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Pesquisa : D02.241.223.701.450 [Categoria DeCS]
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  1 / 137 MEDLINE  
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[PMID]:26951145
[Au] Autor:Ye X; Sun Y; Xu Y; Chen Z; Lu S
[Ti] Título:Integrated In Silico-In Vitro Discovery of Lung Cancer-related Tumor Pyruvate Kinase M2 (PKM2) Inhibitors.
[So] Source:Med Chem;12(7):613-620, 2016.
[Is] ISSN:1875-6638
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The tumor pyruvate kinase M2 (PKM2) is involved in the glycolytic pathway of lung cancer and targeting this kinase has been observed to radiosensitize non-small cell lung cancer (NSCLC). OBJECTIVE: An integration of in silico virtual screening and in vitro kinase assay was described to discover novel PKM2 inhibitors from a candidate library containing >400,000 commercially available compounds. METHOD: The method is a stepwise screening scheme that first used empirical strategies to fast exclude those undruggable compounds in the library and then employed molecular docking and molecular dynamics (MD)-based rescoring to identify few potential hits. Subsequently, the computational findings were substantiated using a standard kinase assay protocol. RESULTS: Four compounds, i.e. nalidixic acid, indoprofen, hematoxylin and polydatin, were identified to inhibit PKM2 kinase at micromolar level, with IC50 values of 53, 21, 340 and 128 .M, respectively. CONCLUSION: Structural analysis revealed that hydrogen bonds, salt bridges, π-π stacking and hydrophobic forces co-confer high stability and strong specificity to PKM2-inhibitor binding.
[Mh] Termos MeSH primário: Proteínas de Transporte/antagonistas & inibidores
Proteínas de Membrana/antagonistas & inibidores
Inibidores de Proteínas Quinases/química
Piruvato Quinase/antagonistas & inibidores
[Mh] Termos MeSH secundário: Proteínas de Transporte/química
Domínio Catalítico
Simulação por Computador
Descoberta de Drogas/métodos
Ensaios Enzimáticos
Glucosídeos/química
Hematoxilina/química
Seres Humanos
Indoprofen/química
Neoplasias Pulmonares
Proteínas de Membrana/química
Simulação de Acoplamento Molecular
Simulação de Dinâmica Molecular
Ácido Nalidíxico/química
Piruvato Quinase/química
Estilbenos/química
Hormônios Tireóideos/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Carrier Proteins); 0 (Glucosides); 0 (Membrane Proteins); 0 (Protein Kinase Inhibitors); 0 (Stilbenes); 0 (Thyroid Hormones); 0 (thyroid hormone-binding proteins); 3B91HWA56M (Nalidixic Acid); CPE46ZU14N (Indoprofen); EC 2.7.1.40 (Pyruvate Kinase); XM261C37CQ (polydatin); YKM8PY2Z55 (Hematoxylin)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170704
[Lr] Data última revisão:
170704
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160309
[St] Status:MEDLINE


  2 / 137 MEDLINE  
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[PMID]:19370733
[Au] Autor:Rocco A; Fanali S
[Ad] Endereço:Institute of Chemical Methodologies, Consiglio Nazionale delle Ricerche, Area della Ricerca di Roma I, Monterotondo Scalo, Rome, Italy.
[Ti] Título:Enantiomeric separation of acidic compounds by nano-liquid chromatography with methylated-beta-cyclodextrin as a mobile phase additive.
[So] Source:J Sep Sci;32(10):1696-703, 2009 May.
[Is] ISSN:1615-9314
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Some racemic nonsteroidal anti-inflammatory drugs, namely naproxen, indoprofen, ketoprofen, flurbiprofen, carprofen, cicloprofen, flunoxaprofen and suprofen were separated into their enantiomers by nano-LC. Chiral recognition was achieved adding to the mobile phase heptakis (2,3,6-tri-O-methyl)-beta-cyclodextrin (TM-beta-CD). Capillary columns of 100 microm id, packed with different RP particles were used for experiments. Effect of experimental parameters such as mobile phase composition, stationary phase type and length of packed capillary column on retention factor and chiral resolution of analytes were studied. The stationary phase type played a very important role in the enantiorecognition process. Best results in terms of highest enantioresolution factor and largest number of separated enantiomers were obtained reducing the particles size to 3 microm with RP(18) stationary phase. Most favourable mobile phase for enantiodiscrimination was obtained using relatively low concentrations of ACN (30%, v/v), 30 mM of TM-beta-CD and pH value of 3.0. The retention time of all studied enantiomers decreased by increasing the CD derivative concentration. The retention factors of selected studied compounds, specifically flurbiprofen, naproxen and suprofen, were measured employing TM-beta-CD concentrations in the range 0-40 mM. Assuming a 1:1 enantiomer/CD ratio, the apparent association constants of the studied enantiomers were calculated.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/química
Anti-Inflamatórios não Esteroides/isolamento & purificação
Cromatografia Líquida/métodos
Nanotecnologia/métodos
beta-Ciclodextrinas/química
[Mh] Termos MeSH secundário: Benzoxazóis/química
Benzoxazóis/isolamento & purificação
Carbazóis/química
Carbazóis/isolamento & purificação
Cromatografia Líquida/instrumentação
Flurbiprofeno/química
Flurbiprofeno/isolamento & purificação
Concentração de Íons de Hidrogênio
Indoprofen/química
Indoprofen/isolamento & purificação
Cetoprofeno/química
Cetoprofeno/isolamento & purificação
Metilação
Estrutura Molecular
Nanotecnologia/instrumentação
Naproxeno/química
Naproxeno/isolamento & purificação
Propionatos/química
Propionatos/isolamento & purificação
Estereoisomerismo
Suprofeno/química
Suprofeno/isolamento & purificação
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Benzoxazoles); 0 (Carbazoles); 0 (Propionates); 0 (beta-Cyclodextrins); 317745Y683 (heptakis(2,3,6-tri-O-methyl)-beta-cyclodextrin); 325708J22C (cicloprofen); 57Y76R9ATQ (Naproxen); 5GRO578KLP (Flurbiprofen); 90Y4QC304K (Ketoprofen); 988GU2F9PE (Suprofen); CPE46ZU14N (Indoprofen); FFL0D546HO (carprofen); UKU5U19W9M (flunoxaprofen)
[Em] Mês de entrada:0908
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090417
[St] Status:MEDLINE
[do] DOI:10.1002/jssc.200800667


  3 / 137 MEDLINE  
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[PMID]:18647485
[Au] Autor:Costa D; Gomes A; Lima JL; Fernandes E
[Ad] Endereço:REQUIMTE, Departamento de Química-Física, Faculdade de Farmácia, Universidade do Porto, Porto, Portugal.
[Ti] Título:Singlet oxygen scavenging activity of non-steroidal anti-inflammatory drugs.
[So] Source:Redox Rep;13(4):153-60, 2008.
[Is] ISSN:1743-2928
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:It has long been known that singlet oxygen ((1)O2) is generated during inflammatory processes. Once formed in substantial amounts, (1)O2 may have an important role in mediating the destruction of infectious agents during host defense. On the other hand, (1)O2 is capable of damaging almost all biological molecules and is particularly genotoxic, which gives a special relevance to the scavenging of this ROS throughout anti-inflammatory treatments. Considering that the use of non-steroidal anti-inflammatory drugs (NSAIDs) constitutes a first approach in the treatment of persistent inflammatory processes (due to their ability to inhibit cyclooxygenase), a putative scavenging activity of NSAIDs for (1)O2 would also represent a significant component of their therapeutic effect. The aim of the present study was to evaluate the scavenging activity for (1)O2 by several chemical families of NSAIDs. The results suggested that the pyrazole derivatives (dipyrone and aminopyrine) are, by far, the most potent scavengers of (1)O2 (much more potent compared to the other tested NSAIDs), displaying IC(50)-values in the low micromolar range. There was a lack of activity for most of the arylpropionic acid derivatives tested, with only naproxen and indoprofen displaying residual activities, as for the oxazole derivative, oxaprozin. On the other hand, the pyrrole derivatives (tolmetin and ketorolac), the indolacetic acid derivatives (indomethacin, and etodolac), as well as sulindac and its metabolites (sulindac sulfide and sulindac sulfone) displayed scavenging activity in the high micromolar range. Thus, the scavenging effect observed for dipyrone and aminopyrine will almost certainly contribute to their healing effect in the treatment of prolonged or chronic inflammation, while that of the other studied NSAIDs may have a lower contribution, though these assumptions still require further in vivo validation.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/química
Depuradores de Radicais Livres/química
Oxigênio Singlete/química
[Mh] Termos MeSH secundário: Aminopirina/química
Aminopirina/farmacologia
Anti-Inflamatórios não Esteroides/farmacologia
Dipirona/química
Dipirona/farmacologia
Relação Dose-Resposta a Droga
Etodolac/química
Etodolac/farmacologia
Depuradores de Radicais Livres/farmacologia
Indoprofen/química
Indoprofen/farmacologia
Cetorolaco/química
Cetorolaco/farmacologia
Estrutura Molecular
Naproxeno/química
Naproxeno/farmacologia
Propionatos/química
Propionatos/farmacologia
Oxigênio Singlete/antagonistas & inibidores
Tolmetino/química
Tolmetino/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Free Radical Scavengers); 0 (Propionates); 01704YP3MO (Aminopyrine); 17778-80-2 (Singlet Oxygen); 2M36281008 (Etodolac); 57Y76R9ATQ (Naproxen); 6429L0L52Y (Dipyrone); CPE46ZU14N (Indoprofen); D8K2JPN18B (Tolmetin); MHJ80W9LRB (oxaprozin); YZI5105V0L (Ketorolac)
[Em] Mês de entrada:0811
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080724
[St] Status:MEDLINE
[do] DOI:10.1179/135100008X308876


  4 / 137 MEDLINE  
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[PMID]:18295322
[Au] Autor:Jin DQ; Sung JY; Hwang YK; Kwon KJ; Han SH; Min SS; Han JS
[Ad] Endereço:Graduate Program in Neuroscience, Institute for Brain Science and Technology (IBST), Inje University, Daejeon, South Korea.
[Ti] Título:Dexibuprofen (S(+)-isomer ibuprofen) reduces microglial activation and impairments of spatial working memory induced by chronic lipopolysaccharide infusion.
[So] Source:Pharmacol Biochem Behav;89(3):404-11, 2008 May.
[Is] ISSN:0091-3057
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Non-steroidal anti-inflammatory drugs (NSAIDs) have been proposed as a therapeutics to reduce the risk of Alzheimer's disease (AD). The present study shows that the peripheral administration of dexibuprofen (S(+)-isomer ibuprofen), which causes less gastric damage and has better anti-inflammatory effects than ibuprofen, reduces the microglial activation in the cortex and hippocampus, and reduces the phosphorylation of extracellular signal-regulated kinases in the hippocampus, which has been induced by chronic infusion of lipopolysaccharide (LPS) into the fourth ventricle of Wistar rats. The effects of dexibuprofen on impairments of spatial working memory induced by LPS infusions were measured with a trial-unique matching-to-place task in a water maze which assessed memory for place information over varying delays. When performing the water maze task, the rats with the LPS infusions showed spatial working memory impairments relative to the rats with the artificial cerebrospinal fluid. Daily administrations of dexibuprofen reduced the spatial working memory impairment induced by the chronic LPS infusion. The results indicate that NSAID treatments using dexibuprofen significantly attenuate the processes that drive the pathology associated with AD and that this process may involve the suppression of microglial activation.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Indoprofen/farmacologia
Lipopolissacarídeos/toxicidade
Memória de Curto Prazo/efeitos dos fármacos
Microglia/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Córtex Cerebral/efeitos dos fármacos
Córtex Cerebral/enzimologia
MAP Quinases Reguladas por Sinal Extracelular/metabolismo
Hipocampo/efeitos dos fármacos
Hipocampo/enzimologia
Masculino
Microglia/fisiologia
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Lipopolysaccharides); CPE46ZU14N (Indoprofen); EC 2.7.11.24 (Extracellular Signal-Regulated MAP Kinases)
[Em] Mês de entrada:0805
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080226
[St] Status:MEDLINE
[do] DOI:10.1016/j.pbb.2008.01.016


  5 / 137 MEDLINE  
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[PMID]:18242990
[Au] Autor:Lee HJ; Lim SJ; Oh SJ; Moon DH; Kim DJ; Tae J; Yoo KH
[Ad] Endereço:Life Sciences Research Division, Korea Institute of Science and Technology, PO Box 131, Cheongryang, Seoul 130-650, Republic of Korea.
[Ti] Título:Isoindol-1,3-dione and isoindol-1-one derivatives with high binding affinity to beta-amyloid fibrils.
[So] Source:Bioorg Med Chem Lett;18(5):1628-31, 2008 Mar 01.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Based on the structural features of Indoprofen and PIB, a series of isoindol-1,3-diones 1a-k and isoindol-1-ones 2a-l were designed and synthesized. These 23 compounds were evaluated by competitive binding assay against aggregated Abeta42 fibrils using [(125)I]TZDM. All the isoindolone derivatives showed very good binding affinities with K(i) values in the subnanomolar range (0.42-0.94 nM). Among them, isoindol-1,3-diones 1i and 1k and isoindol-1-ones 2c and 2i exhibited excellent binding affinities (K(i)=0.42-0.44 and 0.46-0.49 nM) than those of Indoprofen (K(i)=0.52 nM) and PIB (K(i)=0.70 nM). These results suggest that isoindolones could be served as a scaffold for potential AD diagnostic probes to monitor Abeta fibrils.
[Mh] Termos MeSH primário: Peptídeos beta-Amiloides/química
Compostos Heterocíclicos/química
Compostos Heterocíclicos/farmacologia
Isoindóis/química
Isoindóis/farmacologia
[Mh] Termos MeSH secundário: Peptídeos beta-Amiloides/metabolismo
Benzotiazóis/química
Indoprofen/química
Estrutura Molecular
Ligação Proteica
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amyloid beta-Peptides); 0 (Benzothiazoles); 0 (Heterocyclic Compounds); 0 (Isoindol-1-one); 0 (Isoindoles); 0 (N-methyl-2-(4'-methylaminophenyl)-6-hydroxybenzothiazole); CPE46ZU14N (Indoprofen)
[Em] Mês de entrada:0805
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080205
[St] Status:MEDLINE
[do] DOI:10.1016/j.bmcl.2008.01.066


  6 / 137 MEDLINE  
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[PMID]:18218298
[Au] Autor:Menon S; Kadam N; Patil G; Mhatre P
[Ad] Endereço:Therapeutic Drug Monitoring Laboratory, Sion Koliwada, Sion (E), Mumbai, India.
[Ti] Título:A randomized, crossover study to determine bioequivalence of two brands of dexibuprofen 400 mg tablets in healthy Asian adult male subjects of Indian origin.
[So] Source:Int J Clin Pharmacol Ther;46(1):48-54, 2008 Jan.
[Is] ISSN:0946-1965
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:AIM: To estimate the bioavailability and evaluate bioequivalence of a single dose of a dexibuprofen tablet (test formulation, containing dexibuprofen 400 mg, manufactured by Emcure Pharmaceuticals Ltd., Pune, India) and to compare it with that of a single dose of a Seractil tablet (reference formulation, containing dexibuprofen 400 mg, manufactured by Genus Pharmaceuticals, Bershire, UK) under fasting conditions. SUBJECTS AND METHODS: Using a two-treatment, two-period, two-sequence, randomized crossover design, test and reference formulations were administered as individual single doses to 24 healthy adult Asian male subjects of Indian origin under non-fed conditions, with 4 days washout period between dosing. 17 blood samples were drawn from each subject over a 12-hour period. Pharmacokinetic parameters, Cmax, AUC0-t, AUC0-infinity and Cmax/AUC0-infinity were calculated from the plasma concentration-time data of each individual and during each period by applying non-compartmental analysis. Analysis of variance was carried out using logarithmically transformed and non-transformed values of the stated pharmacokinetic parameters. Data for test and reference formulations were analyzed statistically to test for bioequivalence of the two formulations. RESULTS: All 24 subjects who received the two formulations on two occasions with a washout period of 4 days, completed the study and provided an adequate amount of blood at each sampling point. After oral administration the values of Cmax (microg/ml), tmax (h), AUC0-t (microg/ml x h), AUC0-infinity (microg/ml x h) for reference and test formulations were 23.501 and 22.948, 1.156 and 1.281, 69.795 and 68.455, and 72.454 and 70.208, respectively. ANOVA and CI test showed no significant (p > 0.05) variation in these pharmacokinetic parameters of test and reference formulations. When the AUC0-t values for both formulations for non-transformed and log-transformed data were compared, the test formulation showed a bioavailability of 98.08% and 99.56%, respectively, as compared to reference formulation. These values are within the acceptance limit of 80 - 120%. No adverse events were observed in any of the subjects during the two runs of the study. Both clinical and laboratory parameters of all subjects showed no clinically significant changes. CONCLUSION: The test formulation containing dexibuprofen 400 mg (manufactured by Emcure Pharmaceuticals Ltd., Pune, India) was bioequivalent to reference formulation (Seractil, manufactured by Genus Pharmaceuticals, Berkshire, UK). Both formulations were well tolerated. The test formulation can be considered a pharmaceutically and therapeutically equivalent alternative to Seractil.
[Mh] Termos MeSH primário: Grupo com Ancestrais do Continente Asiático
Inibidores de Ciclo-Oxigenase/farmacocinética
Indoprofen/farmacocinética
[Mh] Termos MeSH secundário: Adulto
Análise de Variância
Área Sob a Curva
Disponibilidade Biológica
Química Farmacêutica
Cromatografia Líquida de Alta Pressão
Estudos Cross-Over
Inibidores de Ciclo-Oxigenase/administração & dosagem
Estabilidade de Medicamentos
Jejum
Seres Humanos
Índia
Indoprofen/administração & dosagem
Masculino
Comprimidos
Equivalência Terapêutica
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cyclooxygenase Inhibitors); 0 (Tablets); CPE46ZU14N (Indoprofen)
[Em] Mês de entrada:0802
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:080126
[St] Status:MEDLINE


  7 / 137 MEDLINE  
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[PMID]:16625984
[Au] Autor:Gómez BJ; Caunedo A; Redondo L; Esteban J; Sáenz-Dana M; Blasco M; Hergueta P; Rodríguez-Téllez M; Romero R; Pellicer FJ; Herrerías JM
[Ad] Endereço:Gastroenterology Service, Virgen Macarena University Hospital, Seville, Spain.
[Ti] Título:Modification of pepsinogen I levels and their correlation with gastrointestinal injury after administration of dexibuprofen, ibuprofen or diclofenac: a randomized, open-label, controlled clinical trial.
[So] Source:Int J Clin Pharmacol Ther;44(4):154-62, 2006 Apr.
[Is] ISSN:0946-1965
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:OBJECTIVE: To assess the effect of a 2-week treatment with dexibuprofen, in comparison with ibuprofen and diclofenac, on pepsinogen plasma concentrations and gastrointestinal mucosa, as well as the correlation of these changes with gastrointestinal mucosal injury. METHODS: 60 patients with rheumatologic disease in chronic therapy with NSAID, were included. After a 7-day run-in period patients were randomly assigned to receive a 14-day treatment with dexibuprofen (Group A; Day 1 - 3 = 400 mg t.i.d; Day 4 - 14 = 400 mg b.i.d.), ibuprofen (Group B; Day 1 - 3 = 800 mg t.i.d; Day 4 -14 = 800 mg b.i.d.) or diclofenac (Group C; Day 1 - 3 = 50 mg t.i.d; Day 4 - 14 = 50 mg b.i.d.). Upper gastrointestinal endoscopy (Day 15), capsule-endoscopy (Day 16, 7 patients of each group) and determination of pepsinogen plasma concentrations were performed (basal and Day 15). A semiquantitative scale was designed for the assessment of the gastrointestinal mucosa. RESULTS: No differences in plasma pepsinogen were found between treatment groups or gastrointestinal injury grades or between basal and post-therapy determinations. Dexibuprofen showed gastroduodenal mucosal injury in fewer patients (42.1%) than was the case with ibuprofen (5%; p = 0.003) and diclofenac (30%; p = N.S.). Dexibuprofen administration was also associated with more patients having no intestinal mucosal damage (42.86% vs. 28.7% in the diclofenac group and 14.29% in the ibuprofen group; p = 0.0175). The rate of clinical adverse events was similar in Groups A, B and C (28%, 38% and 34%). CONCLUSIONS: Dexibuprofen showed a lower rate of gastroduodenal and intestinal mucosal injury. This effect was not mediated by modifications of plasma pepsinogen levels.
[Mh] Termos MeSH primário: Inibidores de Ciclo-Oxigenase/efeitos adversos
Diclofenaco/efeitos adversos
Ibuprofeno/efeitos adversos
Indoprofen/efeitos adversos
Mucosa Intestinal/efeitos dos fármacos
Mucosa Intestinal/patologia
Pepsinogênio A/sangue
[Mh] Termos MeSH secundário: Administração Oral
Adulto
Inibidores de Ciclo-Oxigenase/farmacologia
Diclofenaco/farmacologia
Endoscopia Gastrointestinal
Feminino
Seres Humanos
Ibuprofeno/farmacologia
Indoprofen/farmacologia
Masculino
Meia-Idade
Pepsinogênio A/efeitos dos fármacos
Doenças Reumáticas/tratamento farmacológico
Doenças Reumáticas/patologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cyclooxygenase Inhibitors); 144O8QL0L1 (Diclofenac); 9001-10-9 (Pepsinogen A); CPE46ZU14N (Indoprofen); WK2XYI10QM (Ibuprofen)
[Em] Mês de entrada:0605
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:060422
[St] Status:MEDLINE


  8 / 137 MEDLINE  
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[PMID]:15882220
[Au] Autor:Rosin M; Kähler ST; Hessler M; Schwahn Ch; Kuhr A; Kocher T
[Ad] Endereço:Department of Periodontology, Eastman Dental Institute, University College London, London, UK. rosin@uni-greifswald.de
[Ti] Título:The effect of a dexibuprofen mouth rinse on experimental gingivitis in humans.
[So] Source:J Clin Periodontol;32(6):617-21, 2005 Jun.
[Is] ISSN:0303-6979
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: The pharmacodynamic properties of ibuprofen are related nearly exclusively to the S(+)enantiomer (dexibuprofen). This study investigated the effect of a 1.5% dexibuprofen mouth rinse in an experimentally induced gingivitis. MATERIALS AND METHODS: The trial was a randomized, double-blinded, placebo-controlled, two-period and two-sequence parallel group cross-over study in 24 healthy volunteers aged 21-30 years (16 males, eight females). Customized guards were worn during tooth brushing to prevent any plaque removal from the experimental area (first and second pre-molars and molars in one upper quadrant). After 22 days of plaque accumulation, the mouth rinses (1.5% dexibuprofen and placebo) were administered under supervision three times daily (rinsing for 1 min. with 15 ml) for 8 days. The wash-out time between the two study periods was 14 days. Parameters evaluated at days 0, 7, 14, 22, and 30 were the Löe & Silness gingival index (GI) and the Quigley & Hein plaque index (QHI). Data were tested for treatment, period, and carry-over effects (parametric cross-over analysis). RESULTS: There was no statistically significant difference (p=0.240) in GI between placebo and dexibuprofen. However, the decrease in QHI was significantly greater (p=0.019) with dexibuprofen as compared with the placebo. CONCLUSION: In the present study, a 1.5% dexibuprofen mouth rinse had no effect on gingivitis whereas an anti-plaque effect was demonstrated.
[Mh] Termos MeSH primário: Inibidores de Ciclo-Oxigenase/uso terapêutico
Placa Dentária/tratamento farmacológico
Gengivite/tratamento farmacológico
Indoprofen/uso terapêutico
Antissépticos Bucais/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Métodos Epidemiológicos
Feminino
Seres Humanos
Masculino
Escovação Dentária
[Pt] Tipo de publicação:CLINICAL TRIAL; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cyclooxygenase Inhibitors); 0 (Mouthwashes); CPE46ZU14N (Indoprofen)
[Em] Mês de entrada:0507
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:D; IM
[Da] Data de entrada para processamento:050511
[St] Status:MEDLINE


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[PMID]:15738999
[Au] Autor:Trzcionka J; Noirot A; Fabre PL; Chouini-Lalanne N
[Ad] Endereço:Laboratoire des Interactions Moleculaires et Reactivite Chimique et Photochimique, UMR 5623 au CNRS, Universite Paul Sabatier, 118, route de Narbonne, 31062, Toulouse cedex 4, France.
[Ti] Título:Comparative study of the photophysical properties of indoprofen photoproducts in relation with their DNA photosensitizing properties.
[So] Source:Photochem Photobiol Sci;4(3):298-303, 2005 Mar.
[Is] ISSN:1474-905X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The photophysical properties of indoprofen photoproducts have been examined in various solvents by absorbance and emission spectroscopies in relation with their photosensitizing properties. The photophysical properties of 2-[4-(1-hydroxy)ethylphenyl]isoindolin-1-one (HOINP) and 2-(4-ethylphenyl)isoindolin-1-one (ETINP) are typical of a singlet excited state when the ones of 2-(4-acetylphenyl)isoindolin-1-one (KINP) are based on its triplet excited state according to previous work. The effect of solvent polarity on the absorption and fluorescence properties of HOINP and ETINP has been investigated as a function of Delta f, the Lippert solvent polarity parameter. A solvatochromic effect, function of the polarity region, has been observed for both photoproducts due to a change in the dipole moment of the compound upon excitation. In low-polarity regions, the excited state dipole moment of HOINP undergoes only a moderate increase (11.5 D) as compared to the dipole moment of the ground state (4.5 D) suggesting that the fluorescence arises from the locally excited state while in high-polarity regions it is strongly increased (42.9 D), which can imply that the emission takes place from a charge transfer state. In the case of ETINP, it would seem that the emitting state is rather a charge transfer state whatever the region is (16.9 and 31.8 D for the calculated excited-state dipole moments in the low and high-polarity regions, respectively). HOINP and ETINP do not produce thymine dimers by photosensitization but induce photooxidative damage via an electron transfer mechanism.
[Mh] Termos MeSH primário: DNA/efeitos dos fármacos
Indoprofen/química
Fármacos Fotossensibilizantes/química
[Mh] Termos MeSH secundário: Indoprofen/farmacologia
Fármacos Fotossensibilizantes/farmacologia
Dímeros de Pirimidina/química
Solventes
Espectrofotometria
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Photosensitizing Agents); 0 (Pyrimidine Dimers); 0 (Solvents); 9007-49-2 (DNA); CPE46ZU14N (Indoprofen)
[Em] Mês de entrada:0504
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:050302
[St] Status:MEDLINE


  10 / 137 MEDLINE  
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[PMID]:15555999
[Au] Autor:Lunn MR; Root DE; Martino AM; Flaherty SP; Kelley BP; Coovert DD; Burghes AH; Man NT; Morris GE; Zhou J; Androphy EJ; Sumner CJ; Stockwell BR
[Ad] Endereço:Department of Biological Sciences, Columbia University, Fairchild Center, MC 2406, 1212 Amsterdam Avenue, New York, NY 10027, USA.
[Ti] Título:Indoprofen upregulates the survival motor neuron protein through a cyclooxygenase-independent mechanism.
[So] Source:Chem Biol;11(11):1489-93, 2004 Nov.
[Is] ISSN:1074-5521
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Most patients with the pediatric neurodegenerative disease spinal muscular atrophy have a homozygous deletion of the survival motor neuron 1 (SMN1) gene, but retain one or more copies of the closely related SMN2 gene. The SMN2 gene encodes the same protein (SMN) but produces it at a low efficiency compared with the SMN1 gene. We performed a high-throughput screen of approximately 47,000 compounds to identify those that increase production of an SMN2-luciferase reporter protein, but not an SMN1-luciferase reporter protein. Indoprofen, a nonsteroidal anti-inflammatory drug (NSAID) and cyclooxygenase (COX) inhibitor, selectively increased SMN2-luciferase reporter protein and endogenous SMN protein and caused a 5-fold increase in the number of nuclear gems in fibroblasts from SMA patients. No other NSAIDs or COX inhibitors tested exhibited this activity.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Indoprofen/farmacologia
Proteínas do Tecido Nervoso/biossíntese
[Mh] Termos MeSH secundário: Animais
Proteína de Ligação ao Elemento de Resposta ao AMP Cíclico
Inibidores de Ciclo-Oxigenase/farmacologia
Avaliação Pré-Clínica de Medicamentos
Feminino
Fibroblastos/enzimologia
Seres Humanos
Indoprofen/farmacocinética
Camundongos
Proteínas do Tecido Nervoso/genética
Gravidez
Prostaglandina-Endoperóxido Sintases/fisiologia
Proteínas de Ligação a RNA
Proteínas do Complexo SMN
Proteína 1 de Sobrevivência do Neurônio Motor
Proteína 2 de Sobrevivência do Neurônio Motor
Regulação para Cima
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Cyclic AMP Response Element-Binding Protein); 0 (Cyclooxygenase Inhibitors); 0 (Nerve Tissue Proteins); 0 (RNA-Binding Proteins); 0 (SMN Complex Proteins); 0 (SMN1 protein, human); 0 (SMN2 protein, human); 0 (Smn1 protein, mouse); 0 (Survival of Motor Neuron 1 Protein); 0 (Survival of Motor Neuron 2 Protein); CPE46ZU14N (Indoprofen); EC 1.14.99.1 (Prostaglandin-Endoperoxide Synthases)
[Em] Mês de entrada:0504
[Cu] Atualização por classe:161122
[Lr] Data última revisão:
161122
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:041124
[St] Status:MEDLINE



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