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1.
Biomed Res Int ; 2021: 9987860, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34195290

RESUMO

Purpose: The potential of UV-mediated photofunctionalization to enhance the resin-based luting agent bonding performance to aged materials was investigated. Methods: Sixty samples of each material were prepared. Yttria-stabilized zirconia (YZr) and Pd-Au alloy (Pd-Au) plates were fabricated and sandblasted. Lithium disilicate glass-ceramic (LDS) was CAD-CAM prepared and ground with #800 SiC paper. Half of the specimens were immersed in machine oil for 24 h to simulate the carbon adsorption. Then, all of the specimens (noncarbon- and carbon-adsorbed) were submitted to UV-mediated photofunctionalization with a 15 W UV-LED (265 nm, 300 mA, 7692 µW/cm2) for 0 (control groups), 5, and 15 min and subjected to contact angle (Ɵ) measurement and bonded using a resin cement (Panavia™ V5, Kuraray Noritake, Japan). The tensile bond strength (TBS) test was performed after 24 h. The Ɵ (°) and TBS (MPa) data were statistically analyzed using two-way ANOVA and Bonferroni correction tests (α = 0.05). Results: In the carbon-adsorbed groups, UV-mediated photofunctionalization for 5 min significantly decreased Ɵ of all materials and increased TBS of YZr, and UV for 15 min significantly increased the TBS of LDS and Pd-Au. In noncarbon-adsorbed groups, UV-photofunctionalization did not significantly change the Ɵ or TBS except YZr specimens UV-photofunctionalized for 15 min. Conclusion: UV-mediated photofunctionalization might have removed the adsorbed hydrocarbon molecules from the materials' surfaces and enhanced bond strengths of Panavia™ V5 to YZr, LDS, and Pd-Au. Additionally, UV-mediated photofunctionalization improved the overall TBS of YZr. Further investigation on the optimum conditions of UV photofunctionalization on indirect restorative materials should be conducted.


Assuntos
Ligas Dentárias , Fotoquímica/métodos , Cimentos de Resina/química , Adsorção , Carbono , Cerâmica , Desenho Assistido por Computador , Colagem Dentária , Porcelana Dentária , Análise do Estresse Dentário , Ouro/química , Humanos , Hidrocarbonetos/química , Teste de Materiais , Paládio/química , Estudos Prospectivos , Propriedades de Superfície , Resistência à Tração , Raios Ultravioleta , Ítrio/química , Zircônio/química
2.
J Nutr Sci Vitaminol (Tokyo) ; 65(Supplement): S200-S205, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31619631

RESUMO

Salt is an important seasoning that adds a salty taste to enhance or suppress other tastes in cooking. Porridge is treated with salt, even with the addition of a small amount of salt to tighten its taste. This salty taste intensity is also influenced by the amount of bittern component contained in the salt because not only the bittern component but also the change of pH affects the degree of swelling and penetration into rice. However, excessive salt intake causes lifestyle-related diseases. For that reason, salt intake reduction is recommended. When salt and citric acid are added to the porridge simultaneously, the contrasting effects of acidity and saltiness enhance the salty flavor, allowing for the reduction of salt intake.


Assuntos
Culinária/métodos , Oryza/química , Cloreto de Sódio na Dieta/análise , Cloreto de Sódio/química , Paladar , Ácido Cítrico/administração & dosagem , Grão Comestível , Humanos
3.
Chem Pharm Bull (Tokyo) ; 65(10): 920-929, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28966276

RESUMO

Buprenorphine shows strong analgesic effects on moderate to severe pain. Although buprenorphine can be used more safely than other opioid analgesics, it has room for improvement in clinical utility. Investigation of compounds structurally related to buprenorphine should be an approach to obtain novel analgesics with safer and improved profiles compared to buprenorphine. In the course of our previous studies, we observed that derivatives obtained by cyclizing C-homomorphinans were structurally related to buprenorphine. Hence, we synthesized cyclized C-homomorphinan derivatives with various oxygen functionalities on the side chains and evaluated their in vitro pharmacological profiles for the opioid receptors. Among the tested compounds, methyl ketone 2a with an N-methyl group showed full agonistic activities for the µ and the δ receptors and partial agonistic activity for the κ receptor. These properties were similar to those of norbuprenorphine, a major metabolite of buprenorphine, which reportedly contributes to the antinociceptive effect of buprenorphine. From these results, we concluded that cyclized C-homomorphinan would be a possible lead compound to obtain novel analgesics with buprenorphine-like properties.


Assuntos
Analgésicos Opioides/química , Morfinanos/química , Analgésicos Opioides/síntese química , Animais , Buprenorfina/análogos & derivados , Buprenorfina/química , Células CHO , Cricetinae , Cricetulus , Ciclização , Humanos , Cinética , Conformação Molecular , Morfinanos/síntese química , Ligação Proteica , Receptores Opioides/química , Receptores Opioides/genética , Receptores Opioides/metabolismo , Proteínas Recombinantes/biossíntese , Proteínas Recombinantes/química , Proteínas Recombinantes/isolamento & purificação
4.
Bioorg Med Chem ; 24(10): 2199-205, 2016 05 15.
Artigo em Inglês | MEDLINE | ID: mdl-27079125

RESUMO

As the reports about C-homomorphinans with the seven-membered C-ring are much fewer than those of morphinan derivatives with a six-membered C-ring, we attempted to synthesize C-homomorphinan derivatives and to evaluate their opioid activities. C-Homomorphinan 5 showed sufficient binding affinities to the opioid receptors. C-Homomorphinan derivatives possessing the δ address moiety such as indole (NTI-type), quinoline, or benzylidene (BNTX-type) functionalities showed the strongest binding affinities for the δ receptor among the three types of opioid receptors, which indicated that the C-homomorphinan skeleton sufficiently functions as a message-part in the ligand. Although NTI-type compound 8 and quinoline compound 9 with C-homomorphinan scaffold exhibited lower affinities and selectivities for the δ receptor than the corresponding morphinan derivatives did, both the binding affinity and selectivity for the δ receptor of BNTX-type compound 12 with a seven-membered C-ring were improved compared with the corresponding compounds with a six-membered C-ring including BNTX itself. BNTX-Type compound 12 was the most selective δ receptor antagonist among the tested compounds.


Assuntos
Morfinanos/química , Morfinanos/farmacologia , Antagonistas de Entorpecentes/química , Antagonistas de Entorpecentes/farmacologia , Receptores Opioides delta/antagonistas & inibidores , Receptores Opioides/metabolismo , Analgésicos Opioides/síntese química , Analgésicos Opioides/química , Analgésicos Opioides/farmacologia , Animais , Compostos de Benzilideno/síntese química , Compostos de Benzilideno/química , Compostos de Benzilideno/farmacologia , Células CHO , Cricetulus , Humanos , Ligantes , Modelos Moleculares , Morfinanos/síntese química , Naltrexona/análogos & derivados , Naltrexona/síntese química , Naltrexona/química , Naltrexona/farmacologia , Antagonistas de Entorpecentes/síntese química , Quinolinas/síntese química , Quinolinas/química , Quinolinas/farmacologia , Receptores Opioides delta/metabolismo , Relação Estrutura-Atividade
5.
Sangyo Eiseigaku Zasshi ; 54(3): 101-7, 2012.
Artigo em Japonês | MEDLINE | ID: mdl-22869201

RESUMO

OBJECTIVE: It is reported that presenteeism costs more than absenteeism. However, it is difficult to measure presenteeism in Japan because there are few available instruments. We examined the reliability and validity of the Japanese version of the Work limitations Questionnaire (the WLQ-J). METHODS: We conducted an internet survey with the WLQ-J and Brief Job Stress Questionnaire (BJSQ) of 1,545 males and females working for an IT company and a medical institution (21-61 years of age). The number of employees of the IT company and nursing staff of the medical institution included in the analysis were 373 and 337, respectively (effective response rate: 46.0 %). RESULTS: The subjects' average age and the ratio of females were 33.2 ± 9.5 yr old and 60.3%, respectively. Factor analysis showed that the number of factors and items of subscales of the WLQ-J accorded with those of the original WLQ. This supports the factorial validity of the WLQ-J. Additionally, sufficient internal consistency was recognized by Cronbach's alpha (the whole scale=0.97, the subscales=0.88-0.95). Criterion-related validity was supported by the significant dose-response relationship between the subscale scores of the WLQ-J and the stress response of BJSQ as an external criterion (p<0.01). CONCLUSIONS: The study results demonstrate the reliability and validity of the WLQ-J. It is expected that human resource functions such as senior management, personnel affairs, line management, and occupational health staff over a wide range of industries will use the WLQ-J. Further studies are needed to verify the reliability and validity of the WLQ-J by examining differences in the WLQ-J arising from gender, age, industry, and occupation between multiple studies, and by finding relationships between the WLQ-J and other evaluation scales.


Assuntos
Saúde do Trabalhador , Psicologia Industrial , Adulto , Análise Fatorial , Feminino , Humanos , Japão , Masculino , Pessoa de Meia-Idade , Reprodutibilidade dos Testes , Estresse Psicológico , Inquéritos e Questionários , Adulto Jovem
6.
J Neurosci ; 29(15): 4972-80, 2009 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-19369566

RESUMO

In Drosophila, odor information received by olfactory receptor neurons (ORNs) is processed by glomeruli, which are organized in a stereotypic manner in the antennal lobe (AL). This glomerular organization is regulated by Wnt5 signaling. In the embryonic CNS, Wnt5 signaling is transduced by the Drl receptor, a member of the Ryk family. During development of the olfactory system, however, it is antagonized by Drl. Here, we identify Drl-2 as a receptor mediating Wnt5 signaling. Drl is found in the neurites of brain cells in the AL and specific glia, whereas Drl-2 is predominantly found in subsets of growing ORN axons. A drl-2 mutation produces only mild deficits in glomerular patterning, but when it is combined with a drl mutation, the phenotype is exacerbated and more closely resembles the Wnt5 phenotype. Wnt5 overexpression in ORNs induces aberrant glomeruli positioning. This phenotype is ameliorated in the drl-2 mutant background, indicating that Drl-2 mediates Wnt5 signaling. In contrast, forced expression of Drl-2 in the glia of drl mutants rescues the glomerular phenotype caused by the loss of antagonistic Drl function. Therefore, Drl-2 can also antagonize Wnt5 signaling. Additionally, our genetic data suggest that Drl localized to developing glomeruli mediates Wnt5 signaling. Thus, these two members of the Ryk family are capable of carrying out a similar molecular function, but they can play opposing roles in Wnt5 signaling, depending on the type of cells in which they are expressed. These molecules work cooperatively to establish the olfactory circuitry in Drosophila.


Assuntos
Proteínas de Drosophila/fisiologia , Regulação da Expressão Gênica no Desenvolvimento/fisiologia , Condutos Olfatórios/crescimento & desenvolvimento , Proteínas Proto-Oncogênicas/fisiologia , Receptores Proteína Tirosina Quinases/fisiologia , Transdução de Sinais/fisiologia , Olfato/fisiologia , Proteínas Wnt/fisiologia , Animais , Animais Geneticamente Modificados , Drosophila , Proteínas de Drosophila/biossíntese , Proteínas de Drosophila/genética , Mutação , Neuroglia/metabolismo , Neuroglia/fisiologia , Proteínas Proto-Oncogênicas/biossíntese , Proteínas Proto-Oncogênicas/genética , Receptores Proteína Tirosina Quinases/biossíntese , Receptores Proteína Tirosina Quinases/genética , Transdução de Sinais/genética , Proteínas Wnt/biossíntese , Proteínas Wnt/genética
7.
Bioorg Med Chem ; 16(3): 1090-5, 2008 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-18024044

RESUMO

The preparation of both enantiomers of 8-[1-(2,4-dichlorophenyl)-2-imidazol-1-yl-ethoxy] octanoic acid heptyl ester (JM-8686), a potent inhibitor of allene oxide synthase, has been achieved using 2,4-dichlorophenacyl bromide as a starting material. The key step was the asymmetric reduction of 1-(2,4-dichlorophenyl)-2-imidazol-1-yl-ethanone with chiral BINAL-H. The products were purified by chiral high-performance liquid chromatography (HPLC) to afford pure (R)-JM-8686 and (S)-JM-8686. The inhibitory activities and binding affinities of these enantiomers toward allene oxide synthase were determined. We found that the inhibition potency of (R)-JM-8686 is approximately 200 times greater than that of (S)-JM-8686, with IC(50) values of approximately 5+/-0.2 nM and 950+/-18 nM, respectively. The dissociation constants of (R)-JM-8686 and (S)-JM-8686 with respect to the recombinant allene oxide synthase were approximately 1.4+/-0.3 microM and 4.8+/-0.6 microM, respectively.


Assuntos
Caprilatos/química , Caprilatos/farmacologia , Imidazóis/química , Imidazóis/farmacologia , Oxirredutases Intramoleculares/antagonistas & inibidores , Oxirredutases Intramoleculares/metabolismo , Cromatografia Líquida de Alta Pressão , Dicroísmo Circular , Estrutura Molecular , Estereoisomerismo , Relação Estrutura-Atividade
8.
FEBS Lett ; 577(1-2): 60-6, 2004 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-15527762

RESUMO

The Sox6 gene is a member of the Sox gene family, which encodes transcription factors, and previous studies have suggested that it plays an important role in the development of the central nervous system. Aggregation of embryonic carcinoma P19 cells with retinoic acid (RA) results in the development of neurons, glia, and fibroblast-like cells. Sox6 mRNA increases rapidly in P19 cells during RA induction and then decreases during differentiation into neuronal cells. To investigate whether Sox6 expression is essential for neuronal differentiation, we established Sox6-suppressed P19 (P19[anti-Sox6]) cells by transfection of antisense-Sox6 cDNA. Most of the P19[anti-Sox6] cells showed no neurites and were not stained by the anti-MAP 2 antibody, while the suppression of Sox6 expression nearly totally blocked neuronal differentiation in P19 cells. Further, Sox6 suppression caused RA-dependent apoptosis by P19[anti-Sox6] cells: RA-treated P19[anti-Sox6] cells showed chromatin condensation, DNA fragmentation, and an increase in caspase-3-like activity. Thus, Sox6 is considered essential for neuronal differentiation and may play an important role in the early stages of neuronal differentiation or apoptosis.


Assuntos
Apoptose/efeitos dos fármacos , Diferenciação Celular/efeitos dos fármacos , Proteínas de Ligação a DNA/genética , Proteínas de Grupo de Alta Mobilidade/genética , Neurônios/citologia , Fatores de Transcrição/genética , Animais , Apoptose/genética , Linhagem Celular , Imuno-Histoquímica , Camundongos , Reação em Cadeia da Polimerase Via Transcriptase Reversa , Fatores de Transcrição SOXD
9.
FEBS Lett ; 560(1-3): 192-8, 2004 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-14988021

RESUMO

The Sox6 gene is a member of the Sox gene family that encodes transcription factors. Previous studies have suggested that Sox6 plays an important role in the development of the central nervous system. Aggregation of embryonic carcinoma P19 cells with retinoic acid (RA) results in the development of neurons, glia and fibroblast-like cells. In this report, we have shown that Sox6 mRNA increased rapidly in P19 cells during RA induction and then decreased during the differentiation of P19 into neuronal cells. To explore the possible roles of Sox6 during this process, stably Sox6-overexpressing P19 cell lines (P19[Sox6]) were established. These P19[Sox6] had acquired both characteristics of the wild-type P19 induced by RA. First, P19[Sox6] cells showed a marked cellular aggregation in the absence of RA. Second, P19[Sox6] could differentiate into microtubule-associated protein 2 (MAP2)-expressing neuronal cells in the absence of RA. Sox6 expression could cause the activation of endogenous genes including the neuronal transcription factor Mash-1, the neuronal development-related gene Wnt-1, the neuron-specific cell adhesion molecule N-cadherin, and the neuron-specific protein MAP2, resulting in neurogenesis. Moreover, E-cadherin, a major cell adhesion molecule of wild-type P19, was strongly induced by Sox6, resulting in cellular aggregation without RA. Thus Sox6 may play a critical role in cellular aggregation and neuronal differentiation of P19 cells.


Assuntos
Carcinoma Embrionário/genética , Diferenciação Celular/genética , Proteínas de Ligação a DNA/metabolismo , Regulação Neoplásica da Expressão Gênica/genética , Proteínas de Grupo de Alta Mobilidade/metabolismo , Neurônios , Neurônios/metabolismo , Fatores de Transcrição/metabolismo , Animais , Moléculas de Adesão Celular/genética , Moléculas de Adesão Celular/metabolismo , Agregação Celular , Linhagem Celular Tumoral , Perfilação da Expressão Gênica , Camundongos , Proteínas Associadas aos Microtúbulos/metabolismo , Neurônios/patologia , RNA Mensageiro/análise , RNA Mensageiro/biossíntese , Fatores de Transcrição SOXD , Ativação Transcricional , Transfecção , Tretinoína
10.
Appl Spectrosc ; 57(11): 1399-406, 2003 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-14658155

RESUMO

The potential of near-infrared (NIR) spectroscopy to measure the main inorganic components of seawater as salt-manufacturing materials was investigated. A total of 72 seawater samples collected from six locations was used, and spectra (1100-1800 nm) were acquired by a NIR spectrophotometer with a 1-mm path length. Principal component analysis (PCA), canonical correlation analysis (CCA), and partial least-squares (PLS) regression were performed based on the reference inorganic components. As a result, the principal component analysis and canonical correlation analysis showed that the near-infrared spectra could be related to the inorganic components of seawater. The partial least-squares regression analysis showed that the inorganic components (ion concentration of Cl, Na+, K+, SO4(2-), and Ca2+) could be predicted with good accuracy using NIR spectra and their second derivatives. For Cl ion and K+ ion concentrations, the accuracy was high.


Assuntos
Algoritmos , Compostos Inorgânicos/análise , Compostos Inorgânicos/química , Análise de Componente Principal , Água do Mar/análise , Água do Mar/química , Espectrofotometria Infravermelho/métodos , Japão , Sensibilidade e Especificidade
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