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  1 / 1329 MEDLINE  
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[PMID]:29195145
[Au] Autor:Sundberg J; Wibrand F; Lund AM; Christensen M
[Ad] Endereço:Department of Clinical Genetics, Rigshospitalet, Copenhagen University Hospital, Blegdamsvej 9, 2100 Copenhagen, Denmark.
[Ti] Título:Simultaneous quantification of succinylacetone and nitisinone for therapeutic drug monitoring in the treatment of Tyrosinemia type 1.
[So] Source:J Chromatogr B Analyt Technol Biomed Life Sci;1072:259-266, 2018 Jan 01.
[Is] ISSN:1873-376X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:We present a straightforward and robust method for simultaneous quantification of succinylacetone and nitisinone in plasma using LC-ESI-MS/MS. The method has been developed for routine therapeutic drug monitoring in hepatorenal tyrosinemia type 1 (HT1) patients undergoing nitisinone treatment. Previous methods are based on separate analyses of succinylacetone and nitisinone, often using the potentially harmful compound hydrazine for derivatization of the former. In the present procedure, succinylacetone is derivatized in a single-step using butanolic HCl. Analyte extraction and sample clean-up is carried out by simple protein precipitation. The linear range for both analytes is 0.1 up to 125µM, covering the vast majority of encountered levels in real-life samples. The sensitivity and limit of quantification allows measurement of succinylacetone in the therapeutical range for HT1 patients. Stability studies show that succinylacetone is highly sensitive to storage conditions, whereas nitisinone shows little to no degradation. Correct sample handling is therefore important for reliable results when monitoring succinylacetone concentrations.
[Mh] Termos MeSH primário: Cicloexanonas/sangue
Monitoramento de Medicamentos/métodos
Heptanoatos/sangue
Nitrobenzoatos/sangue
Tirosinemias/tratamento farmacológico
[Mh] Termos MeSH secundário: Cromatografia Líquida/métodos
Cicloexanonas/uso terapêutico
Seres Humanos
Modelos Lineares
Nitrobenzoatos/uso terapêutico
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclohexanones); 0 (Heptanoates); 0 (Nitrobenzoates); 51568-18-4 (succinylacetone); K5BN214699 (nitisinone)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180221
[Lr] Data última revisão:
180221
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171202
[St] Status:MEDLINE


  2 / 1329 MEDLINE  
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[PMID]:29214974
[Au] Autor:Cavalcante CSP; de Aguiar FLL; Fontenelle ROS; de Menezes RRPPB; Martins AMC; Falcão CB; Andreu D; Rádis-Baptista G
[Ad] Endereço:1​Post-graduate Program in Pharmaceutical Sciences, Federal University of Ceará, 60740-000, Fortaleza, CE, Brazil.
[Ti] Título:Insights into the candidacidal mechanism of Ctn[15-34] - a carboxyl-terminal, crotalicidin-derived peptide related to cathelicidins.
[So] Source:J Med Microbiol;67(1):129-138, 2018 Jan.
[Is] ISSN:1473-5644
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Ctn[15-34], a carboxyl-terminal fragment of crotalicidin (a cathelicidin from the venom gland of a South American rattlesnake), has shown antifungal activity against clinical and standard strains of Candida species. The aim of the present work was to investigate the underlying mechanisms of the candidicidal activity of Ctn[15-34]. METHODOLOGY: The time-kill profile and drug synergism were evaluated by means of a microdilution assay and multi-parametric flow cytometry. The presumptive interaction of Ctn[15-34] with lipid membranes was estimated in vitro with a lipid-mimic compound, the chromogenic substance 4-nitro-3-(octanoyloxy)benzoic acid (4N3OBA).Results/Key findings. The absorbance increment (at 425 nm) indicated a concentration- and time-dependent in-solution association between Ctn[15-34] and 4N3OBA. The interaction of Ctn[15-34] with Candida cells was confirmed by flow cytometric measurements with the 5(6)-carboxyfluorescein-labelled peptide (CF-Ctn[15-34]). Analysis of the killing time of Candida exposed to Ctn[15-34] and amphotericin B (AMB) showed that both the peptide and polyene drug reduce the number of c.f.u. but in mechanistically different ways. The Ctn[15-34] peptide alone caused yeast cell membrane disruption, which was confirmed by lactate dehydrogenase leakage and biomarkers of cell death mediated by necrosis. CONCLUSION: Overall, Ctn[15-34] displays a synergistic antifungal activity with AMB, an effect that can be further developed into a multi-target therapeutic option with other antimycotics currently in use.
[Mh] Termos MeSH primário: Antifúngicos/farmacologia
Candida/efeitos dos fármacos
Catelicidinas/farmacologia
Fragmentos de Peptídeos/farmacologia
Peptídeos/farmacologia
[Mh] Termos MeSH secundário: Anfotericina B/farmacologia
Candidíase/tratamento farmacológico
Sinergismo Farmacológico
Fluoresceínas/farmacologia
Seres Humanos
Testes de Sensibilidade Microbiana/métodos
Nitrobenzoatos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-nitro-3-(octanoyloxy)benzoic acid); 0 (Antifungal Agents); 0 (Cathelicidins); 0 (Fluoresceins); 0 (Nitrobenzoates); 0 (Peptide Fragments); 0 (Peptides); 0 (crotalicidin); 3301-79-9 (6-carboxyfluorescein); 7XU7A7DROE (Amphotericin B)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171227
[Lr] Data última revisão:
171227
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171208
[St] Status:MEDLINE
[do] DOI:10.1099/jmm.0.000652


  3 / 1329 MEDLINE  
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[PMID]:28966278
[Au] Autor:Yamano Y; Sasaki H; Wada A
[Ad] Endereço:Department of Organic Chemistry for Life Science, Kobe Pharmaceutical University.
[Ti] Título:Versatile Amine-Promoted Mild Methanolysis of 3,5-Dinitrobenzoates and Its Application to the Synthesis of Colorado Potato Beetle Pheromone.
[So] Source:Chem Pharm Bull (Tokyo);65(10):940-944, 2017.
[Is] ISSN:1347-5223
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:A mild deacylation method for 3,5-dinitrobenzoates using methanolic solutions of amines, such as dialkylamines, was developed. The method's versatility was confirmed by applying it to synthesizing a key intermediate for Colorado potato beetle pheromone.
[Mh] Termos MeSH primário: Aminas/química
Coleópteros/química
Nitrobenzoatos/química
Feromônios/química
[Mh] Termos MeSH secundário: Animais
Coleópteros/metabolismo
Colorado
Metanol/química
Nitrobenzoatos/síntese química
Feromônios/síntese química
Solanum tuberosum/parasitologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Nitrobenzoates); 0 (Pheromones); 4V3F9Q018P (3,5-dinitrobenzoic acid); Y4S76JWI15 (Methanol)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171003
[St] Status:MEDLINE
[do] DOI:10.1248/cpb.c17-00462


  4 / 1329 MEDLINE  
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[PMID]:28368593
[Au] Autor:Gau J; Prévost M; Van Antwerpen P; Sarosi MB; Rodewald S; Arnhold J; Flemmig J
[Ad] Endereço:Institute for Medical Physics and Biophysics, Medical Faculty, University of Leipzig , Härtelstraße 16-18, 04107 Leipzig, Germany.
[Ti] Título:Tannins and Tannin-Related Derivatives Enhance the (Pseudo-)Halogenating Activity of Lactoperoxidase.
[So] Source:J Nat Prod;80(5):1328-1338, 2017 May 26.
[Is] ISSN:1520-6025
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Several hydrolyzable tannins, proanthocyanidins, tannin derivatives, and a tannin-rich plant extract of tormentil rhizome were tested for their potential to regenerate the (pseudo-)halogenating activity, i.e., the oxidation of SCN to hypothiocyanite OSCN, of lactoperoxidase (LPO) after hydrogen peroxide-mediated enzyme inactivation. Measurements were performed using 5-thio-2-nitrobenzoic acid in the presence of tannins and related substances in order to determine kinetic parameters and to trace the LPO-mediated OSCN formation. The results were combined with docking studies and molecular orbital analysis. The OSCN-regenerating effect of tannin derivatives relates well with their binding properties toward LPO as well as their occupied molecular orbitals. Especially simple compounds like ellagic acid or methyl gallate and the complex plant extract were found as potent enzyme-regenerating compounds. As the (pseudo-)halogenating activity of LPO contributes to the maintenance of oral bacterial homeostasis, the results provide new insights into the antibacterial mode of action of tannins and related compounds. Furthermore, chemical properties of the tested compounds that are important for efficient enzyme-substrate interaction and regeneration of the OSCN formation by LPO were identified.
[Mh] Termos MeSH primário: Peróxido de Hidrogênio/metabolismo
Taninos Hidrolisáveis/isolamento & purificação
Lactoperoxidase/metabolismo
Nitrobenzoatos/isolamento & purificação
Extratos Vegetais/isolamento & purificação
Proantocianidinas/isolamento & purificação
Rizoma/metabolismo
Compostos de Sulfidrila/isolamento & purificação
Taninos/isolamento & purificação
Tiocianatos/isolamento & purificação
[Mh] Termos MeSH secundário: Halogenação
Peróxido de Hidrogênio/química
Taninos Hidrolisáveis/química
Cinética
Lactoperoxidase/química
Estrutura Molecular
Nitrobenzoatos/química
Oxirredução
Extratos Vegetais/química
Proantocianidinas/química
Compostos de Sulfidrila/química
Taninos/química
Tiocianatos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hydrolyzable Tannins); 0 (Nitrobenzoates); 0 (Plant Extracts); 0 (Proanthocyanidins); 0 (Sulfhydryl Compounds); 0 (Tannins); 0 (Thiocyanates); 15139-21-6 (thionitrobenzoic acid); 63296-34-4 (hypothiocyanite ion); BBX060AN9V (Hydrogen Peroxide); EC 1.11.1.- (Lactoperoxidase)
[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:170404
[St] Status:MEDLINE
[do] DOI:10.1021/acs.jnatprod.6b00915


  5 / 1329 MEDLINE  
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[PMID]:28081634
[Au] Autor:Milan AM; Hughes AT; Davison AS; Devine J; Usher J; Curtis S; Khedr M; Gallagher JA; Ranganath LR
[Ad] Endereço:1 Department of Clinical Biochemistry and Metabolic Medicine, Liverpool Clinical Laboratories, Royal Liverpool University Hospitals Trust, Liverpool, UK.
[Ti] Título:The effect of nitisinone on homogentisic acid and tyrosine: a two-year survey of patients attending the National Alkaptonuria Centre, Liverpool.
[So] Source:Ann Clin Biochem;54(3):323-330, 2017 May.
[Is] ISSN:1758-1001
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Background Alkaptonuria is a rare, debilitating autosomal recessive disorder affecting tyrosine metabolism. Deficiency of homogentisate 1,2-dioxygenase leads to increased homogentisic acid which is deposited as ochronotic pigment. Clinical sequelae include severe early onset osteoarthritis, increased renal and prostate stone formation and cardiac complications. Treatment has been largely based on analgaesia and arthroplasty. The National Alkaptonuria Centre in Liverpool has been using 2 mg nitisinone (NTBC) off-license for all patients in the United Kingdom with alkaptonuria and monitoring the tyrosine metabolite profiles. Methods Patients with confirmed alkaptonuria are commenced on 2 mg dose (alternative days) of NTBC for three months with daily dose thereafter. Metabolite measurement by LC-MS/MS is performed at baseline, day 4, three-months, six-months and one-year post-commencing NTBC. Thereafter, monitoring and clinical assessments are performed annually. Results Urine homogentisic acid concentration decreased from a mean baseline 20,557 µmol/24 h (95th percentile confidence interval 18,446-22,669 µmol/24 h) by on average 95.4% by six months, 94.8% at one year and 94.1% at two year monitoring. A concurrent reduction in serum homogentisic acid concentration of 83.2% compared to baseline was also measured. Serum tyrosine increased from normal adult reference interval to a mean ± SD of 594 ± 184 µmol /L at year-two monitoring with an increased urinary excretion from 103 ± 81 µmol /24 h at baseline to 1071 ± 726 µmol /24 h two years from therapy. Conclusions The data presented represent the first longitudinal survey of NTBC use in an NHS service setting and demonstrate the sustained effect of NTBC on the tyrosine metabolite profile.
[Mh] Termos MeSH primário: Alcaptonúria/tratamento farmacológico
Cicloexanonas/uso terapêutico
Inibidores Enzimáticos/uso terapêutico
Ácido Homogentísico
Nitrobenzoatos/uso terapêutico
Tirosina
[Mh] Termos MeSH secundário: Adulto
Idoso
Alcaptonúria/sangue
Alcaptonúria/patologia
Alcaptonúria/urina
Cromatografia Líquida
Esquema de Medicação
Feminino
Homogentisato 1,2-Dioxigenase/deficiência
Ácido Homogentísico/sangue
Ácido Homogentísico/urina
Seres Humanos
Estudos Longitudinais
Masculino
Meia-Idade
Monitorização Fisiológica
Espectrometria de Massas em Tandem
Tirosina/sangue
Tirosina/urina
Reino Unido
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclohexanones); 0 (Enzyme Inhibitors); 0 (Nitrobenzoates); 42HK56048U (Tyrosine); EC 1.13.11.5 (Homogentisate 1,2-Dioxygenase); K5BN214699 (nitisinone); NP8UE6VF08 (Homogentisic Acid)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170114
[St] Status:MEDLINE
[do] DOI:10.1177/0004563217691065


  6 / 1329 MEDLINE  
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[PMID]:28006662
[Au] Autor:Ouyang R; Yang Y; Tong X; Feng K; Yang Y; Tao H; Zhang X; Zong T; Cao P; Xiong F; Guo N; Li Y; Miao Y; Zhou S
[Ad] Endereço:University of Shanghai for Science and Technology, Shanghai 200093, China. Electronic address: ouyangrz@usst.edu.cn.
[Ti] Título:Potent anticancer activity of a new bismuth (III) complex against human lung cancer cells.
[So] Source:J Inorg Biochem;168:18-26, 2017 Mar.
[Is] ISSN:1873-3344
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The aim of this work is experimental study of an interesting bismuth(III) complex derived from pentadentate 2,6-pyridinedicarboxaldehyde bis( N-methylthiosemicarbazone), [BiL(NO ) ]NO {L=2,6-pyridinedicarboxaldehyde bis( N-methylthiosemicarbazone)}. A series of in vitro biological studies indicate that the newly prepared [BiL(NO ) ]NO greatly suppressed colony formation, migration and significantly induced apoptosis of human lung cancer cells A549 and H460, but did not obviously decrease the cell viability of non-cancerous human lung fibroblast (HLF) cell line, showing much higher anticancer activities than its parent ligands, especially with half maximum inhibitory concentration (IC ) <3.5µM. Moreover, in vivo study provides enough evidence that the treatment with [BiL(NO ) ]NO effectively inhibited A549 xenograft tumor growth on tumor-bearing mice (10mgkg , tumor volume reduced by 97.92% and tumor weight lightened by 94.44% compared to control) and did not indicate harmful effect on mouse weight and liver. These results suggest that the coordination of free ligand with Bi(III) might be an interesting and potent strategy in the discovery of new anticancer drug candidates.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Bismuto/farmacologia
[Mh] Termos MeSH secundário: Animais
Antineoplásicos/síntese química
Antineoplásicos/química
Apoptose/efeitos dos fármacos
Bismuto/química
Peso Corporal/efeitos dos fármacos
Carcinoma Pulmonar de Células não Pequenas/tratamento farmacológico
Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Seres Humanos
Concentração Inibidora 50
Fígado/efeitos dos fármacos
Neoplasias Pulmonares/tratamento farmacológico
Camundongos
Estrutura Molecular
Nitrobenzoatos/química
Compostos de Piridínio/química
Carga Tumoral/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Nitrobenzoates); 0 (Pyridinium Compounds); 0 (pyridinium 2,4-dinitrobenzoate); U015TT5I8H (Bismuth)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171113
[Lr] Data última revisão:
171113
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161223
[St] Status:MEDLINE


  7 / 1329 MEDLINE  
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[PMID]:27894959
[Au] Autor:Hall C; Ehrlich L; Venter J; O'Brien A; White T; Zhou T; Dang T; Meng F; Invernizzi P; Bernuzzi F; Alpini G; Lairmore TC; Glaser S
[Ad] Endereço:Scott & White Medical Center, Department of Surgery, Temple, TX 76508, USA.
[Ti] Título:Inhibition of the apelin/apelin receptor axis decreases cholangiocarcinoma growth.
[So] Source:Cancer Lett;386:179-188, 2017 02 01.
[Is] ISSN:1872-7980
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Cholangiocarcinoma (CCA) is a malignancy of the biliary epithelium that is associated with low five-year survival. The apelin receptor (APLNR), which is activated by the apelin peptide, has not been studied in CCA. The purpose of this study is to determine if inhibition of the apelin/APLNR axis can inhibit CCA growth. METHODS: Immunohistochemistry, rtPCR, immunofluorescence, flow cytometry, and ELISA was used to measure APLNR expression in human CCA cells and tissues. Mz-ChA-1 cells were treated with increasing concentrations of apelin and ML221, an APLNR antagonist. Expression of proliferative and angiogenic genes were measured via rtPCR. In vivo, Mz-ChA-1 cells were injected into the flanks of nu/nu mice, which were treated with ML221 (150 µg/kg) via tail vein injection. RESULTS: Expression of the apelin/APLNR axis was increased in CCA. In vitro, CCA proliferation and angiogenesis was inhibited by ML221 treatment. ML221 treatment significantly decreased tumor growth in nu/nu mice. CONCLUSION: The apelin/APLNR axis regulates CCA proliferation and angiogenesis. Inhibition of the apelin/APLNR axis decreases tumor growth in our xenograft model. Targeting APLNR signaling has the potential to serve as a novel, tumor directed therapy for CCA.
[Mh] Termos MeSH primário: Inibidores da Angiogênese/farmacologia
Neoplasias dos Ductos Biliares/tratamento farmacológico
Proliferação Celular/efeitos dos fármacos
Colangiocarcinoma/tratamento farmacológico
Peptídeos e Proteínas de Sinalização Intercelular/metabolismo
Neovascularização Patológica
Nitrobenzoatos/farmacologia
Piranos/farmacologia
Receptores Acoplados a Proteínas-G/antagonistas & inibidores
[Mh] Termos MeSH secundário: Adulto
Idoso de 80 Anos ou mais
Animais
Apelina
Receptores de Apelina
Neoplasias dos Ductos Biliares/genética
Neoplasias dos Ductos Biliares/metabolismo
Neoplasias dos Ductos Biliares/patologia
Linhagem Celular Tumoral
Movimento Celular/efeitos dos fármacos
Colangiocarcinoma/genética
Colangiocarcinoma/metabolismo
Colangiocarcinoma/patologia
Feminino
Seres Humanos
Peptídeos e Proteínas de Sinalização Intercelular/genética
Masculino
Camundongos Endogâmicos BALB C
Camundongos Nus
Meia-Idade
Invasividade Neoplásica
Receptores Acoplados a Proteínas-G/genética
Receptores Acoplados a Proteínas-G/metabolismo
Transdução de Sinais/efeitos dos fármacos
Carga Tumoral/efeitos dos fármacos
Ensaios Antitumorais Modelo de Xenoenxerto
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate); 0 (APLN protein, human); 0 (APLNR protein, human); 0 (Angiogenesis Inhibitors); 0 (Apelin); 0 (Apelin Receptors); 0 (Intercellular Signaling Peptides and Proteins); 0 (Nitrobenzoates); 0 (Pyrans); 0 (Receptors, G-Protein-Coupled)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161130
[St] Status:MEDLINE


  8 / 1329 MEDLINE  
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[PMID]:27871626
[Au] Autor:Luning Prak DJ; Breuer JE; Rios EA; Jedlicka EE; O'Sullivan DW
[Ad] Endereço:Chemistry Department, U.S. Naval Academy, 572 M Holloway Road, Annapolis, MD 21402, United States. Electronic address: prak@usna.edu.
[Ti] Título:Photolysis of 2,4,6-trinitrotoluene in seawater and estuary water: Impact of pH, temperature, salinity, and dissolved organic matter.
[So] Source:Mar Pollut Bull;114(2):977-986, 2017 Jan 30.
[Is] ISSN:1879-3363
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The influence of salinity, pH, temperature, and dissolved organic matter on the photolysis rate of 2,4,6-trinitrotoluene (TNT) in marine, estuary, and laboratory-prepared waters was studied using a Suntest CPS+® solar simulator equipped with optical filters. TNT degradation rates were determined using HPLC analysis, and products were identified using LC/MS. Minimal or no TNT photolysis occurred under a 395-nm long pass filter, but under a 295-nm filter, first-order TNT degradation rate constants and apparent quantum yields increased with increasing salinity in both natural and artificial seawater. TNT rate constants increased slightly with increasing temperature (10 to 32°C) but did not change significantly with pH (6.4 to 8.1). The addition of dissolved organic matter (up to 5mg/L) to ultrapure water, artificial seawater, and natural seawater increased the TNT photolysis rate constant. Products formed by TNT photolysis in natural seawater were determined to be 2,4,6-trinitrobenzaldehyde, 1,3,5-trinitrobenzene, 2,4,6-trinitrobenzoic acid, and 2-amino-4,6-dinitrobenzoic acid.
[Mh] Termos MeSH primário: Estuários
Fotólise
Água do Mar/química
Trinitrotolueno/química
Poluentes Químicos da Água/química
[Mh] Termos MeSH secundário: Substâncias Húmicas
Concentração de Íons de Hidrogênio
Nitrobenzoatos
Salinidade
Luz Solar
Temperatura Ambiente
Trinitrobenzenos
Trinitrotolueno/análise
Água
Poluentes Químicos da Água/análise
ortoaminobenzoatos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-amino-4,6-dinitrobenzoic acid); 0 (Humic Substances); 0 (Nitrobenzoates); 0 (Trinitrobenzenes); 0 (Water Pollutants, Chemical); 0 (ortho-Aminobenzoates); 059QF0KO0R (Water); 118-96-7 (Trinitrotoluene); 2H75703R1X (sym-trinitrobenzene)
[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:161123
[St] Status:MEDLINE


  9 / 1329 MEDLINE  
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[PMID]:27863748
[Au] Autor:Yeong KY; Liew WL; Murugaiyah V; Ang CW; Osman H; Tan SC
[Ad] Endereço:Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden, 11800 Penang, Malaysia; School of Science, Monash University Malaysia Campus, Jalan Lagoon Selatan, Bandar Sunway, 47500 Selangor, Malaysia. Electronic address: Yeong.KengYoon@monash.edu.
[Ti] Título:Ethyl nitrobenzoate: A novel scaffold for cholinesterase inhibition.
[So] Source:Bioorg Chem;70:27-33, 2017 Feb.
[Is] ISSN:1090-2120
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A series of novel cholinesterase inhibitors containing nitrobenzoate core structure were synthesized by a facile and efficient method. The structure of the novel compounds were fully characterized and confirmed by analytical as well as spectroscopic methods. Compound indicated as 2f was found to possess the best cholinesterase inhibitory activities of all the evaluated compounds. Results suggest that 2f is a selective acetylcholinesterase inhibitor, although it also inhibits butyrylcholinesterase at higher concentration. Kinetics inhibition result suggest that 2f is a mixed-mode inhibitor of acetylcholinesterase. In addition, it was found to have low cytotoxicity. Molecular docking on compound 2f was carried out to rationalize the observed in vitro enzymatic assay results. Most importantly, the potential of nitrobenzoate derivatives as cholinesterase inhibitor was shown through this study. In summary, we discovered nitrobenzoates as a new scaffold that may eventually yield useful compounds in treatment of Alzheimer's disease.
[Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo
Inibidores da Colinesterase/química
Inibidores da Colinesterase/farmacologia
Nitrobenzoatos/química
Nitrobenzoatos/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/química
Doença de Alzheimer/tratamento farmacológico
Doença de Alzheimer/enzimologia
Animais
Butirilcolinesterase/química
Butirilcolinesterase/metabolismo
Linhagem Celular
Electrophorus
Seres Humanos
Simulação de Acoplamento Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinesterase Inhibitors); 0 (Nitrobenzoates); EC 3.1.1.7 (Acetylcholinesterase); EC 3.1.1.8 (Butyrylcholinesterase)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161120
[St] Status:MEDLINE


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[PMID]:27305933
[Au] Autor:Ward JP; Dunster JL; Derks G; Mistry P; Salazar JD
[Ad] Endereço:Department of Mathematical Sciences, Loughborough University, Loughborough LE11 3TU, UK.
[Ti] Título:Predicting tyrosinaemia: a mathematical model of 4-hydroxyphenylpyruvate dioxygenase inhibition by nitisinone in rats.
[So] Source:Math Med Biol;34(3):335-390, 2017 Sep 01.
[Is] ISSN:1477-8602
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nitisinone or 2-(2-nitro-4-trifluoromethylbenzoyl)cyclohexane-1,3-dione is a reversible inhibitor of 4-hydroxyphenylpyruvate dioxygenase (HPPD), an enzyme important in tyrosine catabolism. Today, nitisinone is successfully used to treat Hereditary Tyrosinaemia type 1, although its original expected role was as a herbicide. In laboratory animals, treatment with nitisinone leads to the elevation of plasma tyrosine (tyrosinaemia). In rats and Beagle dogs, repeat low-dose exposure to nitisinone leads to corneal opacities whilst similar studies in the mouse and Rhesus monkey showed no comparable toxicities or other treatment related findings. The differences in toxicological sensitivities have been related to the upper limit of the concentration of tyrosine that accumulates in plasma, which is driven by the amount/activity of tyrosine aminotransferase. A physiologically based, pharmacodynamics ordinary differential equation model of HPPD inhibition to bolus exposure of nitisinone in vivo is presented. Going beyond traditional approaches, asymptotic analysis is used to separate the different timescales of events involved in HPPD inhibition and tyrosinaemia. This analysis elucidates, in terms of the model parameters, a critical inhibitor concentration (at which tyrosine concentration starts to rise) and highlights the contribution of in vitro measured parameters to events in an in vivo system. Furthermore, using parameter-fitting methods, a systematically derived reduced model is shown to fit well to rat data, making explicit how the parameters are informed by such data. This model in combination with in vitro descriptors has potential as a surrogate for animal experimentation to predict tyrosinaemia, and further development can extend its application to other related medical scenarios.
[Mh] Termos MeSH primário: 4-Hidroxifenilpiruvato Dioxigenase/antagonistas & inibidores
Cicloexanonas/efeitos adversos
Modelos Biológicos
Nitrobenzoatos/efeitos adversos
Tirosinemias/etiologia
[Mh] Termos MeSH secundário: 4-Hidroxifenilpiruvato Dioxigenase/metabolismo
Animais
Simulação por Computador
Cicloexanonas/administração & dosagem
Inibidores Enzimáticos/administração & dosagem
Inibidores Enzimáticos/efeitos adversos
Cinética
Fígado/efeitos dos fármacos
Fígado/metabolismo
Conceitos Matemáticos
Modelos Animais
Nitrobenzoatos/administração & dosagem
Ratos
Tirosina/metabolismo
Tirosinemias/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclohexanones); 0 (Enzyme Inhibitors); 0 (Nitrobenzoates); 42HK56048U (Tyrosine); EC 1.13.11.27 (4-Hydroxyphenylpyruvate Dioxygenase); K5BN214699 (nitisinone)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160617
[St] Status:MEDLINE
[do] DOI:10.1093/imammb/dqw006



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