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[PMID]:29328639
[Au] Autor:Dubovina D; Mihailovic B; Bukumiric Z; Vlahovic Z; Miladinovic M; Mikovic N; Lazic Z
[Ti] Título:The use of hyaluronic and aminocaproic acid in the treatment of alveolar osteitis.
[So] Source:Vojnosanit Pregl;73(11):1010-5, 2016 Nov.
[Is] ISSN:0042-8450
[Cp] País de publicação:Serbia
[La] Idioma:eng
[Ab] Resumo:Background/Aim: Alveolar osteitis (AO), also known as "dry socket", is relatively common post-extraction complication. It probably occurs due to excessive fibrinolytic activity in the coagulum and is characterized by intense pain sensations. The aim of this clinical study was to examine the role of hyaluronic acid and aminocaproic acid in the treatment of AO. Methods: The study included 60 patients with the clinical diagnosis of AO. All the patients were divided into two groups of 30 patients each according to the applied non-pharmacological measure: irrigation ­ irrigation of dry socket with sterile saline; curettage ­ careful curettage. Both of these groups were further divided into three subgroups regarding the applied treatment (hyaluronic acid; hyaluronic acid + aminocaproic acid; Alvogyl ®, an anesthetic and antiseptic paste), each with 10 patients, according to the following protocol: 0.2 mL of hyaluronic acid in the form of a 0.8% gel; 2 mL of aminocaproic acid and hyaluronic acid; Alvogyl®. During each visit, scheduled for every two days until complete absence of painful sensations, the patients had the therapeutic method repeated as at the first examination. At each control visit the number of present symptoms and signs of AO was recorded, as well as the level of pain (measured with a visual analogue scale). Results: With the use of hyaluronic acid, with or without aminocaproic one, a statistically significantly faster reduction in pain sensations was achieved, along with the reduction in the number of symptoms and signs of AO compared to the use of Alvogyl®. Conclusion: Hyaluronic acid, applied alone or in combination with aminocaproic acid significantly reduces pain sensation, thus it can be successfully used in the treatment of AO.
[Mh] Termos MeSH primário: Ácido Aminocaproico/uso terapêutico
Analgésicos/uso terapêutico
Alvéolo Seco/tratamento farmacológico
Eugenol/uso terapêutico
Dor Facial/prevenção & controle
Ácido Hialurônico/uso terapêutico
Hidrocarbonetos Iodados/uso terapêutico
Óleos Voláteis/uso terapêutico
para-Aminobenzoatos/uso terapêutico
[Mh] Termos MeSH secundário: Adulto
Ácido Aminocaproico/efeitos adversos
Analgésicos/efeitos adversos
Curetagem/efeitos adversos
Combinação de Medicamentos
Alvéolo Seco/diagnóstico
Eugenol/efeitos adversos
Dor Facial/diagnóstico
Dor Facial/etiologia
Dor Facial/fisiopatologia
Feminino
Seres Humanos
Ácido Hialurônico/efeitos adversos
Hidrocarbonetos Iodados/efeitos adversos
Masculino
Meia-Idade
Óleos Voláteis/efeitos adversos
Medição da Dor
Percepção da Dor/efeitos dos fármacos
Limiar da Dor/efeitos dos fármacos
Estudos Prospectivos
Sérvia
Irrigação Terapêutica
Fatores de Tempo
Resultado do Tratamento
para-Aminobenzoatos/efeitos adversos
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Analgesics); 0 (Drug Combinations); 0 (Hydrocarbons, Iodinated); 0 (Oils, Volatile); 0 (butyl aminobenzoate, eugenol, iodoform, spearmint oil drug combinations); 0 (para-Aminobenzoates); 3T8H1794QW (Eugenol); 9004-61-9 (Hyaluronic Acid); U6F3787206 (Aminocaproic Acid)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180213
[Lr] Data última revisão:
180213
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180113
[St] Status:MEDLINE
[do] DOI:10.2298/VSP150304125D


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[PMID]:29232553
[Au] Autor:Pan R; Ruvolo V; Mu H; Leverson JD; Nichols G; Reed JC; Konopleva M; Andreeff M
[Ad] Endereço:Section of Molecular Hematology and Therapy, Department of Leukemia, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA.
[Ti] Título:Synthetic Lethality of Combined Bcl-2 Inhibition and p53 Activation in AML: Mechanisms and Superior Antileukemic Efficacy.
[So] Source:Cancer Cell;32(6):748-760.e6, 2017 Dec 11.
[Is] ISSN:1878-3686
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Evasion of apoptosis is a hallmark of cancer. Bcl-2 and p53 represent two important nodes in apoptosis signaling pathways. We find that concomitant p53 activation and Bcl-2 inhibition overcome apoptosis resistance and markedly prolong survival in three mouse models of resistant acute myeloid leukemia (AML). Mechanistically, p53 activation negatively regulates the Ras/Raf/MEK/ERK pathway and activates GSK3 to modulate Mcl-1 phosphorylation and promote its degradation, thus overcoming AML resistance to Bcl-2 inhibition. Moreover, Bcl-2 inhibition reciprocally overcomes apoptosis resistance to p53 activation by switching cellular response from G arrest to apoptosis. The efficacy, together with the mechanistic findings, reveals the potential of simultaneously targeting these two apoptosis regulators and provides a rational basis for clinical testing of this therapeutic approach.
[Mh] Termos MeSH primário: Protocolos de Quimioterapia Combinada Antineoplásica/farmacologia
Resistência a Medicamentos Antineoplásicos/efeitos dos fármacos
Leucemia Mieloide Aguda/patologia
Proteínas Proto-Oncogênicas c-bcl-2/antagonistas & inibidores
Mutações Sintéticas Letais/efeitos dos fármacos
Proteína Supressora de Tumor p53/metabolismo
[Mh] Termos MeSH secundário: Animais
Apoptose/efeitos dos fármacos
Compostos Bicíclicos Heterocíclicos com Pontes/farmacologia
Linhagem Celular Tumoral
Feminino
Seres Humanos
Camundongos
Camundongos Endogâmicos NOD
Camundongos SCID
Pirrolidinas/farmacologia
Sulfonamidas/farmacologia
Ensaios Antitumorais Modelo de Xenoenxerto
para-Aminobenzoatos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (Proto-Oncogene Proteins c-bcl-2); 0 (Pyrrolidines); 0 (RG7388); 0 (Sulfonamides); 0 (Tumor Suppressor Protein p53); 0 (para-Aminobenzoates); N54AIC43PW (venetoclax)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171220
[Lr] Data última revisão:
171220
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171213
[St] Status:MEDLINE


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[PMID]:28877280
[Au] Autor:Epasinghe DJ; Yiu CKY; Burrow MF
[Ad] Endereço:Prince Philip Dental Hospital, University of Hong Kong, Faculty of Dentistry, Hong Kong SAR, China.
[Ti] Título:Mechanical properties, water sorption characteristics, and compound release of grape seed extract-incorporated resins.
[So] Source:J Appl Oral Sci;25(4):412-419, 2017 Jul-Aug.
[Is] ISSN:1678-7765
[Cp] País de publicação:Brazil
[La] Idioma:eng
[Ab] Resumo:Objective: This study evaluated the effect of grape seed extract (GSE) incorporation on the mechanical properties, water sorption, solubility, and GSE release from the experimental adhesive resins. Material and Methods: An experimental comonomer mixture, consisting of 40% Bis-GMA, 30% Bis MP, 28% HEMA, 0.26% camphorquinone and 1% EDMAB, was used to prepare four GSE-incorporated adhesive resins at concentrations of 0.5, 1, 1.5, and 2 wt%. The neat resin without GSE was used as the control. Six resin beams (25 mm x 2 mm x 2 mm) per group were prepared for flexural strength and modulus of elasticity evaluations using a universal testing machine at a crosshead speed of 1 mm/min. Five disks (6 mm in diameter and 2 mm in thickness) per group were used for microhardness measurements using a Leitz micro-hardness tester with Leica Qgo software. Five disks (7 mm in diameter and 2 mm in thickness) per group were prepared and stored in deionized water for 28 days. Water sorption, solubility, and GSE release in deionized water were calculated for each GSE-incorporated adhesive at the end of 28th day. Data was evaluated using one-way ANOVA and Tukey multiple comparisons. Results: Flexural strength, modulus of elasticity and microhardness of GSE-incorporated adhesive decreased significantly with incorporation of 1.5% of GSE (p<0.05). Addition of GSE had no effect on the water sorption of the adhesive resins (p=0.33). The solubility of the resin also increased significantly with incorporation of 1.5% of GSE (p<0.05). Quantities of GSE release increased with increased concentration of GSE in the adhesive resin. Conclusion: Up to 1% of GSE can be incorporated into a dental adhesive resin without interfering with the mechanical properties or solubility of the resins.
[Mh] Termos MeSH primário: Bis-Fenol A-Glicidil Metacrilato/química
Cânfora/análogos & derivados
Extrato de Sementes de Uva/química
Metacrilatos/química
Cimentos de Resina/química
para-Aminobenzoatos/química
[Mh] Termos MeSH secundário: Análise de Variância
Cânfora/química
Módulo de Elasticidade
Testes de Dureza
Teste de Materiais
Maleabilidade
Proantocianidinas/química
Valores de Referência
Reprodutibilidade dos Testes
Solubilidade
Estatísticas não Paramétricas
Fatores de Tempo
Água/química
[Pt] Tipo de publicação:EVALUATION STUDIES; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Grape Seed Extract); 0 (Methacrylates); 0 (Proanthocyanidins); 0 (Resin Cements); 0 (ethyl 4-N,N-dimethylaminobenzoate); 0 (para-Aminobenzoates); 059QF0KO0R (Water); 18206-61-6 (proanthocyanidin); 454I75YXY0 (Bisphenol A-Glycidyl Methacrylate); 6E1I4IV47V (hydroxyethyl methacrylate); 76-22-2 (Camphor); RAL3591W33 (camphorquinone)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171006
[Lr] Data última revisão:
171006
[Sb] Subgrupo de revista:D; IM
[Da] Data de entrada para processamento:170907
[St] Status:MEDLINE


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[PMID]:28596292
[Au] Autor:Kistemaker LEM; Oenema TA; Baarsma HA; Bos IST; Schmidt M; Facchinetti F; Civelli M; Villetti G; Gosens R
[Ad] Endereço:Department of Molecular Pharmacology, University of Groningen, The Netherlands; l.e.m.kistemaker@rug.nl.
[Ti] Título:The PDE4 inhibitor CHF-6001 and LAMAs inhibit bronchoconstriction-induced remodeling in lung slices.
[So] Source:Am J Physiol Lung Cell Mol Physiol;313(3):L507-L515, 2017 Sep 01.
[Is] ISSN:1522-1504
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Combination therapy of PDE4 inhibitors and anticholinergics induces bronchoprotection in COPD. Mechanical forces that arise during bronchoconstriction may contribute to airway remodeling. Therefore, we investigated the impact of PDE4 inhibitors and anticholinergics on bronchoconstriction-induced remodeling. Because of the different mechanism of action of PDE4 inhibitors and anticholinergics, we hypothesized functional interactions of these two drug classes. Guinea pig precision-cut lung slices were preincubated with the PDE4 inhibitors CHF-6001 or roflumilast and/or the anticholinergics tiotropium or glycopyorrolate, followed by stimulation with methacholine (10 µM) or TGF-ß (2 ng/ml) for 48 h. The inhibitory effects on airway smooth muscle remodeling, airway contraction, and TGF-ß release were investigated. Methacholine-induced protein expression of smooth muscle-myosin was fully inhibited by CHF-6001 (0.3-100 nM), whereas roflumilast (1 µM) had smaller effects. Tiotropium and glycopyrrolate fully inhibited methacholine-induced airway remodeling (0.1-30 nM). The combination of CHF-6001 and tiotropium or glycopyrrolate, in concentrations partially effective by themselves, fully inhibited methacholine-induced remodeling in combination. CHF-6001 did not affect airway closure and had limited effects on TGF-ß -induced remodeling, but rather, it inhibited methacholine-induced TGF-ß release. The PDE4 inhibitor CHF-6001, and to a lesser extent roflumilast, and the LAMAs tiotropium and glycopyrrolate inhibit bronchoconstriction-induced remodeling. The combination of CHF-6001 and anticholinergics was more effective than the individual compounds. This cooperativity might be explained by the distinct mechanisms of action inhibiting TGF-ß release and bronchoconstriction.
[Mh] Termos MeSH primário: Remodelação das Vias Aéreas/efeitos dos fármacos
Broncoconstrição/efeitos dos fármacos
Antagonistas Colinérgicos/farmacologia
Nucleotídeo Cíclico Fosfodiesterase do Tipo 4/metabolismo
Pulmão/efeitos dos fármacos
Pulmão/fisiopatologia
Inibidores da Fosfodiesterase 4/farmacologia
Sulfonamidas/farmacologia
para-Aminobenzoatos/farmacologia
[Mh] Termos MeSH secundário: Aminopiridinas
Animais
Benzamidas
Ciclopropanos
Interações Medicamentosas
Glicopirrolato/farmacologia
Cobaias
Masculino
Cloreto de Metacolina/farmacologia
Brometo de Tiotrópio/farmacologia
Fator de Crescimento Transformador beta/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (3,5-dichloro-4-(2-(3-(cyclopropylmethoxy)-4-(difluoromethoxy)phenyl)-2-(3-(cyclopropylmethoxy)-4-(methylsulfonamido)benzoyloxy)ethyl)pyridine 1-oxide); 0 (Aminopyridines); 0 (Benzamides); 0 (Cholinergic Antagonists); 0 (Cyclopropanes); 0 (Phosphodiesterase 4 Inhibitors); 0 (Sulfonamides); 0 (Transforming Growth Factor beta); 0 (para-Aminobenzoates); 0P6C6ZOP5U (Roflumilast); 0W5ETF9M2K (Methacholine Chloride); EC 3.1.4.17 (Cyclic Nucleotide Phosphodiesterases, Type 4); V92SO9WP2I (Glycopyrrolate); XX112XZP0J (Tiotropium Bromide)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170918
[Lr] Data última revisão:
170918
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170610
[St] Status:MEDLINE
[do] DOI:10.1152/ajplung.00069.2017


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[PMID]:28391487
[Au] Autor:Giraldo A; Montes R; Rodil R; Quintana JB; Vidal-Liñán L; Beiras R
[Ad] Endereço:Toralla Marine Station (ECIMAT), University of Vigo, 36331, Vigo, Galicia, Spain. aritzgiraldo@gmail.com.
[Ti] Título:Ecotoxicological Evaluation of the UV Filters Ethylhexyl Dimethyl p-Aminobenzoic Acid and Octocrylene Using Marine Organisms Isochrysis galbana, Mytilus galloprovincialis and Paracentrotus lividus.
[So] Source:Arch Environ Contam Toxicol;72(4):606-611, 2017 May.
[Is] ISSN:1432-0703
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The growing concern regarding the negative effects of solar radiation on the skin has led to a drastic increase in the use of sunscreens containing in its composition up to 10% of aromatic chemicals, such as ethylhexyl dimethyl p-aminobenzoic acid (OD-PABA) and octocrylene (OC). The objective of this study was to evaluate the toxicity and to assess the environmental risk posed by these two ultraviolet filters, widely used in cosmetics and as plastic additives, in the marine environment. Several ecotoxicological bioassays were performed with three model organisms belonging to different trophic levels: the microalgae Isochrysis galbana, the mussel Mytilus galloprovincialis, and the sea urchin Paracentrotus lividus. The results show remarkable toxicity to marine species for both OD-PABA (EC values range 26,5-127 µg L ) and OC (EC range 103-511 µg L ). The cell division in the microalgae I. galbana was the most sensitive endpoint tested. To determine the environmental risk of these substances, the risk coefficient (RQ) was calculated. Due to the higher concentrations reported, OC showed remarkable risk (RQ = 0.27), whereas for OD-PABA the risk was low (RQ = 0.007).
[Mh] Termos MeSH primário: Acrilatos/toxicidade
Organismos Aquáticos/fisiologia
Protetores Solares/toxicidade
Testes de Toxicidade/métodos
Poluentes Químicos da Água/toxicidade
para-Aminobenzoatos/toxicidade
[Mh] Termos MeSH secundário: Animais
Monitoramento Ambiental
Haptófitas
Mytilus
Paracentrotus
Medição de Risco
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acrylates); 0 (Sunscreening Agents); 0 (Water Pollutants, Chemical); 0 (para-Aminobenzoates); 5A68WGF6WM (octocrylene); Z11006CMUZ (padimate-O)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170713
[Lr] Data última revisão:
170713
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170410
[St] Status:MEDLINE
[do] DOI:10.1007/s00244-017-0399-4


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[PMID]:28343007
[Au] Autor:Ma B; Lu G; Liu J; Yan Z; Yang H; Pan T
[Ad] Endereço:Key Laboratory of Integrated Regulation and Resources Development of Shallow Lakes of Ministry of Education, College of Environment, Hohai University, Nanjing 210098, China.
[Ti] Título:Bioconcentration and multi-biomarkers of organic UV filters (BM-DBM and OD-PABA) in crucian carp.
[So] Source:Ecotoxicol Environ Saf;141:178-187, 2017 Jul.
[Is] ISSN:1090-2414
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Organic UV filters (OUV-Fs) are increasingly used in sunscreens and personal care products. In the present work, the bioconcentration and multi-biomarker effects of butyl methoxydibenzoylmethane (BM-DBM) and ethylhexyl dimethyl p-aminobenzoate (OD-PABA) were investigated in crucian carp (Carassius auratus). The fish were exposed to various concentrations of BM-DBM (3.88, 35.61, 181.85 and 337.15µg/L), OD-PABA (4.66, 53.83, 264.22 and 459.32µg/L) and their mixture (2.31+2.79, 23.69+26.18, 97.37+134.81 and 193.93+246.08µg/L) for 28 days. The maximal concentrations of two OUV-Fs were detected in the fish liver, followed by the brain, kidney, gill and muscle in most cases. The maximal BCF values of OD-PABA calculated in various exposure concentrations were 0.37 - 101.21 in single exposure groups and 0.11 - 31.09 in mixed exposure groups. Acetylcholinesterase (AChE) activity was significantly inhibited by BM-DBM as well as the mixtures at all of the exposure concentrations and by OD-PABA at higher concentrations (≥264.22µg/L) during 28 days of exposure. The maximal inhibition rates of AChE activity reached 64.04% for BM-DBM, 41.05% for OD-PABA and 61.50% for the mixtures at the highest concentration, which indicated that these two OUV-Fs might damage the central nervous system. Concerning oxidative stress status, BM-DBM and the mixtures significantly increased superoxide dismutase (SOD) and glutathione reductase (GR) activities and inhibited catalase (CAT) activity, while OD-PABA caused a significant increase of GR and CAT activities. AChE and GR activities seemed to be more sensitive biomarkers for BM-DBM and OD-PABA.
[Mh] Termos MeSH primário: Alcanos/análise
Chalconas/análise
Carpa Dourada/metabolismo
Protetores Solares/análise
Poluentes Químicos da Água/análise
para-Aminobenzoatos/análise
[Mh] Termos MeSH secundário: Alcanos/farmacocinética
Alcanos/toxicidade
Animais
Biomarcadores/metabolismo
Encéfalo/efeitos dos fármacos
Encéfalo/enzimologia
Chalconas/farmacocinética
Chalconas/toxicidade
Relação Dose-Resposta a Droga
Brânquias/efeitos dos fármacos
Brânquias/metabolismo
Fígado/efeitos dos fármacos
Fígado/enzimologia
Estresse Oxidativo/efeitos dos fármacos
Propiofenonas
Protetores Solares/farmacocinética
Protetores Solares/toxicidade
Distribuição Tecidual
Poluentes Químicos da Água/farmacocinética
Poluentes Químicos da Água/toxicidade
para-Aminobenzoatos/farmacocinética
para-Aminobenzoatos/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Alkanes); 0 (Biomarkers); 0 (Chalcones); 0 (Propiophenones); 0 (Sunscreening Agents); 0 (Water Pollutants, Chemical); 0 (para-Aminobenzoates); G63QQF2NOX (avobenzone); Z11006CMUZ (padimate-O)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170327
[St] Status:MEDLINE


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[PMID]:28270519
[Au] Autor:Honjo K; Munakata S; Tashiro Y; Salama Y; Shimazu H; Eiamboonsert S; Dhahri D; Ichimura A; Dan T; Miyata T; Takeda K; Sakamoto K; Hattori K; Heissig B
[Ad] Endereço:Division of Stem Cell Dynamics, Center for Stem Cell Biology and Regenerative Medicine, The Institute of Medical Science, The University of Tokyo, Tokyo, Japan.
[Ti] Título:Plasminogen activator inhibitor-1 regulates macrophage-dependent postoperative adhesion by enhancing EGF-HER1 signaling in mice.
[So] Source:FASEB J;31(6):2625-2637, 2017 Jun.
[Is] ISSN:1530-6860
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Adhesive small bowel obstruction remains a common problem for surgeons. After surgery, platelet aggregation contributes to coagulation cascade and fibrin clot formation. With clotting, fibrin degradation is simultaneously enhanced, driven by tissue plasminogen activator-mediated cleavage of plasminogen to form plasmin. The aim of this study was to investigate the cellular events and proteolytic responses that surround plasminogen activator inhibitor (PAI-1; ) inhibition of postoperative adhesion. Peritoneal adhesion was induced by gauze deposition in the abdominal cavity in C57BL/6 mice and those that were deficient in fibrinolytic factors, such as and In addition, C57BL/6 mice were treated with the novel PAI-1 inhibitor, TM5275. Some animals were treated with clodronate to deplete macrophages. Epidermal growth factor (EGF) experiments were performed to understand the role of macrophages and how EGF contributes to adhesion. In the early phase of adhesive small bowel obstruction, increased PAI-1 activity was observed in the peritoneal cavity. Genetic and pharmacologic PAI-1 inhibition prevented progression of adhesion and increased circulating plasmin. Whereas Serpine1 mice showed intra-abdominal bleeding, mice that were treated with TM5275 did not. Mechanistically, PAI-1, in combination with tissue plasminogen activator, served as a chemoattractant for macrophages that, in turn, secreted EGF and up-regulated the receptor, HER1, on peritoneal mesothelial cells, which led to PAI-1 secretion, further fueling the vicious cycle of impaired fibrinolysis at the adhesive site. Controlled inhibition of PAI-1 not only enhanced activation of the fibrinolytic system, but also prevented recruitment of EGF-secreting macrophages. Pharmacologic PAI-1 inhibition ameliorated adhesion formation in a macrophage-dependent manner.-Honjo, K., Munakata, S., Tashiro, Y., Salama, Y., Shimazu, H., Eiamboonsert, S., Dhahri, D., Ichimura, A., Dan, T., Miyata, T., Takeda, K., Sakamoto, K., Hattori, K., Heissig, B. Plasminogen activator inhibitor-1 regulates macrophage-dependent postoperative adhesion by enhancing EGF-HER1 signaling in mice.
[Mh] Termos MeSH primário: Macrófagos/fisiologia
Piperazinas/uso terapêutico
Receptor do Fator de Crescimento Epidérmico/metabolismo
Serpina E2/antagonistas & inibidores
Aderências Teciduais/patologia
para-Aminobenzoatos/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Antígeno CD11b
Ensaios de Migração Celular
Movimento Celular/efeitos dos fármacos
Cetuximab/farmacologia
Fator de Crescimento Epidérmico
Regulação da Expressão Gênica/fisiologia
Camundongos
Camundongos Endogâmicos C57BL
Complicações Pós-Operatórias/prevenção & controle
Células RAW 264.7
Receptor do Fator de Crescimento Epidérmico/genética
Serpina E2/genética
Serpina E2/metabolismo
Transdução de Sinais
Aderências Teciduais/metabolismo
Ativador de Plasminogênio Tecidual/genética
Ativador de Plasminogênio Tecidual/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (5-chloro-2-(((2-(4-(diphenylmethyl)piperazin-1-yl)-2-oxoethoxy)acetyl)amino)benzoate); 0 (CD11b Antigen); 0 (Piperazines); 0 (Serpin E2); 0 (Serpine2 protein, mouse); 0 (para-Aminobenzoates); 62229-50-9 (Epidermal Growth Factor); EC 2.7.10.1 (Receptor, Epidermal Growth Factor); EC 3.4.21.68 (Tissue Plasminogen Activator); PQX0D8J21J (Cetuximab)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170309
[St] Status:MEDLINE
[do] DOI:10.1096/fj.201600871RR


  8 / 826 MEDLINE  
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[PMID]:28224182
[Au] Autor:Zakaria EM; El-Maraghy NN; Ahmed AF; Ali AA; El-Bassossy HM
[Ad] Endereço:Department of Pharmacology, Faculty of Pharmacy, Zagazig University, P.O. Box 44519, Zagazig, Egypt. emzakaria@zu.edu.eg.
[Ti] Título:PARP inhibition ameliorates nephropathy in an animal model of type 2 diabetes: focus on oxidative stress, inflammation, and fibrosis.
[So] Source:Naunyn Schmiedebergs Arch Pharmacol;390(6):621-631, 2017 Jun.
[Is] ISSN:1432-1912
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Poly(ADP-ribose) polymerase (PARP) enzyme contributes to nephropathy, a serious diabetic complication which may lead to end-stage renal disease. The study aims to investigate the effect of PARP over-activation on kidney functions in a type 2 diabetic rat model. The study also tests the therapeutic use of PARP inhibitors in diabetic nephropathy. Type 2 diabetes was induced in adult male rats by high-fructose/high-fat diet and low streptozotocin dose. Then, the PARP inhibitor 4-aminobenzamide (4-AB) was administered daily for 10 weeks. At the end, urine samples were collected to measure urine creatinine, albumin, and total proteins. PARP activity, superoxide dismutase (SOD) activity, and nitrite content were measured in kidney tissue homogenate. Glucose, fructosamine, insulin, and tumor necrosis factor-alpha (TNF-α) were measured in serum. Furthermore, histological studies, collagen deposition, and immunofluorescence of nuclear factor kappa B (NFκB) and transforming growth factor beta1 (TGF-ß1) were carried out. PARP enzyme activity was significantly higher in the diabetic group and was significantly reduced by 4-AB administration. Diabetic animals had clear nephropathy indicated by proteinuria and increased albumin excretion rate (AER) which were significantly decreased by PARP inhibition. In addition, PARP inhibition increased creatinine clearance in diabetic animals and reduced renal TGF-ß1 and glomerular fibrosis. Moreover, PARP inhibition alleviated the elevated serum TNF-α level, renal NFκB, nitrite, and the decrease in SOD activity in diabetic animals. However, PARP inhibition did not significantly affect neither hyperglycemia nor insulin sensitivity. PARP enzyme inhibition alleviates diabetic nephropathy through decreasing inflammation, oxidative stress, and renal fibrosis.
[Mh] Termos MeSH primário: Diabetes Mellitus Experimental/tratamento farmacológico
Diabetes Mellitus Tipo 2/tratamento farmacológico
Nefropatias Diabéticas/tratamento farmacológico
Inibidores de Poli(ADP-Ribose) Polimerases/farmacologia
[Mh] Termos MeSH secundário: Animais
Benzamidas/farmacologia
Diabetes Mellitus Experimental/complicações
Diabetes Mellitus Tipo 2/complicações
Nefropatias Diabéticas/patologia
Dieta Hiperlipídica
Fibrose/tratamento farmacológico
Fibrose/patologia
Inflamação/tratamento farmacológico
Inflamação/patologia
Masculino
NF-kappa B/metabolismo
Estresse Oxidativo/efeitos dos fármacos
Poli(ADP-Ribose) Polimerases/efeitos dos fármacos
Poli(ADP-Ribose) Polimerases/metabolismo
Ratos
Ratos Sprague-Dawley
Estreptozocina/toxicidade
Superóxido Dismutase/metabolismo
Fator de Necrose Tumoral alfa/sangue
para-Aminobenzoatos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzamides); 0 (NF-kappa B); 0 (Poly(ADP-ribose) Polymerase Inhibitors); 0 (Tumor Necrosis Factor-alpha); 0 (para-Aminobenzoates); 5W494URQ81 (Streptozocin); 77722I6PAC (4-aminobenzamide); EC 1.15.1.1 (Superoxide Dismutase); EC 2.4.2.30 (Poly(ADP-ribose) Polymerases)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171108
[Lr] Data última revisão:
171108
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170223
[St] Status:MEDLINE
[do] DOI:10.1007/s00210-017-1360-9


  9 / 826 MEDLINE  
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[PMID]:28223019
[Au] Autor:Wang M; Gao M; Xu Z; Zheng QH
[Ad] Endereço:Department of Radiology and Imaging Sciences, Indiana University School of Medicine, 1345 West 16th Street, Room 202, Indianapolis, IN 46202, USA.
[Ti] Título:Synthesis of [ C]HG-10-102-01 as a new potential PET agent for imaging of LRRK2 enzyme in Parkinson's disease.
[So] Source:Bioorg Med Chem Lett;27(6):1351-1355, 2017 03 15.
[Is] ISSN:1464-3405
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The reference standard (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone (HG-10-102-01) and its precursor (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-hydroxyphenyl)(morpholino)methanone (desmethyl-HG-10-102-01) were synthesized from 2,4,5-trichloropyrimide and 3-methoxy-4-nitrobenzoic acid with overall chemical yield 49% in four steps and 14% in five steps, respectively. The target tracer (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-[ C]methoxyphenyl)(morpholino)methanone ([ C]HG-10-102-01) was prepared from the precursor desmethyl-HG-10-102-01 with [ C]CH OTf through O-[ C]methylation and isolated by HPLC combined with SPE in 45-55% radiochemical yield, based on [ C]CO and decay corrected to end of bombardment (EOB). The radiochemical purity was >99%, and the specific activity (SA) at EOB was 370-1110GBq/µmol with a total synthesis time of ∼40-min from EOB.
[Mh] Termos MeSH primário: Serina-Treonina Proteína Quinase-2 com Repetições Ricas em Leucina/metabolismo
Doença de Parkinson/enzimologia
Tomografia por Emissão de Pósitrons
Pirimidinas/síntese química
para-Aminobenzoatos/síntese química
[Mh] Termos MeSH secundário: Seres Humanos
Compostos Radiofarmacêuticos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
0 (HG-10-102-01); 0 (Pyrimidines); 0 (Radiopharmaceuticals); 0 (para-Aminobenzoates); EC 2.7.11.1 (LRRK2 protein, human); EC 2.7.11.1 (Leucine-Rich Repeat Serine-Threonine Protein Kinase-2)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171124
[Lr] Data última revisão:
171124
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170223
[St] Status:MEDLINE


  10 / 826 MEDLINE  
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[PMID]:28133704
[Au] Autor:Studzinski W; Gackowska A; Przybylek M; Gaca J
[Ad] Endereço:Faculty of Chemical Technology and Engineering, University of Technology and Life Sciences, Seminaryjna 3, 85-326, Bydgoszcz, Poland.
[Ti] Título:Studies on the formation of formaldehyde during 2-ethylhexyl 4-(dimethylamino)benzoate demethylation in the presence of reactive oxygen and chlorine species.
[So] Source:Environ Sci Pollut Res Int;24(9):8049-8061, 2017 Mar.
[Is] ISSN:1614-7499
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:In order to protect the skin from UV radiation, personal care products (PCPS) often contain chemical UV-filters. These compounds can enter the environment causing serious consequences on the water ecosystems. The aim of this study was to examine, the effect of different factors, such as UV light, the presence of NaOCl and H O on the formaldehyde formation during popular UV filter, 2-ethylhexyl 4-(dimethylamino)benzoate (ODPABA) demethylation. The concentration of formaldehyde was determined by VIS spectrophotometry after derivatization. The reaction mixtures were qualitatively analyzed using GC/MS chromatography. The highest concentration of formaldehyde was observed in the case of ODPABA/H O /UV reaction mixture. In order to describe two types of demethylation mechanisms, namely, radical and ionic, the experimental results were enriched with Fukui function analysis and thermodynamic calculations. In the case of non-irradiated system containing ODPABA and NaOCl, demethylation reaction probably proceeds via ionic mechanism. As it was established, amino nitrogen atom in the ODPABA molecule is the most susceptible site for the HOCl electrophilic attack, which is the first step of ionic demethylation mechanism. In the case of irradiated mixtures, the reaction is probably radical in nature. The results of thermodynamic calculations showed that abstraction of the hydrogen from N(CH ) group is more probable than from 2-ethylhexyl moiety, which indicates higher susceptibility of N(CH ) to the oxidation.
[Mh] Termos MeSH primário: Cloro/química
Formaldeído/química
Peróxido de Hidrogênio/química
Protetores Solares
Raios Ultravioleta
Poluentes Químicos da Água
para-Aminobenzoatos
[Mh] Termos MeSH secundário: Cromatografia Gasosa-Espectrometria de Massas
Protetores Solares/química
Protetores Solares/efeitos da radiação
Poluentes Químicos da Água/química
Poluentes Químicos da Água/efeitos da radiação
para-Aminobenzoatos/química
para-Aminobenzoatos/efeitos da radiação
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Sunscreening Agents); 0 (Water Pollutants, Chemical); 0 (para-Aminobenzoates); 1HG84L3525 (Formaldehyde); 4R7X1O2820 (Chlorine); BBX060AN9V (Hydrogen Peroxide); Z11006CMUZ (padimate-O)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:170531
[Lr] Data última revisão:
170531
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170131
[St] Status:MEDLINE
[do] DOI:10.1007/s11356-017-8477-8



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