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[PMID]:29031450
[Au] Autor:Li H; Cao L; Yang C; Zhang Z; Zhang B; Deng K
[Ad] Endereço:Key Laboratory of Catalysis and Material Sciences of the State Ethnic Affairs Commission & Ministry of Education, College of Chemistry and Material Science, South-Central University For Nationalities, Wuhan 430074, China.
[Ti] Título:Selective oxidation of benzyl alcohols to benzoic acid catalyzed by eco-friendly cobalt thioporphyrazine catalyst supported on silica-coated magnetic nanospheres.
[So] Source:J Environ Sci (China);60:84-90, 2017 Oct.
[Is] ISSN:1001-0742
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:A novel magnetically recoverable thioporphyrazine catalyst (CoPz(S-Bu) /SiO @Fe O ) was prepared by immobilization of the cobalt octkis(butylthio) porphyrazine complex (CoPz(S-Bu) ) on silica-coated magnetic nanospheres (SiO @Fe O ). The composite CoPz(S-Bu) /SiO @Fe O appeared to be an active catalyst in the oxidation of benzyl alcohol in aqueous solution using hydrogen peroxide (H O ) as oxidant under Xe-lamp irradiation, with 36.4% conversion of benzyl alcohol, about 99% selectivity for benzoic acid and turnover number (TON) of 61.7 at ambient temperature. The biomimetic catalyst CoPz(S-Bu) was supported on the magnetic carrier SiO @Fe O so as to suspend it in aqueous solution to react with substrates, utilizing its lipophilicity. Meanwhile the CoPz(S-Bu) can use its unique advantages to control the selectivity of photocatalytic oxidation without the substrate being subjected to deep oxidation. The influence of various reaction parameters on the conversion rate of benzyl alcohol and selectivity of benzoic acid was investigated in detail. Moreover, photocatalytic oxidation of substituted benzyl alcohols was obtained with high conversion and excellent selectivity, specifically conversion close to 70%, selectivity close to 100% and TON of 113.6 for para-position electron-donating groups. The selectivity and eco-friendliness of the biomimetic photocatalyst give it great potential for practical applications.
[Mh] Termos MeSH primário: Ácido Benzoico/química
Álcoois Benzílicos/química
Modelos Químicos
Nanosferas/química
[Mh] Termos MeSH secundário: Catálise
Peróxido de Hidrogênio
Magnetismo
Oxirredução
Dióxido de Silício
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzyl Alcohols); 7631-86-9 (Silicon Dioxide); 8SKN0B0MIM (Benzoic Acid); BBX060AN9V (Hydrogen Peroxide)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171019
[Lr] Data última revisão:
171019
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171017
[St] Status:MEDLINE


  2 / 1852 MEDLINE  
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[PMID]:28750276
[Au] Autor:Kite GC; Hetterscheid WLA
[Ad] Endereço:Royal Botanic Gardens, Kew, Richmond, Surrey TW9 3AB, UK. Electronic address: g.kite@kew.org.
[Ti] Título:Phylogenetic trends in the evolution of inflorescence odours in Amorphophallus.
[So] Source:Phytochemistry;142:126-142, 2017 Oct.
[Is] ISSN:1873-3700
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The chemical composition of inflorescence odours of 80 species of Amorphophallus (Araceae) were determined by headspace-thermal desorption GC-MS. When compared to published molecular phylogenies of the genus, the data reveal evidence both of phylogenetic constraint and plasticity of odours. Dimethyl oligosulphides were found as common constituents of Amorphophallus odours and were the most abundant components in almost half of the species studied. Odours composed mainly of dimethyl oligosulphides, and perceived as being 'gaseous', were only found among Asian species, and some of these species clustered in certain clades in molecular phylogenies; e.g. in two clades in Amorphophallus subgenus Metandrium. However, some species with gaseous odours were found to be closely related to species producing odours more reminiscent of rotting meat in which various minor components accompany the dominant dimethyl oligosulphides. These two broad types of odours have co-evolved with other inflorescence characteristics such as colour, with species with rotting meat odours having darker inflorescences. Species producing pleasant odours characterised by benzenoid compounds constitute two broad groups that are not related in published phylogenies. Species having fruity odours containing 1-phenylethanol derivatives mainly occur in a clade in subgenus Metandrium while those with anise odours composed almost solely of the 2-phenylethanol derivative 4-methoxyphenethyl alcohol are restricted to a clade in subgenus Scutandrium. Phylogenetic mapping of odours also indicates that the evolution of some odour types is likely to have been influenced by ecological factors. For example, species producing fishy odours dominated by trimethylamine and occurring in N and NE Borneo are not all closely related. Conversely, two sister species, A. mossambicensis and A. abyssinicus, which are morphologically very similar and have overlapping geographical distribution, produce odours which are very different chemically. The pressure of pollinator resource has therefore been a factor influencing the evolution of odours in Amorphophallus, driving both the divergence of odour types in some taxa and the convergence of odour types in others.
[Mh] Termos MeSH primário: Amorphophallus/química
Amorphophallus/genética
Odorantes
[Mh] Termos MeSH secundário: Álcoois Benzílicos/análise
Álcoois Benzílicos/química
Ecologia
Evolução Molecular
Cromatografia Gasosa-Espectrometria de Massas
Inflorescência/química
Álcool Feniletílico/química
Filogenia
Polinização
Sulfetos/análise
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Benzyl Alcohols); 0 (Sulfides); E6O895DQ52 (methylphenyl carbinol); ML9LGA7468 (Phenylethyl Alcohol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170915
[Lr] Data última revisão:
170915
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170728
[St] Status:MEDLINE


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[PMID]:28717004
[Au] Autor:Ewing TA; Nguyen QT; Allan RC; Gygli G; Romero E; Binda C; Fraaije MW; Mattevi A; van Berkel WJH
[Ad] Endereço:From the Laboratory of Biochemistry, Wageningen University & Research, Stippeneng 4, 6708 WE Wageningen, The Netherlands.
[Ti] Título:Two tyrosine residues, Tyr-108 and Tyr-503, are responsible for the deprotonation of phenolic substrates in vanillyl-alcohol oxidase.
[So] Source:J Biol Chem;292(35):14668-14679, 2017 Sep 01.
[Is] ISSN:1083-351X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:A number of oxidoreductases from the VAO/ -cresol methylhydroxylase flavoprotein family catalyze the oxidation of -substituted phenols. One of the best-studied is vanillyl-alcohol oxidase (VAO) from the fungus For oxidation of phenols by VAO to occur, they must first be bound in the active site of the enzyme in their phenolate anion form. The crystal structure of VAO reveals that two tyrosine residues, Tyr-108 and Tyr-503, are positioned to facilitate this deprotonation. To investigate their role in catalysis, we created three VAO variants, Y108F, Y503F, and Y108F/Y503F, and studied their biochemical properties. Steady-state kinetics indicated that the presence of at least one of the tyrosine residues is essential for efficient catalysis by VAO. Stopped-flow kinetics revealed that the reduction of VAO by chavicol or vanillyl alcohol occurs at two different rates: , which corresponds to its reaction with the deprotonated form of the substrate, and , which corresponds to its reaction with the protonated form of the substrate. In Y108F, Y503F, and Y108F/Y503F, the relative contribution of to the reduction is larger than in wild-type VAO, suggesting deprotonation is impaired in these variants. Binding studies disclosed that the competitive inhibitor isoeugenol is predominantly in its deprotonated form when bound to wild-type VAO, but predominantly in its protonated form when bound to the variants. These results indicate that Tyr-108 and Tyr-503 are responsible for the activation of substrates in VAO, providing new insights into the catalytic mechanism of VAO and related enzymes that oxidize -substituted phenols.
[Mh] Termos MeSH primário: Oxirredutases do Álcool/metabolismo
Proteínas Fúngicas/metabolismo
Modelos Moleculares
Penicillium/enzimologia
Fenóis/metabolismo
Tirosina/química
[Mh] Termos MeSH secundário: Oxirredutases do Álcool/antagonistas & inibidores
Oxirredutases do Álcool/química
Oxirredutases do Álcool/genética
Compostos Alílicos/química
Compostos Alílicos/metabolismo
Substituição de Aminoácidos
Álcoois Benzílicos/química
Álcoois Benzílicos/metabolismo
Ligação Competitiva
Biocatálise/efeitos dos fármacos
Domínio Catalítico
Cristalografia por Raios X
Inibidores Enzimáticos/química
Inibidores Enzimáticos/metabolismo
Inibidores Enzimáticos/farmacologia
Estabilidade Enzimática
Eugenol/análogos & derivados
Eugenol/química
Eugenol/metabolismo
Eugenol/farmacologia
Proteínas Fúngicas/antagonistas & inibidores
Proteínas Fúngicas/química
Proteínas Fúngicas/genética
Mutagênese Sítio-Dirigida
Oxirredução
Fenóis/química
Conformação Proteica
Desdobramento de Proteína
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4-allylphenol); 0 (Allyl Compounds); 0 (Benzyl Alcohols); 0 (Enzyme Inhibitors); 0 (Fungal Proteins); 0 (Phenols); 3T8H1794QW (Eugenol); 42HK56048U (Tyrosine); 5M0MWY797U (isoeugenol); EC 1.1.- (Alcohol Oxidoreductases); EC 1.1.3.38 (vanillyl-alcohol oxidase); X7EA1JUA6M (vanillyl alcohol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170926
[Lr] Data última revisão:
170926
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170719
[St] Status:MEDLINE
[do] DOI:10.1074/jbc.M117.778449


  4 / 1852 MEDLINE  
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[PMID]:28606510
[Au] Autor:Haque AKMM; Leong KH; Lo YL; Awang K; Nagoor NH
[Ad] Endereço:Institute of Biological Sciences (Genetics and Molecular Biology), Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia.
[Ti] Título:In vitro inhibitory mechanisms and molecular docking of 1'-S-1'-acetoxychavicol acetate on human cytochrome P450 enzymes.
[So] Source:Phytomedicine;31:1-9, 2017 Jul 15.
[Is] ISSN:1618-095X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The compound, 1'-S-1'-acetoxychavicol acetate (ACA), isolated from the rhizomes of a Malaysian ethno-medicinal plant, Alpinia conchigera Griff. (Zingiberaceae), was previously shown to have potential in vivo antitumour activities. In the development of a new drug entity, potential interactions of the compound with the cytochrome P450 superfamily metabolizing enzymes need to be ascertain. PURPOSE: The concomitant use of therapeutic drugs may cause potential drug-drug interactions by decreasing or increasing plasma levels of the administered drugs, leading to a suboptimal clinical efficacy or a higher risk of toxicity. Thus, evaluating the inhibitory potential of a new chemical entity, and to clarify the mechanism of inhibition and kinetics in the various CYP enzymes is an important step to predict drug-drug interactions. STUDY DESIGN: This study was designed to assess the potential inhibitory effects of Alpinia conchigera Griff. rhizomes extract and its active constituent, ACA, on nine c-DNA expressed human cytochrome P450s (CYPs) enzymes using fluorescent CYP inhibition assay. METHODS/RESULTS: The half maximal inhibitory concentration (IC ) of Alpinia conchigera Griff. rhizomes extract and ACA was determined for CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C19, CYP2D6, CYP2E1, CYP3A4 and CYP3A5. A. conchigera extract only moderately inhibits on CYP3A4 (IC = 6.76 ± 1.88µg/ml) whereas ACA moderately inhibits the activities of CYP1A2 (IC = 4.50 ± 0.10µM), CYP2D6 (IC = 7.50 ± 0.17µM) and CYP3A4 (IC = 9.50 ± 0.57µM) while other isoenzymes are weakly inhibited. In addition, mechanism-based inhibition studies reveal that CYP1A2 and CYP3A4 exhibited non-mechanism based inhibition whereas CYP2D6 showed mechanism-based inhibition. Lineweaver-Burk plots depict that ACA competitively inhibited both CYP1A2 and CYP3A4, with a K values of 2.36 ± 0.03 µM and 5.55 ± 0.06µM, respectively, and mixed inhibition towards CYP2D6 with a K value of 4.50 ± 0.08µM. Further, molecular docking studies show that ACA is bound to a few key amino acid residues in the active sites of CYP1A2 and CYP3A4, while one amino residue of CYP2D6 through predominantly Pi-Pi interactions. CONCLUSION: Overall, ACA may demonstrate drug-drug interactions when co-administered with other therapeutic drugs that are metabolized by CYP1A2, CYP2D6 or CYP3A4 enzymes. Further in vivo studies, however, are needed to evaluate the clinical significance of these interactions.
[Mh] Termos MeSH primário: Alpinia/química
Álcoois Benzílicos/farmacologia
Inibidores das Enzimas do Citocromo P-450/farmacologia
[Mh] Termos MeSH secundário: Álcoois Benzílicos/química
Citocromo P-450 CYP1A2/genética
Citocromo P-450 CYP1A2/metabolismo
Inibidores das Enzimas do Citocromo P-450/química
Sistema Enzimático do Citocromo P-450/genética
Sistema Enzimático do Citocromo P-450/metabolismo
Interações Medicamentosas
Seres Humanos
Concentração Inibidora 50
Simulação de Acoplamento Molecular
Extratos Vegetais/química
Extratos Vegetais/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzyl Alcohols); 0 (Cytochrome P-450 Enzyme Inhibitors); 0 (Plant Extracts); 9035-51-2 (Cytochrome P-450 Enzyme System); EC 1.14.14.1 (CYP1A2 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP1A2); SQV3080A20 (1'-acetoxychavicol acetate)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170614
[St] Status:MEDLINE


  5 / 1852 MEDLINE  
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[PMID]:28573890
[Au] Autor:Bosak A; Knezevic A; Gazic Smilovic I; Sinko G; Kovarik Z
[Ad] Endereço:a Institute for Medical Research and Occupational Health , Zagreb , Croatia.
[Ti] Título:Resorcinol-, catechol- and saligenin-based bronchodilating ß2-agonists as inhibitors of human cholinesterase activity.
[So] Source:J Enzyme Inhib Med Chem;32(1):789-797, 2017 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:We investigated the influence of bronchodilating ß2-agonists on the activity of human acetylcholinesterase (AChE) and usual, atypical and fluoride-resistant butyrylcholinesterase (BChE). We determined the inhibition potency of racemate and enantiomers of fenoterol as a resorcinol derivative, isoetharine and epinephrine as catechol derivatives and salbutamol and salmeterol as saligenin derivatives. All of the tested compounds reversibly inhibited cholinesterases with K constants ranging from 9.4 µM to 6.4 mM and had the highest inhibition potency towards usual BChE, but generally none of the cholinesterases displayed any stereoselectivity. Kinetic and docking results revealed that the inhibition potency of the studied compounds could be related to the size of the hydroxyaminoethyl chain on the benzene ring. The additional π-π interaction of salmeterol's benzene ring and Trp286 and hydrogen bond with His447 probably enhanced inhibition by salmeterol which was singled out as the most potent inhibitor of all the cholinesterases.
[Mh] Termos MeSH primário: Agonistas de Receptores Adrenérgicos beta 2/farmacologia
Álcoois Benzílicos/farmacologia
Catecóis/farmacologia
Inibidores da Colinesterase/farmacologia
Colinesterases/metabolismo
Resorcinóis/farmacologia
[Mh] Termos MeSH secundário: Agonistas de Receptores Adrenérgicos beta 2/síntese química
Agonistas de Receptores Adrenérgicos beta 2/química
Álcoois Benzílicos/síntese química
Álcoois Benzílicos/química
Catecóis/síntese química
Catecóis/química
Inibidores da Colinesterase/síntese química
Inibidores da Colinesterase/química
Relação Dose-Resposta a Droga
Seres Humanos
Estrutura Molecular
Receptores Adrenérgicos beta 2/metabolismo
Resorcinóis/síntese química
Resorcinóis/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Adrenergic beta-2 Receptor Agonists); 0 (Benzyl Alcohols); 0 (Catechols); 0 (Cholinesterase Inhibitors); 0 (Receptors, Adrenergic, beta-2); 0 (Resorcinols); EC 3.1.1.8 (Cholinesterases); FA1N0842KB (salicyl alcohol); LF3AJ089DQ (catechol); YUL4LO94HK (resorcinol)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170906
[Lr] Data última revisão:
170906
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170603
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2017.1326109


  6 / 1852 MEDLINE  
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[PMID]:28538202
[Au] Autor:Dwivedee BP; Bhaumik J; Rai SK; Laha JK; Banerjee UC
[Ad] Endereço:Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research, Sector 67, S.A.S. Nagar, 160062 Punjab, India.
[Ti] Título:Development of nanobiocatalysts through the immobilization of Pseudomonas fluorescens lipase for applications in efficient kinetic resolution of racemic compounds.
[So] Source:Bioresour Technol;239:464-471, 2017 Sep.
[Is] ISSN:1873-2976
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The present work reports covalent immobilization of Pseudomonas fluorescens lipase (PFL) on functionalized multiwalled carbon nanotubes (MWCNTs) as a nanobiocatalyst (NBC). This nanobiocatalyst facilitates efficient kinetic resolution of (RS)-1-phenylethanol into (S)-1-phenylethanol [C=49.7%, ee =99.5%, ee =98.1% and E value=191.4]. The immobilized preparation (MWCNTs-PFL) showed ten-fold increase in activity, thermal stability upto 80 °C and recyclability (8 cycles). MWCNTs-PFL nanobioconjugate demonstrated better stability and enhanced activity compared to covalently immobilized PFL on other matrices (silver nanoparticles, gold nanoparticles and chitosan beads) used for the study. A statistical design [response surface methodology (RSM)] employed for the optimization of enzyme immobilization parameters made this study statistically more significant. Overall, the newly developed nanobiocatalyst has applications towards the kinetic resolution of racemic compounds.
[Mh] Termos MeSH primário: Lipase
Nanotubos de Carbono
Pseudomonas fluorescens
[Mh] Termos MeSH secundário: Álcoois Benzílicos
Enzimas Imobilizadas
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzyl Alcohols); 0 (Enzymes, Immobilized); 0 (Nanotubes, Carbon); E6O895DQ52 (methylphenyl carbinol); EC 3.1.1.3 (Lipase)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171109
[Lr] Data última revisão:
171109
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170525
[St] Status:MEDLINE


  7 / 1852 MEDLINE  
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[PMID]:28489907
[Au] Autor:Luo L; Kim SW; Lee HK; Kim ID; Lee H; Lee JK
[Ad] Endereço:Department of Anatomy, Inha University School of Medicine, Inchon, Korea.
[Ti] Título:Anti-oxidative effects of 4-hydroxybenzyl alcohol in astrocytes confer protective effects in autocrine and paracrine manners.
[So] Source:PLoS One;12(5):e0177322, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:4-Hydroxybenzyl alcohol (4-HBA) is an important phenolic constituent of Gastrodia elata Blume (GEB), a traditional herbal medicine used in East Asia. Many activities have been reported to underlie the beneficial effects of 4-HBA in the brain, and in particular, its anti-inflammatory, anti-oxidative, and anti-zinc-toxic effects have been implicated in the postischemic brain. Here, the authors investigated the anti-oxidative effect of 4-HBA on astrocytes and sought to identify the underlying molecular mechanisms involved. 4-HBA dose-dependently suppressed H2O2-induced astrocyte cell death. More specifically, pre-incubation of C6 cells (an astrocyte cell line) with 100 µM 4-HBA for 6 hrs increased survival when cells were treated with H2O2 (100 µM, 1 hr) from 54.2±0.7% to 85.9±1.5%. In addition, 4-HBA was found to up-regulate and activate Nrf2, and subsequently, to induce the expressions of several anti-oxidative genes, such as, HO-1, NQO1, and GCLM. Notably, HO-1 was induced by 3.4-fold in 4-HBA-treated C6 cells, and siRNA-mediated HO-1 knockdown demonstrated that Nrf2 activation and HO-1 induction were responsible for the observed cytoprotective effect of 4-HBA. ERK and Akt signaling pathways were activated by 4-HBA in C6 cells, suggesting their involvements in protective effect of 4-HBA. In addition, 4-HBA-conditioned astrocyte culture medium was found to have neuroprotective effects on primary neuronal cultures or fresh C6 cells exposed to oxidative stress, and these effects seemed to be mediated by glial cell line-derived neurotrophic factor (GDNF) and vascular endothelial growth factor (VEGF), which both accumulated in 4-HBA-treated astrocyte culture media. Thus, the 4-HBA-mediated activation of Nrf2 and induction of HO-1 in astrocytes were found to act via autocrine and paracrine mechanisms to confer protective effects. Furthermore, given the pleiotropic effects of 4-HBA with respect to its targeting of various brain cell types and functions, it would appear that 4-HBA has therapeutic potential for the prevention and amelioration of various brain diseases.
[Mh] Termos MeSH primário: Antioxidantes/farmacologia
Astrócitos/efeitos dos fármacos
Álcoois Benzílicos/farmacologia
Morte Celular/efeitos dos fármacos
Fármacos Neuroprotetores/farmacologia
Estresse Oxidativo/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Antioxidantes/química
Astrócitos/citologia
Astrócitos/metabolismo
Álcoois Benzílicos/química
Células Cultivadas
Feminino
Gastrodia/química
Fator Neurotrófico Derivado de Linhagem de Célula Glial/metabolismo
Heme Oxigenase-1/metabolismo
Peróxido de Hidrogênio/metabolismo
Sistema de Sinalização das MAP Quinases/efeitos dos fármacos
Camundongos
Camundongos Endogâmicos ICR
Fator 2 Relacionado a NF-E2/metabolismo
Fármacos Neuroprotetores/química
Proteínas Proto-Oncogênicas c-akt/metabolismo
Regulação para Cima/efeitos dos fármacos
Fator A de Crescimento do Endotélio Vascular/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Benzyl Alcohols); 0 (Glial Cell Line-Derived Neurotrophic Factor); 0 (NF-E2-Related Factor 2); 0 (Neuroprotective Agents); 0 (Vascular Endothelial Growth Factor A); 1A3AH1FP1B (4-hydroxybenzyl alcohol); BBX060AN9V (Hydrogen Peroxide); EC 1.14.14.18 (Heme Oxygenase-1); EC 2.7.11.1 (Proto-Oncogene Proteins c-akt)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170908
[Lr] Data última revisão:
170908
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170511
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0177322


  8 / 1852 MEDLINE  
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[PMID]:28480434
[Au] Autor:Jessica GG; Mario GL; Alejandro Z; Cesar APJ; Ivan JVE; Ruben RR; Javier AF
[Ad] Endereço:Postgrad in Experimental Biology, Division of Health and Biological Sciences (DCBS), Metropolitan Autonomous University Campus Iztapalapa (UAMI), D.F. Mexico 09340, Mexico.
[Ti] Título:CHEMICAL CHARACTERIZATION OF A HYPOGLYCEMIC EXTRACT FROM BOUCHE THAT INDUCES LIVER GLYCOGEN ACCUMULATION IN DIABETIC MICE.
[So] Source:Afr J Tradit Complement Altern Med;14(3):218-230, 2017.
[Is] ISSN:2505-0044
[Cp] País de publicação:Nigeria
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The aqueous extract of ( ) fruit has demonstrated hypoglycemic effect, which may be attributed to some components in the extract. However, the major secondary metabolites in this fruit have not yet been identified and little is known about its extra-pancreatic action, in particular, on liver carbohydrate metabolism. Therefore, in addition to the isolation and structural elucidation of the principal components in the aqueous extract of , the aim of this study was to determine whether or not the hypoglycemic effect of the aqueous extract of ( ) fruit is due to accumulation of liver glycogen in diabetic mice. MATERIALS AND METHODS: The aqueous extract from fruit of was fractionated and its main secondary metabolites were purified and chemically characterized (NMR and GC-MS). Alloxan-induced diabetic mice received daily by gavage the aqueous extract (30 days). The liver glycogen content was quantified by spectroscopic method and by PAS stain; ALT and AST by spectrometric method; glycogen synthase, glycogen phosphorylase and GLUT2 by Western blot; the mRNA expression of GLUT2 and glucagon-receptor by RT-PCR; while serum insulin was quantified by ELISA method. A liver histological analysis was also performed by H&E stain. RESULTS: Chemical fingerprint showed five majoritarian compounds in the aqueous extract of : -coumaric acid, p-hydroxybenzoic acid, salicin, stigmast-7,2,2-dien-3-ol and stigmast-7-en-3-ol. The histological analysis showed accumulation of liver glycogen. Also, increased glycogen synthase and decreased glycogen phosphorylase were observed. Interestingly, the histological architecture evidenced a liver-protective effect due the extract. CONCLUSION: Five compounds were identified in aqueous extract. The hypoglycemic effect of this extract may be partially explained by liver glycogen accumulation. The bioactive compound responsible for the hypoglycemic effect of this extract will be elucidated in subsequent studies.
[Mh] Termos MeSH primário: Cucurbita/química
Diabetes Mellitus Experimental/tratamento farmacológico
Hipoglicemiantes/química
Glicogênio Hepático/metabolismo
Compostos Fitoquímicos/análise
Fitoterapia/métodos
Extratos Vegetais/química
[Mh] Termos MeSH secundário: Aloxano
Animais
Álcoois Benzílicos/análise
Álcoois Benzílicos/farmacologia
Ácidos Cumáricos/análise
Ácidos Cumáricos/farmacologia
Diabetes Mellitus Experimental/sangue
Diabetes Mellitus Experimental/induzido quimicamente
Glucosídeos/análise
Glucosídeos/farmacologia
Hidroxibenzoatos/análise
Hidroxibenzoatos/farmacologia
Hipoglicemiantes/farmacologia
Insulina/sangue
Fígado/efeitos dos fármacos
Fígado/metabolismo
Masculino
Camundongos
Compostos Fitoquímicos/farmacologia
Extratos Vegetais/farmacologia
Propionatos
Sitosteroides/análise
Sitosteroides/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzyl Alcohols); 0 (Coumaric Acids); 0 (Glucosides); 0 (Hydroxybenzoates); 0 (Hypoglycemic Agents); 0 (Insulin); 0 (Liver Glycogen); 0 (Phytochemicals); 0 (Plant Extracts); 0 (Propionates); 0 (Sitosterols); 4649620TBZ (salicin); 6869-99-4 (stigmast-7-enol); 6SW5YHA5NG (Alloxan); IBS9D1EU3J (trans-3-(4'-hydroxyphenyl)-2-propenoic acid)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170509
[St] Status:MEDLINE
[do] DOI:10.21010/ajtcam.v14i3.24


  9 / 1852 MEDLINE  
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[PMID]:28445455
[Au] Autor:Cheng RKY; Fiez-Vandal C; Schlenker O; Edman K; Aggeler B; Brown DG; Brown GA; Cooke RM; Dumelin CE; Doré AS; Geschwindner S; Grebner C; Hermansson NO; Jazayeri A; Johansson P; Leong L; Prihandoko R; Rappas M; Soutter H; Snijder A; Sundström L; Tehan B; Thornton P; Troast D; Wiggin G; Zhukov A; Marshall FH; Dekker N
[Ad] Endereço:Heptares Therapeutics Ltd, BioPark, Broadwater Road, Welwyn Garden City, Hertfordshire AL7 3AX, UK.
[Ti] Título:Structural insight into allosteric modulation of protease-activated receptor 2.
[So] Source:Nature;545(7652):112-115, 2017 05 04.
[Is] ISSN:1476-4687
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Protease-activated receptors (PARs) are a family of G-protein-coupled receptors (GPCRs) that are irreversibly activated by proteolytic cleavage of the N terminus, which unmasks a tethered peptide ligand that binds and activates the transmembrane receptor domain, eliciting a cellular cascade in response to inflammatory signals and other stimuli. PARs are implicated in a wide range of diseases, such as cancer and inflammation. PARs have been the subject of major pharmaceutical research efforts but the discovery of small-molecule antagonists that effectively bind them has proved challenging. The only marketed drug targeting a PAR is vorapaxar, a selective antagonist of PAR1 used to prevent thrombosis. The structure of PAR1 in complex with vorapaxar has been reported previously. Despite sequence homology across the PAR isoforms, discovery of PAR2 antagonists has been less successful, although GB88 has been described as a weak antagonist. Here we report crystal structures of PAR2 in complex with two distinct antagonists and a blocking antibody. The antagonist AZ8838 binds in a fully occluded pocket near the extracellular surface. Functional and binding studies reveal that AZ8838 exhibits slow binding kinetics, which is an attractive feature for a PAR2 antagonist competing against a tethered ligand. Antagonist AZ3451 binds to a remote allosteric site outside the helical bundle. We propose that antagonist binding prevents structural rearrangements required for receptor activation and signalling. We also show that a blocking antibody antigen-binding fragment binds to the extracellular surface of PAR2, preventing access of the tethered ligand to the peptide-binding site. These structures provide a basis for the development of selective PAR2 antagonists for a range of therapeutic uses.
[Mh] Termos MeSH primário: Receptor PAR-2/química
Receptor PAR-2/metabolismo
[Mh] Termos MeSH secundário: Regulação Alostérica/efeitos dos fármacos
Sítio Alostérico/efeitos dos fármacos
Anticorpos Bloqueadores/química
Anticorpos Bloqueadores/farmacologia
Benzimidazóis/química
Benzimidazóis/farmacologia
Benzodioxóis/química
Benzodioxóis/farmacologia
Álcoois Benzílicos/química
Álcoois Benzílicos/farmacologia
Cristalografia por Raios X
Seres Humanos
Imidazóis/química
Imidazóis/farmacologia
Fragmentos Fab das Imunoglobulinas/química
Fragmentos Fab das Imunoglobulinas/farmacologia
Cinética
Ligantes
Modelos Moleculares
Receptor PAR-2/antagonistas & inibidores
Transdução de Sinais/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (AZ3451); 0 (AZ8838); 0 (Antibodies, Blocking); 0 (Benzimidazoles); 0 (Benzodioxoles); 0 (Benzyl Alcohols); 0 (Imidazoles); 0 (Immunoglobulin Fab Fragments); 0 (Ligands); 0 (Receptor, PAR-2)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170919
[Lr] Data última revisão:
170919
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170427
[St] Status:MEDLINE
[do] DOI:10.1038/nature22309


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[PMID]:28416587
[Au] Autor:Brook RD; Anderson JA; Calverley PM; Celli BR; Crim C; Denvir MA; Magder S; Martinez FJ; Rajagopalan S; Vestbo J; Yates J; Newby DE; SUMMIT Investigators
[Ad] Endereço:Division of Cardiovascular Medicine, University of Michigan, Ann Arbor, Michigan, USA.
[Ti] Título:Cardiovascular outcomes with an inhaled beta2-agonist/corticosteroid in patients with COPD at high cardiovascular risk.
[So] Source:Heart;103(19):1536-1542, 2017 Oct.
[Is] ISSN:1468-201X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:OBJECTIVES: Cardiovascular disease (CVD) and chronic obstructive pulmonary disease (COPD) often coexist. We assessed the effect of inhaled COPD treatments on CVD outcomes and safety in patients with COPD and at heightened CVD risk. METHODS: The SUMMIT (Study to Understand Mortality and MorbidITy) was a multicentre, randomised, double-blind, placebo-controlled, event-driven trial in 16 485 patients with moderate COPD who had or were at high risk of CVD. Here, we assessed the prespecified secondary endpoint of time to first on-treatment composite CVD event (CVD death, myocardial infarction, stroke, unstable angina or transient ischaemic attack (TIA)) by Cox regression and by clinician-reported CVD adverse events across the four groups: once-daily inhaled placebo (n=4111), long-acting beta -agonist (vilanterol (VI) 25 µg; n=4118), corticosteroid (fluticasone furoate (FF) 100 µg; n=4135) and combination therapy (FF/VI; n=4121). RESULTS: Participants were predominantly middle-aged (mean 65 (SD 8) years) men (75%) with overt CVD (66%). The composite CVD endpoint occurred in 688 patients (first event: sudden death (35%), acute coronary syndrome (37%) and stroke or TIA (23%), and was not reduced in any treatment group versus placebo: VI (HR 0.99, 95% CI 0.80 to 1.22), FF (HR 0.90, 95% CI 0.72 to 1.11) and their combination (HR 0.93, 95% CI 0.75 to 1.14). Outcomes were similar among all subgroups. Adverse events, including palpitations and arrhythmias, did not differ by treatment. CONCLUSIONS: In patients with COPD with moderate airflow limitation and heightened CVD risk, treatment with inhaled VI, FF or their combination has an excellent safety profile and does not impact CVD outcomes. TRIAL REGISTRATION NUMBER: NCT01313676.
[Mh] Termos MeSH primário: Androstadienos/administração & dosagem
Álcoois Benzílicos/administração & dosagem
Doenças Cardiovasculares/tratamento farmacológico
Clorobenzenos/administração & dosagem
Doença Pulmonar Obstrutiva Crônica/tratamento farmacológico
[Mh] Termos MeSH secundário: Administração por Inalação
Antagonistas de Receptores Adrenérgicos beta 2/administração & dosagem
Adulto
Idoso
Idoso de 80 Anos ou mais
Doenças Cardiovasculares/etiologia
Doenças Cardiovasculares/fisiopatologia
Relação Dose-Resposta a Droga
Método Duplo-Cego
Combinação de Medicamentos
Feminino
Seguimentos
Volume Expiratório Forçado
Glucocorticoides/administração & dosagem
Seres Humanos
Masculino
Meia-Idade
Doença Pulmonar Obstrutiva Crônica/complicações
Doença Pulmonar Obstrutiva Crônica/fisiopatologia
Fatores de Risco
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; MULTICENTER STUDY; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Adrenergic beta-2 Receptor Antagonists); 0 (Androstadienes); 0 (Benzyl Alcohols); 0 (Chlorobenzenes); 0 (Drug Combinations); 0 (Glucocorticoids); 028LZY775B (vilanterol); JS86977WNV (fluticasone furoate)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:171013
[Lr] Data última revisão:
171013
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170419
[St] Status:MEDLINE
[do] DOI:10.1136/heartjnl-2016-310897



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