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[PMID]:29216584
[Au] Autor:DeBoyace K; Zdaniewski C; Wildfong PLD
[Ad] Endereço:Duquesne University Graduate School of Pharmaceutical Sciences, 600 Forbes Ave, Pittsburgh, PA 15282, United States.
[Ti] Título:Differential scanning calorimetry isothermal hold times can impact interpretations of drug-polymer dispersability in amorphous solid dispersions.
[So] Source:J Pharm Biomed Anal;150:43-50, 2018 Feb 20.
[Is] ISSN:1873-264X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Differential scanning calorimetry (DSC) is a commonly employed analytical technique for the analysis and characterization of amorphous solid dispersions. However, steps typical of standard temperature programs can alter the material in situ. Data for two active pharmaceutical ingredients are detailed, wherein isothermal hold times, traditionally employed to remove thermal history and/or residual solvent, were observed to impact the observed dispersability of the compounds in polyvinylpyrrolidone vinyl-acetate copolymer (PVPva). Re-crystallized tolbutamide was observed to re-dissolve in PVPva, while terfenadine was observed to crystallize during the isothermal hold period. Exposing co-solidified drug-polymer mixtures to temperature changes and experimental hold times can potentially confound correct categorization of dispersability, particularly when DSC is used as the lone characterization technique. This work illustrates the importance of using a combination of techniques to improve the certainty of conclusions made with respect to the true, initial physical state of a co-solidified mixture.
[Mh] Termos MeSH primário: Varredura Diferencial de Calorimetria/métodos
Pirrolidinas/química
Terfenadina/química
Tolbutamida/química
Compostos de Vinila/química
[Mh] Termos MeSH secundário: Química Farmacêutica/métodos
Cristalização
Polímeros/química
Solubilidade
Solventes/química
Temperatura Ambiente
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Polymers); 0 (Pyrrolidines); 0 (Solvents); 0 (Vinyl Compounds); 0 (poly(vinylpyrrolidone-co-vinyl-acetate)); 7BA5G9Y06Q (Terfenadine); 982XCM1FOI (Tolbutamide)
[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:171208
[St] Status:MEDLINE


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[PMID]:28362348
[Au] Autor:Szkudlarek A; Pentak D; Ploch A; Pozycka J; Maciazek-Jurczyk M
[Ad] Endereço:Department of Physical Pharmacy, School of Pharmacy with the Division of Laboratory Medicine in Sosnowiec, Medical University of Silesia, Jagiellonska 4, 41-200 Sosnowiec, Poland. aszkudlarek@sum.edu.pl.
[Ti] Título:Effect of Temperature on Tolbutamide Binding to Glycated Serum Albumin.
[So] Source:Molecules;22(4), 2017 Mar 31.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:Glycation process occurs in protein and becomes more pronounced in diabetes when an increased amount of reducing sugar is present in bloodstream. Glycation of protein may cause conformational changes resulting in the alterations of its binding properties even though they occur at a distance from the binding sites. The changes in protein properties could be related to several pathological consequences such as diabetic and nondiabetic cardiovascular diseases, cataract, renal dysfunction and Alzheimer's disease. The experiment was designed to test the impact of glycation process on sulfonylurea drug tolbutamide-albumin binding under physiological (T = 309 K) and inflammatory (T = 311 K and T = 313 K) states using fluorescence and UV-VIS spectroscopies. It was found in fluorescence analysis experiments that the modification of serum albumin in tryptophanyl and tyrosyl residues environment may affect the tolbutamide (TB) binding to albumin in subdomain IIA and/or IIIA (Sudlow's site I and/or II), and also in subdomains IB and IIB. We estimated the binding of tolbutamide to albumin described by a mixed nature of interaction (specific and nonspecific). The association constants Ka (L∙mol ) for tolbutamide at its high affinity sites on non-glycated albumin were in the range of 1.98-7.88 × 104 L∙mol (λ = 275 nm), 1.20-1.64 × 104 L∙mol (λ = 295 nm) and decreased to 1.24-0.42 × 104 L∙mol at λ = 275 nm (T = 309 K and T = 311 K) and increased to 2.79 × 104 L∙mol at λ = 275 nm (T = 313 K) and to 4.43-6.61 × 104 L∙mol at λ = 295 nm due to the glycation process. Temperature dependence suggests the important role of van der Waals forces and hydrogen bonding in hydrophobic interactions between tolbutamide and both glycated and non-glycated albumin. We concluded that the changes in the environment of TB binding of albumin in subdomain IIA and/or IIIA as well as in subdomains IB and IIB influence on therapeutic effect and therefore the studies of the binding of tolbutamide (in diabetes) to transporting protein under glycation that refers to the modification of a protein are of great importance in pharmacology and biochemistry. This information may lead to the development of more effective drug therapy in people with diabetes.
[Mh] Termos MeSH primário: Albumina Sérica/metabolismo
Temperatura Ambiente
Tolbutamida/metabolismo
[Mh] Termos MeSH secundário: Animais
Bovinos
Produtos Finais de Glicação Avançada
Cinética
Ligação Proteica
Estabilidade Proteica
Soroalbumina Bovina/metabolismo
Espectrometria de Fluorescência
Tolbutamida/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Glycation End Products, Advanced); 0 (Serum Albumin); 0 (glycosylated serum albumin); 27432CM55Q (Serum Albumin, Bovine); 982XCM1FOI (Tolbutamide)
[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:170401
[St] Status:MEDLINE


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[PMID]:28253826
[Au] Autor:Wang S; Dong Y; Su K; Zhang J; Wang L; Han A; Wen C; Wang X; He Y
[Ad] Endereço:a The Laboratory of Clinical Pharmacy , The People's Hospital of Lishui , Lishui , China.
[Ti] Título:Effect of codeine on CYP450 isoform activity of rats.
[So] Source:Pharm Biol;55(1):1223-1227, 2017 Dec.
[Is] ISSN:1744-5116
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:CONTEXT: Codeine, also known as 3-methylmorphine, is an opiate used to treat pain, as a cough medicine and for diarrhoea. No study on the effects of codeine on the metabolic capacity of CYP enzyme is reported. OBJECTIVE: In order to investigate the effects of codeine on the metabolic capacity of cytochrome P450 (CYP) enzymes, a cocktail method was employed to evaluate the activities of CYP2B1, CYP2D1, CYP1A2, CYP3A2 and CYP2C11. MATERIALS AND METHODS: Sprague-Dawley rats were randomly divided into codeine group (low, medium, high) and control group. The codeine group rats were given 4, 8, 16 mg/kg (low, medium, high) codeine by continuous intragastric administration for 14 days. Five probe drugs bupropion, metroprolol, phenacetin, midazolam and tolbutamide were given to rats through intragastric administration, and the plasma concentrations were determined by UPLC-MS/MS. RESULTS AND CONCLUSION: The pharmacokinetic parameters of bupropion and metroprolol experienced obvious change with AUC , C increased and CL decreased for bupropion in medium dosage group and midazolam low dosage group. This result indicates that the 14 day-intragastric administration of codeine may inhibit the metabolism of bupropion (CYP2B1) and midazolam (CYP3A2) in rat. Additional, there are no statistical differences for albumin (ALB), alkaline phosphatase (ALP), creatinine (Cr) after 14 intragastric administration of codeine, while alanine aminotransferase (ALT), aspartate aminotransferase (AST), uric acid (UA) increased compared to control group. The biomedical test results show continuous 14 day-intragastric administration of codeine would cause liver damage.
[Mh] Termos MeSH primário: Codeína/metabolismo
Codeína/farmacologia
Sistema Enzimático do Citocromo P-450/metabolismo
[Mh] Termos MeSH secundário: Animais
Bupropiona/metabolismo
Relação Dose-Resposta a Droga
Interações Medicamentosas/fisiologia
Ativação Enzimática/efeitos dos fármacos
Ativação Enzimática/fisiologia
Isoenzimas/metabolismo
Masculino
Distribuição Aleatória
Ratos
Ratos Sprague-Dawley
Tolbutamida/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Isoenzymes); 01ZG3TPX31 (Bupropion); 9035-51-2 (Cytochrome P-450 Enzyme System); 982XCM1FOI (Tolbutamide); Q830PW7520 (Codeine)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170313
[Lr] Data última revisão:
170313
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170304
[St] Status:MEDLINE
[do] DOI:10.1080/13880209.2017.1297466


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[PMID]:28120427
[Au] Autor:Brown J; Martis R; Hughes B; Rowan J; Crowther CA
[Ad] Endereço:Liggins Institute, The University of Auckland, Park Rd, Grafton, Auckland, New Zealand, 1142.
[Ti] Título:Oral anti-diabetic pharmacological therapies for the treatment of women with gestational diabetes.
[So] Source:Cochrane Database Syst Rev;1:CD011967, 2017 01 25.
[Is] ISSN:1469-493X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Gestational diabetes mellitus (GDM) is a major public health issue with rates increasing globally. Gestational diabetes, glucose intolerance first recognised during pregnancy, usually resolves after birth and is associated with short- and long-term complications for the mother and her infant. Treatment options can include oral anti-diabetic pharmacological therapies. OBJECTIVES: To evaluate the effects of oral anti-diabetic pharmacological therapies for treating women with GDM. SEARCH METHODS: We searched Cochrane Pregnancy and Childbirth's Trials Register (14 May 2016), ClinicalTrials.gov, WHO ICTRP (14 May 2016) and reference lists of retrieved studies. SELECTION CRITERIA: We included published and unpublished randomised controlled trials assessing the effects of oral anti-diabetic pharmacological therapies for treating pregnant women with GDM. We included studies comparing oral anti-diabetic pharmacological therapies with 1) placebo/standard care, 2) another oral anti-diabetic pharmacological therapy, 3) combined oral anti-diabetic pharmacological therapies. Trials using insulin as the comparator were excluded as they are the subject of a separate Cochrane systematic review.Women with pre-existing type 1 or type 2 diabetes were excluded. DATA COLLECTION AND ANALYSIS: Two review authors independently assessed trials for inclusion and trial quality. Two review authors independently extracted data and data were checked for accuracy. MAIN RESULTS: We included 11 studies (19 publications) (1487 women and their babies). Eight studies had data that could be included in meta-analyses. Studies were conducted in Brazil, India, Israel, UK, South Africa and USA. The studies varied in diagnostic criteria and treatment targets for glycaemic control for GDM. The overall risk of bias was 'unclear' due to inadequate reporting of methodology. Using GRADE the quality of the evidence ranged from moderate to very low quality. Evidence was downgraded for risk of bias (reporting bias, lack of blinding), inconsistency, indirectness, imprecision and for oral anti-diabetic therapy versus placebo for generalisability. Oral anti-diabetic pharmacological therapies versus placebo/standard careThere was no evidence of a difference between glibenclamide and placebo groups for hypertensive disorders of pregnancy (risk ratio (RR) 1.24, 95% confidence interval (CI) 0.81 to 1.90; one study, 375 women, very low-quality evidence), birth by caesarean section (RR 1.03, 95% CI 0.79 to 1.34; one study, 375 women, very low-quality evidence), perineal trauma (RR 0.98, 95% CI 0.06 to 15.62; one study, 375 women, very low-quality evidence) or induction of labour (RR 1.18, 95% CI 0.79 to 1.76; one study, 375 women; very low-quality evidence). No data were reported for development of type 2 diabetes or other pre-specified GRADE maternal outcomes (return to pre-pregnancy weight, postnatal depression). For the infant, there was no evidence of a difference in the risk of being born large-for-gestational age (LGA) between infants whose mothers had been treated with glibenclamide and those in the placebo group (RR 0.89, 95% CI 0.51 to 1.58; one study, 375, low-quality evidence). No data were reported for other infant primary or GRADE outcomes (perinatal mortality, death or serious morbidity composite, neurosensory disability in later childhood, neonatal hypoglycaemia, adiposity, diabetes). Metformin versus glibenclamideThere was no evidence of a difference between metformin- and glibenclamide-treated groups for the risk of hypertensive disorders of pregnancy (RR 0.70, 95% CI 0.38 to 1.30; three studies, 508 women, moderate-quality evidence), birth by caesarean section (average RR 1.20, 95% CI 1.20; 95% CI 0.83 to 1.72, four studies, 554 women, I = 61%, Tau = 0.07 low-quality evidence), induction of labour (0.81, 95% CI 0.61 to 1.07; one study, 159 women; low-quality evidence) or perineal trauma (RR 1.67, 95% CI 0.22 to 12.52; two studies, 158 women; low-quality evidence). No data were reported for development of type 2 diabetes or other pre-specified GRADE maternal outcomes (return to pre-pregnancy weight, postnatal depression). For the infant there was no evidence of a difference between the metformin- and glibenclamide-exposed groups for the risk of being born LGA (average RR 0.67, 95% CI 0.24 to 1.83; two studies, 246 infants, I = 54%, Tau = 0.30 low-quality evidence). Metformin was associated with a decrease in a death or serious morbidity composite (RR 0.54, 95% CI 0.31 to 0.94; one study, 159 infants, low-quality evidence). There was no clear difference between groups for neonatal hypoglycaemia (RR 0.86, 95% CI 0.42 to 1.77; four studies, 554 infants, low-quality evidence) or perinatal mortality (RR 0.92, 95% CI 0.06 to 14.55, two studies, 359 infants). No data were reported for neurosensory disability in later childhood or for adiposity or diabetes. Glibenclamide versus acarboseThere was no evidence of a difference between glibenclamide and acarbose from one study (43 women) for any of their maternal or infant primary outcomes (caesarean section, RR 0.95, 95% CI 0.53 to 1.70; low-quality evidence; perinatal mortality - no events; low-quality evidence; LGA , RR 2.38, 95% CI 0.54 to 10.46; low-quality evidence). There was no evidence of a difference between glibenclamide and acarbose for neonatal hypoglycaemia (RR 6.33, 95% CI 0.87 to 46.32; low-quality evidence). There were no data reported for other pre-specified GRADE or primary maternal outcomes (hypertensive disorders of pregnancy, development of type 2 diabetes, perineal trauma, return to pre-pregnancy weight, postnatal depression, induction of labour) or neonatal outcomes (death or serious morbidity composite, adiposity or diabetes). AUTHORS' CONCLUSIONS: There were insufficient data comparing oral anti-diabetic pharmacological therapies with placebo/standard care (lifestyle advice) to inform clinical practice. There was insufficient high-quality evidence to be able to draw any meaningful conclusions as to the benefits of one oral anti-diabetic pharmacological therapy over another due to limited reporting of data for the primary and secondary outcomes in this review. Short- and long-term clinical outcomes for this review were inadequately reported or not reported. Current choice of oral anti-diabetic pharmacological therapy appears to be based on clinical preference, availability and national clinical practice guidelines.The benefits and potential harms of one oral anti-diabetic pharmacological therapy compared with another, or compared with placebo/standard care remains unclear and requires further research. Future trials should attempt to report on the core outcomes suggested in this review, in particular long-term outcomes for the woman and the infant that have been poorly reported to date, women's experiences and cost benefit.
[Mh] Termos MeSH primário: Diabetes Gestacional/tratamento farmacológico
Hipoglicemiantes/administração & dosagem
[Mh] Termos MeSH secundário: Acarbose/administração & dosagem
Administração Oral
Feminino
Glibureto/administração & dosagem
Seres Humanos
Hipoglicemia/induzido quimicamente
Hipoglicemia/prevenção & controle
Hipoglicemiantes/efeitos adversos
Metformina/administração & dosagem
Gravidez
Ensaios Clínicos Controlados Aleatórios como Assunto
Tolbutamida/administração & dosagem
[Pt] Tipo de publicação:JOURNAL ARTICLE; META-ANALYSIS; RESEARCH SUPPORT, NON-U.S. GOV'T; REVIEW
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 9100L32L2N (Metformin); 982XCM1FOI (Tolbutamide); SX6K58TVWC (Glyburide); T58MSI464G (Acarbose)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170421
[Lr] Data última revisão:
170421
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170126
[St] Status:MEDLINE
[do] DOI:10.1002/14651858.CD011967.pub2


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[PMID]:26354504
[Au] Autor:Lu J; Ding T; Qin X; Liu M; Wang X
[Ad] Endereço:Shanghai Key Laboratory of Regulatory Biology, Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, Shanghai, 200241, China.
[Ti] Título:In vitro and in vivo evaluation of cucurbitacin E on rat hepatic CYP2C11 expression and activity using LC-MS/MS.
[So] Source:Sci China Life Sci;60(2):215-224, 2017 Feb.
[Is] ISSN:1869-1889
[Cp] País de publicação:China
[La] Idioma:eng
[Ab] Resumo:This study explored the effects of cucurbitacin E (CuE), a bioactive compound from Cucurbitaceae, on the metabolism/pharmacokinetic of tolbutamide, a model CYP2C9/11 probe substrate, and hepatic CYP2C11 expression in rats. Liquid chromatography-(tandem) mass spectrometry (LC-MS/MS) assay was used to detect tolbutamide as well as 4-hydroxytolbutamide, and then successfully applied to the pharmacokinetic study of tolbutamide in rats. The effect of CuE on CYP2C11 expression was determined by western blot. CuE (1.25-100 µmol L ) competitively inhibited tolbutamide 4-hydroxylation (CYP2C11) activity only in concentration-dependent manner with a K value of 55.5 µmol L in vitro. In whole animal studies, no significant difference in metabolism/pharmacokinetic of tolbutamide was found for the single pretreatment groups. In contrast, multiple pretreatments of CuE (200 µg kg d , 3 d, i.p.) significantly decreased tolbutamide clearance (CL) by 25% and prolonged plasma half-time (T ) by 37%. Moreover, CuE treatment (50-200 µg kg d , i.p.) for 3 d did not affect CYP2C11 expression. These findings demonstrated that CuE competitively inhibited the metabolism of CYP2C11 substrates but had no effect on rat CYP2C11 expression. This study may provide a useful reference for the reasonable and safe use of herbal or natural products containing CuE to avoid unnecessary drug-drug interactions.
[Mh] Termos MeSH primário: Hidrocarboneto de Aril Hidroxilases/metabolismo
Família 2 do Citocromo P450/metabolismo
Fígado/efeitos dos fármacos
Esteroide 16-alfa-Hidroxilase/metabolismo
Triterpenos/farmacologia
[Mh] Termos MeSH secundário: Animais
Cromatografia Líquida de Alta Pressão
Hidroxilação
Masculino
Microssomos Hepáticos/efeitos dos fármacos
Ratos
Ratos Sprague-Dawley
Espectrometria de Massas em Tandem
Tolbutamida/análogos & derivados
Tolbutamida/farmacocinética
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (4'-hydroxytolbutamide); 0 (Triterpenes); 982XCM1FOI (Tolbutamide); EC 1.14.14.1 (Aryl Hydrocarbon Hydroxylases); EC 1.14.14.1 (CYP2C11 protein, rat); EC 1.14.14.1 (Cytochrome P450 Family 2); EC 1.14.14.1 (Steroid 16-alpha-Hydroxylase); V8A45XYI21 (cucurbitacin E)
[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:150911
[St] Status:MEDLINE
[do] DOI:10.1007/s11427-015-4911-7


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[PMID]:28057172
[Au] Autor:Niwa T; Imagawa Y
[Ad] Endereço:School of Pharmacy, Shujitsu University, 1-6-1 Nishigawara, Naka-ku, Okayama 703-8516, Japan.
[Ti] Título:Substrate Specificity of Human Cytochrome P450 (CYP) 2C Subfamily and Effect of Azole Antifungal Agents on CYP2C8.
[So] Source:J Pharm Pharm Sci;19(4):423-429, 2016 Oct - Dec.
[Is] ISSN:1482-1826
[Cp] País de publicação:Canada
[La] Idioma:eng
[Ab] Resumo:PURPOSE: The metabolic activities of aminopyrine N-demethylation and tolbutamide methylhydroxylation by the human hepatic cytochrome P450 (P450 or CYP) 2C subfamily were compared and the effects of azole antifungal agent on the drug-metabolizing activity of CYP2C8 were investigated. METHODS: Aminopyrine N-demethylation and tolbutamide methylhydroxylation by CYP2C8, CYP2C9, and CYP2C19 were determined by the previous reported methods. The effects of five azole antifungal agents, fluconazole, itraconazole, ketoconazole, miconazole, and voriconazole, on the aminopyrine N-demethylation activity by CYP2C8 were investigated. RESULTS: With regard to aminopyrine N-demethylation, CYP2C19 had the lowest Michaelis constant (Km) and CYP2C8 had the highest maximal velocity (Vmax) among the CYP2C subfamily members. The Vmax/Km values for CYP2C8 were the highest, followed by CYP2C19. For tolbutamide methylhydroxylation, the Km and Vmax for CYP2C19 were three and six times higher than the corresponding values for CYP2C9, and the Vmax/Km value for CYP2C19 was twice that for CYP2C9, whereas hydroxylated tolbutamide formed by CYP2C8 was not detected. Fluconazole, itraconazole, and voriconazole at a concentration of 2 or 10 µM neither inhibited nor stimulated CYP2C8-mediated aminopyrine N-demethylation activity at substrate concentrations around the Km (5 mM). However, ketoconazole and miconazole noncompetitively inhibited CYP2C8-mediated aminopyrine N-demethylation with the inhibitory constant values of 1.98 and 0.86 µM, respectively. CONCLUSION: These results suggest that ketoconazole and miconazole might inhibit CYP2C8 clinically. This article is open to POST-PUBLICATION REVIEW. Registered readers (see "For Readers") may comment by clicking on ABSTRACT on the issue's contents page.
[Mh] Termos MeSH primário: Aminopirina/farmacologia
Antifúngicos/farmacologia
Azóis/farmacologia
Inibidores das Enzimas do Citocromo P-450/farmacologia
Sistema Enzimático do Citocromo P-450/metabolismo
Tolbutamida/farmacologia
[Mh] Termos MeSH secundário: Aminopirina/química
Antifúngicos/química
Azóis/química
Inibidores das Enzimas do Citocromo P-450/química
Relação Dose-Resposta a Droga
Seres Humanos
Relação Estrutura-Atividade
Especificidade por Substrato
Tolbutamida/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antifungal Agents); 0 (Azoles); 0 (Cytochrome P-450 Enzyme Inhibitors); 0 (cytochrome P-450 CYP2C subfamily); 01704YP3MO (Aminopyrine); 9035-51-2 (Cytochrome P-450 Enzyme System); 982XCM1FOI (Tolbutamide)
[Em] Mês de entrada:1711
[Cu] Atualização por classe:171110
[Lr] Data última revisão:
171110
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170107
[St] Status:MEDLINE
[do] DOI:10.18433/J31S53


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[PMID]:27882460
[Au] Autor:Zakhariants AA; Burmistrova OA; Shkurnikov MY; Poloznikov AA; Sakharov DA
[Ad] Endereço:Biocilicum Research and Production Center, Moscow, Russia. zakhariants@bioclinicum.com.
[Ti] Título:Development of a Specific Substrate-Inhibitor Panel (Liver-on-a-Chip) for Evaluation of Cytochrome P450 Activity.
[So] Source:Bull Exp Biol Med;162(1):170-174, 2016 Nov.
[Is] ISSN:1573-8221
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:We developed a cytochrome P450 substrate-inhibitor panel for preclinical in vitro evaluation of drugs in a 3D histotypical microfluidic cell model of human liver (liver-on-a-chip technology). The concentrations of substrates and inhibitors were optimized to ensure reliable detection of the principal metabolites by HPLC-mass-spectroscopy. The selected specific substrate-inhibitor pairs, namely bupropion/2-phenyl-2-(1-piperidinyl)propane) for evaluation of CYP2B6B activity, tolbutamide/sulfaphenazole for CYP2C9, omeprazole/(+)-N-benzylnirvanol for CYP2C19, and testosterone/ketoconazole for CYP3A4, enable reliable evaluation of the drug metabolism pathway. In contrast to animal models characterized by species-specific expression profile and activity of cytochrome P450 isoforms, our in vitro model reflects the metabolism of human hepatocytes in vivo.
[Mh] Termos MeSH primário: Citocromo P-450 CYP2B6/metabolismo
Citocromo P-450 CYP2C19/metabolismo
Citocromo P-450 CYP2C9/metabolismo
Citocromo P-450 CYP3A/metabolismo
Dispositivos Lab-On-A-Chip
[Mh] Termos MeSH secundário: Bupropiona/metabolismo
Cromatografia Líquida de Alta Pressão
Citocromo P-450 CYP2B6/análise
Citocromo P-450 CYP2C19/análise
Citocromo P-450 CYP2C9/análise
Citocromo P-450 CYP3A/análise
Inibidores das Enzimas do Citocromo P-450/farmacologia
Seres Humanos
Cetoconazol/farmacologia
Fígado/efeitos dos fármacos
Fígado/enzimologia
Espectrometria de Massas
Mefenitoína/análogos & derivados
Mefenitoína/farmacologia
Microssomos Hepáticos/efeitos dos fármacos
Microssomos Hepáticos/enzimologia
Omeprazol/metabolismo
Fenciclidina/análogos & derivados
Fenciclidina/farmacologia
Especificidade por Substrato
Sulfafenazol/farmacologia
Testosterona/metabolismo
Tolbutamida/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (2-phenyl-2-(1-piperidinyl)propane); 0 (Cytochrome P-450 Enzyme Inhibitors); 0 (N-3-benzylnirvanol); 01ZG3TPX31 (Bupropion); 0J8L4V3F81 (Sulfaphenazole); 3XMK78S47O (Testosterone); 982XCM1FOI (Tolbutamide); EC 1.14.13.- (CYP2C9 protein, human); EC 1.14.13.- (Cytochrome P-450 CYP2C9); EC 1.14.13.67 (CYP3A4 protein, human); EC 1.14.14.1 (CYP2B6 protein, human); EC 1.14.14.1 (CYP2C19 protein, human); EC 1.14.14.1 (Cytochrome P-450 CYP2B6); EC 1.14.14.1 (Cytochrome P-450 CYP2C19); EC 1.14.14.1 (Cytochrome P-450 CYP3A); J1DOI7UV76 (Phencyclidine); KG60484QX9 (Omeprazole); R420KW629U (Mephenytoin); R9400W927I (Ketoconazole)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:170207
[Lr] Data última revisão:
170207
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161125
[St] Status:MEDLINE


  8 / 4213 MEDLINE  
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[PMID]:27806105
[Au] Autor:Henquin JC; Nenquin M
[Ad] Endereço:Unit of Endocrinology and Metabolism, Faculty of Medicine, University of Louvain, Brussels, Belgium.
[Ti] Título:Dynamics and Regulation of Insulin Secretion in Pancreatic Islets from Normal Young Children.
[So] Source:PLoS One;11(11):e0165961, 2016.
[Is] ISSN:1932-6203
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Insulin secretion has only exceptionally been investigated in pancreatic islets from healthy young children. It remains unclear whether those islets behave like adult islets despite substantial differences in cellular composition and higher ß-cell replication rates. Islets were isolated from 5 infants/toddlers (11-36 month-old) and perifused to characterize their dynamics of insulin secretion when subjected to various stimuli and inhibitors. Their insulin responses were compared to those previously reported for similarly treated adult islets. Qualitatively, infant islets responded like adult islets to stimulation by glucose, tolbutamide, forskolin (to increase cAMP), arginine and the combination of leucine and glutamine, and to inhibition by diazoxide and CaCl2 omission. This similarity included the concentration-dependency and biphasic pattern of glucose-induced insulin secretion, the dynamics of the responses to non-glucose stimuli and metabolic amplification of these responses. The insulin content was not different, but fractional insulin secretion rates were lower in infant than adult islets irrespective of the stimulus. However, the stimulation index was similar because basal secretion rates were also lower in infant islets. In conclusion, human ß-cells are functionally mature by the age of one year, before expansion of their mass is complete. Their responsiveness (stimulation index) to all stimuli is not smaller than that of adult ß-cells. Yet, under basal and stimulated conditions, they secrete smaller proportions of their insulin stores in keeping with smaller in vivo insulin needs during infancy.
[Mh] Termos MeSH primário: Glucose/farmacologia
Insulina/secreção
Ilhotas Pancreáticas/metabolismo
[Mh] Termos MeSH secundário: Aminoácidos/farmacologia
Cloreto de Cálcio/farmacologia
Pré-Escolar
Colforsina/farmacologia
Diazóxido/farmacologia
Feminino
Seres Humanos
Lactente
Ilhotas Pancreáticas/efeitos dos fármacos
Masculino
Tolbutamida/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Amino Acids); 0 (Insulin); 1F7A44V6OU (Colforsin); 982XCM1FOI (Tolbutamide); IY9XDZ35W2 (Glucose); M4I0D6VV5M (Calcium Chloride); O5CB12L4FN (Diazoxide)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170622
[Lr] Data última revisão:
170622
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161103
[St] Status:MEDLINE
[do] DOI:10.1371/journal.pone.0165961


  9 / 4213 MEDLINE  
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[PMID]:27592832
[Au] Autor:Suzuki S; Sato Y; Umegaki K; Chiba T
[Ad] Endereço:Information Center, National Institute of Health and Nutrition, National Institutes of Biomedical Innovation, Health and Nutrition.
[Ti] Título:Influence of High-fat and High-cholesterol Diet on Major CYP Activities in the Liver.
[So] Source:Yakugaku Zasshi;136(9):1297-305, 2016.
[Is] ISSN:1347-5231
[Cp] País de publicação:Japan
[La] Idioma:jpn
[Ab] Resumo:We previously reported that a high-fat and high-cholesterol (HFHC) diet for 12 weeks induced non-alcoholic steatohepatitis (NASH) and influenced major CYP subtype gene expression levels and activities in a mouse model. In the present study, we determined the effects of the HFHC diet on CYP expression levels and activities prior to the establishment of NASH. When male C57BL/6J mice were fed the HFHC or a normal chow diet (Control) ad libitum for 4 weeks, body weights were significantly lower, whereas liver weights and hepatic lipid contents were significantly higher in the HFHC group than in the Control group. Under these conditions, hepatic microsomal luciferin-H (human CYP2C9 substrate) hydroxylation activity was significantly lower in the HFHC group than in the Control group. In order to investigate drug efficacy in mice fed the HFHC diet, an intraperitoneal glucose tolerance test was conducted with or without a pretreatment with tolbutamide (a CYP2C substrate) after 4 weeks of feeding. The plasma glucose-lowering effects of tolbutamide were attenuated in the HFHC group even though luciferin-H hydroxylation activity was suppressed in this group. The reason for this discrepancy was attributed to the mRNA expression levels of Cyp2c44 being lower and those of Cyp2c29 and Cyp2c66, which are involved in the metabolism of tolbutamide, being higher in the HFHC group than in the Control group. These results indicate that the expression of Cyp2c in the liver is influenced by the HFHC diet prior to the establishment of NASH and its regulation differed among the subtypes examined.
[Mh] Termos MeSH primário: Colesterol na Dieta/efeitos adversos
Sistema Enzimático do Citocromo P-450/metabolismo
Dieta Hiperlipídica/efeitos adversos
Fígado/enzimologia
Hepatopatia Gordurosa não Alcoólica/enzimologia
Hepatopatia Gordurosa não Alcoólica/etiologia
[Mh] Termos MeSH secundário: Animais
Sistema Enzimático do Citocromo P-450/genética
Sistema Enzimático do Citocromo P-450/fisiologia
Modelos Animais de Doenças
Expressão Gênica
Hipoglicemiantes/metabolismo
Hipoglicemiantes/farmacologia
Metabolismo dos Lipídeos
Fígado/metabolismo
Fígado/patologia
Masculino
Camundongos Endogâmicos C57BL
Microssomos Hepáticos/metabolismo
Tamanho do Órgão
Tolbutamida/metabolismo
Tolbutamida/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholesterol, Dietary); 0 (Hypoglycemic Agents); 9035-51-2 (Cytochrome P-450 Enzyme System); 982XCM1FOI (Tolbutamide)
[Em] Mês de entrada:1705
[Cu] Atualização por classe:171016
[Lr] Data última revisão:
171016
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160906
[St] Status:MEDLINE
[do] DOI:10.1248/yakushi.16-00034


  10 / 4213 MEDLINE  
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[PMID]:27504459
[Au] Autor:Lau J; Grapengiesser E; Hellman B
[Ad] Endereço:Department of Medical Cell Biology, Uppsala University, Box 571, 751 23 Uppsala, Sweden.
[Ti] Título:Small Mouse Islets Are Deficient in Glucagon-Producing Alpha Cells but Rich in Somatostatin-Secreting Delta Cells.
[So] Source:J Diabetes Res;2016:4930741, 2016.
[Is] ISSN:2314-6753
[Cp] País de publicação:Egypt
[La] Idioma:eng
[Ab] Resumo:Small and big mouse islets were compared with special reference to their content of glucagon-producing α-cells and somatostatin-producing δ-cells. Areas stained for glucagon and somatostatin were measured in the largest cross section of small (diameter < 60 µm) and big (diameter > 100 µm) islets. Comparison of the areas indicated proportionally more δ- than α-cells in the small islets. After isolation with collagenase these islets were practically devoid of α-cells. We evaluated the functional importance of the islet size by measuring the Ca(2+) signal for insulin release. A majority of the small islets responded to the hyperpolarization action of somatostatin with periodic decrease of cytoplasmic Ca(2+) when glucose was elevated after tolbutamide blockade of the KATP channels.
[Mh] Termos MeSH primário: Células Secretoras de Glucagon/citologia
Glucose/metabolismo
Insulina/secreção
Ilhotas Pancreáticas/citologia
Células Secretoras de Somatostatina/citologia
[Mh] Termos MeSH secundário: Animais
Sinalização do Cálcio/efeitos dos fármacos
Glucagon/metabolismo
Células Secretoras de Glucagon/secreção
Hipoglicemiantes/farmacologia
Imuno-Histoquímica
Técnicas In Vitro
Ilhotas Pancreáticas/metabolismo
Ilhotas Pancreáticas/patologia
Ilhotas Pancreáticas/secreção
Camundongos
Tamanho do Órgão
Somatostatina/metabolismo
Células Secretoras de Somatostatina/secreção
Tolbutamida/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Hypoglycemic Agents); 0 (Insulin); 51110-01-1 (Somatostatin); 9007-92-5 (Glucagon); 982XCM1FOI (Tolbutamide); IY9XDZ35W2 (Glucose)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170606
[Lr] Data última revisão:
170606
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160810
[St] Status:MEDLINE
[do] DOI:10.1155/2016/4930741



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