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[PMID]:29317625
[Au] Autor:Hall MP; Woodroofe CC; Wood MG; Que I; Van't Root M; Ridwan Y; Shi C; Kirkland TA; Encell LP; Wood KV; Löwik C; Mezzanotte L
[Ad] Endereço:Promega Corporation, Madison, WI, 53711, USA.
[Ti] Título:Click beetle luciferase mutant and near infrared naphthyl-luciferins for improved bioluminescence imaging.
[So] Source:Nat Commun;9(1):132, 2018 01 09.
[Is] ISSN:2041-1723
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The sensitivity of bioluminescence imaging in animals is primarily dependent on the amount of photons emitted by the luciferase enzyme at wavelengths greater than 620 nm where tissue penetration is high. This area of work has been dominated by firefly luciferase and its substrate, D-luciferin, due to the system's peak emission (~ 600 nm), high signal to noise ratio, and generally favorable biodistribution of D-luciferin in mice. Here we report on the development of a codon optimized mutant of click beetle red luciferase that produces substantially more light output than firefly luciferase when the two enzymes are compared in transplanted cells within the skin of black fur mice or in deep brain. The mutant enzyme utilizes two new naphthyl-luciferin substrates to produce near infrared emission (730 nm and 743 nm). The stable luminescence signal and near infrared emission enable unprecedented sensitivity and accuracy for performing deep tissue multispectral tomography in mice.
[Mh] Termos MeSH primário: Benzotiazóis/metabolismo
Coleópteros/enzimologia
Proteínas de Insetos/metabolismo
Luciferases/metabolismo
[Mh] Termos MeSH secundário: Animais
Benzotiazóis/química
Células HEK293
Seres Humanos
Proteínas de Insetos/genética
Luciferases/genética
Luminescência
Medições Luminescentes/métodos
Células MCF-7
Camundongos Endogâmicos C57BL
Camundongos Nus
Microscopia de Fluorescência
Mutação
Espectroscopia de Luz Próxima ao Infravermelho
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (D-luciferin); 0 (Insect Proteins); EC 1.13.12.- (Luciferases)
[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:180111
[St] Status:MEDLINE
[do] DOI:10.1038/s41467-017-02542-9


  2 / 5207 MEDLINE  
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[PMID]:28467708
[Au] Autor:Watanabe H; Ono M; Ariyoshi T; Katayanagi R; Saji H
[Ad] Endereço:Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University , 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan.
[Ti] Título:Novel Benzothiazole Derivatives as Fluorescent Probes for Detection of ß-Amyloid and α-Synuclein Aggregates.
[So] Source:ACS Chem Neurosci;8(8):1656-1662, 2017 08 16.
[Is] ISSN:1948-7193
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Deposits of ß-amyloid (Aß) and α-synuclein (α-syn) are the hallmark of Alzheimer's disease (AD) and Parkinson's disease (PD), respectively. The detection of these protein aggregates with fluorescent probes is particularly of interest for preclinical studies using fluorescence microscopy on human brain tissue. In this study, we newly designed and synthesized three push-pull benzothiazole (PP-BTA) derivatives as fluorescent probes for detection of Aß and α-syn aggregates. Fluorescence intensity of all PP-BTA derivatives significantly increased upon binding to Aß(1-42) and α-syn aggregates in solution. In in vitro saturation binding assays, PP-BTA derivatives demonstrated affinity for both Aß(1-42) (K = 40-148 nM) and α-syn (K = 48-353 nM) aggregates. In particular, PP-BTA-4 clearly stained senile plaques composed of Aß aggregates in the AD brain section. Moreover, it also labeled Lewy bodies composed of α-syn aggregates in the PD brain section. These results suggest that PP-BTA-4 may serve as a promising fluorescent probe for the detection of Aß and α-syn aggregates.
[Mh] Termos MeSH primário: Peptídeos beta-Amiloides/metabolismo
Benzotiazóis
Encéfalo/metabolismo
Encéfalo/patologia
Corantes Fluorescentes
Fragmentos de Peptídeos/metabolismo
alfa-Sinucleína/metabolismo
[Mh] Termos MeSH secundário: Idoso
Doença de Alzheimer/metabolismo
Doença de Alzheimer/patologia
Benzotiazóis/síntese química
Benzotiazóis/química
Feminino
Corantes Fluorescentes/síntese química
Corantes Fluorescentes/química
Seres Humanos
Imuno-Histoquímica
Corpos de Lewy/metabolismo
Corpos de Lewy/patologia
Masculino
Estrutura Molecular
Doença de Parkinson/metabolismo
Doença de Parkinson/patologia
Placa Amiloide/metabolismo
Placa Amiloide/patologia
Ligação Proteica
Soluções
Espectrometria de Fluorescência
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Amyloid beta-Peptides); 0 (Benzothiazoles); 0 (Fluorescent Dyes); 0 (Peptide Fragments); 0 (SNCA protein, human); 0 (Solutions); 0 (alpha-Synuclein); 0 (amyloid beta-protein (1-42))
[Em] Mês de entrada:1712
[Cu] Atualização por classe:180226
[Lr] Data última revisão:
180226
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170504
[St] Status:MEDLINE
[do] DOI:10.1021/acschemneuro.6b00450


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[PMID]:29199735
[Au] Autor:Elsayed MSA; Chang S; Cushman M
[Ad] Endereço:Department of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, and the Purdue Center for Cancer Research, Purdue University, West Lafayette, Indiana 47907, USA. cushman@purdue.edu.
[Ti] Título:Ligand-free, palladacycle-facilitated Suzuki coupling of hindered 2-arylbenzothiazole derivatives yields potent and selective COX-2 inhibitors.
[So] Source:Org Biomol Chem;16(1):108-118, 2017 Dec 19.
[Is] ISSN:1477-0539
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A similarity search and molecular modeling study suggested the 2'-aryl-2-arylbenzothiazole framework as a novel scaffold for the design of COX-2-selective inhibitors. Conventional Suzuki coupling conditions did not furnish the designed compounds in good yield from 2'-bromo-2-arylbenzothiazole as the starting material. A novel ligand-free Suzuki-Miyaura coupling methodology was developed for sterically hindered 2'-bromo-2-arylbenzothiazoles. The reaction depends on the coordination properties of the benzothiazole ring nitrogen, which is involved in the formation of a palladacyclic intermediate that was synthesized independently and converted to the final product. The new method provides good to excellent yields (up to 99%) with favorable functional group tolerability. Six compounds had potencies in the submicromolar range against COX-2 and higher selectivity for COX-2 vs. COX-1 compared to the currently used drug celecoxib. Molecular modeling was used to investigate the possible binding mode with COX-2.
[Mh] Termos MeSH primário: Benzotiazóis/farmacologia
Inibidores de Ciclo-Oxigenase 2/farmacologia
Ciclo-Oxigenase 2/metabolismo
[Mh] Termos MeSH secundário: Benzotiazóis/síntese química
Benzotiazóis/química
Inibidores de Ciclo-Oxigenase 2/síntese química
Inibidores de Ciclo-Oxigenase 2/química
Relação Dose-Resposta a Droga
Seres Humanos
Modelos Moleculares
Estrutura Molecular
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (Cyclooxygenase 2 Inhibitors); EC 1.14.99.1 (Cyclooxygenase 2); G5BW2593EP (benzothiazole)
[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:171205
[St] Status:MEDLINE
[do] DOI:10.1039/c7ob02386c


  4 / 5207 MEDLINE  
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[PMID]:29295712
[Au] Autor:Ovais M; Ayaz M; Khalil AT; Shah SA; Jan MS; Raza A; Shahid M; Shinwari ZK
[Ad] Endereço:Department of Biotechnology, Quaid-i-Azam University, Islamabad, 44000, Pakistan.
[Ti] Título:HPLC-DAD finger printing, antioxidant, cholinesterase, and α-glucosidase inhibitory potentials of a novel plant Olax nana.
[So] Source:BMC Complement Altern Med;18(1):1, 2018 Jan 03.
[Is] ISSN:1472-6882
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: The medicinal importance of a novel plant Olax nana Wall. ex Benth. (family: Olacaceae) was revealed for the first time via HPLC-DAD finger printing, qualitative phytochemical analysis, antioxidant, cholinesterase, and α-glucosidase inhibitory assays. METHODS: The crude methanolic extract of O. nana (ON-Cr) was subjected to qualitative phytochemical analysis and HPLC-DAD finger printing. The antioxidant potential of ON-Cr was assessed via 1,1-diphenyl,2-picrylhydrazyl (DPPH), 2,2-azinobis[3-ethylbenzthiazoline]-6-sulfonic acid (ABTS) and hydrogen peroxide (H O ) free radical scavenging assays. Furthermore, acetylcholinesterase (AChE) & butyrylcholinesterase (BChE) inhibitory activities were performed using Ellman's assay, while α- glucosidase inhibitory assay was carried out using a standard protocol. RESULTS: The qualitative phytochemical analysis of ON-Cr revealed the presence of secondary metabolites like alkaloids, flavonoids, tannins, sterols, saponins and terpenoids. The HPLC-DAD finger printing revealed the presence of 40 potential compounds in ON-Cr. Considerable anti-radical activities was revealed by ON-Cr in the DPPH, ABTS and H O free radical scavenging assays with IC values of 71.46, 72.55 and 92.33 µg/mL, respectively. Furthermore, ON-Cr showed potent AChE and BChE inhibitory potentials as indicated by their IC values of 33.2 and 55.36 µg/mL, respectively. In the α-glucosidase inhibition assay, ON-Cr exhibited moderate inhibitory propensity with an IC value of 639.89 µg/mL. CONCLUSIONS: This study investigated Olax nana for the first time for detailed qualitative phytochemical tests, HPLC-DAD finger printing analysis, antioxidant, anticholinesterase and α-glucosidase inhibition assays. The antioxidant and cholinesterase inhibitory results were considerable and can provide scientific basis for further studies on the neuroprotective and anti-Alzheimer's potentials of this plant. ON-Cr may further be subjected to fractionation and polarity guided fractionation to narrow down the search for isolation of bioactive compounds.
[Mh] Termos MeSH primário: Antioxidantes/análise
Inibidores da Colinesterase/análise
Cromatografia Líquida de Alta Pressão/métodos
Inibidores de Glicosídeo Hidrolases/análise
Olacaceae/química
Extratos Vegetais/análise
[Mh] Termos MeSH secundário: Antioxidantes/química
Antioxidantes/metabolismo
Benzotiazóis/análise
Benzotiazóis/metabolismo
Compostos de Bifenilo/análise
Compostos de Bifenilo/metabolismo
Inibidores da Colinesterase/química
Inibidores da Colinesterase/metabolismo
Inibidores de Glicosídeo Hidrolases/química
Inibidores de Glicosídeo Hidrolases/metabolismo
Peróxido de Hidrogênio/análise
Peróxido de Hidrogênio/metabolismo
Picratos/análise
Picratos/metabolismo
Extratos Vegetais/química
Extratos Vegetais/metabolismo
Ácidos Sulfônicos/análise
Ácidos Sulfônicos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Benzothiazoles); 0 (Biphenyl Compounds); 0 (Cholinesterase Inhibitors); 0 (Glycoside Hydrolase Inhibitors); 0 (Picrates); 0 (Plant Extracts); 0 (Sulfonic Acids); 28752-68-3 (2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid); BBX060AN9V (Hydrogen Peroxide); DFD3H4VGDH (1,1-diphenyl-2-picrylhydrazyl)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180216
[Lr] Data última revisão:
180216
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180104
[St] Status:MEDLINE
[do] DOI:10.1186/s12906-017-2057-9


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[PMID]:29273507
[Au] Autor:Furuya T; Takehara I; Shimura A; Kishimoto H; Yasujima T; Ohta K; Shirasaka Y; Yuasa H; Inoue K
[Ad] Endereço:Department of Biopharmaceutics, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
[Ti] Título:Organic anion transporter 1 (OAT1/SLC22A6) enhances bioluminescence based on d-luciferin-luciferase reaction in living cells by facilitating the intracellular accumulation of d-luciferin.
[So] Source:Biochem Biophys Res Commun;495(3):2152-2157, 2018 01 15.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Bioluminescence (BL) imaging based on d-luciferin (d-luc)-luciferase reaction allows noninvasive and real-time monitoring of luciferase-expressing cells. Because BL intensity depends on photons generated through the d-luc-luciferase reaction, an approach to increase intracellular levels of d-luc could improve the detection sensitivity. In the present study, we showed that organic anion transporter 1 (OAT1) is useful, as a d-luc transporter, in boosting the BL intensity in luciferase-expressing cells. Functional screening of several transporters showed that the expression of OAT1 in HEK293 cells stably expressing Pyrearinus termitilluminans luciferase (HEK293/eLuc) markedly enhanced BL intensity in the presence of d-luc. When OAT1 was transiently expressed in HEK293 cells, intracellular accumulation of d-luc was higher than that in control cells, and the specific d-luc uptake mediated by OAT1 was saturable with a Michaelis constant (K ) of 0.23 µM. The interaction between OAT1 and d-luc was verified using 6-carboxyfluorescein, a typical substrate of OAT1, which showed that d-luc inhibited the uptake of 6-carboxyfluorescein mediated by OAT1. BL intensity was concentration-dependent at steady states in HEK293/eLuc cells stably expressing OAT1, and followed Michaelis-Menten kinetics with an apparent K of 0.36 µM. In addition, the enhanced BL was significantly inhibited by OAT1-specific inhibitors. Thus, OAT1-mediated transport of d-luc could be a rate-limiting step in the d-luc-luciferase reaction. Furthermore, we found that expressing OAT1 in HEK293/eLuc cells implanted subcutaneously in mice also significantly increased the BL after intraperitoneal injection of d-luc. Our findings suggest that because OAT1 is capable of transporting d-luc, it can also be used to improve visualization and monitoring of luciferase-expressing cells.
[Mh] Termos MeSH primário: Benzotiazóis/metabolismo
Aumento da Imagem/métodos
Luciferases/metabolismo
Medições Luminescentes/métodos
Proteína 1 Transportadora de Ânions Orgânicos/metabolismo
[Mh] Termos MeSH secundário: Genes Reporter/genética
Células HEK293
Seres Humanos
Luciferases/genética
Imagem Molecular/métodos
Reprodutibilidade dos Testes
Sensibilidade e Especificidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (D-luciferin); 0 (Organic Anion Transport Protein 1); EC 1.13.12.- (Luciferases)
[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:171224
[St] Status:MEDLINE


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[PMID]:29372659
[Au] Autor:Ugwu DI; Okoro UC; Ukoha PO; Gupta A; Okafor SN
[Ad] Endereço:a Department of Pure and Industrial Chemistry , University of Nigeria , Nsukka , Nigeria.
[Ti] Título:Novel anti-inflammatory and analgesic agents: synthesis, molecular docking and in vivo studies.
[So] Source:J Enzyme Inhib Med Chem;33(1):405-415, 2018 Dec.
[Is] ISSN:1475-6374
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Twelve new derivatives of benzothiazole bearing benzenesulphonamide and carboxamide were synthesised and investigated for their in vivo anti-inflammatory, analgesic and ulcerogenic activities. Molecular docking showed an excellent binding interaction of the synthesised compounds with the receptors, with 17c showing the highest binding energy (-12.50 kcal/mol). Compounds 17c and 17i inhibited carrageenan-induced rat paw oedema at 72, 76, and 80% and 64, 73, and 78% at 1 h, 2 h, and 3 h, respectively. In the analgesic activity experiment, compounds 17c, 17 g, and 17i had ED (µM/kg) of 96, 127, and 84 after 0.5 h; 102, 134, and 72 after 1 h and 89, 156, and 69 µM/kg after 2 h, respectively, which were comparable with 156, 72, and 70 µM/kg for celecoxib. The ulcerogenic index of the most active derivatives 17c and 17i were 0.82 and 0.89, respectively, comparable to 0.92 for celecoxib. The physicochemical studies of the new derivatives showed that they will not have oral bioavailability problems.
[Mh] Termos MeSH primário: Analgésicos/farmacologia
Anti-Inflamatórios não Esteroides/farmacologia
Antiulcerosos/farmacologia
Benzotiazóis/farmacologia
Simulação de Acoplamento Molecular
[Mh] Termos MeSH secundário: Analgésicos/síntese química
Analgésicos/química
Animais
Anti-Inflamatórios não Esteroides/síntese química
Anti-Inflamatórios não Esteroides/química
Antiulcerosos/síntese química
Antiulcerosos/química
Benzotiazóis/síntese química
Benzotiazóis/química
Edema/tratamento farmacológico
Masculino
Camundongos
Estrutura Molecular
Ratos
Úlcera/induzido quimicamente
Úlcera/tratamento farmacológico
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Analgesics); 0 (Anti-Inflammatory Agents, Non-Steroidal); 0 (Anti-Ulcer Agents); 0 (Benzothiazoles)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180212
[Lr] Data última revisão:
180212
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:180127
[St] Status:MEDLINE
[do] DOI:10.1080/14756366.2018.1426573


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[PMID]:29224279
[Au] Autor:Bai J; Zhang Y; Wang YF; Lan J; Li XQ
[Ad] Endereço:Department of Pathophysiology, Shanxi Medical University, Taiyuan 030001, China.
[Ti] Título:[Overexpression of TRPV1 after periphery nerve injury attenuates nerve regeneration in rats].
[So] Source:Zhonghua Bing Li Xue Za Zhi;46(12):847-852, 2017 Dec 08.
[Is] ISSN:0529-5807
[Cp] País de publicação:China
[La] Idioma:chi
[Ab] Resumo:To observe the effect of the expressive or functional blockage of TRPV1 on nerve regeneration after sciatic trans-section injury. AMG-517, a kind of TRPV1 inhibitor, was injected into the surrounding area of the ipsilateral lumbar dorsal root ganglia while unilateral sciatic nerve was transected. A total of 24 healthy male Sprague-Dawley rats were divided into 4 groups: control group, injury only group, injury+ AMG-517 150 µg/kg group, injury+ AMG-517 300 µg/kg group. The injury only group was injected the same volume of medium. The release of CGRP from dorsal-horn of spinal cord, the number of axons at proximal stem of sciatic nerve after transection, and the expression of TRPV1 in dorsal root ganglion were detected using the methods of ELISA, Western blot and semi-thin section (1 µm)- toluidine blue staining 2 weeks after injury. The release of CGRP in lumbar spinal dorsal horn was obviously decreased after AMG-517 treatment, which was the evidence of TRPV1 functional inhibition. CGRP in the control group was 0.15 ng/g, the injury only group 0.17 ng/g, AMG-517 150 µg/kg group 0.09 ng/g, and AMG-517 300 µg/kg group 0.11 ng/g( <0.01). The number of axons which were myelinated or unmyelinated increased after the TRPV1 was inhibited by AMG-517( <0.01). In addition, the injection of AMG-517 into surrounding dorsal root ganglion decreased the expression of TRPV1 in dorsal root ganglion( <0.01). Over expression or activation of TRPV1 after periphery nerve injury has negative effect on nerve regeneration in fact; Inhibiting the over-expression or over-activation of TRPV1 after nerve injury facilitates axonal regeneration and nerve repair.
[Mh] Termos MeSH primário: Regeneração Nervosa
Nervo Isquiático/lesões
Canais de Cátion TRPV/metabolismo
[Mh] Termos MeSH secundário: Animais
Axônios
Benzotiazóis/farmacologia
Gânglios Espinais/efeitos dos fármacos
Gânglios Espinais/metabolismo
Masculino
Pirimidinas/farmacologia
Ratos
Ratos Sprague-Dawley
Medula Espinal
Canais de Cátion TRPV/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (N-(4-(6-(4-trifluoromethylphenyl)pyrimidin-4-yloxy)benzothiazol-2-yl)acetamide); 0 (Pyrimidines); 0 (TRPV Cation Channels); 0 (Trpv1 protein, rat)
[Em] Mês de entrada:1802
[Cu] Atualização por classe:180202
[Lr] Data última revisão:
180202
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171212
[St] Status:MEDLINE
[do] DOI:10.3760/cma.j.issn.0529-5807.2017.12.007


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[PMID]:28462585
[Au] Autor:Ye Z; Hammer A; Münte TF
[Ad] Endereço:1 Department of Neurology, University of Lübeck , Lübeck, Germany .
[Ti] Título:Pramipexole Modulates Interregional Connectivity Within the Sensorimotor Network.
[So] Source:Brain Connect;7(4):258-263, 2017 May.
[Is] ISSN:2158-0022
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Pramipexole is widely prescribed to treat Parkinson's disease but has been reported to cause impulse control disorders such as pathological gambling. Recent neurocomputational models suggested that D2 agonists may distort functional connections between the striatum and the motor cortex, resulting in impaired reinforcement learning and pathological gambling. To examine how D2 agonists modulate the striatal-motor connectivity, we carried out a pharmacological resting-state functional magnetic resonance imaging study with a double-blind randomized within-subject crossover design. We analyzed the medication-induced changes of network connectivity and topology with two approaches, an independent component analysis (ICA) and a graph theoretical analysis (GTA). The ICA identified the sensorimotor network (SMN) as well as other classical resting-state networks. Within the SMN, the connectivity between the right caudate nucleus and other cortical regions was weaker under pramipexole than under placebo. The GTA measured the topological properties of the whole-brain network at global and regional levels. Both the whole-brain network under placebo and that under pramipexole were identified as small-world networks. The two whole-brain networks were similar in global efficiency, clustering coefficient, small-world index, and modularity. However, the degree of the right caudate nucleus decreased under pramipexole mainly due to the loss of the connectivity with the supplementary motor area, paracentral lobule, and precentral and postcentral gyrus of the SMN. The two network analyses consistently revealed that pramipexole weakened the functional connectivity between the caudate nucleus and the SMN regions.
[Mh] Termos MeSH primário: Benzotiazóis/farmacologia
Agonistas de Dopamina/farmacologia
Neostriado/efeitos dos fármacos
Córtex Sensório-Motor/efeitos dos fármacos
[Mh] Termos MeSH secundário: Adulto
Encéfalo/diagnóstico por imagem
Encéfalo/efeitos dos fármacos
Encéfalo/fisiologia
Estudos Cross-Over
Método Duplo-Cego
Neuroimagem Funcional
Voluntários Saudáveis
Seres Humanos
Masculino
Córtex Motor/diagnóstico por imagem
Córtex Motor/efeitos dos fármacos
Córtex Motor/fisiologia
Neostriado/diagnóstico por imagem
Neostriado/fisiologia
Vias Neurais/diagnóstico por imagem
Vias Neurais/efeitos dos fármacos
Vias Neurais/fisiologia
Córtex Sensório-Motor/diagnóstico por imagem
Córtex Sensório-Motor/fisiologia
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (Dopamine Agonists); 83619PEU5T (pramipexole)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180130
[Lr] Data última revisão:
180130
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170503
[St] Status:MEDLINE
[do] DOI:10.1089/brain.2017.0484


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[PMID]:29179216
[Au] Autor:Sakai G; Tokuda H; Fujita K; Kainuma S; Kawabata T; Matsushima-Nishiwaki R; Kozawa O; Otsuka T
[Ad] Endereço:Department of Orthopedic Surgery, Nagoya City University Graduate School of Medical Sciences, Nagoya, Japan.
[Ti] Título:Heat Shock Protein 70 Negatively Regulates TGF-ß-Stimulated VEGF Synthesis via p38 MAP Kinase in Osteoblasts.
[So] Source:Cell Physiol Biochem;44(3):1133-1145, 2017.
[Is] ISSN:1421-9778
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND/AIMS: We previously demonstrated that transforming growth factor-ß (TGF-ß) stimulates the synthesis of vascular endothelial growth factor (VEGF) through the activation of p38 mitogen-activated protein (MAP) kinase in osteoblast-like MC3T3-E1 cells. Heat shock protein70 (HSP70) is a ubiquitously expressed molecular chaperone. In the present study, we investigated the involvement of HSP70 in the TGF-ß-stimulated VEGF synthesis and the underlying mechanism in these cells. METHODS: Culture MC3T3-E1 cells were stimulated by TGF-ß. Released VEGF was measured using an ELISA assay. VEGF mRNA level was quantified by RT-PCR. Phosphorylation of each protein kinase was analyzed by Western blotting. RESULTS: VER-155008 and YM-08, both of HSP70 inhibitors, significantly amplified the TGF-ß-stimulated VEGF release. In addition, the expression level of VEGF mRNA induced by TGF-ß was enhanced by VER-155008. These inhibitors markedly strengthened the TGF-ß-induced phosphorylation of p38 MAP kinase. The TGF-ß-induced phosphorylation of p38 MAP kinase was amplified in HSP70-knockdown cells. SB203580, an inhibitor of p38 MAP kinase, significantly suppressed the amplification by these inhibitors of the TGF-ß-induced VEGF release. CONCLUSION: These results strongly suggest that HSP70 acts as a negative regulator in the TGF-ß-stimulated VEGF synthesis in osteoblasts, and that the inhibitory effect of HSP70 is exerted at a point upstream of p38 MAP kinase.
[Mh] Termos MeSH primário: Proteínas de Choque Térmico HSP70/metabolismo
Fator de Crescimento Transformador beta/farmacologia
Fator A de Crescimento do Endotélio Vascular/metabolismo
Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
[Mh] Termos MeSH secundário: Animais
Benzotiazóis/farmacologia
Linhagem Celular
Ensaio de Imunoadsorção Enzimática
Proteínas de Choque Térmico HSP70/antagonistas & inibidores
Proteínas de Choque Térmico HSP70/genética
Imidazóis/farmacologia
Camundongos
Osteoblastos/citologia
Osteoblastos/efeitos dos fármacos
Osteoblastos/metabolismo
Fosforilação/efeitos dos fármacos
Nucleosídeos de Purina/farmacologia
Piridinas/farmacologia
Interferência de RNA
RNA Interferente Pequeno
Reação em Cadeia da Polimerase em Tempo Real
Proteína Smad2/metabolismo
Proteína Smad3/metabolismo
Tiazolidinas/farmacologia
Fator A de Crescimento do Endotélio Vascular/análise
Fator A de Crescimento do Endotélio Vascular/genética
Proteínas Quinases p38 Ativadas por Mitógeno/antagonistas & inibidores
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Benzothiazoles); 0 (HSP70 Heat-Shock Proteins); 0 (Imidazoles); 0 (Purine Nucleosides); 0 (Pyridines); 0 (RNA, Small Interfering); 0 (Smad2 Protein); 0 (Smad3 Protein); 0 (Thiazolidines); 0 (Transforming Growth Factor beta); 0 (VER 155008); 0 (Vascular Endothelial Growth Factor A); 0 (YM-08 compound); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); OU13V1EYWQ (SB 203580)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180118
[Lr] Data última revisão:
180118
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.1159/000485418


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[PMID]:29197733
[Au] Autor:Alborz M; Jarrahpour A; Pournejati R; Karbalaei-Heidari HR; Sinou V; Latour C; Brunel JM; Sharghi H; Aberi M; Turos E; Wojtas L
[Ad] Endereço:Department of Chemistry, College of Sciences, Shiraz University, Shiraz, 71946-84795, Iran.
[Ti] Título:Synthesis and biological evaluation of some novel diastereoselective benzothiazole ß-lactam conjugates.
[So] Source:Eur J Med Chem;143:283-291, 2018 Jan 01.
[Is] ISSN:1768-3254
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:Highly diastereoselective synthesis of some novel benzothiazole-substituted ß-lactam hybrids was achieved starting from (benzo[d]thiazol-2-yl)phenol as an available precursor. This is the first time (benzo[d]thiazol-2-yl)phenoxyacetic acid has been used as ketene source in synthesizing monocyclic 2-azetidinones. These compounds were evaluated for their antimicrobial activities against a large panel of Gram-positive and Gram-negative bacterial strains and moderate activities were encountered. Antimalarial data revealed that adding methoxyphenyl or ethoxyphenyl group on the ß-lactam ring makes compounds that are more potent. Moreover, hemolytic activity and mammalian cell toxicity survey of the compounds showed their potential as a medicine.
[Mh] Termos MeSH primário: Antibacterianos/farmacologia
Antifúngicos/farmacologia
Antimaláricos/farmacologia
Benzotiazóis/farmacologia
beta-Lactamas/farmacologia
[Mh] Termos MeSH secundário: Antibacterianos/síntese química
Antibacterianos/química
Anti-Infecciosos
Antifúngicos/síntese química
Antifúngicos/química
Antimaláricos/síntese química
Antimaláricos/química
Bactérias/efeitos dos fármacos
Bactérias/crescimento & desenvolvimento
Benzotiazóis/síntese química
Benzotiazóis/química
Sobrevivência Celular/efeitos dos fármacos
Relação Dose-Resposta a Droga
Fungos/efeitos dos fármacos
Fungos/crescimento & desenvolvimento
Células Hep G2
Seres Humanos
Estrutura Molecular
Plasmodium falciparum/efeitos dos fármacos
Estereoisomerismo
Relação Estrutura-Atividade
beta-Lactamas/síntese química
beta-Lactamas/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Anti-Infective Agents); 0 (Antifungal Agents); 0 (Antimalarials); 0 (Benzothiazoles); 0 (beta-Lactams); G5BW2593EP (benzothiazole)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180101
[Lr] Data última revisão:
180101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171204
[St] Status:MEDLINE



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