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[PMID]:29459024
[Au] Autor:Fang P; Yu M; Min W; Wan D; Han S; Shan Y; Wang R; Shi M; Zhang Z; Bo P
[Ad] Endereço:Department of Physiology, Nanjing University of Chinese Medicine Hanlin College, Taizhou, Jiangsu 225300, China; Department of Endocrinology, Clinical Medical College, Yangzhou University, Yangzhou, Jiangsu 225001, China.
[Ti] Título:Effect of baicalin on GLUT4 expression and glucose uptake in myotubes of rats.
[So] Source:Life Sci;196:156-161, 2018 Mar 01.
[Is] ISSN:1879-0631
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:AIMS: Although baicalin could attenuate obesity-induced insulin resistance, the detailed mechanism of baicalin on glucose uptake has not been sufficiently explored as yet. The aim of this study was to survey if baicalin might facilitate glucose uptake and to explore its signal mechanisms in L6 myotubes. MATERIALS AND METHODS: L6 myotubes were treated with 100, 200, 400 µM baicalin for 6 h, 12 h and 24 h in this study. Then 2-NBDG and insulin signal protein levels in myotubes of L6 cells were examined. KEY FINDINGS: We discovered that administration of baicalin enhanced GLUT4, PGC-1α, pP38MAPK, pAKT and pAS160 contents, as well as GLUT4 mRNA and PGC-1α mRNA levels in L6 myotubes. The beneficial metabolic changes elicited by baicalin were abrogated in myotubes of L6 by P38MAPK or AKT inhibitors. SIGNIFICANCE: These results suggest that baicalin promoted glucose uptake in myotubes by differential regulation on P38MAPK and AKT activity. In conclusion, these data provide insight that baicalin is a powerful and promising agent for the treament of hyperglycemia via AKT/AS160/GLUT4 and P38MAPK/PGC1α/GLUT4 pathway.
[Mh] Termos MeSH primário: Flavonoides/farmacologia
Transportador de Glucose Tipo 4/biossíntese
Glucose/metabolismo
Hipoglicemiantes/farmacologia
Fibras Musculares Esqueléticas/metabolismo
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/metabolismo
Animais
Células Cultivadas
Desoxiglucose/análogos & derivados
Desoxiglucose/metabolismo
Insulina/metabolismo
Fibras Musculares Esqueléticas/efeitos dos fármacos
Músculo Esquelético/efeitos dos fármacos
Músculo Esquelético/metabolismo
Proteína Oncogênica v-akt/efeitos dos fármacos
Proteína Oncogênica v-akt/metabolismo
Coativador 1-alfa do Receptor gama Ativado por Proliferador de Peroxissomo/efeitos dos fármacos
Coativador 1-alfa do Receptor gama Ativado por Proliferador de Peroxissomo/metabolismo
Ratos
Transdução de Sinais/efeitos dos fármacos
Frações Subcelulares/efeitos dos fármacos
Frações Subcelulares/metabolismo
Proteínas Quinases p38 Ativadas por Mitógeno/efeitos dos fármacos
Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Flavonoids); 0 (Glucose Transporter Type 4); 0 (Hypoglycemic Agents); 0 (Insulin); 0 (Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha); 0 (Ppargc1a protein, rat); 0 (Slc2a4 protein, rat); 347Q89U4M5 (baicalin); 9G2MP84A8W (Deoxyglucose); EC 2.7.11.1 (Oncogene Protein v-akt); EC 2.7.11.24 (p38 Mitogen-Activated Protein Kinases); EQF2794IRE (4-Chloro-7-nitrobenzofurazan); IY9XDZ35W2 (Glucose); JE4F4P486R (2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose)
[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:180221
[St] Status:MEDLINE


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[PMID]:29176801
[Au] Autor:Xing J; Singh S; Zhao Y; Duan Y; Guo H; Hu C; Ma A; George R; Xing JZ; Kalluri A; Macwan I; Patra P; Chen J
[Ad] Endereço:Department of Electrical and Computer Engineering, University of Alberta, Edmonton, Canada.
[Ti] Título:Increasing vaccine production using pulsed ultrasound waves.
[So] Source:PLoS One;12(11):e0187048, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Vaccination is a safe and effective approach to prevent deadly diseases. To increase vaccine production, we propose that a mechanical stimulation can enhance protein production. In order to prove this hypothesis, Sf9 insect cells were used to evaluate the increase in the expression of a fusion protein from hepatitis B virus (HBV S1/S2). We discovered that the ultrasound stimulation at a frequency of 1.5 MHz, intensity of 60 mW/cm2, for a duration of 10 minutes per day increased HBV S1/S2 by 27%. We further derived a model for transport through a cell membrane under the effect of ultrasound waves, tested the key assumptions of the model through a molecular dynamics simulation package, NAMD (Nanoscale Molecular Dynamics program) and utilized CHARMM force field in a steered molecular dynamics environment. The results show that ultrasound waves can increase cell permeability, which, in turn, can enhance nutrient / waste exchange thus leading to enhanced vaccine production. This finding is very meaningful in either shortening vaccine production time, or increasing the yield of proteins for use as vaccines.
[Mh] Termos MeSH primário: Vacinas contra Hepatite B/biossíntese
Ondas Ultrassônicas
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/metabolismo
Animais
Western Blotting
Permeabilidade da Membrana Celular
Desoxiglucose/análogos & derivados
Desoxiglucose/metabolismo
Vacinas contra Hepatite B/imunologia
Simulação de Dinâmica Molecular
Fosfatidilcolinas/química
Proteínas/metabolismo
Células Sf9
Sonicação
Termodinâmica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hepatitis B Vaccines); 0 (Phosphatidylcholines); 0 (Proteins); 9G2MP84A8W (Deoxyglucose); EDS2L3ODLV (1,2-oleoylphosphatidylcholine); EQF2794IRE (4-Chloro-7-nitrobenzofurazan); JE4F4P486R (2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose)
[Em] Mês de entrada:1712
[Cu] Atualização por classe:171219
[Lr] Data última revisão:
171219
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:171128
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0187048


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[PMID]:28859155
[Au] Autor:Yoshitomi H; Tsuru R; Li L; Zhou J; Kudo M; Liu T; Gao M
[Ad] Endereço:School of Pharmaceutical Sciences, Mukogawa Women's University, Hyogo, Japan.
[Ti] Título:Cyclocarya paliurus extract activates insulin signaling via Sirtuin1 in C2C12 myotubes and decreases blood glucose level in mice with impaired insulin secretion.
[So] Source:PLoS One;12(8):e0183988, 2017.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Diabetes is caused by the lack of release or action of insulin. Some foods and supplements can compensate for this deficiency; thus, they can aid in the prevention or treatment of diabetes. The aim of this study was to investigate the effects of Cyclocarya paliurus extract (CPE) on insulin signaling and its capacity to correct hyperglycemia in the absence of insulin. To investigate the hypoglycemic effects of CPE, C2C12 cells were exposed to CPE (50 and 100 µg/mL). CPE promoted 2-(N-(7-Nitrobenz-2-oxa-1,3-diazol-4-yl)Amino)-2-Deoxyglucose (2NBDG) uptake into the cells via translocation of glucose transporter 4 (Glut4) to the plasma membrane. In addition, CPE enhanced tyrosine phosphorylation of insulin receptor substrate and activated phosphatidylinositol 3-kinase and protein kinase B (Akt) via sirtuin1 in C2C12 cells. Moreover, we found that oral administration of CPE (1 g/kg) to streptozotocin-induced hyperglycemic mice produced a progressive decrease in plasma glucose levels at 1 h after single dosing. At that point, CPE significantly increased the expression of skeletal muscle membrane Glut4 and enhanced the phosphorylation of Akt. These results suggest that CPE exerts antidiabetic effects similar to those of insulin, and may be an oral therapeutic alternative for the management of diabetes.
[Mh] Termos MeSH primário: Diabetes Mellitus Experimental/tratamento farmacológico
Medicamentos de Ervas Chinesas/farmacologia
Fagaceae/química
Hipoglicemiantes/farmacologia
Insulina/agonistas
Transdução de Sinais/efeitos dos fármacos
Sirtuína 1/genética
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/metabolismo
Animais
Transporte Biológico/efeitos dos fármacos
Linhagem Celular
Desoxiglucose/análogos & derivados
Desoxiglucose/metabolismo
Diabetes Mellitus Experimental/genética
Diabetes Mellitus Experimental/metabolismo
Diabetes Mellitus Experimental/patologia
Medicamentos de Ervas Chinesas/isolamento & purificação
Regulação da Expressão Gênica
Transportador de Glucose Tipo 4/genética
Transportador de Glucose Tipo 4/metabolismo
Hipoglicemiantes/isolamento & purificação
Insulina/metabolismo
Proteínas Substratos do Receptor de Insulina/genética
Proteínas Substratos do Receptor de Insulina/metabolismo
Masculino
Camundongos
Camundongos Endogâmicos ICR
Fibras Musculares Esqueléticas/citologia
Fibras Musculares Esqueléticas/efeitos dos fármacos
Fibras Musculares Esqueléticas/metabolismo
Músculo Esquelético/efeitos dos fármacos
Músculo Esquelético/metabolismo
Fosfatidilinositol 3-Quinase/genética
Fosfatidilinositol 3-Quinase/metabolismo
Fosforilação/efeitos dos fármacos
Transporte Proteico
Proteínas Proto-Oncogênicas c-akt/genética
Proteínas Proto-Oncogênicas c-akt/metabolismo
Sirtuína 1/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Drugs, Chinese Herbal); 0 (Glucose Transporter Type 4); 0 (Hypoglycemic Agents); 0 (Insulin); 0 (Insulin Receptor Substrate Proteins); 0 (Irs1 protein, mouse); 0 (Slc2a4 protein, mouse); 9G2MP84A8W (Deoxyglucose); EC 2.7.1.137 (Phosphatidylinositol 3-Kinase); EC 2.7.11.1 (Proto-Oncogene Proteins c-akt); EC 3.5.1.- (Sirt1 protein, mouse); EC 3.5.1.- (Sirtuin 1); EQF2794IRE (4-Chloro-7-nitrobenzofurazan); JE4F4P486R (2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose)
[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:170901
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0183988


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[PMID]:28739255
[Au] Autor:Tsurumaki H; Katano H; Sato K; Imai R; Niino S; Hirabayashi Y; Ichikawa S
[Ad] Endereço:Laboratory for Animal Cell Engineering, Niigata University of Pharmacy and Applied Life Sciences (NUPALS), 265-1 Higashijima, Akiha-ku, Niigata-shi, Niigata 956-8603, Japan.
[Ti] Título:WP1066, a small molecule inhibitor of the JAK/STAT3 pathway, inhibits ceramide glucosyltransferase activity.
[So] Source:Biochem Biophys Res Commun;491(2):265-270, 2017 Sep 16.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:WP1066 is a well-known inhibitor of the JAK/STAT3 signaling pathway. By a screen of known small molecule inhibitors of various enzymes and protein factors, we identified WP1066 as a ceramide glucosyltransferase inhibitor. Ceramide glucosyltransferase catalyzes the first glycosylation step during glycosphingolipid synthesis. We found that WP1066 inhibited the activity of ceramide glucosyltransferase with an IC of 7.2 µM, and that its action was independent of JAK/STAT3 pathway blockade. Moreover, the modes of inhibition of ceramide glucosyltransferase were uncompetitive with respect to both C -NBD-cermide and UDP-glucose.
[Mh] Termos MeSH primário: Inibidores Enzimáticos/farmacologia
Glucosiltransferases/antagonistas & inibidores
Melanócitos/efeitos dos fármacos
Piridinas/farmacologia
Bibliotecas de Moléculas Pequenas/farmacologia
Tirfostinas/farmacologia
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/química
4-Cloro-7-nitrobenzofurazano/metabolismo
Animais
Linhagem Celular
Ceramidas/química
Ceramidas/metabolismo
Ensaios Enzimáticos
Inibidores Enzimáticos/química
Expressão Gênica
Glucosiltransferases/genética
Glucosiltransferases/metabolismo
Seres Humanos
Janus Quinases/antagonistas & inibidores
Janus Quinases/genética
Janus Quinases/metabolismo
Cinética
Melanócitos/citologia
Melanócitos/enzimologia
Piridinas/química
Ratos
Fator de Transcrição STAT3/antagonistas & inibidores
Fator de Transcrição STAT3/genética
Fator de Transcrição STAT3/metabolismo
Transdução de Sinais
Bibliotecas de Moléculas Pequenas/química
Tirfostinas/química
Uridina Difosfato Glucose/química
Uridina Difosfato Glucose/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Ceramides); 0 (Enzyme Inhibitors); 0 (Pyridines); 0 (STAT3 Transcription Factor); 0 (STAT3 protein, human); 0 (Small Molecule Libraries); 0 (Tyrphostins); 0 (WP1066); 86701-10-2 (N-(7-(4-nitrobenzo-2-oxa-1,3-diazole))-6-aminocaproyl sphingosine); EC 2.4.1.- (Glucosyltransferases); EC 2.4.1.80 (ceramide glucosyltransferase); EC 2.7.10.2 (Janus Kinases); EQF2794IRE (4-Chloro-7-nitrobenzofurazan); V50K1D7P4Y (Uridine Diphosphate Glucose)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170824
[Lr] Data última revisão:
170824
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170726
[St] Status:MEDLINE


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[PMID]:28490875
[Au] Autor:Yang L; Wu L; Wu D; Shi D; Wang T; Zhu X
[Ad] Endereço:Department of Dermatology, Nanfang Hospital, Southern Medical University, Guangzhou.
[Ti] Título:Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes.
[So] Source:Int J Nanomedicine;12:3357-3364, 2017.
[Is] ISSN:1178-2013
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:Ethosomes can promote the penetration of lipophilic drugs into the skin, but the underlying mechanism is still unknown. The purpose of this study was to investigate the mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes. The formulation of ethosomes was optimized using the Box-Behnken experimental design, in which Rhodamine B and 1-palmitoyl-2-{12-[(7-nitro-2-1,3-benzoxadiazol-4-yl)amino]dodecanoyl}- -glycero-3-phosphocholine were used to simulate a model lipophilic drug and act as a fluorescent tracer of ethosomal phospholipids, respectively. Liposomes with the same phospholipid concentration and a hydroethanolic solution with the same ethanol concentration were also prepared as controls. The percutaneous progression of the above fluorescent preparations was observed by confocal laser scanning microscopy, and the fluorescence intensity of the images was analyzed. The optimized ethosome formulation consisted of 2.45% yolk phospholipids, 30% ethanol, and 67.55% distilled water. The percutaneous permeation of Rhodamine B in the optimized ethosomes was superior to that in hydroethanolic solution ( <0.05) and liposomes ( <0.05). The ethosomes could penetrate the skin via the percutaneous pathway of the hair follicle and stratum corneum, while during the process of penetration, the vesicles were broken and the phospholipids were retained in the upper epidermis, with the test compounds penetrating gradually. The superior percutaneous penetration of ethosomes was linked to the synergistic effects of their ingredients. The percutaneous pathways of ethosomes included open hair follicles and stratum corneum pathways. In addition, the vesicles might break up during percutaneous penetration in the superficial layer of the skin, allowing the test compounds to keep permeating into the deeper layer alone, while the phospholipid was retained in the upper epidermis.
[Mh] Termos MeSH primário: Portadores de Fármacos/farmacocinética
Lipossomos/química
Lipossomos/farmacocinética
Absorção Cutânea/efeitos dos fármacos
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/farmacocinética
Administração Cutânea
Animais
Portadores de Fármacos/administração & dosagem
Portadores de Fármacos/química
Epiderme/metabolismo
Etanol/química
Lipossomos/administração & dosagem
Masculino
Microscopia Confocal
Fosfatidilcolinas/farmacocinética
Fosfolipídeos/química
Ratos Sprague-Dawley
Rodaminas/farmacocinética
Pele/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (1-acyl-2-(12-((7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)dodecanoyl)phosphatidylcholine); 0 (Drug Carriers); 0 (Liposomes); 0 (Phosphatidylcholines); 0 (Phospholipids); 0 (Rhodamines); 3K9958V90M (Ethanol); EQF2794IRE (4-Chloro-7-nitrobenzofurazan); K7G5SCF8IL (rhodamine B)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170512
[St] Status:MEDLINE
[do] DOI:10.2147/IJN.S134708


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[PMID]:28333446
[Au] Autor:Li J; Qiu XJ
[Ad] Endereço:Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases and College of Pharmaceutical Sciences, Soochow University , Suzhou, Jiangsu 215123, China.
[Ti] Título:Quantification of Membrane Protein Self-Association with a High-Throughput Compatible Fluorescence Assay.
[So] Source:Biochemistry;56(14):1951-1954, 2017 Apr 11.
[Is] ISSN:1520-4995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:For many membrane proteins, self-association serves both structural and functional roles. Studies of such association can be simplified by switching to micelles as the membrane-mimicking environment, but native interaction is not preserved in all detergents. The selection of suitable conditions for biochemical experiments would be greatly facilitated by a quantitative high-throughput assay. Here we showed that the fluorescence polarization reduction, which resulted from homo-Förster resonance energy transfer and was measured in a high-throughput compatible format, can be used to determine both association states and constants for membrane proteins in micelles.
[Mh] Termos MeSH primário: Transferência Ressonante de Energia de Fluorescência/métodos
Glicoforina/química
Ensaios de Triagem em Larga Escala
Proteínas da Matriz Viral/química
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/química
Motivos de Aminoácidos
Betaína/análogos & derivados
Betaína/química
Membrana Celular/química
Membrana Celular/metabolismo
Detergentes
Polarização de Fluorescência
Glicoforina/metabolismo
Concentração de Íons de Hidrogênio
Cinética
Bicamadas Lipídicas/química
Bicamadas Lipídicas/metabolismo
Maltose/química
Micelas
Fosforilcolina/química
Ligação Proteica
Multimerização Proteica
Coloração e Rotulagem/métodos
Proteínas da Matriz Viral/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Detergents); 0 (Glycophorin); 0 (Lipid Bilayers); 0 (M2 protein, Influenza A virus); 0 (Micelles); 0 (Viral Matrix Proteins); 107-73-3 (Phosphorylcholine); 3SCV180C9W (Betaine); 69-79-4 (Maltose); 8CVU22OCJW (sulfobetaine); EQF2794IRE (4-Chloro-7-nitrobenzofurazan)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170324
[St] Status:MEDLINE
[do] DOI:10.1021/acs.biochem.7b00009


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[PMID]:28216158
[Au] Autor:Varshney P; Dey CS
[Ad] Endereço:Kusuma School of Biological Sciences, Indian Institute of Technology-Delhi, Hauz Khas, New Delhi 110016, India.
[Ti] Título:Resveratrol regulates neuronal glucose uptake and insulin sensitivity via P21-activated kinase 2 (PAK2).
[So] Source:Biochem Biophys Res Commun;485(2):372-378, 2017 Apr 01.
[Is] ISSN:1090-2104
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We have recently reported P21-activated kinase 2 (PAK2), a serine/threonine kinase as a negative regulator of neuronal glucose uptake and insulin sensitivity. Resveratrol (RSV), a natural polyphenol with anti-oxidative, anti-inflammatory and anti-diabetic properties, regulates PAK2 activity in HepG2 and ESC-B5 cell apoptosis. However, regulation of PAK2 by RSV in neuronal insulin signaling pathway, if any, is still unknown. In the present study, RSV treatment significantly increased PAK2 activity under insulin-sensitive and insulin-resistant condition, along with a marked decrease in glucose uptake in differentiated N2A cells. Pretreatment with AMPK inhibitor, followed by RSV treatment resulted in reduction in PAK2 activity whereas glucose uptake showed an increase. However, pretreatment with Akt inhibitor and then RSV exposure significantly increased PAK2 activity, with a corresponding decrease in glucose uptake. RSV treatment increased AMPK activity and decreased Akt activity. In conclusion, RSV negatively regulates neuronal glucose uptake and insulin sensitivity via PAK2.
[Mh] Termos MeSH primário: Glucose/metabolismo
Insulina/farmacologia
Neurônios/efeitos dos fármacos
Estilbenos/farmacologia
Quinases Ativadas por p21/metabolismo
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/metabolismo
4-Cloro-7-nitrobenzofurazano/farmacocinética
Proteínas Quinases Ativadas por AMP/metabolismo
Animais
Antioxidantes/farmacologia
Western Blotting
Linhagem Celular
Linhagem Celular Tumoral
Desoxiglucose/análogos & derivados
Desoxiglucose/metabolismo
Desoxiglucose/farmacocinética
Relação Dose-Resposta a Droga
Glucose/farmacocinética
Neurônios/metabolismo
Fosforilação/efeitos dos fármacos
Proteínas Proto-Oncogênicas c-akt/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antioxidants); 0 (Insulin); 0 (Stilbenes); 9G2MP84A8W (Deoxyglucose); EC 2.7.11.1 (Proto-Oncogene Proteins c-akt); EC 2.7.11.1 (p21-Activated Kinases); EC 2.7.11.31 (AMP-Activated Protein Kinases); EQF2794IRE (4-Chloro-7-nitrobenzofurazan); IY9XDZ35W2 (Glucose); JE4F4P486R (2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose); Q369O8926L (resveratrol)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170221
[St] Status:MEDLINE


  8 / 1006 MEDLINE  
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[PMID]:27791278
[Au] Autor:Shree N; Bhonde RR
[Ad] Endereço:School of Regenerative Medicine, GKVK Post, Bellary Road, Bangalore, India.
[Ti] Título:Conditioned Media From Adipose Tissue Derived Mesenchymal Stem Cells Reverse Insulin Resistance in Cellular Models.
[So] Source:J Cell Biochem;118(8):2037-2043, 2017 Aug.
[Is] ISSN:1097-4644
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The link between insulin resistance (IR) and type 2 diabetes has been recognized for a long time. Type 2 diabetes is often associated with basal hyperinsulinemia, reduced sensitivity to insulin, and disturbances in insulin release. There are evidences showing the reversal of IR by mesenchymal stem cells. However, the effect of conditioned media from adipose derived mesenchymal stem cells (ADSCs-CM) in reversal of IR has not been established. We established an insulin resistant model of 3T3L1 and C2C12 cells and treated with ADSCs-CM. 2-NBDG (2-[N-[7-Nitrobenz-2-oxa-1,3-diazol-4-yl]Amino]-2-Deoxyglucose) uptake was performed to assess improvement in glucose uptake. Genes involved in glucose transport and in inflammation were also analysed. Western blot for glucose transporter-4 and Akt was performed to evaluate translocation of Glut4 and insulin signaling respectively. We found that the ADSCs-CM treated cells restored insulin, stimulated glucose uptake as compared to the untreated control indicating the insulin sensitizing effect of the CM. The treated cells also showed inhibition adipogenesis in 3T3L1 cells and significant reduction of intramuscular triglyceride accumulation in C2C12 cells. Gene expressions studies revealed the drastic upregulation of GLUT4 gene and significant reduction in IL6 and PAI1 gene in both 3T3L1 and C2C12 cells, indicating possible mechanism of glucose uptake with concomitant decrease in inflammation. Enhancement of GLUT4 and phospho Akt protein expression seems to be responsible for the increment in glucose uptake and enhanced insulin signaling, respectively. Our study revealed for the first time that ADSCs-CM acts as an alternative insulin sensitizer providing stem cell solution to IR. J. Cell. Biochem. 118: 2037-2043,2017. © 2016 Wiley Periodicals, Inc.
[Mh] Termos MeSH primário: Adipócitos/efeitos dos fármacos
Meios de Cultivo Condicionados/farmacologia
Resistência à Insulina
Insulina/farmacologia
Células Mesenquimais Estromais/secreção
Mioblastos/efeitos dos fármacos
[Mh] Termos MeSH secundário: Células 3T3-L1
4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/farmacologia
Adipócitos/citologia
Adipócitos/metabolismo
Tecido Adiposo/citologia
Tecido Adiposo/efeitos dos fármacos
Tecido Adiposo/metabolismo
Animais
Transporte Biológico/efeitos dos fármacos
Diferenciação Celular
Células Cultivadas
Desoxiglucose/análogos & derivados
Desoxiglucose/farmacologia
Regulação da Expressão Gênica
Transportador de Glucose Tipo 4/genética
Transportador de Glucose Tipo 4/metabolismo
Insulina/metabolismo
Interleucina-6/genética
Interleucina-6/metabolismo
Células Mesenquimais Estromais/citologia
Camundongos
Mioblastos/citologia
Mioblastos/metabolismo
Proteínas Proto-Oncogênicas c-akt/genética
Proteínas Proto-Oncogênicas c-akt/metabolismo
Serpina E2/genética
Serpina E2/metabolismo
Transdução de Sinais
Triglicerídeos/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Culture Media, Conditioned); 0 (Glucose Transporter Type 4); 0 (Insulin); 0 (Interleukin-6); 0 (Serpin E2); 0 (Serpine2 protein, mouse); 0 (Slc2a4 protein, mouse); 0 (Triglycerides); 0 (interleukin-6, mouse); 9G2MP84A8W (Deoxyglucose); EC 2.7.11.1 (Proto-Oncogene Proteins c-akt); EQF2794IRE (4-Chloro-7-nitrobenzofurazan); JE4F4P486R (2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161030
[St] Status:MEDLINE
[do] DOI:10.1002/jcb.25777


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[PMID]:27705823
[Au] Autor:Muz M; Ost N; Kühne R; Schüürmann G; Brack W; Krauss M
[Ad] Endereço:Department Effect-Directed Analysis, Helmholtz Centre for Environmental Research - UFZ, Permoserstraße 15, 04318, Leipzig, Germany; RWTH Aachen University, Department of Ecosystem Analyses, Institute for Environmental Research, Worringerweg 1, 52074, Aachen, Germany. Electronic address: melis.muz@uf
[Ti] Título:Nontargeted detection and identification of (aromatic) amines in environmental samples based on diagnostic derivatization and LC-high resolution mass spectrometry.
[So] Source:Chemosphere;166:300-310, 2017 Jan.
[Is] ISSN:1879-1298
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The presence of aromatic amines in the environment has been in the focus of research, as many of these compounds are known or suspected mutagens and carcinogens. To facilitate the detection of aromatic amines in complex environmental samples by LC-high resolution mass spectrometry, an on-line-post-column and a pre-column derivatization method to label (in an ideal case) all aromatic amines was evaluated by applying different derivatization reagents. 4-Fluoro-7-nitro-2,1,3-benzoxadiazole (NBD-F) was found to be the most promising labeling reagent due to its high reactivity with both primary and secondary amines and its low signal in positive mode electrospray ionization (ESI+). Post-column on-line derivatization did not result in sufficient signal intensities of derivatives. With pre-column derivatization most of the selected aromatic amines resulted in a derivative that shows common fragments of diagnostic value. The selectivity of NBD-F was studied in depth with a data set of 220 compounds with different functional groups showing that also aliphatic amines and some thiols yield a derivative. The developed method was successfully applied to wastewater effluent samples and several derivatives were confirmed by diagnostic neutral losses.
[Mh] Termos MeSH primário: Aminas/análise
Cromatografia Líquida
Espectrometria de Massas
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/química
Aminas/química
Carcinógenos/análise
Cromatografia Líquida de Alta Pressão
Meio Ambiente
Indicadores e Reagentes
Limite de Detecção
Mutagênicos/análise
Espectrometria de Massas por Ionização por Electrospray
Compostos de Sulfidrila
Espectrometria de Massas em Tandem
Poluentes Químicos da Água/análise
Poluentes Químicos da Água/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amines); 0 (Carcinogens); 0 (Indicators and Reagents); 0 (Mutagens); 0 (Sulfhydryl Compounds); 0 (Water Pollutants, Chemical); 29270-56-2 (7-fluoro-4-nitrobenzo-2-oxa-1,3-diazole); EQF2794IRE (4-Chloro-7-nitrobenzofurazan)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170912
[Lr] Data última revisão:
170912
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161006
[St] Status:MEDLINE


  10 / 1006 MEDLINE  
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[PMID]:27595398
[Au] Autor:Bhavsar SK; Singh Y; Sharma P; Khairnar V; Hosseinzadeh Z; Zhang S; Palmada M; Sabolic I; Koepsell H; Lang KS; Lang PA; Lang F
[Ad] Endereço:Department of Cardiology, Vascular Medicine and Physiology, University of Tuebingen, Tuebigen, Germany.
[Ti] Título:Expression of JAK3 Sensitive Na+ Coupled Glucose Carrier SGLT1 in Activated Cytotoxic T Lymphocytes.
[So] Source:Cell Physiol Biochem;39(3):1209-28, 2016.
[Is] ISSN:1421-9778
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Similar to tumor cells, activated T-lymphocytes generate ATP mainly by glycolytic degradation of glucose. Lymphocyte glucose uptake involves non-concentrative glucose carriers of the GLUT family. In contrast to GLUT isoforms, Na+-coupled glucose-carrier SGLT1 accumulates glucose against glucose gradients and is effective at low extracellular glucose concentrations. The present study explored expression and regulation of SGLT1 in activated murine splenic cytotoxic T cells (CTLs) and human Jurkat T cells. METHODS: FACS analysis, immunofluorescence, confocal microscopy, chemiluminescence and Western blotting were employed to estimate SGLT1 expression, function and regulation in lymphocytes, as well as dual electrode voltage clamp in SGLT1 ± JAK3 expressing Xenopus oocytes to quantify the effect of janus kinase3 (JAK3) on SGLT1 function. RESULTS: SGLT1 is expressed in murine CTLs and also in human Jurkat T cells. 2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose uptake was significantly decreased by SGLT1-blocker phloridzin (0.2 mM) and by pharmacological inhibition of JAK3 with WHI-P131 (156 µM), WHI-P154 (11.2 µM) and JAK3 inhibitor VI (0.5 µM). Electrogenic glucose transport (Iglucose) in Xenopus oocytes expressing human SGLT1 was increased by additional expression of human wild type JAK3, active A568VJAK3 but not inactive K851AJAK3. Coexpression of JAK3 enhanced the maximal transport rate without significantly modifying affinity of the carrier. Iglucose in SGLT1+JAK3 expressing oocytes was significantly decreased by WHI-P154 (11.2 µM). JAK3 increased the SGLT1 protein abundance in the cell membrane. Inhibition of carrier insertion by brefeldin A (5 µM) in SGLT1+JAK3 expressing oocytes resulted in a decline of Iglucose, which was similar in presence and absence of JAK3. CONCLUSIONS: SGLT1 is expressed in murine cytotoxic T cells and human Jurkat T cells and significantly contributes to glucose uptake in those cells post activation. JAK3 up-regulates SGLT1 activity by increasing the carrier protein abundance in the cell membrane, an effect enforcing cellular glucose uptake into activated lymphocytes and thus contributing to the immune response.
[Mh] Termos MeSH primário: Glucose/imunologia
Janus Quinase 3/genética
Oócitos/metabolismo
Transportador 1 de Glucose-Sódio/genética
Linfócitos T Citotóxicos/imunologia
[Mh] Termos MeSH secundário: 4-Cloro-7-nitrobenzofurazano/análogos & derivados
4-Cloro-7-nitrobenzofurazano/farmacologia
Animais
Transporte Biológico
Brefeldina A/farmacologia
Células CACO-2
Desoxiglucose/análogos & derivados
Desoxiglucose/farmacologia
Regulação da Expressão Gênica
Glucose/farmacologia
Seres Humanos
Janus Quinase 3/imunologia
Células Jurkat
Ativação Linfocitária
Camundongos
Oócitos/citologia
Oócitos/efeitos dos fármacos
Técnicas de Patch-Clamp
Florizina/farmacologia
Cultura Primária de Células
Quinazolinas/farmacologia
Transdução de Sinais
Transportador 1 de Glucose-Sódio/imunologia
Baço/citologia
Baço/efeitos dos fármacos
Baço/imunologia
Linfócitos T Citotóxicos/citologia
Linfócitos T Citotóxicos/efeitos dos fármacos
Transgenes
Xenopus laevis
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Quinazolines); 0 (SLC5A1 protein, human); 0 (Sodium-Glucose Transporter 1); 0 (WHI P131); 0 (WHI P154); 20350-15-6 (Brefeldin A); 9G2MP84A8W (Deoxyglucose); CU9S17279X (Phlorhizin); EC 2.7.10.2 (JAK3 protein, human); EC 2.7.10.2 (Janus Kinase 3); EQF2794IRE (4-Chloro-7-nitrobenzofurazan); IY9XDZ35W2 (Glucose); JE4F4P486R (2-(N-(7-nitrobenz-2-oxa-1,3-diazol-4-yl)amino)-2-deoxyglucose)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160906
[St] Status:MEDLINE
[do] DOI:10.1159/000447827



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