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[PMID]:29274491
[Au] Autor:Srivastava P; Singh K; Verma M; Sivakumar S; Patra AK
[Ad] Endereço:Department of Chemistry, Indian Institute of Technology Kanpur, Kanpur 208016, Uttar Pradesh, India.
[Ti] Título:Photoactive platinum(II) complexes of nonsteroidal anti-inflammatory drug naproxen: Interaction with biological targets, antioxidant activity and cytotoxicity.
[So] Source:Eur J Med Chem;144:243-254, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:The effect on the therapeutic efficacy of Pt(II) complexes on combining non-steroidal anti-inflammatory drugs (NSAIDs) is an attractive strategy to circumvent chronic inflammation mediated by cancer and metastasis. Two square-planar platinum(II) complexes: [Pt(dach)(nap)Cl] (1) and [Pt(dach)(nap) ] (2), where dach = (1R,2R)-dichloro(cyclohexane-1,2-diamine) and NSAID drug naproxen (nap), have been designed for studying their biological activity. The naproxen bound to the Pt(II) centre get released upon photoirradiation with low-power UV-A light as confirmed by the significant enhancement in emission intensities of the complexes. The compounds were evaluated for their photophysical properties, photostability, reactivity with 5'-guanosine monophophosphate (5'-GMP), interactions with CT-DNA and BSA, antioxidant activity and reactive oxygen species mediated photo-induced DNA damage properties. ESI-MS studies demonstrated the formation of bis-adduct with 5'-GMP and the formation of Pt -DNA crosslinks by gel electrophoretic mobility shift assay and ITC studies. The interaction of the complexes 1 and 2 with the CT-DNA exhibits potential binding affinity (K âˆ¼ 10 M , K ∼ 10 M ), implying intercalation to CT-DNA through planar naphthyl ring of the complexes. Both the complexes also exhibit strong binding affinity towards BSA (K ∼ 10 M ). The complexes exhibit efficient DNA damage activity on irradiation at 365 nm via formation of singlet oxygen ( O ) and hydroxyl radical ( OH) under physiological conditions. Both the complexes were cytotoxic in dark and exhibit significant enhancement of cytotoxicity upon photo-exposure against HeLa and HepG2 cancer cells giving IC values ranging from 8 to 12 µM for 1 and 2. The cellular internalization data showed cytosolic and nuclear localization of the complexes in the HeLa cells.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/química
Antineoplásicos/química
Antioxidantes/química
Naproxeno/análogos & derivados
Compostos Organoplatínicos/química
[Mh] Termos MeSH secundário: Anti-Inflamatórios não Esteroides/farmacologia
Antineoplásicos/farmacologia
Antioxidantes/farmacologia
Sobrevivência Celular/efeitos dos fármacos
Sobrevivência Celular/efeitos da radiação
Dano ao DNA/efeitos dos fármacos
Dano ao DNA/efeitos da radiação
Células HeLa
Células Hep G2
Seres Humanos
Naproxeno/farmacologia
Neoplasias/tratamento farmacológico
Neoplasias/genética
Compostos Organoplatínicos/farmacologia
Fármacos Fotossensibilizantes/química
Fármacos Fotossensibilizantes/farmacologia
Raios Ultravioleta
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Antineoplastic Agents); 0 (Antioxidants); 0 (Organoplatinum Compounds); 0 (Photosensitizing Agents); 57Y76R9ATQ (Naproxen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180309
[Lr] Data última revisão:
180309
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171224
[St] Status:MEDLINE


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[PMID]:29441918
[Au] Autor:Wang S; Li A; Guo S
[Ti] Título:Ligustrazine attenuates neuropathic pain by inhibition of JAK/STAT3 pathway in a rat model of chronic constriction injury.
[So] Source:Pharmazie;71(7):408-412, 2016 Jul 07.
[Is] ISSN:0031-7144
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:AIM: Neuropathic pain is a common clinical complication of nerve injury, and the effective treatment of neuropathic pain is still challenging. Ligustrazine is mainly used for the treatment of cardiovascular disease and its role in neuropathic pain is less investigated. The purpose of our study was to explore the effects of ligustrazine on neuropathic pain, as well as the underlying molecular mechanism. METHODS: Neuropathic pain was induced by chronic constriction injury (CCI) of the right sciatic nerve in Sprague-Dawley (SD) rats. After CCI, rats received ligustrazine, IL-6, or both. Mechanical withdrawal threshold (MWT) and paw withdrawal thermal latency (PWTL) were assessed on days 1, 3, 7, and 14 after surgery. Expression levels of tumor necrosis factor (TNF)-α, interleukin (IL)-ß, IL-2, and phosphorylation of Signal Transducer and Activator of Transcription (STAT) 3 were analyzed. RESULTS: Our results showed that both MWT and PWTL were significantly decreased by CCI on days 1, 3, 7 and 14 compared to sham group, however, ligustrazine reversed this effects. Additionally, the elevated levels of TNF-α, IL-1ß, and IL-2 in CCI spinal cord were inhibited by ligustrazine. Quantitative real-time (qRT-PCR) and Western blotting analysis showed that the test substance reduced the elevated expression of pSTAT3 in the spinal cord induced by CCI, and while IL-6 administration reversed the levels as well as the behavior responses. CONCLUSION: Our results suggest that ligustrazine could effectively attenuate neuropathic pain by inhibition of Janus Kinase (JAK)/STAT3 pathway in CCI rats.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/uso terapêutico
Constrição Patológica/complicações
Neuralgia/tratamento farmacológico
Pirazinas/uso terapêutico
Fator de Transcrição STAT3/antagonistas & inibidores
Transdução de Sinais/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Comportamento Animal/efeitos dos fármacos
Citocinas/antagonistas & inibidores
Citocinas/biossíntese
Temperatura Alta
Masculino
Neuralgia/etiologia
Neuralgia/psicologia
Limiar da Dor/efeitos dos fármacos
Ratos
Ratos Sprague-Dawley
Fator de Transcrição STAT3/biossíntese
Nervo Isquiático/lesões
Medula Espinal/efeitos dos fármacos
Medula Espinal/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Cytokines); 0 (Pyrazines); 0 (STAT3 Transcription Factor); 0 (Stat3 protein, rat); V80F4IA5XG (tetramethylpyrazine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180215
[St] Status:MEDLINE
[do] DOI:10.1691/ph.2016.6546


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[PMID]:29357800
[Au] Autor:Siverio-Mota D; Andujar I; Marrero-Ponce Y; Giner RM; Diaz-Mendoza C; Paba GM; Vicet-Muro L; Cordero-Maldonado ML; de Witte PAM; Crawford AD; Veitia MS; Perez-Jimenez F; Aran VJ
[Ad] Endereço:Laboratory for Molecular Biodiscovery, Department of Pharmaceutical and Pharmacological Sciences, University of Leuven, Herestraat 49, 3000 Leuven, Belgium.
[Ti] Título:Anti-Inflammatory Activity and Cheminformatics Analysis of New Poten t 2-Substituted 1-Methyl-5-Nitroindazolinones.
[So] Source:Curr Top Med Chem;17(30):3236-3248, 2018 Feb 09.
[Is] ISSN:1873-4294
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:After the identification of the anti-inflammatory properties of VA5-13l (2-benzyl-1- methyl-5-nitroindazolinone) in previous investigations, some of its analogous compounds were designed, synthesized and evaluated in two anti-inflammatory methods: LPS-enhanced leukocyte migration assay in zebrafish; and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced mouse ear edema. The products evaluated (3, 6, 8, 9 and 10) showed the lower values of relative leukocyte migration at 30 µM (0.14, 0.07, 0.10, 0.13 and 0.07, respectively), while in ear edema and myeloperoxidase activity methods, all the compounds reduced inflammation, only 4 and 16 yielded unsatisfactory results. The relationship linking structure and activity (SAR analysis) was determinate by using SARANEA software. The importance of the 5-Nitro group of the indazole ring for the activity was evident, and showed modest reduction when benzyl (Bn) is changed by alkyl group. A substituted Bn moiety at N2 (R) is the best substituent (5-10); nevertheless, if methylene group of Bn is deleted, the activity is affected. Also, introduction of halogen atoms mainly at positions 3 or 4 of the benzyl moiety (6 and 10) leads in general to strong activities. In fact, compounds 7 and 8 (R = 4-FBn or 4-ClBn, respectively) exhibit satisfactory results in in vivo tests and appear promising. The production of IL-6 at all doses assayed was significantly reduced, except with 16. Nonetheless, the production of TNF-α was significantly inhibited only by this chemical (16) at concentration of 50 µM. On the other hand, compound 2 was the one that mostly inhibited the expression of COX-2 and iNOS. From these results, it can be concluded that the inhibition in the release of cytokines can be one of the mechanisms of action responsible for the anti-inflammatory effect for 2-benzyl derivates while other 2-alkyl derivatives can inhibit production of NO. Therefore, nitroindazolinone chemical prototype could be an interesting structural group with anti-inflammatory purposes in the therapeutic.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Inibidores de Ciclo-Oxigenase 2/farmacologia
Indazóis/farmacologia
Informática
Nitrocompostos/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/química
Ciclo-Oxigenase 2/metabolismo
Inibidores de Ciclo-Oxigenase 2/química
Relação Dose-Resposta a Droga
Seres Humanos
Indazóis/química
Lipopolissacarídeos/antagonistas & inibidores
Lipopolissacarídeos/farmacologia
Estrutura Molecular
Óxido Nítrico/antagonistas & inibidores
Óxido Nítrico/biossíntese
Óxido Nítrico Sintase Tipo II/antagonistas & inibidores
Óxido Nítrico Sintase Tipo II/metabolismo
Nitrocompostos/química
Relação Estrutura-Atividade
Fator de Necrose Tumoral alfa/antagonistas & inibidores
Peixe-Zebra
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Cyclooxygenase 2 Inhibitors); 0 (Indazoles); 0 (Lipopolysaccharides); 0 (Nitro Compounds); 0 (Tumor Necrosis Factor-alpha); 31C4KY9ESH (Nitric Oxide); EC 1.14.13.39 (Nitric Oxide Synthase Type II); EC 1.14.99.1 (Cyclooxygenase 2)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180124
[St] Status:MEDLINE
[do] DOI:10.2174/1568026618666180119125255


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[PMID]:28453754
[Au] Autor:Turner D; Yerushalmi B; Kori M; Broide E; Mozer-Glassberg Y; Shaoul R; Kolho KL; Shteyer E; Shamaly H; Ledder O; Cohen S; Peleg S; On A; Levine A
[Ad] Endereço:Institute of Paediatric Gastroenterology, Hebrew University of Jerusalem, Jerusalem, Israel.
[Ti] Título:Once- Versus Twice-daily Mesalazine to Induce Remission in Paediatric Ulcerative Colitis: A Randomised Controlled Trial.
[So] Source:J Crohns Colitis;11(5):527-533, 2017 May 01.
[Is] ISSN:1876-4479
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Background: Trials in adults suggested that, in ulcerative colitis [UC], once-daily [OD] dosing of 5-ASA [5-amino salicylic acid] may be as or more effective than twice-daily [BD] dosing. In this induction of remission, investigator-blinded, randomised controlled-trial, we aimed to compare effectiveness and safety of once- versus twice-daily mesalazine in paediatric UC. Methods: Children, aged 4-18 years with a PUCAI [Paediatric Ulcerative Colitis Activity Index] of 10-55 points at inclusion, were randomised in blocks of six with blinded allocation to OD or BD mesalazine, using a weight-based dosing table. The primary outcome was mean PUCAI score at Week 6. Results: A total of 83/86 randomised children were eligible and analysed: 43 in the OD group and 40 in the BD group (mean age 14 ± 2.7 years, 43 [52%] males, 51 [62%] extensive colitis). The groups did not differ with regard to disease activity or any other parameter at baseline. There was no difference in median PUCAI score between the OD group and BD group at Week 6: 15 ( interquartile range [IQR] 5-40) versus 10 [0-40]; p = 0.48]. Response was seen in 25 [60%] OD versus 25 [63%] BD dosing [p = 0.78]. Proportion of children in remission [PUCAI < 10] at Week 6 was 13 [30%] OD versus 16 [40%] BD; p = 0.35]. Most adverse events were related to disease aggravation; the rates of serious adverse events were similar [p > 0.2]. Conclusions: In this first randomised controlled trial in children, no differences were found between OD and BD dosing for any clinical outcome. Remission was achieved in 35% of children treated with mesalazine for active UC.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/uso terapêutico
Colite Ulcerativa/tratamento farmacológico
Mesalamina/uso terapêutico
[Mh] Termos MeSH secundário: Adolescente
Anti-Inflamatórios não Esteroides/administração & dosagem
Criança
Pré-Escolar
Esquema de Medicação
Feminino
Seres Humanos
Masculino
Mesalamina/administração & dosagem
Indução de Remissão/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 4Q81I59GXC (Mesalamine)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170429
[St] Status:MEDLINE
[do] DOI:10.1093/ecco-jcc/jjw180


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[PMID]:29211672
[Au] Autor:Stevens DL; Bryant AE
[Ad] Endereço:From the Veterans Affairs Medical Center, Boise, ID; and the University of Washington School of Medicine, Seattle.
[Ti] Título:Necrotizing Soft-Tissue Infections.
[So] Source:N Engl J Med;377(23):2253-2265, 2017 Dec 07.
[Is] ISSN:1533-4406
[Cp] País de publicação:United States
[La] Idioma:eng
[Mh] Termos MeSH primário: Antibacterianos/uso terapêutico
Desbridamento
Fasciite Necrosante
[Mh] Termos MeSH secundário: Anti-Inflamatórios não Esteroides/efeitos adversos
Biomarcadores/sangue
Biópsia
Proteína C-Reativa/análise
Estado Terminal
Fasciite Necrosante/diagnóstico
Fasciite Necrosante/etiologia
Fasciite Necrosante/patologia
Fasciite Necrosante/terapia
Gangrena Gasosa
Seres Humanos
Oxigenação Hiperbárica
Imunoglobulinas Intravenosas/uso terapêutico
Infecções dos Tecidos Moles
Infecções Estreptocócicas/induzido quimicamente
Streptococcus pyogenes
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Biomarkers); 0 (Immunoglobulins, Intravenous); 9007-41-4 (C-Reactive Protein)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:180308
[Lr] Data última revisão:
180308
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:171207
[St] Status:MEDLINE
[do] DOI:10.1056/NEJMra1600673


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[PMID]:29419381
[Ti] Título:How to estimate the effect of treatment duration on survival outcomes using observational data.
[So] Source:BMJ;360:k182, 2018 02 01.
[Is] ISSN:1756-1833
[Cp] País de publicação:England
[La] Idioma:eng
[Mh] Termos MeSH primário: Assistência de Longa Duração/métodos
Análise de Sobrevida
Resultado do Tratamento
[Mh] Termos MeSH secundário: Anti-Inflamatórios não Esteroides/administração & dosagem
Anti-Inflamatórios não Esteroides/farmacologia
Aspirina/administração & dosagem
Aspirina/farmacologia
Seres Humanos
Ensaios Clínicos Controlados Aleatórios como Assunto
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; OBSERVATIONAL STUDY; RESEARCH SUPPORT, N.I.H., EXTRAMURAL
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); R16CO5Y76E (Aspirin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:180209
[St] Status:MEDLINE
[do] DOI:10.1136/bmj.k182


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[PMID]:28985539
[Au] Autor:Naidoo V; Taggart MA; Duncan N; Wolter K; Chipangura J; Green RE; Galligan TH
[Ad] Endereço:Department of Paraclinical Sciences, Faculty of Veterinary Science, University of Pretoria, South Africa; Biomedical Research Centre, Faculty of Veterinary Science, University of Pretoria, South Africa. Electronic address: vinny.naidoo@up.ac.za.
[Ti] Título:The use of toxicokinetics and exposure studies to show that carprofen in cattle tissue could lead to secondary toxicity and death in wild vultures.
[So] Source:Chemosphere;190:80-89, 2018 Jan.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Veterinary medicines can be extremely damaging to the environment, as seen with the catastrophic declines in Gyps vulture in South Asia due to their secondary exposure to diclofenac in their primary food source. Not surprisingly, concern has been raised over other similar drugs. In this study, we evaluate the toxicity of carprofen to the Gyps vulture clade through plasma pharmacokinetics evaluations in Bos taurus cattle (their food source) and Gyps africanus (a validated model species); tissue residues in cattle; and the effect of carprofen as a secondary toxicant as both tissue-bound residue or pure drug at levels expected in cattle tissues. Carprofen residues were highest in cattle kidney (7.72 ± 2.38 mg/kg) and injection site muscle (289.05 ± 98.96 mg/kg of dimension of 5 × 5 × 5 cm). Vultures exposed to carprofen as residues in the kidney tissue or pure drug equivalents showed no toxic signs. When exposed to average injection site concentrations (64 mg/kg) one of two birds died with evidence of severe renal and liver damage. Toxicokinetic analysis revealed a prolonged drug half-life of 37.75 h in the dead bird as opposed to 13.99 ± 5.61 h from healthy birds dosed intravenously at 5 mg/kg. While carprofen may generally be harmless to Gyps vultures, its high levels at the injection site in treated cattle can result in lethal exposure in foraging vultures, due to relative small area of tissue it is found therein. We thus suggest that carprofen not be used in domesticated ungulates in areas where carcasses are accessible or provided to vultures at supplementary feeding sites.
[Mh] Termos MeSH primário: Carbazóis/toxicidade
Falconiformes
Drogas Veterinárias/toxicidade
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/farmacocinética
Anti-Inflamatórios não Esteroides/toxicidade
Ásia
Carbazóis/farmacocinética
Bovinos
Morte
Diclofenaco/farmacocinética
Diclofenaco/toxicidade
Meia-Vida
Rim/efeitos dos fármacos
Rim/patologia
Fígado/efeitos dos fármacos
Fígado/patologia
Toxicocinética
Drogas Veterinárias/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Carbazoles); 0 (Veterinary Drugs); 144O8QL0L1 (Diclofenac); FFL0D546HO (carprofen)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180305
[Lr] Data última revisão:
180305
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171007
[St] Status:MEDLINE


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[PMID]:27775689
[Au] Autor:Yang J; Wang T; Li Y; Yao W; Ji X; Wu Q; Han L; Han R; Yan W; Yuan J; Ni C
[Ad] Endereço:Department of Occupational Medicine and Environmental Health and Key Laboratory of Modern Toxicology of Ministry of Education, School of Public Health, Nanjing Medical University, Nanjing, China.
[Ti] Título:Earthworm extract attenuates silica-induced pulmonary fibrosis through Nrf2-dependent mechanisms.
[So] Source:Lab Invest;96(12):1279-1300, 2016 12.
[Is] ISSN:1530-0307
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Silicosis is an occupational pulmonary fibrosis caused by inhalation of silica (SiO ) and there are no ideal drugs to treat this disease. Earthworm extract (EE), a natural nutrient, has been reported to have anti-inflammatory, antioxidant, and anti-apoptosis effects. The purpose of the current study was to test the protective effects of EE against SiO -induced pulmonary fibrosis and to explore the underlying mechanisms using both in vivo and in vitro models. We found that treatment with EE significantly reduced lung inflammation and fibrosis and improved lung structure and function in SiO -instilled mice. Further mechanistic investigations revealed that EE administration markedly inhibited SiO -induced oxidative stress, mitochondrial apoptotic pathway, and epithelial-mesenchymal transition in HBE and A549 cells. Furthermore, we demonstrate that Nrf2 activation partly mediates the interventional effects of EE against SiO -induced pulmonary fibrosis. Our study has identified EE to be a potential anti-oxidative, anti-inflammatory, and anti-fibrotic drug for silicosis.
[Mh] Termos MeSH primário: Antioxidantes/uso terapêutico
Modelos Animais de Doenças
Pulmão/efeitos dos fármacos
Materia Medica/uso terapêutico
Oligoquetos/química
Fibrose Pulmonar/prevenção & controle
Silicose/tratamento farmacológico
Extratos de Tecidos/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/administração & dosagem
Anti-Inflamatórios não Esteroides/farmacologia
Anti-Inflamatórios não Esteroides/uso terapêutico
Antioxidantes/administração & dosagem
Antioxidantes/farmacologia
Apoptose/efeitos dos fármacos
Linhagem Celular
Células Cultivadas
Transição Epitelial-Mesenquimal/efeitos dos fármacos
Injeções Intraperitoneais
Pulmão/metabolismo
Pulmão/patologia
Pulmão/fisiopatologia
Masculino
Materia Medica/administração & dosagem
Materia Medica/farmacologia
Camundongos Endogâmicos C57BL
Fator 2 Relacionado a NF-E2/agonistas
Fator 2 Relacionado a NF-E2/antagonistas & inibidores
Fator 2 Relacionado a NF-E2/genética
Fator 2 Relacionado a NF-E2/metabolismo
Estresse Oxidativo/efeitos dos fármacos
Fibrose Pulmonar/etiologia
Fibrose Pulmonar/imunologia
Interferência de RNA
Distribuição Aleatória
Mucosa Respiratória/citologia
Mucosa Respiratória/efeitos dos fármacos
Mucosa Respiratória/metabolismo
Mucosa Respiratória/patologia
Silicose/metabolismo
Silicose/patologia
Silicose/fisiopatologia
Organismos Livres de Patógenos Específicos
Extratos de Tecidos/administração & dosagem
Extratos de Tecidos/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 (Antioxidants); 0 (Materia Medica); 0 (NF-E2-Related Factor 2); 0 (Tissue Extracts)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:180306
[Lr] Data última revisão:
180306
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161025
[St] Status:MEDLINE
[do] DOI:10.1038/labinvest.2016.101


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[PMID]:29465556
[Au] Autor:Ni Y; Jiang C
[Ad] Endereço:Department of Spine Surgery.
[Ti] Título:Identification of potential target genes for ankylosing spondylitis treatment.
[So] Source:Medicine (Baltimore);97(8):e9760, 2018 Feb.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:This study aimed to identify the potential target genes for the treatment of ankylosing spondylitis (AS).Dataset GSE25101 was downloaded from Gene Expression Omnibus, including 16 AS and 16 normal control blood samples. Differentially expressed genes (DEGs) were identified using unmatched t-test in limma package with adjusted P < .05. Gene ontology-biological process (GO-BP) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were conducted using multifaceted analysis tool for human transcriptome. Protein-protein interaction (PPI) network was constructed using STRING and Cytoscape, and module analysis was performed using MCODE plug-in. Webgestal was utilized to predict transcriptional factor (TF)-microRNA-target network and Comparative Toxicogenomics Database (CTD) was applied to predict chemical-target network.A total of 334 DEGs were identified, including 136 upregulated genes and 198 downregulated genes. According to STRING, a PPI network was constructed and 1 significant clustered module was screen out with score = 6.33. MAPK7 (degree = 11) and NDUFS4 (degree = 10) were 2 important nodes in PPI network, and both of them were significantly enriched in cAMP mediated signaling pathway (P = 2.02E-02). MAPK7 could be regulated by NFY. Both MAPK7 and NDUFS4 were 2 potential targets for Indomethacin.MAPK7 and NDUFS4 played important roles in the pathogenesis of AS via cAMP mediated signaling pathway. Both of them could be targeted by Indomethacin.
[Mh] Termos MeSH primário: Proteína Quinase 7 Ativada por Mitógeno/sangue
NADH Desidrogenase/sangue
Mapeamento de Interação de Proteínas/métodos
Mapas de Interação de Proteínas/genética
Espondilite Anquilosante/genética
[Mh] Termos MeSH secundário: Anti-Inflamatórios não Esteroides/farmacologia
Estudos de Casos e Controles
Análise por Conglomerados
Biologia Computacional
Redes Reguladoras de Genes
Seres Humanos
Indometacina/farmacologia
Transdução de Sinais/genética
Espondilite Anquilosante/sangue
Espondilite Anquilosante/tratamento farmacológico
Transcriptoma
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); EC 1.6.5.3 (NDUFS4 protein, human); EC 1.6.99.3 (NADH Dehydrogenase); EC 2.7.11.24 (MAPK7 protein, human); EC 2.7.11.24 (Mitogen-Activated Protein Kinase 7); XXE1CET956 (Indomethacin)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:180222
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000009760


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[PMID]:29289887
[Au] Autor:Moussa G; Alaaeddine R; Alaeddine LM; Nassra R; Belal ASF; Ismail A; El-Yazbi AF; Abdel-Ghany YS; Hazzaa A
[Ad] Endereço:Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt.
[Ti] Título:Novel click modifiable thioquinazolinones as anti-inflammatory agents: Design, synthesis, biological evaluation and docking study.
[So] Source:Eur J Med Chem;144:635-650, 2018 Jan 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Click chemistry was used to synthesize a new series of thioquinazolinone molecules equipped with propargyl moiety,1,2,3-triazolyl and isoxazolyl rings. Our design was based on merging pharmacophores previously reported to exhibit COX-2 inhibitory activities to a thioquinazolinone-privileged scaffold. The synthesized compounds were subjected to in vitro cyclooxygenase COX-1/COX-2 and 15-LOX inhibition assays. Compounds 2c, 3b, 3h, 3j, and 3k showed COX-2 inhibition with IC (µM) 0.18, 0.19, 0.11, 0.16 and 0.17 respectively. These values were compared to celecoxib (IC 0.05 µM), diclofenac (IC 0.8 µM) and indomethacin (IC 0.49 µM) reference drugs. They also showed 15-LOX inhibition with IC (µM) 6.21, 4.33, 7.62, 5.21 and 3.98 respectively. These values were compared with Zileuton (IC 2.41 µM) and Meclofenamate sodium (IC 5.64 µM) as positive controls. These compounds were further challenged by PMA-induced THP-1 differentiation assay where compounds 2c and 3j inhibited monocyte to macrophage differentiation efficiently with IC values of 4.78 µM and 5.63 µM, respectively, compared to that of diclofenac sodium (4.86 µM). On the other hand, 3h demonstrated a significantly increased potency compared to diclofenac in this assay (IC = 0.13 µM). The same compounds exhibited significant in vivo anti-inflammatory effect as indicated by the formalin-induced rat-paw edema test. Docking experiments of compounds 2c, 3b, 3h, 3j, and 3k into COX-2 binding pocket have been conducted, where strong binding interactions have been identified and effective overall docking scores have been recorded. Their drug-likeness has been assessed using Molinspiration, Molsoft and Pre-ADMET software products.
[Mh] Termos MeSH primário: Anti-Inflamatórios não Esteroides/farmacologia
Inibidores de Ciclo-Oxigenase/farmacologia
Desenho de Drogas
Inibidores de Lipoxigenase/farmacologia
Quinazolinonas/farmacologia
Compostos de Sulfidrila/farmacologia
[Mh] Termos MeSH secundário: Animais
Anti-Inflamatórios não Esteroides/síntese química
Anti-Inflamatórios não Esteroides/química
Araquidonato 15-Lipoxigenase/metabolismo
Diferenciação Celular/efeitos dos fármacos
Química Click
Ciclo-Oxigenase 1/metabolismo
Ciclo-Oxigenase 2/metabolismo
Inibidores de Ciclo-Oxigenase/síntese química
Inibidores de Ciclo-Oxigenase/química
Relação Dose-Resposta a Droga
Feminino
Seres Humanos
Inibidores de Lipoxigenase/síntese química
Inibidores de Lipoxigenase/química
Macrófagos/efeitos dos fármacos
Simulação de Acoplamento Molecular
Estrutura Molecular
Quinazolinonas/síntese química
Quinazolinonas/química
Ratos
Ratos Wistar
Relação Estrutura-Atividade
Compostos de Sulfidrila/síntese química
Compostos de Sulfidrila/química
Células Tumorais Cultivadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Cyclooxygenase Inhibitors); 0 (Lipoxygenase Inhibitors); 0 (Quinazolinones); 0 (Sulfhydryl Compounds); EC 1.13.11.33 (Arachidonate 15-Lipoxygenase); EC 1.14.99.1 (Cyclooxygenase 1); EC 1.14.99.1 (Cyclooxygenase 2); EC 1.14.99.1 (PTGS1 protein, human); EC 1.14.99.1 (PTGS2 protein, human)
[Em] Mês de entrada:1803
[Cu] Atualização por classe:180302
[Lr] Data última revisão:
180302
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180101
[St] Status:MEDLINE



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