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[PMID]:28744886
[Au] Autor:Zhao A; Zhang L; Li R; Shang J; Yi H; Wang Y; Zhang D; Wang S; Fang M
[Ad] Endereço:Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi'an, China.
[Ti] Título:Development and validation of an LC-MS/MS method for the simultaneous quantification of seven constituents in rat plasma and application in a pharmacokinetic study of the Zaoren Anshen prescription.
[So] Source:Biomed Chromatogr;32(2), 2018 Feb.
[Is] ISSN:1099-0801
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A sensitive, specific and accurate liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous determination of seven constituents of the Zaoren Anshen prescription (ZAP) in rat plasma after oral administration of the ZAP: spinosin, salvianic acid A, 6'''-feruloylspinosin, protocatechualdehyde, salvianolic acid B, schisandrin and deoxyschisandrin. The plasma samples and the internal standard (IS) sulfamethoxazole were extracted using acetonitrile. Chromatographic separation was performed with an Agilent HC-C column using a gradient elution profile and a mobile phase consisting of 0.01% formic acid in water (A) and acetonitrile (B). The analytes were quantified simultaneously in a single run using an ion trap mass spectrometer operated in the multiple reaction monitoring mode and electrospray ion-source polarity in the positive and negative modes. The calibration curves for spinosin, salvianic acid A, 6'''-feruloylspinosin, protocatechualdehyde, salvianolic acid B, schisandrin and deoxyschisandrin were linear over the concentration ranges of 2.90-1160, 2.50-1000, 1.80-720, 0.65-260, 2.50-1000, 8.00-1600 and 1.30-520 ng/mL, respectively. The intra- and inter-day precisions in terms of relative standard deviation were <18.9%, and the accuracies in terms of relative error were within ±14.2%. Consequently, the proposed method was successfully applied to the pharmacokinetic analysis of these seven major active compounds in rats administered ZAP. These results will facilitate research aiming to predict the effectiveness of the optimal dose of ZAP and might be beneficial for the therapeutic use of ZAP in the clinical setting.
[Mh] Termos MeSH primário: Benzaldeídos/sangue
Benzofuranos/sangue
Catecóis/sangue
Ciclo-Octanos/sangue
Medicamentos de Ervas Chinesas/farmacocinética
Flavonoides/sangue
Lignanas/sangue
Compostos Policíclicos/sangue
[Mh] Termos MeSH secundário: Animais
Benzaldeídos/química
Benzaldeídos/farmacocinética
Benzofuranos/química
Benzofuranos/farmacocinética
Catecóis/química
Catecóis/farmacocinética
Cromatografia Líquida/métodos
Ciclo-Octanos/química
Ciclo-Octanos/farmacocinética
Estabilidade de Medicamentos
Medicamentos de Ervas Chinesas/análise
Medicamentos de Ervas Chinesas/química
Flavonoides/química
Flavonoides/farmacocinética
Lignanas/química
Lignanas/farmacocinética
Limite de Detecção
Modelos Lineares
Masculino
Compostos Policíclicos/química
Compostos Policíclicos/farmacocinética
Ratos
Ratos Sprague-Dawley
Reprodutibilidade dos Testes
Espectrometria de Massas em Tandem/métodos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzaldehydes); 0 (Benzofurans); 0 (Catechols); 0 (Cyclooctanes); 0 (Drugs, Chinese Herbal); 0 (Flavonoids); 0 (Lignans); 0 (Polycyclic Compounds); 4PVP2HCH4T (protocatechualdehyde); 72063-39-9 (spinosin); C1GQ844199 (salvianolic acid B); G01BQC0879 (schizandrin)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170727
[St] Status:MEDLINE
[do] DOI:10.1002/bmc.4055


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[PMID]:29413989
[Au] Autor:Marques RA; Gomes AOCV; de Brito MV; Dos Santos ALP; da Silva GS; de Lima LB; Nunes FM; de Mattos MC; de Oliveira FCE; do Ó Pessoa C; de Moraes MO; de Fátima Â; Franco LL; Silva MM; Dantas MDA; Santos JCC; Figueiredo IM; da Silva-Júnior EF; de Aquino TM; de Araújo-Júnior JX; de Oliveira MCF; Leslie Gunatilaka AA
[Ad] Endereço:Department of Organic and Inorganic Chemistry, Federal University of Ceará, Fortaleza, Ceará, Brazil; Northern Educational Union - UNINORTE, Rio Branco, Acre, Brazil.
[Ti] Título:Annonalide and derivatives: Semisynthesis, cytotoxic activities and studies on interaction of annonalide with DNA.
[So] Source:J Photochem Photobiol B;179:156-166, 2018 Feb.
[Is] ISSN:1873-2682
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:The cytotoxic activity of the pimarane diterpene annonalide (1) and nine of its semisynthetic derivatives (2-10) was investigated against the human tumor cell lines HL-60 (leukemia), PC-3 (prostate adenocarcinoma), HepG2 (hepatocellular carcinoma), SF-295 (glioblastoma) and HCT-116 (colon cancer), and normal mouse fibroblast (L929) cells. The preparation of 2-10 involved derivatization of the side chain of 1 at C-13. Except for 2, all derivatives are being reported for the first time. Most of the tested compounds presented IC s below 4.0 µM, being considered potential antitumor agents. The structures of all new compounds were elucidated by spectroscopic analyses including 2D NMR and HRMS. Additionally, the interaction of annonalide (1) with ctDNA was evaluated using spectroscopic techniques, and the formation of a supramolecular complex with the macromolecule was confirmed. Competition assays with fluorescent probes (Hoechst and ethidium bromide) and theoretical studies confirmed that 1 interacts preferentially via DNA intercalation with stoichiometric ratio of 1:1 (1:ctDNA). The ΔG value was calculated as -28.24 kJ mol , and indicated that the interaction process occurs spontaneously. Docking studies revealed that van der Walls is the most important interaction in 1-DNA and EB-DNA complexes, and that both ligands (1 and EB) interact with the same DNA residues (DA6, DA17 and DT19).
[Mh] Termos MeSH primário: Ciclo-Octanos/química
DNA/química
Cetonas/química
[Mh] Termos MeSH secundário: Animais
Sítios de Ligação
Bovinos
Linhagem Celular Tumoral
Sobrevivência Celular
Ciclo-Octanos/síntese química
Ciclo-Octanos/toxicidade
DNA/metabolismo
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Cetonas/síntese química
Cetonas/toxicidade
Simulação de Acoplamento Molecular
Conformação de Ácido Nucleico
Espectrofotometria
Eletricidade Estática
Termodinâmica
Temperatura de Transição
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclooctanes); 0 (Ketones); 502-49-8 (cyclooctanone); 9007-49-2 (DNA); 91080-16-9 (calf thymus DNA)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180223
[Lr] Data última revisão:
180223
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180208
[St] Status:MEDLINE


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[PMID]:28463490
[Au] Autor:Tomita T; Kim SY; Teramoto K; Meguro A; Ozaki T; Yoshida A; Motoyoshi Y; Mori N; Ishigami K; Watanabe H; Nishiyama M; Kuzuyama T
[Ti] Título:Structural Insights into the CotB2-Catalyzed Cyclization of Geranylgeranyl Diphosphate to the Diterpene Cyclooctat-9-en-7-ol.
[So] Source:ACS Chem Biol;12(6):1621-1628, 2017 06 16.
[Is] ISSN:1554-8937
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The diterpene cyclase CotB2 catalyzes the cyclization of geranylgeranyl diphosphate (GGPP) to the tricyclic cyclooctat-9-en-7-ol, which is characterized by a 5-8-5-fused ring skeleton. We have previously proposed a cyclization cascade involving a unique carbon-carbon bond rearrangement combined with multiple hydride shifts, all occurring at a single active site. Here, we report the first high-resolution X-ray crystal structure of CotB2 with bound substrate analog geranylgeranyl thiodiphosphate (GGSPP). In the GGSPP-bound form, GGSPP folds into a unique S-shaped conformation that probably reflects the substrate-bound state prior to ionization of the substrate GGPP. The folded framework of GGSPP is surrounded by hydrophobic residues and several aromatic and asparagine residues that are well-positioned to stabilize a series of reactive carbocation intermediates through a combination of cation-π and dipole charge interactions. The combined crystal structures and mutagenesis-based biochemical assays provide a structural basis for exquisite control of ring formation and stereochemistry during CotB2 catalysis.
[Mh] Termos MeSH primário: Proteínas de Bactérias/metabolismo
Biocatálise
Diterpenos/química
Oxirredutases Intramoleculares/metabolismo
Fosfatos de Poli-Isoprenil/química
[Mh] Termos MeSH secundário: Proteínas de Bactérias/química
Cristalografia por Raios X
Ciclização
Ciclo-Octanos/química
Ciclo-Octanos/metabolismo
Enzimas/química
Enzimas/metabolismo
Mutagênese Sítio-Dirigida
Streptomyces/enzimologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Cyclooctanes); 0 (Diterpenes); 0 (Enzymes); 0 (Polyisoprenyl Phosphates); EC 5.3.- (Intramolecular Oxidoreductases); N21T0D88LX (geranylgeranyl pyrophosphate)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:180201
[Lr] Data última revisão:
180201
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.1021/acschembio.7b00154


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[PMID]:29191024
[Au] Autor:Billaud EMF; Belderbos S; Cleeren F; Maes W; Van de Wouwer M; Koole M; Verbruggen A; Himmelreich U; Geukens N; Bormans G
[Ad] Endereço:Laboratory for Radiopharmaceutical Research, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven , Campus Gasthuisberg, O&N2, Herestraat 49, Box 821, 3000 Leuven, Belgium.
[Ti] Título:Pretargeted PET Imaging Using a Bioorthogonal F-Labeled trans-Cyclooctene in an Ovarian Carcinoma Model.
[So] Source:Bioconjug Chem;28(12):2915-2920, 2017 Dec 20.
[Is] ISSN:1520-4812
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In cancer research, pretargeted positron emission tomography (PET) imaging has emerged as an effective two-step approach that combines the excellent target affinity and selectivity of antibodies with the advantages of using short-lived radionuclides such as fluorine-18. One possible approach is based on the bioorthogonal inverse-electron-demand Diels-Alder (IEDDA) reaction between tetrazines and trans-cyclooctene (TCO) derivatives. Here, we report the first successful use of an F-labeled small TCO compound, [ F]1 recently developed in our laboratory, to perform pretargeted immuno-PET imaging. The study was performed in an ovarian carcinoma mouse model, using a trastuzumab-tetrazine conjugate.
[Mh] Termos MeSH primário: Ciclo-Octanos/química
Radioisótopos de Flúor
Neoplasias Ovarianas/patologia
Tomografia por Emissão de Pósitrons/métodos
[Mh] Termos MeSH secundário: Animais
Linhagem Celular Tumoral
Reação de Cicloadição
Feminino
Seres Humanos
Imunoconjugados/química
Imunoconjugados/farmacocinética
Marcação por Isótopo
Camundongos
Neoplasias Ovarianas/diagnóstico por imagem
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclooctanes); 0 (Fluorine Radioisotopes); 0 (Fluorine-18); 0 (Immunoconjugates)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180105
[Lr] Data última revisão:
180105
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171202
[St] Status:MEDLINE
[do] DOI:10.1021/acs.bioconjchem.7b00635


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[PMID]:27771781
[Au] Autor:Müller CA; Weingartner AM; Dennig A; Ruff AJ; Gröger H; Schwaneberg U
[Ad] Endereço:Institute of Biotechnology, RWTH Aachen University, Worringerweg 3, 52074, Aachen, Germany.
[Ti] Título:A whole cell biocatalyst for double oxidation of cyclooctane.
[So] Source:J Ind Microbiol Biotechnol;43(12):1641-1646, 2016 Dec.
[Is] ISSN:1476-5535
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:A novel whole cell cascade for double oxidation of cyclooctane to cyclooctanone was developed. The one-pot oxidation cascade requires only a minimum of reaction components: resting E. coli cells in aqueous buffered medium (=catalyst), the target substrate and oxygen as environmental friendly oxidant. Conversion of cyclooctane was catalysed with high efficiency (50% yield) and excellent selectivity (>94%) to cyclooctanone. The reported oxidation cascade represents a novel whole cell system for double oxidation of non-activated alkanes including an integrated cofactor regeneration. Notably, two alcohol dehydrogenases from Lactobacillus brevis and from Rhodococcus erythropolis with opposite cofactor selectivities and one monooxygenase P450 BM3 were produced in a coexpression system in one single host. The system represents the most efficient route with a TTN of up to 24363 being a promising process in terms of sustainability as well.
[Mh] Termos MeSH primário: Álcool Desidrogenase/química
Proteínas de Bactérias/química
Ciclo-Octanos/química
Oxigenases de Função Mista/química
[Mh] Termos MeSH secundário: Álcool Desidrogenase/biossíntese
Proteínas de Bactérias/metabolismo
Biocatálise
Reatores Biológicos
Evolução Molecular Direcionada
Escherichia coli/genética
Escherichia coli/metabolismo
Lactobacillus brevis/enzimologia
Oxigenases de Função Mista/biossíntese
Oxirredução
Rhodococcus/enzimologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Bacterial Proteins); 0 (Cyclooctanes); EC 1.- (Mixed Function Oxygenases); EC 1.1.1.1 (Alcohol Dehydrogenase); KKZ3KBS654 (cyclooctane)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171128
[Lr] Data última revisão:
171128
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161025
[St] Status:MEDLINE


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[PMID]:28844238
[Au] Autor:Ono Y; Tomimori N; Hori H; Kitagawa Y; Shibata H
[Ad] Endereço:Suntory Wellness Limited, 8-1-1 Seikadai, Seika-cho, Soraku-gun, Kyoto 619-0284, Japan. Electronic address: Yoshiko_Toyoda@suntory.co.jp.
[Ti] Título:Mechanisms of chromosomal aberrations induced by sesamin metabolites in Chinese hamster lung cells.
[So] Source:Mutat Res;822:19-26, 2017 Oct.
[Is] ISSN:1873-135X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Sesamin is a major lignan in sesame seeds and oil. We previously demonstrated that sesamin induces chromosomal aberrations (CA) in Chinese hamster lung (CHL/IU) cells in the presence of a metabolic activation system (S9 mix), although no genotoxicity was detected in vivo. To clarify the mechanism of CA induction by sesamin, we identified its principal active metabolite. A mono-catechol derivative, [2-(3,4-methylenedioxyphenyl)-6-(3,4-dihydroxyphenyl)-3,7-dioxabi-cyclo[3.3.0]octane (SC-1)], was previously identified in culture medium when sesamin was incubated with S9 mix. In the present study, we show that SC-1 induces CA in CHL/IU cells but not in human hepatoblastoma (HepG2) cells. SC-1 was unstable in culture medium. Addition of glutathione (GSH) to the incubation mixture decreased the rate of decomposition and also suppressed induction of CA in CHL/IU cells. These results indicate that SC-1 itself may not contribute to the induction of CA. Two GSH adducts of SC-1 were identified when SC-1 was incubated with GSH, suggesting that SC-1 was converted to the semiquinone/quinone form and then conjugated with GSH in the culture medium. Sodium sulfite (a quinone-responsive compound) also suppressed CA induction by SC-1. These findings strongly suggest that SC-1 is oxidized to semiquinone/quinone derivatives extracellularly in culture medium, that these derivatives are responsible for the induction of CA in CHL/IU cells, and therefore that the positive results obtained with sesamin in in vitro CA tests using CHL/IU cells may not be relevant to the assessment of in vivo activity.
[Mh] Termos MeSH primário: Compostos Bicíclicos Heterocíclicos com Pontes/toxicidade
Aberrações Cromossômicas/induzido quimicamente
Ciclo-Octanos/toxicidade
Dioxóis/toxicidade
Lignanas/toxicidade
[Mh] Termos MeSH secundário: Animais
Compostos Bicíclicos Heterocíclicos com Pontes/metabolismo
Técnicas de Cultura de Células
Cricetinae
Ciclo-Octanos/metabolismo
Dioxóis/metabolismo
Relação Dose-Resposta a Droga
Glutationa/metabolismo
Células Hep G2
Seres Humanos
Lignanas/metabolismo
Fígado/metabolismo
Extratos Hepáticos
Pulmão/citologia
Pulmão/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-(3,4-methylenedioxyphenyl)-6-(3,4-dihydroxyphenyl)-3,7-dioxabicyclo(3.3.0)octane); 0 (Bridged Bicyclo Compounds, Heterocyclic); 0 (Cyclooctanes); 0 (Dioxoles); 0 (Lignans); 0 (Liver Extracts); GAN16C9B8O (Glutathione); S7946O4P76 (sesamin)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170913
[Lr] Data última revisão:
170913
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170829
[St] Status:MEDLINE


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[PMID]:28818768
[Au] Autor:Poornima B; Siva B; Venkanna A; Shankaraiah G; Jain N; Yadav DK; Misra S; Babu KS
[Ad] Endereço:Division of Natural Products Chemistry, CSIR-Indian Institute of Chemical Technology, Hyderabad, 500 007, India.
[Ti] Título:Novel Gomisin B analogues as potential cytotoxic agents: Design, synthesis, biological evaluation and docking studies.
[So] Source:Eur J Med Chem;139:441-453, 2017 Oct 20.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:As part of pharmacological-phytochemical integrated studies on medicinal flora, Gomisin B (1) was isolated as major phytochemical lead from schisandra grandiflora, a plant traditionally used in different Asian systems of medicine. A series of 1,2,3-triazoles derivatives were synthesized at the C-7' position of the gomisin B core through diastereoselective Michael addition followed by regioselective Huisgen 1,3-dipolar cycloaddition reactions. All these triazolyl derivatives (5a-5q) were well characterized using modern spectroscopic techniques and evaluated for their anti-cancer activity against a panel of five human cancerous cell-lines. Among them, compound 5b exhibited the best cytotoxicity against SIHA cell (IC 0.24 µM) which was more than the standard drug doxorubicin, while the other derivatives were exhibited moderate to low activities in tested cell lines. The cell cycle analysis indicated that compound 5b stalled HeLa cells at G2/M phase. 5b promoted tubulin polymerization and this was supported by the docking studies, wherein 5b showed significant binding affinity at the colchicine binding pocket of tubulin. Overall, we identified a novel small molecule that demonstrated anticancer activity by promoting in vitro tubulin assembly.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Citotoxinas/farmacologia
Dioxóis/farmacologia
Desenho de Drogas
Lignanas/farmacologia
Simulação de Acoplamento Molecular
Compostos Policíclicos/farmacologia
[Mh] Termos MeSH secundário: Antineoplásicos/síntese química
Antineoplásicos/química
Linhagem Celular Tumoral
Proliferação Celular/efeitos dos fármacos
Ciclo-Octanos/síntese química
Ciclo-Octanos/química
Ciclo-Octanos/farmacologia
Citotoxinas/síntese química
Citotoxinas/química
Dioxóis/síntese química
Dioxóis/química
Relação Dose-Resposta a Droga
Ensaios de Seleção de Medicamentos Antitumorais
Seres Humanos
Lignanas/síntese química
Lignanas/química
Estrutura Molecular
Compostos Policíclicos/síntese química
Compostos Policíclicos/química
Schisandra/química
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Cyclooctanes); 0 (Cytotoxins); 0 (Dioxoles); 0 (Lignans); 0 (Polycyclic Compounds); 58546-55-7 (schisantherin B)
[Em] Mês de entrada:1710
[Cu] Atualização por classe:171018
[Lr] Data última revisão:
171018
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170819
[St] Status:MEDLINE


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[PMID]:28570601
[Au] Autor:Ketelboeter LM; Bardy SL
[Ad] Endereço:Department of Biological Sciences, University of Wisconsin-Milwaukee, Milwaukee, Wisconsin, United States of America.
[Ti] Título:Characterization of 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione resistance in pyomelanogenic Pseudomonas aeruginosa DKN343.
[So] Source:PLoS One;12(6):e0178084, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Pyomelanin is a reddish-brown pigment that provides bacteria and fungi protection from oxidative stress, and is reported to contribute to infection persistence. Production of this pigment can be inhibited by the anti-virulence agent 2-(2-nitro-4-trifluoromethylbenzoyl)-1,3-cyclohexanedione (NTBC). The Pseudomonas aeruginosa clinical isolate DKN343 exhibited high levels of resistance to NTBC, and the mechanism of pyomelanin production in this strain was uncharacterized. We determined that pyomelanin production in the clinical Pseudomonas aeruginosa isolate DKN343 was due to a loss of function in homogentisate 1,2-dioxygenase (HmgA). Several potential resistance mechanisms were investigated, and the MexAB-OprM efflux pump is required for resistance to NTBC. DKN343 has a frameshift mutation in NalC, which is a known indirect repressor of the mexAB-oprM operon. This frameshift mutation may contribute to the increased resistance of DKN343 to NTBC. Additional studies investigating the prevalence of resistance in pyomelanogenic microbes are necessary to determine the future applications of NTBC as an anti-virulence therapy.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Ciclo-Octanos/química
Pseudomonas aeruginosa/efeitos dos fármacos
[Mh] Termos MeSH secundário: Sequência de Aminoácidos
Antibacterianos/química
Melaninas/biossíntese
Mutação
Homologia de Sequência de Aminoácidos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1,3-cyclooctadiene); 0 (Anti-Bacterial Agents); 0 (Cyclooctanes); 0 (Melanins)
[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:170602
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0178084


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[PMID]:28426149
[Au] Autor:Wang T; Yuan C; Dai B; Liu Y; Li M; Feng Z; Jiang Q; Xu Z; Zhao N; Gu N; Yang F
[Ad] Endereço:State Key Laboratory of Bioelectronics, Jiangsu Key Laboratory for Biomaterials and Devices, School of Biological Sciences and Medical Engineering, Southeast University, Sipailou 2, Nanjing, Jiangsu, 210009, China.
[Ti] Título:Click-Chemistry-Mediated Rapid Microbubble Capture for Acute Thrombus Ultrasound Molecular Imaging.
[So] Source:Chembiochem;18(14):1364-1368, 2017 Jul 18.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Bioorthogonal coupling chemistry has been studied as a potentially advantageous approach for molecular imaging because it offers rapid, efficient, and strong binding, which might also benefit stability, production, and chemical conjugation. The inverse-electron-demand Diels-Alder reaction between a 1,2,4,5-tetrazine and trans-cyclooctene (TCO) is an example of a highly selective and rapid bioorthogonal coupling reaction that has been used successfully to prepare targeted molecular imaging probes. Here we report a fast, reliable, and highly sensitive approach, based on a two-step pretargeting bioorthogonal approach, to achieving activated-platelet-specific CD62p-targeted thrombus ultrasound molecular imaging. Tetrazine-modified microbubbles (tetra-MBs) could be uniquely and rapidly captured by subsequent click chemistry of thrombus tagged with a trans-cyclooctene-pretreated CD62p antibody. Moreover, such tetra-MBs showed great long-term stability under physiological conditions, thus offering the ability to monitor thrombus changes in real time. We demonstrated for the first time that a bioorthogonal targeting molecular ultrasound imaging strategy based on tetra-MBs could be a simple but powerful tool for rapid diagnosis of acute thrombosis.
[Mh] Termos MeSH primário: Química Click
Microbolhas
Imagem Molecular/métodos
Sondas Moleculares/química
Compostos Radiofarmacêuticos/química
Trombose/diagnóstico por imagem
[Mh] Termos MeSH secundário: Doença Aguda
Ciclo-Octanos/química
Seres Humanos
Sondas Moleculares/síntese química
Compostos Radiofarmacêuticos/síntese química
Triazóis/química
Ultrassonografia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclooctanes); 0 (Molecular Probes); 0 (Radiopharmaceuticals); 0 (Triazoles)
[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:170421
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201700068


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[PMID]:28344076
[Au] Autor:Zhao J; Sun T; Wu JJ; Cao YF; Fang ZZ; Sun HZ; Zhu ZT; Yang K; Liu YZ; Gonzalez FJ; Yin J
[Ad] Endereço:School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, China.
[Ti] Título:Inhibition of human CYP3A4 and CYP3A5 enzymes by gomisin C and gomisin G, two lignan analogs derived from Schisandra chinensis.
[So] Source:Fitoterapia;119:26-31, 2017 Jun.
[Is] ISSN:1873-6971
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Gomisin C (GC) and gomisin G (GG) are two lignan analogs isolated from the Traditional Chinese Medicine Schisandra chinensis which possesses multiple pharmacological activities. However, the potential herb-drug interactions (HDI) between these lignans and other drugs through inhibiting human cytochrome P450 3A4 (CYP3A4) and CYP3A5 remains unclear. In the present study, the inhibitory action of GC and GG on CYP3A4 and CYP3A5 were investigated. The results demonstrated that both GC and GG strongly inhibited CYP3A-mediated midazolam 1'-hydroxylation, nifedipine oxidation and testosterone 6ß-hydroxylation. Notably, the inhibitory intensity of GC towards CYP3A4 was stronger than CYP3A5 when using midazolam and nifedipine as substrates. While inhibition of GC towards CYP3A5 was weaker than CYP3A4 when using testosterone as substrate. In contrast, GG showed a stronger inhibitory activity on CYP3A5 than CYP3A4 without substrate-dependent behavior. In addition, docking simulations indicated that the π-π interaction between CYP3A4 and GC, and hydrogen-bond interaction between CYP3A5 and GG might result in their different inhibitory actions. Furthermore, the AUC of drugs metabolized by CYP3A was estimated to increase by 8%-321% and 2%-3190% in the presence of GC and GG, respectively. These findings strongly suggested that GC and GG showed high HDI potentials, and the position of methylenedioxy group determined their different inhibitory effect towards CYP3A4 and CYP3A5, which are of significance for the application of Schisandra chinensis-containing herbs.
[Mh] Termos MeSH primário: Ciclo-Octanos/farmacologia
Inibidores das Enzimas do Citocromo P-450/farmacologia
Dioxóis/farmacologia
Lignanas/farmacologia
Schisandra/química
[Mh] Termos MeSH secundário: Citocromo P-450 CYP3A/metabolismo
Interações Ervas-Drogas
Seres Humanos
Hidroxilação
Midazolam/farmacologia
Estrutura Molecular
Nifedipino/farmacologia
Oxirredução
Testosterona/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cyclooctanes); 0 (Cytochrome P-450 Enzyme Inhibitors); 0 (Dioxoles); 0 (Lignans); 3XMK78S47O (Testosterone); 82042-38-4 (schizandrer A); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (CYP3A5 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP3A); I9ZF7L6G2L (Nifedipine); R60L0SM5BC (Midazolam)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170615
[Lr] Data última revisão:
170615
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170328
[St] Status:MEDLINE



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