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[PMID]:28806947
[Au] Autor:Siriyong T; Srimanote P; Chusri S; Yingyongnarongkul BE; Suaisom C; Tipmanee V; Voravuthikunchai SP
[Ad] Endereço:Department of Microbiology and Excellence Research Laboratory on Natural Products, Faculty of Science and Natural Product Research Center of Excellence, Prince of Songkla University, Hat Yai, Songkhla, 90112, Thailand.
[Ti] Título:Conessine as a novel inhibitor of multidrug efflux pump systems in Pseudomonas aeruginosa.
[So] Source:BMC Complement Altern Med;17(1):405, 2017 Aug 14.
[Is] ISSN:1472-6882
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Holarrhena antidysenterica has been employed as an ethnobotanical plant for the treatment of dysentery, diarrhoea, fever, and bacterial infections. Biological activities of the principle compound, conessine including anti-diarrhoea and anti-plasmodial effects were documented. Our previous study reported potency of Holarrhena antidysenterica extract and conessine as resistance modifying agents against extensively drug-resistant Acinetobacter baumannii. This study aimed to investigate (i) whether conessine, a steroidal alkaloid compound, could act as a resistance modifying agent against multidrug-resistant Pseudomonas aeruginosa, and (ii) whether MexAB-OprM efflux pump involved in the mechanism. METHODS: Conessine combined with various antibiotics were determined for synergistic activity against P. aeruginosa PAO1 strain K767 (wild-type), K1455 (MexAB-OprM overexpressed), and K1523 (MexB deletion). H33342 accumulation assay was used to evaluate efflux pump inhibition while NPN uptake assay was assessed membrane permeabilization. RESULTS: Conessine significantly reduced MICs of all antibiotics by at least 8-fold in MexAB-OprM overexpressed strain. The levels were comparable to those obtained in wild-type strain for cefotaxime, levofloxacin, and tetracycline. With erythromycin, novobiocin, and rifampicin, MICs were 4- to 8-fold less than MICs of the wild-type strain. Loss of MexAB-OprM due to deletion of mexB affected susceptibility to almost all antibiotics, except novobiocin. Synergistic activities between other antibiotics (except novobiocin) and conessine observed in MexB deletion strain suggested that conessine might inhibit other efflux systems present in P. aeruginosa. Inhibition of H33342 efflux in the tested strains clearly demonstrated that conessine inhibited MexAB-OprM pump. In contrast, the mode of action as a membrane permeabilizer was not observed after treatment with conessine as evidenced by no accumulation of 1-N-phenylnaphthylamine. CONCLUSIONS: The results suggested that conessine could be applied as a novel efflux pump inhibitor to restore antibiotic activity by inhibiting efflux pump systems in P. aeruginosa. The findings speculated that conessine may also have a potential to be active against homologous resistance-nodulation-division (RND) family in other Gram-negative pathogens.
[Mh] Termos MeSH primário: Alcaloides/farmacologia
Antibacterianos/farmacologia
Proteínas de Bactérias/antagonistas & inibidores
Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos
Holarrhena/química
Extratos Vegetais/farmacologia
Pseudomonas aeruginosa/efeitos dos fármacos
[Mh] Termos MeSH secundário: 1-Naftilamina/análogos & derivados
Proteínas da Membrana Bacteriana Externa/antagonistas & inibidores
Benzimidazóis
Sinergismo Farmacológico
Quimioterapia Combinada
Proteínas de Membrana Transportadoras
Testes de Sensibilidade Microbiana
Pseudomonas aeruginosa/crescimento & desenvolvimento
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkaloids); 0 (Anti-Bacterial Agents); 0 (Bacterial Outer Membrane Proteins); 0 (Bacterial Proteins); 0 (Benzimidazoles); 0 (Membrane Transport Proteins); 0 (MexB protein, Pseudomonas aeruginosa); 0 (OprM protein, Pseudomonas aeruginosa); 0 (Plant Extracts); 90-30-2 (N-phenyl-1-naphthylamine); 9753I242R5 (1-Naphthylamine); EZ38J9BBDF (conessine); P976261J69 (bisbenzimide ethoxide trihydrochloride)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170901
[Lr] Data última revisão:
170901
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170816
[St] Status:MEDLINE
[do] DOI:10.1186/s12906-017-1913-y


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[PMID]:28527428
[Au] Autor:Pulido-Reyes G; Martín E; Gu Coronado JL; Leganes F; Rosal R; Fernández-Piñas F
[Ad] Endereço:Departamento de Biología, Facultad de Ciencias, Universidad Autónoma de Madrid, E-28049, Spain; Departamento de Ingeniería Química, Universidad de Alcalá, E-28871 Alcalá de Henares, Madrid, Spain. Electronic address: gerardo.pulido@uam.es.
[Ti] Título:Physicochemical and biological interactions between cerium oxide nanoparticles and a 1,8-naphthalimide derivative.
[So] Source:J Photochem Photobiol B;172:61-69, 2017 Jul.
[Is] ISSN:1873-2682
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Cerium (Ce) oxide nanoparticles (CNPs) have attracted attention due to their high bioactivity and unique redox-chemistry. The oxygen vacancies at the surface of the nanoparticle explain the autocatalytic properties of CNPs in which the Ce atoms occupy the center of the oxygen vacancies surrounded by Ce atoms. Until now, CNPs have been associated with organic molecules at the synthesis stage to extend their applications or improve their stability. However, there is a lack of information regarding the post-synthesis interaction of CNPs and organic molecules that could enhance or induce new properties. Due to their unique optical properties and their many uses in different areas such as supramolecular chemistry or biomedicine, we have chosen a derivative from the family of naphthalimides (the 4-amino-1,8-naphthalimide-N-substituted; ANN) to study the interaction with different CNPs (CNP1-4) and their joint bioactivity compared to that of the same compounds alone. ANN-CNP complexes were formed as revealed by spectroscopic studies, but, the interaction was markedly different depending on the physicochemical properties of CNPs and their surface content of Ce sites. The ANN adsorption on all CNPs involved the amino group in the naphthalene moiety as shown by NMR spectroscopy, while the pyrrolidine ring was mainly involved in the specific interaction between ANN and CNP1. The biological effect of each CNP and ANN individually and forming complexes was assessed using a bioluminescent model bacterium. The results showed that ANN and CNP with the higher content of surface Ce (CNP1) when combined acted additively towards the used model organism. In the opposite, ANN-CNP2, ANN-CNP3 and ANN-CNP4 complexes were antagonistic when the nanoparticles dominated the mixture. The results of this study contribute to expand the knowledge of the interaction between nanoparticles and organic molecules which may be useful for understanding the behavior of nanoparticles in complex matrices.
[Mh] Termos MeSH primário: 1-Naftilamina/análogos & derivados
Cério/química
Nanopartículas Metálicas/química
Naftalimidas/química
Quinolonas/química
[Mh] Termos MeSH secundário: 1-Naftilamina/química
Complexos de Coordenação/química
Complexos de Coordenação/metabolismo
Difusão Dinâmica da Luz
Espectroscopia de Ressonância Magnética
Photorhabdus/metabolismo
Espectrometria de Fluorescência
Espectroscopia de Infravermelho com Transformada de Fourier
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Coordination Complexes); 0 (Naphthalimides); 0 (Quinolones); 1742-95-6 (4-amino-1,8-naphthalimide); 30K4522N6T (Cerium); 619G5K328Y (ceric oxide); 9753I242R5 (1-Naphthylamine)
[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:170521
[St] Status:MEDLINE


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[PMID]:28342809
[Au] Autor:Yang M; Camara AKS; Aldakkak M; Kwok WM; Stowe DF
[Ad] Endereço:Department of Anesthesiology, Medical College of Wisconsin, Milwaukee, WI, USA.
[Ti] Título:Identity and function of a cardiac mitochondrial small conductance Ca -activated K channel splice variant.
[So] Source:Biochim Biophys Acta;1858(6):442-458, 2017 06.
[Is] ISSN:0006-3002
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:We provide evidence for location and function of a small conductance, Ca -activated K (SK ) channel isoform 3 (SK3) in mitochondria (m) of guinea pig, rat and human ventricular myocytes. SK agonists protected isolated hearts and mitochondria against ischemia/reperfusion (IR) injury; SK antagonists worsened IR injury. Intravenous infusion of a SK channel agonist/antagonist, respectively, in intact rats was effective in reducing/enhancing regional infarct size induced by coronary artery occlusion. Localization of SK3 in mitochondria was evidenced by Western blot of inner mitochondrial membrane, immunocytochemical staining of cardiomyocytes, and immunogold labeling of isolated mitochondria. We identified a SK3 splice variant in guinea pig (SK3.1, aka SK3a) and human ventricular cells (SK3.2) by amplifying mRNA, and show mitochondrial expression in mouse atrial tumor cells (HL-1) by transfection with full length and truncated SK3.1 protein. We found that the N-terminus is not required for mitochondrial trafficking but the C-terminus beyond the Ca calmodulin binding domain is required for Ca sensing to induce mK influx and/or promote mitochondrial localization. In isolated guinea pig mitochondria and in SK3 overexpressed HL-1 cells, mK influx was driven by adding CaCl . Moreover, there was a greater fall in membrane potential (ΔΨ ), and enhanced cell death with simulated cell injury after silencing SK3.1 with siRNA. Although SK channel opening protects the heart and mitochondria against IR injury, the mechanism for favorable bioenergetics effects resulting from SK channel opening remains unclear. SK channels could play an essential role in restraining cardiac mitochondria from inducing oxidative stress-induced injury resulting from mCa overload.
[Mh] Termos MeSH primário: Mitocôndrias Cardíacas/metabolismo
Canais de Potássio Ativados por Cálcio de Condutância Baixa/fisiologia
[Mh] Termos MeSH secundário: 1-Naftilamina/análogos & derivados
1-Naftilamina/farmacologia
Sequência de Aminoácidos
Animais
Benzimidazóis/farmacologia
Benzimidazóis/uso terapêutico
Cloreto de Cálcio/farmacologia
Hipóxia Celular
Linhagem Celular
Cobaias
Seres Humanos
Potencial da Membrana Mitocondrial/efeitos dos fármacos
Potencial da Membrana Mitocondrial/fisiologia
Camundongos
Mitocôndrias Cardíacas/química
Traumatismo por Reperfusão Miocárdica/metabolismo
Traumatismo por Reperfusão Miocárdica/prevenção & controle
Miócitos Cardíacos/efeitos dos fármacos
Miócitos Cardíacos/metabolismo
Potássio/metabolismo
Bloqueadores dos Canais de Potássio/farmacologia
Isoformas de Proteínas/fisiologia
Interferência de RNA
RNA Mensageiro/biossíntese
Ratos
Proteínas Recombinantes de Fusão/metabolismo
Alinhamento de Sequência
Homologia de Sequência de Aminoácidos
Canais de Potássio Ativados por Cálcio de Condutância Baixa/agonistas
Canais de Potássio Ativados por Cálcio de Condutância Baixa/antagonistas & inibidores
Canais de Potássio Ativados por Cálcio de Condutância Baixa/isolamento & purificação
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, N.I.H., EXTRAMURAL; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 ((R)-N-(benzimidazol-2-yl)-1,2,3,4-tetrahydro-1-naphthylamine); 0 (5,6-dichloro-1-ethyl-1,3-dihydro-2H-benzimidazol-2-one); 0 (Benzimidazoles); 0 (KCNN3 protein, human); 0 (Potassium Channel Blockers); 0 (Protein Isoforms); 0 (RNA, Messenger); 0 (Recombinant Fusion Proteins); 0 (SK3 protein, rat); 0 (Small-Conductance Calcium-Activated Potassium Channels); 9753I242R5 (1-Naphthylamine); M4I0D6VV5M (Calcium Chloride); RWP5GA015D (Potassium)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171024
[Lr] Data última revisão:
171024
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170327
[St] Status:MEDLINE


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[PMID]:28260658
[Au] Autor:Cheng L; He Y; Tian Y; Liu B; Zhang Y; Zhou Q; Wu Z
[Ad] Endereço:State Key Laboratory of Freshwater Ecology and Biotechnology, Institute of Hydrobiology, Chinese Academy of Sciences, Wuhan 430072, China; University of Chinese Academy of Sciences, Beijing 100049, China.
[Ti] Título:Comparative biotoxicity of N-Phenyl-1-naphthylamine and N-Phenyl-2-naphthylamine on cyanobacteria Microcystis aeruginosa.
[So] Source:Chemosphere;176:183-191, 2017 Jun.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:N-Phenyl-1-naphthylamine (P NA) and N-Phenyl-2-naphthylamine (P NA) are both widely used as antioxidant and plant secondary metabolites. In this study, growth, esterase, photosynthetic activity and cell membrane integrity were used as biomarkers to compare biotoxicity of P NA and P NA on Microcystis aeruginosa. According to the results, a dose-response relationship was observed only between P NA concentrations and growth inhibition. The EC (48 h) of P NA calculated from growth inhibition was 16.62 µM, while that of P NA was not detected. When the esterase and photosynthetic activity were applied to evaluate the biotoxicity, it was found that a concentration of 20 µM P NA, P NA caused reduction of esterase activity and Fv/Fm of M. aeruginosa to 22.2 and 3.3%, 97.5 and 92.1%, respectively, after 48 h exposure. The percentage of membrane-damaged cells was increased as P NA exposure concentration increased, but that was not detected when exposure to P NA. The difference substituted position in the molecular structure of P NA and P NA leads to different toxicological properties and only P NA was found highly toxic to M. aeruginosa. The toxicity is due to that only P NA can be biotransformed to 1,4-naphthoquinone, which could induce overproduction of intracellular ROS as well as result in oxidative damage and growth inhibition of test organism.
[Mh] Termos MeSH primário: 1-Naftilamina/análogos & derivados
2-Naftilamina/análogos & derivados
Microcystis/efeitos dos fármacos
[Mh] Termos MeSH secundário: 1-Naftilamina/metabolismo
1-Naftilamina/toxicidade
2-Naftilamina/toxicidade
Antioxidantes/metabolismo
Antioxidantes/toxicidade
Biotransformação/efeitos dos fármacos
Membrana Celular/efeitos dos fármacos
Microcystis/metabolismo
Naftoquinonas/metabolismo
Oxirredução/efeitos dos fármacos
Fotossíntese/efeitos dos fármacos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Naphthoquinones); 456KT854AJ (neozone); 90-30-2 (N-phenyl-1-naphthylamine); 9753I242R5 (1-Naphthylamine); CKR7XL41N4 (2-Naphthylamine); RBF5ZU7R7K (1,4-naphthoquinone)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170428
[Lr] Data última revisão:
170428
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170307
[St] Status:MEDLINE


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[PMID]:28213307
[Au] Autor:Gao YN; Ge FJ; Zhang LP; He Y; Lu ZY; Zhang YY; Liu BY; Zhou QH; Wu ZB
[Ad] Endereço:College of Fisheries, Engineering Technology Research Center of Henan Province for Aquatic Animal Cultivation, Henan Normal University, Xinxiang, Henan, 453007, China.
[Ti] Título:Enhanced toxicity to the cyanobacterium Microcystis aeruginosa by low-dosage repeated exposure to the allelochemical N-phenyl-1-naphthylamine.
[So] Source:Chemosphere;174:732-738, 2017 May.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:It has been puzzling whether and how a plant could exert a strong allelopathic inhibition to the target organisms by releasing low concentrations of allelochemicals. Plant allelochemicals have been proposed to be released continuously, however, direct evidence from specific allelochemicals is urgently required. In the present study, the toxicity of allelochemical N-phenyl-1-naphthylamine (NPN) towards the cyanobacterium Microcystis aeruginosa by two different exposure patterns was compared. One was low-dosage repeated exposure (LRE), in which 50  µg L NPN was repeatedly dosed to simulate the continual release of allelochemicals, and the other one was high-dosage single exposure (HSE) as per the routine toxicity assay. The results showed a significant growth inhibition to M. aeruginosa in the LRE group, where the inhibition rate reached above 90% from day 6 to day 9. The cell-membrane damage ratio increased from 64.05% on day 5 up to 96.60% on day 9. PSII photosynthesis activity expressed as Fv/Fm, Φ , NPQ and ETRmax was also thoroughly inhibited in this group. Whereas the growth and PSII photosynthesis activity of M. aeruginosa in the HSE group were inhibited initially, but recovered gradually from day 4 or 5, which was accompanied by a continuous reduction of NPN content in culture solutions. Although NPN content in the LRE group was relatively lower, it remained at a more stable level throughout the experiment. These results indicate that continual release of low-dosage allelochemicals by aquatic plants plays crucial roles in their potent inhibition against cyanobacteria. Low-dosage continual exposure pattern needs to be investigated further.
[Mh] Termos MeSH primário: 1-Naftilamina/análogos & derivados
Poluentes Ambientais/toxicidade
Microcystis/efeitos dos fármacos
Feromônios/toxicidade
[Mh] Termos MeSH secundário: 1-Naftilamina/toxicidade
Relação Dose-Resposta a Droga
Microcystis/crescimento & desenvolvimento
Microcystis/metabolismo
Fotossíntese/efeitos dos fármacos
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Environmental Pollutants); 0 (Pheromones); 90-30-2 (N-phenyl-1-naphthylamine); 9753I242R5 (1-Naphthylamine)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170508
[Lr] Data última revisão:
170508
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170219
[St] Status:MEDLINE


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[PMID]:28027837
[Au] Autor:Bie Z; Lu W; Zhu Y; Chen Y; Ren H; Ji L
[Ad] Endereço:Quality Supervision & Test Center, China National Tobacco Corporation Shandong Branch, Jinan 250098, China.
[Ti] Título:Rapid determination of six carcinogenic primary aromatic amines in mainstream cigarette smoke by two-dimensional online solid phase extraction combined with liquid chromatography tandem mass spectrometry.
[So] Source:J Chromatogr A;1482:39-47, 2017 Jan 27.
[Is] ISSN:1873-3778
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A fully automated, rapid, and reliable method for simultaneous determination of six carcinogenic primary aromatic amines (AAs), including o-toluidine (o-TOL), 2, 6-dimethylaniline (2, 6-DMA), o-anisidine (o-ASD), 1-naphthylamine (1-ANP), 2-naphthylamine (2-ANP), and 4-aminobiphenyl (4-ABP), in mainstream cigarette smoke was established. The proposed method was based on two-dimensional online solid phase extraction combined with liquid chromatography tandem mass spectrometry (SPE/LC-MS/MS). The particulate phase of the mainstream cigarette smoke was collected on a Cambridge filter pad and pretreated via ultrasonic extraction with 2% formic acid (FA), while the gas phase was trapped by 2% FA without pretreatment for determination. The two-dimensional online SPE comprised of two cartridges with different absorption characteristics was applied for sample pretreatment. Analysis was performed by liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) under multiple reaction monitoring mode. Each sample required about 0.5h for solid phase extraction and analysis. The limit of detections (LODs) for six AAs ranged from 0.04 to 0.58ng/cig and recoveries were within 84.5%-122.9%. The relative standard deviations of intra- and inter-day tests for 3R4F reference cigarette were less than 6% and 7%, respectively, while no more than 7% and 8% separately for a type of Virginia cigarette. The proposed method enabled minimum sample pretreatment, full automation, and high throughput with high selectivity, sensitivity, and accuracy. As a part of the validation procedure, fifteen brands of cigarettes were tested by the designed method.
[Mh] Termos MeSH primário: Carcinógenos/análise
Fumaça/análise
Extração em Fase Sólida/métodos
Espectrometria de Massas em Tandem/métodos
Tabaco/química
[Mh] Termos MeSH secundário: 1-Naftilamina/análise
Compostos de Aminobifenil/análise
Compostos de Anilina/análise
Cromatografia Líquida
Limite de Detecção
Produtos do Tabaco/classificação
Toluidinas/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aminobiphenyl Compounds); 0 (Aniline Compounds); 0 (Carcinogens); 0 (Smoke); 0 (Toluidines); 16054949HJ (4-biphenylamine); 4FT62OX08D (2,6-xylidine); 9753I242R5 (1-Naphthylamine); B635MZ0ZLU (2-toluidine); NUX042F201 (2-anisidine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161229
[St] Status:MEDLINE


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[PMID]:27712995
[Au] Autor:Komirishetty P; Areti A; Gogoi R; Sistla R; Kumar A
[Ad] Endereço:Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER)-Hyderabad, Balanagar, India; Division of Neurology, Department of Medicine, University of Alberta, 2E3.26 Walter C Mackenzie, Health Sciences Center, Edmonton, AB, T6G 2B7, Canada.
[Ti] Título:Combination strategy of PARP inhibitor with antioxidant prevent bioenergetic deficits and inflammatory changes in CCI-induced neuropathy.
[So] Source:Neuropharmacology;113(Pt A):137-147, 2017 Feb.
[Is] ISSN:1873-7064
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Neuropathic pain, a debilitating pain condition and the underlying pathogenic mechanisms are complex and interwoven amongst each other and still there is scant information available regarding therapies which promise to treat the condition. Evidence indicate that oxidative/nitrosative stress induced poly (ADP-ribose) polymerase (PARP) overactivation initiate neuroinflammation and bioenergetic crisis culminating into neurodegenerative changes following nerve injury. Hence, we investigated the therapeutic effect of combining an antioxidant, quercetin and a PARP inhibitor, 4-amino 1, 8-naphthalimide (4-ANI) on the hallmark deficits induced by chronic constriction injury (CCI) of sciatic nerve in rats. Quercetin (25 mg/kg, p.o.) and 4-ANI (3 mg/kg, p.o.) were administered either alone or in combination for 14 days to examine sciatic functional index, allodynia and hyperalgesia using walking track analysis, Von Frey, acetone spray and hot plate tests respectively. Malondialdehyde, nitrite and glutathione levels were estimated to detect oxidative/nitrosative stress; mitochondrial membrane potential and cytochrome c oxidase activity to assess mitochondrial function; NAD & ATP levels to examine the bioenergetic status and levels of inflammatory markers were evaluated in ipsilateral sciatic nerve. Quercetin and 4-ANI alone improved the pain behaviour and biochemical alterations but the combination therapy demonstrated an appreciable reversal of CCI-induced changes. Nitrotyrosine and Poly ADP-Ribose (PAR) immunopositivity was decreased and nuclear factor erythroid 2-related factor (Nrf-2) levels were increased significantly in micro-sections of the sciatic nerve and dorsal root ganglion (DRG) of treatment group. These results suggest that simultaneous inhibition of oxidative stress-PARP activation cascade may potentially be useful strategies for management of trauma induced neuropathic pain.
[Mh] Termos MeSH primário: 1-Naftilamina/análogos & derivados
Antioxidantes/administração & dosagem
Encefalite/prevenção & controle
Naftalimidas/administração & dosagem
Neuralgia/prevenção & controle
Inibidores de Poli(ADP-Ribose) Polimerases/administração & dosagem
Poli(ADP-Ribose) Polimerases/metabolismo
Quercetina/administração & dosagem
Quinolonas/administração & dosagem
[Mh] Termos MeSH secundário: 1-Naftilamina/administração & dosagem
1-Naftilamina/uso terapêutico
Trifosfato de Adenosina/metabolismo
Animais
Antioxidantes/uso terapêutico
Encefalite/complicações
Encefalite/enzimologia
Hiperalgesia/prevenção & controle
Masculino
Mitocôndrias/efeitos dos fármacos
Mitocôndrias/metabolismo
NAD/metabolismo
Naftalimidas/uso terapêutico
Neuralgia/complicações
Neuralgia/enzimologia
Estresse Oxidativo/efeitos dos fármacos
Inibidores de Poli(ADP-Ribose) Polimerases/uso terapêutico
Quercetina/uso terapêutico
Quinolonas/uso terapêutico
Ratos
Ratos Sprague-Dawley
Nervo Isquiático/lesões
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Naphthalimides); 0 (Poly(ADP-ribose) Polymerase Inhibitors); 0 (Quinolones); 0U46U6E8UK (NAD); 1742-95-6 (4-amino-1,8-naphthalimide); 8L70Q75FXE (Adenosine Triphosphate); 9753I242R5 (1-Naphthylamine); 9IKM0I5T1E (Quercetin); EC 2.4.2.30 (Poly(ADP-ribose) Polymerases)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170902
[Lr] Data última revisão:
170902
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161105
[St] Status:MEDLINE


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[PMID]:27839920
[Au] Autor:Yasuda D; Nakajima M; Yuasa A; Obata R; Takahashi K; Ohe T; Ichimura Y; Komatsu M; Yamamoto M; Imamura R; Kojima H; Okabe T; Nagano T; Mashino T
[Ad] Endereço:Department of Pharmaceutical Sciences, Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato-ku, Tokyo, Japan.
[Ti] Título:Synthesis of Keap1-phosphorylated p62 and Keap1-Nrf2 protein-protein interaction inhibitors and their inhibitory activity.
[So] Source:Bioorg Med Chem Lett;26(24):5956-5959, 2016 12 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The Keap1-Nrf2 system is involved not only in biological defense but also in malignancy progression and chemoresistance. The ubiquitin-binding protein p62/Sqstm1 (p62), which is highly expressed in several cancers, competes with Nrf2 for Keap1 binding, leading to activation of Nrf2-mediated gene expression and survival of cancer cells. We had previously identified an inhibitor for the Keap1-phosphorylated-p62 (p-p62) protein-protein interaction (PPI), the acetonyl naphthalene derivative K67. In this study, we established facile synthetic routes for K67 and derivatives with various side chains on the C-2 position of naphthalene ring. K67 possessed high selectivity in the inhibition of Keap1-p-p62. Other derivatives showed potent Keap1-Nrf2 and Keap1-p-p62 PPI inhibitory activities, though the selectivity between the two activities was lower than K67.
[Mh] Termos MeSH primário: 1-Naftilamina/análogos & derivados
Proteína 1 Associada a ECH Semelhante a Kelch/antagonistas & inibidores
Fator 2 Relacionado a NF-E2/antagonistas & inibidores
Naftalenos/farmacologia
Proteínas de Ligação a RNA/antagonistas & inibidores
Sulfonamidas/farmacologia
Proteínas Ativadoras de ras GTPase/antagonistas & inibidores
[Mh] Termos MeSH secundário: 1-Naftilamina/síntese química
1-Naftilamina/química
1-Naftilamina/farmacologia
Relação Dose-Resposta a Droga
Seres Humanos
Proteína 1 Associada a ECH Semelhante a Kelch/química
Estrutura Molecular
Fator 2 Relacionado a NF-E2/química
Naftalenos/química
Ligação Proteica/efeitos dos fármacos
Proteínas de Ligação a RNA/química
Relação Estrutura-Atividade
Sulfonamidas/síntese química
Sulfonamidas/química
Proteínas Ativadoras de ras GTPase/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (2-acetonyl-1,4-bis((4-etoxybenzensulfonyl)amino)naphthalene); 0 (KEAP1 protein, human); 0 (Kelch-Like ECH-Associated Protein 1); 0 (NF-E2-Related Factor 2); 0 (Naphthalenes); 0 (P62 protein, human); 0 (RNA-Binding Proteins); 0 (Sulfonamides); 0 (ras GTPase-Activating Proteins); 2166IN72UN (naphthalene); 9753I242R5 (1-Naphthylamine)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161115
[St] Status:MEDLINE


  9 / 1005 MEDLINE  
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[PMID]:27801837
[Au] Autor:Zhang X; Jiang A; Yu H; Xiong Y; Zhou G; Qin M; Dou J; Wang J
[Ad] Endereço:The Department of Pharmacy, Food and Drug School, Anhui Science and Technology University, Fengyang 233100, China. zhangxiaolin8@126.com.
[Ti] Título:Human Lysozyme Synergistically Enhances Bactericidal Dynamics and Lowers the Resistant Mutant Prevention Concentration for Metronidazole to Helicobacter pylori by Increasing Cell Permeability.
[So] Source:Molecules;21(11), 2016 Oct 28.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Metronidazole (MNZ) is an effective agent that has been employed to eradicate ( ). The emergence of broad MNZ resistance in has affected the efficacy of this therapeutic agent. The concentration of MNZ, especially the mutant prevention concentration (MPC), plays an important role in selecting or enriching resistant mutants and regulating therapeutic effects. A strategy to reduce the MPC that can not only effectively treat but also prevent resistance mutations is needed. is highly resistant to lysozyme. Lysozyme possesses a hydrolytic bacterial cell wall peptidoglycan and a cationic dependent mode. These effects can increase the permeability of bacterial cells and promote antibiotic absorption into bacterial cells. In this study, human lysozyme (hLYS) was used to probe its effects on the integrity of the outer and inner membranes using as fluorescent probe hydrophobic 1- -phenyl-naphthylamine (NPN) and the release of aspartate aminotransferase. Further studies using a propidium iodide staining method assessed whether hLYS could increase cell permeability and promote cell absorption. Finally, we determined the effects of hLYS on the bactericidal dynamics and MPC of MNZ in . Our findings indicate that hLYS could dramatically increase cell permeability, reduce the MPC of MNZ for , and enhance its bactericidal dynamic activity, demonstrating that hLYS could reduce the probability of MNZ inducing resistance mutations.
[Mh] Termos MeSH primário: Parede Celular/efeitos dos fármacos
Farmacorresistência Bacteriana/efeitos dos fármacos
Helicobacter pylori/efeitos dos fármacos
Metronidazol/farmacologia
Muramidase/farmacologia
[Mh] Termos MeSH secundário: 1-Naftilamina/análogos & derivados
1-Naftilamina/metabolismo
Aspartato Aminotransferases
Sinergismo Farmacológico
Helicobacter pylori/genética
Seres Humanos
Testes de Sensibilidade Microbiana
Viabilidade Microbiana/efeitos dos fármacos
Mutação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
140QMO216E (Metronidazole); 90-30-2 (N-phenyl-1-naphthylamine); 9753I242R5 (1-Naphthylamine); EC 2.6.1.1 (Aspartate Aminotransferases); EC 3.2.1.17 (Muramidase); EC 3.2.1.17 (lysozyme C, human)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170417
[Lr] Data última revisão:
170417
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161102
[St] Status:MEDLINE


  10 / 1005 MEDLINE  
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[PMID]:27643437
[Au] Autor:Jin Y; Zhou J; Xu F; Jin B; Cui L; Wang Y; Du X; Li J; Li P; Ren R; Pan J
[Ti] Título:Targeting methyltransferase PRMT5 eliminates leukemia stem cells in chronic myelogenous leukemia.
[So] Source:J Clin Invest;126(10):3961-3980, 2016 Oct 03.
[Is] ISSN:1558-8238
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Imatinib-insensitive leukemia stem cells (LSCs) are believed to be responsible for resistance to BCR-ABL tyrosine kinase inhibitors and relapse of chronic myelogenous leukemia (CML). Identifying therapeutic targets to eradicate CML LSCs may be a strategy to cure CML. In the present study, we discovered a positive feedback loop between BCR-ABL and protein arginine methyltransferase 5 (PRMT5) in CML cells. Overexpression of PRMT5 was observed in human CML LSCs. Silencing PRMT5 with shRNA or blocking PRMT5 methyltransferase activity with the small-molecule inhibitor PJ-68 reduced survival, serial replating capacity, and long-term culture-initiating cells (LTC-ICs) in LSCs from CML patients. Further, PRMT5 knockdown or PJ-68 treatment dramatically prolonged survival in a murine model of retroviral BCR-ABL-driven CML and impaired the in vivo self-renewal capacity of transplanted CML LSCs. PJ-68 also inhibited long-term engraftment of human CML CD34+ cells in immunodeficient mice. Moreover, inhibition of PRMT5 abrogated the Wnt/ß-catenin pathway in CML CD34+ cells by depleting dishevelled homolog 3 (DVL3). This study suggests that epigenetic methylation modification on histone protein arginine residues is a regulatory mechanism to control self-renewal of LSCs and indicates that PRMT5 may represent a potential therapeutic target against LSCs.
[Mh] Termos MeSH primário: 1-Naftilamina/análogos & derivados
Antineoplásicos/farmacologia
Carbazóis/farmacologia
Leucemia Mielogênica Crônica BCR-ABL Positiva/tratamento farmacológico
Células-Tronco Neoplásicas/efeitos dos fármacos
Proteína-Arginina N-Metiltransferases/genética
[Mh] Termos MeSH secundário: 1-Naftilamina/farmacologia
Aminoquinolinas/farmacologia
Animais
Linhagem Celular Tumoral
Proliferação Celular
Sobrevivência Celular
Indução Enzimática
Feminino
Proteínas de Fusão bcr-abl/metabolismo
Expressão Gênica
Regulação Neoplásica da Expressão Gênica
Técnicas de Silenciamento de Genes
Células HEK293
Seres Humanos
Mesilato de Imatinib/farmacologia
Leucemia Mielogênica Crônica BCR-ABL Positiva/enzimologia
Leucemia Mielogênica Crônica BCR-ABL Positiva/patologia
Camundongos Endogâmicos C57BL
Camundongos Endogâmicos NOD
Camundongos SCID
Terapia de Alvo Molecular
Células-Tronco Neoplásicas/enzimologia
Proteína-Arginina N-Metiltransferases/antagonistas & inibidores
Proteína-Arginina N-Metiltransferases/metabolismo
Pirimidinas/farmacologia
RNA Interferente Pequeno/genética
Fator de Transcrição STAT5/metabolismo
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Aminoquinolines); 0 (Antineoplastic Agents); 0 (Carbazoles); 0 (PJ-68 compound); 0 (Pyrimidines); 0 (RNA, Small Interfering); 0 (SGI-1027); 0 (STAT5 Transcription Factor); 8A1O1M485B (Imatinib Mesylate); 9753I242R5 (1-Naphthylamine); EC 2.1.1.319 (PRMT5 protein, human); EC 2.1.1.319 (Protein-Arginine N-Methyltransferases); EC 2.7.10.2 (Fusion Proteins, bcr-abl)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170911
[Lr] Data última revisão:
170911
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:160920
[St] Status:MEDLINE



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