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Pesquisa : D02.455.426.392.368.284.049 [Categoria DeCS]
Referências encontradas : 320 [refinar]
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[PMID]:28863191
[Au] Autor:Sotillo WS; Villagomez R; Smiljanic S; Huang X; Malakpour A; Kempengren S; Rodrigo G; Almanza G; Sterner O; Oredsson S
[Ad] Endereço:Department of Biology, Lund University, Lund, Sweden.
[Ti] Título:Anti-cancer stem cell activity of a sesquiterpene lactone isolated from Ambrosia arborescens and of a synthetic derivative.
[So] Source:PLoS One;12(9):e0184304, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:New regimens are constantly being pursued in cancer treatment, especially in the context of treatment-resistant cancer stem cells (CSCs) that are assumed to be involved in cancer recurrence. Here, we investigated the anti-cancer activity of sesquiterpene lactones (SLs) isolated from Ambrosia arborescens and of synthetic derivatives in breast cancer cell lines, with a specific focus on activity against CSCs. The breast cancer cell lines MCF-7, JIMT-1, and HCC1937 and the normal-like breast epithelial cell line MCF-10A were treated with the SLs damsin and coronopilin, isolated from A. arborescens, and with ambrosin and dindol-01, synthesized using damsin. Inhibitory concentration 50 (IC50) values were obtained from dose-response curves. Based on IC50 values, doses in the µM range were used for investigating effects on cell proliferation, cell cycle phase distribution, cell death, micronuclei formation, and cell migration. Western blot analysis was used to investigate proteins involved in cell cycle regulation as well as in the NF-κB pathway since SLs have been shown to inhibit this transcription factor. Specific CSC effects were investigated using three CSC assays. All compounds inhibited cell proliferation; however, damsin and ambrosin were toxic at single-digit micromolar ranges, while higher concentrations were required for coronopilin and dindol-01. Of the four cell lines, the compounds had the least effect on the normal-like MCF-10A cells. The inhibition of cell proliferation can partly be explained by downregulation of cyclin-dependent kinase 2. All compounds inhibited tumour necrosis factor-α-induced translocation of NF-κB from the cytoplasm to the nucleus. Damsin and ambrosin treatment increased the number of micronuclei; moreover, another sign of DNA damage was the increased level of p53. Treatment with damsin and ambrosin decreased the CSC subpopulation and inhibited cell migration. Our results suggest that these compounds should be further investigated to find efficient CSC-inhibiting compounds.
[Mh] Termos MeSH primário: Ambrosia/química
Antineoplásicos/farmacologia
Lactonas/farmacologia
Células-Tronco Neoplásicas/efeitos dos fármacos
Extratos Vegetais/farmacologia
Sesquiterpenos/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/isolamento & purificação
Azulenos/isolamento & purificação
Azulenos/farmacologia
Ciclo Celular
Linhagem Celular Tumoral
Núcleo Celular/metabolismo
Proliferação Celular/efeitos dos fármacos
Citoplasma/metabolismo
Relação Dose-Resposta a Droga
Seres Humanos
Concentração Inibidora 50
Lactonas/isolamento & purificação
Células MCF-7
Testes para Micronúcleos
NF-kappa B/metabolismo
Células-Tronco Neoplásicas/patologia
Sesquiterpenos/isolamento & purificação
Fator de Necrose Tumoral alfa/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Azulenes); 0 (Lactones); 0 (NF-kappa B); 0 (Plant Extracts); 0 (Sesquiterpenes); 0 (Tumor Necrosis Factor-alpha); 1216-42-8 (damsin); 6XI048644B (ambrosin)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171023
[Lr] Data última revisão:
171023
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170902
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0184304


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[PMID]:28701650
[Au] Autor:Hasegawa T; Yoshitome K; Fujihara T; Santoso M; Aziz MA
[Ad] Endereço:Graduate School of Science and Engineering, Saitama University.
[Ti] Título:Characteristic Changes in the Aroma Profile of Patchouli Depending on Manufacturing Process.
[So] Source:J Oleo Sci;66(8):863-869, 2017 Aug 01.
[Is] ISSN:1347-3352
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Patchouli is used as an incense material and essential oil. The characteristic odor of patchouli leaves results from the drying process used in their production; however, there have to date been no reports on the changes in the odor of patchouli leaves during the drying process. We investigated the aroma profile of dried patchouli leaves using the hexane extracts of fresh and dried patchouli leaves. We focused on the presence or absence of the constituents of the fresh and dried extracts, and the differences in the content of the common constituents. Fourteen constituents were identified as characteristic of dried patchouli extract odor by gas chromatography-olfactometry analysis. The structures of seven of the 14 constituents were determined by gas chromatography-mass spectrometry (α-patchoulene, seychellene, humulene, α-bulnesene, isoaromadendrene epoxide, caryophyllene oxide, and patchouli alcohol). The aroma profile of the essential oil obtained from the dried patchouli leaves was clearly different from that of dried patchouli. The aroma profile of the essential oil was investigated by a similar method. We identified 12 compounds as important odor constituents. The structures of nine of the 12 constituents were determined by gas chromatography-mass spectrometry (cis-thujopsene, caryophyllene, α-guaiene, α-patchoulene, seychellene, α-bulnesene, isoaromadendrene epoxide, patchouli alcohol, and corymbolone). Comparing the odors and constituents demonstrated that the aroma profile of patchouli depends on the manufacturing process.
[Mh] Termos MeSH primário: Azulenos/isolamento & purificação
Odorantes/análise
Óleos Voláteis/química
Óleos Voláteis/isolamento & purificação
Extratos Vegetais/química
Óleos Vegetais/química
Óleos Vegetais/isolamento & purificação
Pogostemon/química
Sesquiterpenos de Guaiano/isolamento & purificação
Sesquiterpenos/isolamento & purificação
[Mh] Termos MeSH secundário: Azulenos/química
Cromatografia Gasosa
Cromatografia Gasosa-Espectrometria de Massas
Hexanos
Extração Líquido-Líquido/métodos
Olfatometria
Folhas de Planta/química
Sesquiterpenos/química
Sesquiterpenos de Guaiano/química
Terpenos/química
Terpenos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azulenes); 0 (Hexanes); 0 (Oils, Volatile); 0 (Plant Extracts); 0 (Plant Oils); 0 (Sesquiterpenes); 0 (Sesquiterpenes, Guaiane); 0 (Terpenes); 0 (alpha-bulnesene); 0 (seychellene); 0 (thujopsene); 88-84-6 (guaiene); BHW853AU9H (caryophyllene)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171010
[Lr] Data última revisão:
171010
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170714
[St] Status:MEDLINE
[do] DOI:10.5650/jos.ess17002


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[PMID]:28649852
[Au] Autor:Wang MY; Zhai YS; Liang CH
[Ad] Endereço:b School of Traditional Chinese Medicine, Capital Medical University , Beijing 100069 , China.
[Ti] Título:Two new guaiane-type sesquiterpenoids from Valeriana hardwickii and their cytotoxicity.
[So] Source:J Asian Nat Prod Res;19(10):987-992, 2017 Oct.
[Is] ISSN:1477-2213
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Two new guaiane-type sesquiterpenoids, named 4α,5α-epoxy-8ß-hydroxy-1α-hydro-α-guaiene (1) and 4α,5α-epoxy-1-hydroxy-α-guaiene (2), were isolated from the whole plants of Valeriana hardwickii. Their structures were elucidated on the basis of spectroscopic analysis. Compounds 1 and 2 showed weak cytotoxicity against the lung adenocarcinoma (A549) and hepatoma (Bel7402) cell lines with IC values of 9.2 and 8.5 µM, respectively.
[Mh] Termos MeSH primário: Antineoplásicos Fitogênicos/isolamento & purificação
Medicamentos de Ervas Chinesas/isolamento & purificação
Sesquiterpenos de Guaiano/isolamento & purificação
Valeriana/química
[Mh] Termos MeSH secundário: Células A549
Antineoplásicos Fitogênicos/química
Antineoplásicos Fitogênicos/farmacologia
Azulenos
Ensaios de Seleção de Medicamentos Antitumorais
Medicamentos de Ervas Chinesas/química
Medicamentos de Ervas Chinesas/farmacologia
Seres Humanos
Concentração Inibidora 50
Estrutura Molecular
Ressonância Magnética Nuclear Biomolecular
Paclitaxel/farmacologia
Sesquiterpenos de Guaiano/química
Sesquiterpenos de Guaiano/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4alpha,5alpha-epoxy-1-hydroxy-alpha-guaiene); 0 (4alpha,5alpha-epoxy-8beta-hydroxy-1alpha-hydro-alpha-guaiene); 0 (Antineoplastic Agents, Phytogenic); 0 (Azulenes); 0 (Drugs, Chinese Herbal); 0 (Sesquiterpenes, Guaiane); 88-84-6 (guaiene); P88XT4IS4D (Paclitaxel)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171003
[Lr] Data última revisão:
171003
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170627
[St] Status:MEDLINE
[do] DOI:10.1080/10286020.2017.1339350


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[PMID]:28644559
[Au] Autor:Wang Z; Udmark J; Börjesson K; Rodrigues R; Roffey A; Abrahamsson M; Nielsen MB; Moth-Poulsen K
[Ad] Endereço:Department of Chemistry and Chemical Engineering, Chalmers University of Technology, Gothenburg, Sweden.
[Ti] Título:Evaluating Dihydroazulene/Vinylheptafulvene Photoswitches for Solar Energy Storage Applications.
[So] Source:ChemSusChem;10(15):3049-3055, 2017 Aug 10.
[Is] ISSN:1864-564X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Efficient solar energy storage is a key challenge in striving toward a sustainable future. For this reason, molecules capable of solar energy storage and release through valence isomerization, for so-called molecular solar thermal energy storage (MOST), have been investigated. Energy storage by photoconversion of the dihydroazulene/vinylheptafulvene (DHA/VHF) photothermal couple has been evaluated. The robust nature of this system is determined through multiple energy storage and release cycles at elevated temperatures in three different solvents. In a nonpolar solvent such as toluene, the DHA/VHF system can be cycled more than 70 times with less than 0.01 % degradation per cycle. Moreover, the [Cu(CH CN) ]PF -catalyzed conversion of VHF into DHA was demonstrated in a flow reactor. The performance of the DHA/VHF couple was also evaluated in prototype photoconversion devices, both in the laboratory by using a flow chip under simulated sunlight and under outdoor conditions by using a parabolic mirror. Device experiments demonstrated a solar energy storage efficiency of up to 0.13 % in the chip device and up to 0.02 % in the parabolic collector. Avenues for future improvements and optimization of the system are also discussed.
[Mh] Termos MeSH primário: Azulenos/química
Cicloeptanos/química
Dispositivos Lab-On-A-Chip
Processos Fotoquímicos
Energia Solar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azulenes); 0 (Cycloheptanes); 0 (dihydroazulene)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171102
[Lr] Data última revisão:
171102
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170624
[St] Status:MEDLINE
[do] DOI:10.1002/cssc.201700679


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[PMID]:28196702
[Au] Autor:Li G; Zhao JY; Niu C; Nie LF; Dong CZ; Aisa HA
[Ad] Endereço:The Key Laboratory of Plant Resources and Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, PR China; State Key Laboratory Basis of Xinjiang Indigenous Medicinal Plants Resource Utilization, Xinjiang Technical Institute of Phys
[Ti] Título:Structure-activity relationship studies of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters against influenza viruses.
[So] Source:Bioorg Med Chem Lett;27(6):1484-1487, 2017 03 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A series of 1-(1'-hydroxyalkyl)rupestonic acid methyl esters were synthesized via the condensation of methyl rupestonate with various aldehydes in the presence of LDA. This mixed aldol reaction was highly stereoselective and all the new compounds were elucidated by detailed NMR and MS analyses. The absolute configurations of the newly formed stereocenters were further confirmed by X-ray crystallographic analysis of 3d, the results of which were found to be opposite to the prediction based on Zimmerman-Traxler's and Houk's models. All the compounds synthesized were then evaluated for their in vitro inhibitory activities against influenza A (H1N1 and H3N2) and B viruses. The data showed that 3p displayed the highest activity against influenza A H1N1 (IC =0.69µg/mL) and H3N2 (IC =0.69µg/mL) viruses, which were even better than Ribavirin and Oseltmivir. On the other hand, both 3c and 3o were found to show comparable activities with the reference drugs in inhibiting both influenza A and B viruses. Further studies will focus on reducing the cytotoxicity of the hits reported in this work.
[Mh] Termos MeSH primário: Antivirais/química
Antivirais/farmacologia
Azulenos/farmacologia
Orthomyxoviridae/efeitos dos fármacos
Sesquiterpenos/farmacologia
[Mh] Termos MeSH secundário: Azulenos/química
Cristalografia por Raios X
Ésteres/química
Testes de Sensibilidade Microbiana
Sesquiterpenos/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antiviral Agents); 0 (Azulenes); 0 (Esters); 0 (Sesquiterpenes); 115473-63-7 (rupestonic acid)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170216
[St] Status:MEDLINE


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[PMID]:27719914
[Au] Autor:Baqueiro-Peña I; Guerrero-Beltrán JÁ
[Ad] Endereço:Departamento de Ingeniería Química, Alimentos y Ambiental, Universidad de las Américas Puebla, Cholula, Puebla 72810, Mexico.
[Ti] Título:Physicochemical and antioxidant characterization of Justicia spicigera.
[So] Source:Food Chem;218:305-312, 2017 Mar 01.
[Is] ISSN:0308-8146
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Extracts with water:ethanol (100:0, 70:30, 50:50, 30:70, 0:100) solutions from fresh (F), just dried (JD), dried and stored for one year (DS) Justicia spicigera leaves were obtained using the stirring and ultrasound techniques. Extracts were analyzed in physicochemical and antioxidant characteristics. Identification of chemical compounds by gas chromatography-mass spectroscopy (GC-MS) was also performed. 2.14±0.91, 5.67±1.70, and 8.52±4.97g Gallic acid equivalents/100g dry weight (d.w.) of phenolic compounds were found, in average, for F, JD, and DS J. spicigera, respectively. 2.22±1.31, 2.58±2.11, and 8.48±3.78g Trolox equivalents/100g d.w. were detected with the ABTS method and 0.49±0.33, 1.23±0.87, and 0.88±0.94g with the DPPH method for F, JD and DS J. spicigera, respectively. Eucalyptol, phytol, and azulene were identified as the main compounds. J. spicigera showed colors (green-iridescent, green-yellow, or pink of different intensities) and antioxidant characteristics depending on the solvent concentration. Extracts could be used in the food and pharmaceutical industries.
[Mh] Termos MeSH primário: Antioxidantes/análise
Fenômenos Químicos
Justicia/química
[Mh] Termos MeSH secundário: Azulenos/análise
Cromanos/análise
Cor
Cicloexanóis/análise
Ácido Gálico/análise
Cromatografia Gasosa-Espectrometria de Massas
Monoterpenos/análise
Fenóis/análise
Fitol/análise
Extratos Vegetais/análise
Extratos Vegetais/farmacologia
Folhas de Planta/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Azulenes); 0 (Chromans); 0 (Cyclohexanols); 0 (Monoterpenes); 0 (Phenols); 0 (Plant Extracts); 150-86-7 (Phytol); 632XD903SP (Gallic Acid); 82R6M9MGLP (azulene); RV6J6604TK (eucalyptol); S18UL9710X (6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid)
[Em] Mês de entrada:1701
[Cu] Atualização por classe:171008
[Lr] Data última revisão:
171008
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161011
[St] Status:MEDLINE


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[PMID]:27863713
[Au] Autor:Sciarrone D; Pantò S; Donato P; Mondello L
[Ad] Endereço:Dipartimento di "Scienze Chimiche, Biologiche, Farmaceutiche ed Ambientali", University of Messina, Polo Annunziata-viale Annunziata, 98168, Messina, Italy.
[Ti] Título:Improving the productivity of a multidimensional chromatographic preparative system by collecting pure chemicals after each of three chromatographic dimensions.
[So] Source:J Chromatogr A;1475:80-85, 2016 Dec 02.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The enhanced sample collection capability of a heart-cutting three-dimensional GC-prep system is reported. In its original configuration, a highly pure component can be usually collected after the last (3D) column outlet by means of a dedicated preparative station. The latter is located after the last chromatographic column, and this poses the requirement for multiple heart cuts even for those components showing satisfactory degree of purity after the first (or second) separation dimension. The feasibility to collect pure components after each chromatographic dimension is here described, employing a three-dimension MDGC system equipped with high-temperature valves, located inside the first and second GC ovens, with the aim to improve the productivity of the collection procedure. In addition to a commercial preparative collector located at the 3D outlet, two laboratory-made collection systems were applied in the first and second dimension, reached by the effluent to be collected trough a high-temperature valve switching the heart-cut fraction between either the detector (FID), or the collector. Highly pure sesquiterpene components were collected, namely: patchouli alcohol after the first column [poly(5% diphenyl/95% dimethylsiloxane)], α-bulnesene after a second column coated with high molecular weight polyethylene glycol, and α-guaiene after an ionic-liquid based column (SLB-IL60), used as the third dimension. Purity levels ranging from 85 to 95% were achieved with an average collection recovery of 90% (n=5). The following average amounts were collected per run: 160µg for α-guaiene, 295µg for α-bulnesene, and 496µg for patchouli alcohol.
[Mh] Termos MeSH primário: Cromatografia Gasosa/métodos
Sesquiterpenos/isolamento & purificação
[Mh] Termos MeSH secundário: Azulenos/isolamento & purificação
Dimetilpolisiloxanos
Polietilenoglicóis
Sesquiterpenos de Guaiano/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Azulenes); 0 (Dimethylpolysiloxanes); 0 (Sesquiterpenes); 0 (Sesquiterpenes, Guaiane); 0 (alpha-bulnesene); 30IQX730WE (Polyethylene Glycols); 88-84-6 (guaiene); HHH8CPR1M2 (patchouli alcohol)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161120
[St] Status:MEDLINE


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[PMID]:27720778
[Au] Autor:Gupta P; Kathawala RJ; Wei L; Wang F; Wang X; Druker BJ; Fu LW; Chen ZS
[Ad] Endereço:Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, Queens, NY, 11439, USA.
[Ti] Título:PBA2, a novel inhibitor of imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia.
[So] Source:Cancer Lett;383(2):220-229, 2016 12 28.
[Is] ISSN:1872-7980
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Chronic Myeloid Leukemia (CML) is largely caused by the Philadelphia (Ph) chromosome carrying the Break point Cluster Region-Abelson (BCR-ABL) oncogene. Imatinib is a BCR-ABL-targeted therapy and considered the standard of care in CML management. Resistance to imatinib therapy often develops because of mutations in the BCR-ABL kinase domain. In this study, we evaluated PBA2, a novel BCR-ABL inhibitor, for its anti-cancer activity against BCR-ABL expressing BaF3 cells. PBA2 shows potent activity against wild-type and T315I mutated BaF3 cells as compared with imatinib. PBA2 inhibited the phosphorylation of BCR-ABL and its downstream signaling in BaF3/WT and BaF3/T315I cells. PBA2 inhibited the mRNA expression of BCR-ABL in BaF3/WT and BaF3/T315I cells. Mechanistically, PBA2 increased the cell population in sub G1 phase of the cell cycle, induced apoptosis and elevated ROS production in both BaF3/WT and BaF3/T315I cells. Taken together, our results indicate that PBA2 exhibits anti-proliferative effects and inhibits the imatinib-resistant T315I BCR-ABL mutation. PBA2 may be a novel drug candidate for overcoming the resistance to imatinib in CML patients.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Azulenos/farmacologia
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Proteínas de Fusão bcr-abl/antagonistas & inibidores
Compostos Heterocíclicos com 3 Anéis/farmacologia
Mesilato de Imatinib/farmacologia
Leucemia Mielogênica Crônica BCR-ABL Positiva/tratamento farmacológico
Mutação
Inibidores de Proteínas Quinases/farmacologia
[Mh] Termos MeSH secundário: Animais
Apoptose/efeitos dos fármacos
Linhagem Celular
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Proteínas de Fusão bcr-abl/genética
Proteínas de Fusão bcr-abl/metabolismo
Pontos de Checagem da Fase G1 do Ciclo Celular/efeitos dos fármacos
Regulação Neoplásica da Expressão Gênica
Leucemia Mielogênica Crônica BCR-ABL Positiva/genética
Leucemia Mielogênica Crônica BCR-ABL Positiva/metabolismo
Leucemia Mielogênica Crônica BCR-ABL Positiva/patologia
Camundongos
Terapia de Alvo Molecular
Estresse Oxidativo/efeitos dos fármacos
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Espécies Reativas de Oxigênio/metabolismo
Transdução de Sinais/efeitos dos fármacos
Fatores de Tempo
Transfecção
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (9-(2-chlorophenyl)-6-ethyl-1-methyl-2,4-dihydro-2,3,4,7,10-pentaaza-benzo(f)azulene); 0 (Antineoplastic Agents); 0 (Azulenes); 0 (Heterocyclic Compounds, 3-Ring); 0 (Protein Kinase Inhibitors); 0 (RNA, Messenger); 0 (Reactive Oxygen Species); 8A1O1M485B (Imatinib Mesylate); EC 2.7.10.2 (Fusion Proteins, bcr-abl)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171029
[Lr] Data última revisão:
171029
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161011
[St] Status:MEDLINE


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[PMID]:27561983
[Au] Autor:Li H; Hu Y; Wang X; He G; Xu Y; Zhu Q
[Ad] Endereço:Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University, Nanjing 21009, China.
[Ti] Título:Novel tricyclic poly (ADP-ribose) polymerase-1/2 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis and biological evaluation.
[So] Source:Bioorg Med Chem;24(19):4731-4740, 2016 Oct 01.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:8,9-Dihydro-2,4,7,9a-tetraazabenzo[cd]azulen-6(7H)-ones were designed and synthesized as a new class of PARP-1/2 inhibitors. The compounds displayed a variable pattern of PARP-1/2 enzymes inhibition profile that, in part, paralleled the antiproliferative activity in cell lines. Among them, compound 9e exhibited not only the significant IC50 value of 28nM in the PARP-1 and 7.7nM in PARP-2 enzyme assay, but also a profound synergic efficacy combined with temozolomide with PF50 values of 2.6, 2.5, and 6.5 against MDA-MB-468, SW-620 and A549 and cell line, respectively.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/farmacologia
Azulenos/química
Azulenos/farmacologia
Inibidores de Poli(ADP-Ribose) Polimerases/química
Inibidores de Poli(ADP-Ribose) Polimerases/farmacologia
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Desenho de Drogas
Seres Humanos
Modelos Moleculares
Neoplasias/tratamento farmacológico
Neoplasias/enzimologia
Neoplasias/patologia
Poli(ADP-Ribose) Polimerase-1/antagonistas & inibidores
Poli(ADP-Ribose) Polimerase-1/metabolismo
Poli(ADP-Ribose) Polimerases/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Azulenes); 0 (Poly(ADP-ribose) Polymerase Inhibitors); EC 2.4.2.30 (PARP2 protein, human); EC 2.4.2.30 (Poly (ADP-Ribose) Polymerase-1); EC 2.4.2.30 (Poly(ADP-ribose) Polymerases)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170919
[Lr] Data última revisão:
170919
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160827
[St] Status:MEDLINE


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[PMID]:27033169
[Au] Autor:de Lima BR; da Silva FM; Soares ER; de Almeida RA; da Silva Filho FA; Pereira Junior RC; Hernandez Tasco ÁJ; Salvador MJ; Koolen HH; de Souza AD; Pinheiro ML
[Ad] Endereço:a Departamento de Química , Universidade Federal do Amazonas , Manaus , Brazil.
[Ti] Título:Chemical composition and antimicrobial activity of the essential oils of Onychopetalum amazonicum R.E.Fr.
[So] Source:Nat Prod Res;30(20):2356-9, 2016 Oct.
[Is] ISSN:1478-6427
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The essential oils from leaves, twigs and trunk bark of Onychopetalum amazonicum R.E. Fr. (Annonaceae), obtained by hydrodistillation, were analysed by GC and GC-MS, and also were evaluated for in vitro antimicrobial activity. Forty-one compounds, which correspond to 75.0-92.2% of the oil components, were identified. Major compounds were sesquiterpenes, including (E)-caryophyllene, caryophyllene oxide, spathulenol, α-gurjunene, allo-aromadendrene and α-epi-cadinol. The oils were evaluated for antimicrobial activities against four bacteria strains and five pathogenic fungi. The oil of the trunk bark exhibited good activity against Staphylococcus epidermidis ATCC 12228, Escherichia coli ATCC 10538 and Kocuria rhizophila ATCC 9341, with a minimal inhibitory concentration of 62.5 µg/mL. The essential oil composition and the antimicrobial evaluation are reported for the first time for the genus Onychopetalum.
[Mh] Termos MeSH primário: Annonaceae/química
Anti-Infecciosos/isolamento & purificação
Óleos Voláteis/química
Óleos Voláteis/farmacologia
Sesquiterpenos
[Mh] Termos MeSH secundário: Anti-Infecciosos/química
Anti-Infecciosos/farmacologia
Azulenos/isolamento & purificação
Escherichia coli/efeitos dos fármacos
Cromatografia Gasosa-Espectrometria de Massas
Testes de Sensibilidade Microbiana
Óleos Voláteis/isolamento & purificação
Folhas de Planta/química
Sesquiterpenos/análise
Sesquiterpenos/isolamento & purificação
Staphylococcus epidermidis/efeitos dos fármacos
Terpenos/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Infective Agents); 0 (Azulenes); 0 (Oils, Volatile); 0 (Sesquiterpenes); 0 (Terpenes); 0 (aromadendrene); 0 (cadinol); 7XV9L96SJJ (spathulenol); BHW853AU9H (caryophyllene); S2XU9K448U (caryophyllene oxide)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160402
[St] Status:MEDLINE
[do] DOI:10.1080/14786419.2016.1163691



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