondialdeído/metabolismo
Ratos Sprague-Dawley
Superóxido Dismutase/metabolismo
Trientina/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents); 0 (Chelating Agents); 0 (Cytokines); 4Y8F71G49Q (Malondialdehyde); 789U1901C5 (Copper); EC 1.15.1.1 (Superoxide Dismutase); EC 2.6.1.1 (Aspartate Aminotransferases); EC 2.6.1.2 (Alanine Transaminase); SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170916
[Lr] Data última revisão:
170916
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160911
[St] Status:MEDLINE


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[PMID]:27553779
[Au] Autor:Tremmel R; Uhl P; Helm F; Wupperfeld D; Sauter M; Mier W; Stremmel W; Hofhaus G; Fricker G
[Ad] Endereço:Institute of Pharmacy and Molecular Biotechnology, Ruprecht-Karls University, Heidelberg, Germany.
[Ti] Título:Delivery of Copper-chelating Trientine (TETA) to the central nervous system by surface modified liposomes.
[So] Source:Int J Pharm;512(1):87-95, 2016 Oct 15.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The existence of the blood-brain barrier (BBB) complicates the treatment of many central nervous system (CNS) disorders, including the copper storage disease, Wilson's disease. Its CNS symptoms represent a serious problem, since therapeutics for Wilson's disease do not cross the BBB. One strategy to overcome this obstacle is the transfer of drugs across the BBB with colloidal carrier systems like liposomes. The aim of the present study was to encapsulate triethylenetetramine (TETA), a copper chelating agent, into surface modified liposomes and to investigate their permeation across the BBB. Liposomes were modified with cationized bovine serum albumin or penetratin, a cell penetrating peptide. Liposomes were characterized regarding size, PDI, zeta potential and encapsulation efficiency. Size was between 139.4±1.9nm to 171.1±3.5nm with PDI's below 0.2. Zeta potentials of vectorized liposomes were at least 6.9mV higher than those of standard liposomes. Cryo-TEM micrographs displayed liposomal structure, integrity and the similarity of structure and size between loaded, unloaded, vectorized and non- vectorized liposomes. In vivo experiments in rats showed an up to 16-fold higher brain uptake of TETA in vectorized liposomes compared to free TETA or TETA in non-vectorized liposomes, proving successful brain delivery using target seeking surface modifications. Tissue analysis indicated TETA concentrations in the brain being high enough to treat Wilson's disease.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Quelantes/administração & dosagem
Quelantes/farmacocinética
Lipossomos/administração & dosagem
Lipossomos/química
Trientina/administração & dosagem
Trientina/farmacocinética
[Mh] Termos MeSH secundário: Animais
Disponibilidade Biológica
Proteínas de Transporte/química
Proteínas de Transporte/farmacocinética
Lipossomos/farmacocinética
Lipossomos/ultraestrutura
Masculino
Tamanho da Partícula
Ratos
Soroalbumina Bovina/administração & dosagem
Soroalbumina Bovina/química
Soroalbumina Bovina/farmacocinética
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carrier Proteins); 0 (Chelating Agents); 0 (Liposomes); 0 (penetratin); 27432CM55Q (Serum Albumin, Bovine); SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160825
[St] Status:MEDLINE


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[PMID]:27553728
[Au] Autor:Kratena N; Enev VS; Gmeiner G; Gärtner P
[Ad] Endereço:Institute of Applied Synthetic Chemistry, Vienna University of Technology, Getreidemarkt 9, 1060 Vienna, Austria.
[Ti] Título:Synthesis of 17ß-hydroxymethyl-17α-methyl-18-norandrosta-1,4,13-trien-3-one: A long-term metandienone metabolite.
[So] Source:Steroids;115:75-79, 2016 Nov.
[Is] ISSN:1878-5867
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The goal of this work was a good-yielding chemical synthesis of a metandienone metabolite which is of interest in doping analysis. 20ßOH-NorMD (IUPAC: 17ß-hydroxymethyl-17α-methyl-18-norandrosta-1,4,13-triene-3-one) has been identified as a long-term urinary metabolite which can be detected and attributed to metandienone up to almost 3weeks after exposure. The chemical synthesis of its epimer 20αOH-NorMD has been described before, as was an enzymatic synthesis of 20ßOH-NorMD, but no chemical synthesis was published.
[Mh] Termos MeSH primário: Metandrostenolona/química
[Mh] Termos MeSH secundário: Cromatografia Líquida de Alta Pressão
Desidroepiandrosterona/análogos & derivados
Cromatografia Gasosa-Espectrometria de Massas
Espectroscopia de Ressonância Magnética
Estrutura Molecular
Trientina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
459AG36T1B (Dehydroepiandrosterone); 853-23-6 (dehydroepiandrosterone acetate); COZ1R7EOCC (Methandrostenolone); SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170830
[Lr] Data última revisão:
170830
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160825
[St] Status:MEDLINE


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[PMID]:27524025
[Au] Autor:Ren Q; Feng L; Fan R; Ge X; Sun Y
[Ad] Endereço:Department of Chemistry, Shenyang Medical College, Shenyang 110034, PR China.
[Ti] Título:Water-dispersible triethylenetetramine-functionalized graphene: Preparation, characterization and application as an amperometric glucose sensor.
[So] Source:Mater Sci Eng C Mater Biol Appl;68:308-16, 2016 Nov 01.
[Is] ISSN:1873-0191
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The triethylenetetramine-functionalized graphene (TFGn) was prepared using graphene oxide (GO) and triethylenetetramine as raw materials through a one-step reaction under alkaline condition. The triethylenetetramine not only acted as cross-linker to combine GO, but also as reductant of GO. The TFGn was characterized by its ultraviolet spectrum (UV), Fourier transform infrared spectroscopy (FTIR), X-ray photoelectron spectroscopy (XPS), X-ray diffraction (XRD), Raman spectroscopy and Scanning electron microscopy (SEM). The results showed that triethylenetetramine was successfully grafted onto the surface of the GO through covalent bonding between amine and epoxy groups. The resultant TFGn was uniformly dispersed in water over several weeks, suggesting that the introduction of amino groups greatly increased the hydrophilicity of TFGn. The triethylenetetramine-functionalized graphene was then applied to fabricate glucose biosensors with IO4(-) oxidized glucose oxidase (GOx) through layer-by-layer (LBL) self-assembly by the covalent bonding between the aldehyde groups of GOx and amino groups of TFGn. The gold electrodes modified with the (GOx/TFGn)n multilayer films were studied by cyclic voltammetry (CV) and showed outstanding electrocatalytical response to the oxidation of glucose when ferrocenemethanol was used as an artificial redox mediator. The response increased with an increasing number of GOx/TFGn bilayers, indicating that the analytical performance, such as the sensitivity of the glucose biosensor, could be adjusted by tuning the number of deposited GOx/TFGn bilayers. The linear response range of the biosensor constructed with six bilayers of GOx/TFGn to the concentration of glucose can extend to at least 8mM with a sensitivity of 19.9µAmM(-1)cm(-2). In addition, the sensor exhibited good stability due to the covalent interactions between the GOx and TFGn.
[Mh] Termos MeSH primário: Técnicas Biossensoriais/métodos
Glucose Oxidase/química
Glucose/análise
Grafite/química
Trientina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
7782-42-5 (Graphite); EC 1.1.3.4 (Glucose Oxidase); IY9XDZ35W2 (Glucose); SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170406
[Lr] Data última revisão:
170406
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160816
[St] Status:MEDLINE


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[PMID]:27509123
[Au] Autor:Nayor J; Vaidya A; Srivastava A; Seifter JL; Rutherford AE
[Ti] Título:INTERACTIVE MEDICAL CASE. Tracing the Cause of Abdominal Pain.
[So] Source:N Engl J Med;375(6):e8, 2016 Aug 11.
[Is] ISSN:1533-4406
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Dor Abdominal/etiologia
Síndrome de Fanconi/diagnóstico
Degeneração Hepatolenticular/diagnóstico
Fígado/patologia
[Mh] Termos MeSH secundário: Biópsia
Ceruloplasmina/análise
Quelantes/uso terapêutico
Cobre/análise
Cobre/metabolismo
Cobre/urina
Síndrome de Fanconi/etiologia
Feminino
Vesícula Biliar/diagnóstico por imagem
Vesícula Biliar/patologia
Degeneração Hepatolenticular/complicações
Degeneração Hepatolenticular/tratamento farmacológico
Seres Humanos
Fígado/química
Baço/diagnóstico por imagem
Transaminases/sangue
Trientina/uso terapêutico
Ultrassonografia
Adulto Jovem
[Pt] Tipo de publicação:INTERACTIVE TUTORIAL
[Nm] Nome de substância:
0 (Chelating Agents); 789U1901C5 (Copper); EC 1.16.3.1 (Ceruloplasmin); EC 2.6.1.- (Transaminases); SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:161126
[Lr] Data última revisão:
161126
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:160811
[St] Status:MEDLINE
[do] DOI:10.1056/NEJMimc1512611


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[PMID]:27377012
[Au] Autor:Henriet T; Gana I; Ghaddar C; Barrio M; Cartigny Y; Yagoubi N; Do B; Tamarit JL; Rietveld IB
[Ad] Endereço:Matériaux et Santé (EA 401), Faculté de Pharmacie, Université Paris Sud, 5, Rue Jean-Baptiste Clément, 92296, Chatenay-Malabry, France.
[Ti] Título:Solid state stability and solubility of triethylenetetramine dihydrochloride.
[So] Source:Int J Pharm;511(1):312-321, 2016 Sep 10.
[Is] ISSN:1873-3476
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The API triethylenetetramine dihydrochloride used as an alternative treatment of Wilson's disease is sensitive to water and it exhibits polymorphism. As this may become an issue for the drug formulation, the physical stability has been studied by differential scanning calorimetry, high-pressure thermal analysis, dynamic vapor sorption, and X-ray diffraction as a function of temperature. In addition, high-pressure liquid chromatography and mass spectrometry have been used to study the purity and chemical stability of the API. A pressure-temperature phase diagram of the pure compound has been constructed and it can be concluded that form II is monotropic in relation to form I, which is the only stable solid. The solubilities of the different solid forms have been determined with the help of a temperature - composition phase diagram. The API is very soluble, at 20° C about 10% of the saturated solution with respect to the dihydrate consists of API and the solubility of the pure form I is twice as high. Moreover, it has been shown that at 20°C, a relative humidity above 40% induces the formation of the dihydrate and at 70% a saturated solution appears. At higher temperatures, the formation of the dihydrate appears at lower relative humidity values. A clear link has been established between the API's chemical stability, its physical stability and the relative humidity in the air. Humidity levels above 40% are detrimental to the quality of the API.
[Mh] Termos MeSH primário: Trientina/química
Trientina/metabolismo
[Mh] Termos MeSH secundário: Varredura Diferencial de Calorimetria/métodos
Estabilidade de Medicamentos
Espectroscopia de Ressonância Magnética/métodos
Solubilidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160706
[St] Status:MEDLINE


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[PMID]:27001865
[Au] Autor:Hyvönen MT; Ucal S; Pasanen M; Peräniemi S; Weisell J; Khomutov M; Khomutov AR; Vepsäläinen J; Alhonen L; Keinänen TA
[Ad] Endereço:School of Pharmacy, University of Eastern Finland, Yliopistonranta 1C, 70210 Kuopio, Finland.
[Ti] Título:Triethylenetetramine modulates polyamine and energy metabolism and inhibits cancer cell proliferation.
[So] Source:Biochem J;473(10):1433-41, 2016 May 15.
[Is] ISSN:1470-8728
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Polyamine metabolism is an attractive anticancer drug target, since polyamines are absolutely required for cellular proliferation, and increased levels of polyamines and their biosynthetic enzyme ornithine decarboxylase (ODC) are associated with cancer. Triethylenetetramine (TETA) is a charge-deficient isosteric analogue of the polyamine spermidine (Spd) and a Cu(II)-chelating compound used for the treatment of Wilson's disease, and it has been implicated as a potential anticancer therapeutic drug. In the present study, we studied the effects of TETA in comparison with two other Cu(II)-chelators, D-penicillamine (PA) and tetrathiomolybdate (TTM), on polyamine metabolism in DU145 prostate carcinoma, MCF-7 breast carcinoma and JEG-3 choriocarcinoma cells. TETA induced antizyme, down-regulated ODC and inhibited [(14)C] Spd uptake. Moreover, it completely prevented α-difluoromethylornithine (DFMO)-induced increase in [(14)C] Spd uptake, and inhibited [(14)C] putrescine (Put) uptake and ODC activity in vivo Seven-day treatment of DU145 cells with TETA caused growth cessation by reducing intracellular polyamine levels and suppressing the formation of hypusinated eukaryotic translation initiation factor 5A (eIF5A). TETA or its N-acetylated metabolites also inhibited spermine (Spm), diamine and semicarbazide-sensitive amine oxidases and decreased the level of intracellular reactive oxygen species. Moreover, TETA inhibited the utilization of Put as energy source via the tricarboxylic acid (TCA) cycle, as indicated by decreased production of (14)CO2 from [(14)C] Put. These results indicate that TETA attacks multiple proven anticancer drug targets not attributed to copper chelation, which warrants further studies to reveal its potential in cancer chemoprevention and cure.
[Mh] Termos MeSH primário: Proliferação Celular/efeitos dos fármacos
Metabolismo Energético/efeitos dos fármacos
Poliaminas/metabolismo
Trientina/farmacologia
[Mh] Termos MeSH secundário: Amina Oxidase (contendo Cobre)
Linhagem Celular Tumoral
Eflornitina/metabolismo
Feminino
Seres Humanos
Células MCF-7
Masculino
Molibdênio/farmacologia
Penicilamina/metabolismo
Putrescina/metabolismo
Espécies Reativas de Oxigênio/metabolismo
Espermina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Polyamines); 0 (Reactive Oxygen Species); 2FZ7Y3VOQX (Spermine); 81AH48963U (Molybdenum); 91U3TGV99T (tetrathiomolybdate); EC 1.4.3.21 (Amine Oxidase (Copper-Containing)); GNN1DV99GX (Penicillamine); SJ76Y07H5F (Trientine); V10TVZ52E4 (Putrescine); ZQN1G5V6SR (Eflornithine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170515
[Lr] Data última revisão:
170515
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160323
[St] Status:MEDLINE
[do] DOI:10.1042/BCJ20160134


  10 / 354 MEDLINE  
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[PMID]:26827161
[Au] Autor:Wang R; Zhang X; Chen C; Chen G; Zhong Q; Zhang Q; Zheng S; Wang G; Chen QH
[Ad] Endereço:Department of Chemistry, California State University, Fresno, 2555 E. San Ramon, M/S SB70, Fresno, CA 93740, USA.
[Ti] Título:Synthesis and evaluation of 1,7-diheteroarylhepta-1,4,6-trien-3-ones as curcumin-based anticancer agents.
[So] Source:Eur J Med Chem;110:164-80, 2016 Mar 03.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Thirty (1E,4E,6E)-1,7-diaryl-1,4,6-heptatrien-3-ones, featuring a central linear trienone linker and two identical nitrogen-containing heteroaromatic rings, were designed and synthesized as curcumin-based anticancer agents on the basis of their structural similarity to the enol-tautomer of curcumin, in addition to taking advantage of the possibly enhanced pharmacokinetic profiles contributed by the basic nitrogen-containing heteroaromatic rings. Their cytotoxicity and antiproliferative activity were evaluated towards both androgen-dependent and androgen-independent prostate cancer cell lines, as well as HeLa human cervical cancer cells. Among them, the ten most potent analogues are 5- to 36-fold more potent than curcumin in inhibiting cancer cell proliferation. The acquired structure-activity relationship data indicate (i) that (1E,4E,6E)-1,7-diaryl-1,4,6-heptatrien-3-ones represent a potential scaffold for development of curcumin-based agents with substantially improved cytotoxicity and anti-proliferative effect; and (ii) 1-alkyl-1H-imidazol-2-yl and 1-alkyl-1H-benzo[d]imidazole-2-yl serve as optimal heteroaromatic rings for increased in vitro potency of this scaffold. Two of most potent compounds displayed no apparent cytotoxicity toward MCF-10A normal mammary epithelial cells at 1 µM concentration. Treatment of PC-3 prostate cancer cells with the most potent compound led to appreciable cell cycle arrest at a G1/G0 phase and cell apoptosis induction.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Proliferação Celular/efeitos dos fármacos
Curcumina/análogos & derivados
Curcumina/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Linhagem Celular Tumoral
Curcumina/síntese química
Desenho de Drogas
Ensaios de Seleção de Medicamentos Antitumorais
Feminino
Células HeLa
Seres Humanos
Masculino
Neoplasias/tratamento farmacológico
Neoplasias da Próstata/tratamento farmacológico
Relação Estrutura-Atividade
Trientina/análogos & derivados
Trientina/síntese química
Trientina/farmacologia
Neoplasias do Colo do Útero/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Antineoplastic Agents); IT942ZTH98 (Curcumin); SJ76Y07H5F (Trientine)
[Em] Mês de entrada:1610
[Cu] Atualização por classe:170303
[Lr] Data última revisão:
170303
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160201
[St] Status:MEDLINE



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