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[PMID]:26363189
[Au] Autor:Cacioppo S; Cacioppo JT
[Ad] Endereço:High-Performance Electrical Neuroimaging Laboratory, Biological Science Division, University of Chicago Pritzker School of Medicine, Chicago, IL 60637, USA. Electronic address: scacioppo@bsd.uchicago.edu.
[Ti] Título:Dynamic spatiotemporal brain analyses using high-performance electrical neuroimaging, Part II: A step-by-step tutorial.
[So] Source:J Neurosci Methods;256:184-97, 2015 Dec 30.
[Is] ISSN:1872-678X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Our recently published analytic toolbox (Cacioppo et al., 2014), running under MATLAB environment and Brainstorm, offered a theoretical framework and set of validation studies for the automatic detection of event-related changes in the global pattern and global field power of electrical brain activity. Here, we provide a step-by-step tutorial of this toolbox along with a detailed description of analytical plans (aka the Chicago Electrical Neuroimaging Analytics, CENA) for the statistical analysis of brain microstate configuration and global field power in within and between-subject designs. Available CENA functions include: (1) a difference wave function; (2) a high-performance microsegmentation suite (HPMS), which consists of three specific analytic tools: (i) a root mean square error (RMSE) metric for identifying stable states and transition states across discrete event-related brain microstates; (ii) a similarity metric based on cosine distance in n dimensional sensor space to determine whether template maps for successive brain microstates differ in configuration of brain activity, and (iii) global field power (GFP) metrics for identifying changes in the overall level of activation of the brain; (3) a bootstrapping function for assessing the extent to which the solutions identified in the HPMS are robust (reliable, generalizable) and for empirically deriving additional experimental hypotheses; and (4) step-by-step procedures for performing a priori contrasts for data analysis. CENA is freely available for brain data spatiotemporal analyses at https://hpenlaboratory.uchicago.edu/page/cena, with sample data, user tutorial videos, and documentation.
[Mh] Termos MeSH primário: Mapeamento Encefálico/métodos
Encéfalo/fisiologia
Eletroencefalografia/métodos
Software
[Mh] Termos MeSH secundário: Acesso à Informação
Cromonar
Potenciais Evocados
Seres Humanos
Modelos Biológicos
Atividade Motora/fisiologia
Teste de Stroop
Interface Usuário-Computador
Percepção Visual/fisiologia
Adulto Jovem
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, NON-P.H.S.
[Nm] Nome de substância:
R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:1608
[Cu] Atualização por classe:151117
[Lr] Data última revisão:
151117
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:150913
[St] Status:MEDLINE


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[PMID]:20110890
[Au] Autor:Quezada E; Delogu G; Picciau C; Santana L; Podda G; Borges F; García-Morales V; Viña D; Orallo F
[Ad] Endereço:Chemistry Department, Faculty of Sciences, University Porto, 4169-007 Porto, Portugal.
[Ti] Título:Synthesis and vasorelaxant and platelet antiaggregatory activities of a new series of 6-halo-3-phenylcoumarins.
[So] Source:Molecules;15(1):270-9, 2010 Jan 12.
[Is] ISSN:1420-3049
[Cp] País de publicação:Switzerland
[La] Idioma:eng
[Ab] Resumo:A series of 6-halo-3-hydroxyphenylcoumarins (resveratrol-coumarins hybrid derivatives) was synthesized in good yields by a Perkin reaction followed by hydrolysis. The new compounds were evaluated for their vasorelaxant activity in intact rat aorta rings pre-contracted with phenylephrine (PE), as well as for their inhibitory effects on platelet aggregation induced by thrombin in washed human platelets. These compounds concentration-dependently relaxed vascular smooth muscle and some of them showed a platelet antiaggregatory activity that was up to thirty times higher than that shown by trans-resveratrol and some other previously synthesized derivatives.
[Mh] Termos MeSH primário: Cumarínicos/síntese química
Cumarínicos/farmacologia
Inibidores da Agregação de Plaquetas/síntese química
Inibidores da Agregação de Plaquetas/farmacologia
Vasodilatadores/síntese química
Vasodilatadores/farmacologia
[Mh] Termos MeSH secundário: Animais
Cromonar/química
Cumarínicos/química
Feminino
Seres Humanos
Técnicas In Vitro
Concentração Inibidora 50
Masculino
Agregação Plaquetária/efeitos dos fármacos
Inibidores da Agregação de Plaquetas/química
Ratos
Ratos Wistar
Estilbenos/química
Vasodilatação/efeitos dos fármacos
Vasodilatadores/química
Varfarina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Coumarins); 0 (Platelet Aggregation Inhibitors); 0 (Stilbenes); 0 (Vasodilator Agents); 5Q7ZVV76EI (Warfarin); Q369O8926L (resveratrol); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:1004
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:100130
[St] Status:MEDLINE
[do] DOI:10.3390/molecules15010270


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[PMID]:19279317
[Au] Autor:Bucolo C; Ward KW; Mazzon E; Cuzzocrea S; Drago F
[Ad] Endereço:Department of Experimental and Clinical Pharmacology, School of Medicine, University of Catania, Catania, Italy. bucocla@unict.it
[Ti] Título:Protective effects of a coumarin derivative in diabetic rats.
[So] Source:Invest Ophthalmol Vis Sci;50(8):3846-52, 2009 Aug.
[Is] ISSN:1552-5783
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Retinal microvascular cells play a crucial role in the pathogenesis of diabetic retinopathy. The endothelial effects of cloricromene, a novel coumarin derivative, on diabetic retinopathy induced by streptozotocin (STZ) in the rat were investigated. METHODS: Cloricromene (10 mg/kg intraperitoneally) was administered daily in diabetic rats, and 60 days later eyes were enucleated for localization of nitrotyrosine, ICAM-1, VEGF, ZO-1, occludin, claudin-5, and VE-cadherin by immunohistochemical analysis. The effect of treatment was also evaluated by TNFalpha, ICAM-1, VEGF, and eNOS protein levels measurement in the retina with the respective ELISA kits. Blood-retinal barrier (BRB) integrity was also evaluated by Evans blue. RESULTS: Increased amounts of cytokines, adhesion molecule, and nitric oxide synthase were observed in retina. Cloricromene treatment significantly lowered retinal TNFalpha, ICAM-1, VEGF, and eNOS. Furthermore, immunohistochemical analysis for VEGF, ICAM-1, nitrotyrosine (a marker of peroxynitrite), and tight junctions revealed positive staining in the retina from STZ-treated rats. The degree of staining for VEGF, ICAM-1, nitrotyrosine, and tight junctions was markedly reduced in tissue sections obtained from diabetic rats treated with cloricromene. Treatment with cloricromene suppressed diabetes-related BRB breakdown by 45%. CONCLUSIONS: This study provides the first evidence that the new coumarin derivative cloricromene attenuates the degree of inflammation preserving the BRB in diabetic rats.
[Mh] Termos MeSH primário: Cromonar/análogos & derivados
Diabetes Mellitus Experimental/tratamento farmacológico
Retinopatia Diabética/tratamento farmacológico
Inibidores da Agregação de Plaquetas/uso terapêutico
[Mh] Termos MeSH secundário: Animais
Antígenos CD/metabolismo
Barreira Hematorretiniana/efeitos dos fármacos
Western Blotting
Caderinas/metabolismo
Cromonar/uso terapêutico
Claudina-5
Diabetes Mellitus Experimental/metabolismo
Diabetes Mellitus Experimental/patologia
Retinopatia Diabética/metabolismo
Retinopatia Diabética/patologia
Ensaio de Imunoadsorção Enzimática
Imuno-Histoquímica
Injeções Intraperitoneais
Molécula 1 de Adesão Intercelular/metabolismo
Masculino
Proteínas de Membrana/metabolismo
Óxido Nítrico Sintase Tipo III/metabolismo
Ocludina
Fosfoproteínas/metabolismo
Ratos
Ratos Sprague-Dawley
Fator de Necrose Tumoral alfa/metabolismo
Tirosina/análogos & derivados
Tirosina/metabolismo
Fator A de Crescimento do Endotélio Vascular/metabolismo
Proteína da Zônula de Oclusão-1
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antigens, CD); 0 (Cadherins); 0 (Claudin-5); 0 (Cldn5 protein, rat); 0 (Membrane Proteins); 0 (Occludin); 0 (Ocln protein, rat); 0 (Phosphoproteins); 0 (Platelet Aggregation Inhibitors); 0 (Tjp1 protein, rat); 0 (Tumor Necrosis Factor-alpha); 0 (Vascular Endothelial Growth Factor A); 0 (Zonula Occludens-1 Protein); 0 (cadherin 5); 0 (vascular endothelial growth factor A, rat); 126547-89-5 (Intercellular Adhesion Molecule-1); 3604-79-3 (3-nitrotyrosine); 42HK56048U (Tyrosine); B9454PE93C (cloricromen); EC 1.14.13.39 (Nitric Oxide Synthase Type III); EC 1.14.13.39 (Nos3 protein, rat); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:0908
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:090313
[St] Status:MEDLINE
[do] DOI:10.1167/iovs.08-3328


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[PMID]:17593009
[Au] Autor:Bucolo C; Maugeri F; Maltese A; Ward KW
[Ad] Endereço:Global Preclinical Development, Bausch & Lomb, Catania, Italy. bucocla@unict.it
[Ti] Título:Retinal and systemic pharmacokinetics of the anti-inflammatory drug cloricromene following oral administration in the rat and rabbit.
[So] Source:J Ocul Pharmacol Ther;23(3):257-63, 2007 Jun.
[Is] ISSN:1080-7683
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:PURPOSE: The aim of this study was to evaluate the retina and plasma distribution of cloricromene, a coumarin derivative, and its active metabolite (MET) after an oral administration in rabbits and rats. METHODS: A single dose of cloricromene was orally administered to rabbits (10 or 100 mg/kg) and to rats (100 mg/kg). Retina and plasma samples were collected at 15, 30, 60, and 90 min following administration. Drug concentrations in the retina and plasma were measured by high-performance liquid chromatography. RESULTS: As anticipated, only the active metabolite was found in all samples. The retina and plasma showed the same T(max); peak levels of the drug were achieved at 15 min in rats and at 30 min in rabbits. In rabbits, MET exposure was approximately dose-proportional in both retina and plasma between the 10- and 100-mg/kg dose. Substantial retinal exposure was observed in both the rat and rabbit, at exposures approximately nine- to sixteenfold lower in the retina than in plasma. CONCLUSIONS: The results showed that the active metabolite of cloricromene reached the retina after a single oral dose with exposures proportional to those in plasma. These data, along with the previously published potency data for cloricromene, suggest that cloricromene could be potentially useful in ischemic-retinal diseases where amelioration of blood flow and inflammation is desirable.
[Mh] Termos MeSH primário: Cromonar/análogos & derivados
Inibidores da Agregação de Plaquetas/farmacocinética
Pró-Fármacos/farmacocinética
Retina/efeitos dos fármacos
[Mh] Termos MeSH secundário: Administração Oral
Animais
Área Sob a Curva
Cromatografia Líquida de Alta Pressão
Cromonar/administração & dosagem
Cromonar/farmacocinética
Relação Dose-Resposta a Droga
Estabilidade de Medicamentos
Isquemia/tratamento farmacológico
Masculino
Inibidores da Agregação de Plaquetas/administração & dosagem
Pró-Fármacos/administração & dosagem
Coelhos
Distribuição Aleatória
Ratos
Ratos Sprague-Dawley
Retina/metabolismo
Doenças Retinianas/tratamento farmacológico
Especificidade da Espécie
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Platelet Aggregation Inhibitors); 0 (Prodrugs); B9454PE93C (cloricromen); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:0708
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:070627
[St] Status:MEDLINE


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[PMID]:16805962
[Au] Autor:Pignatello R; Maltese A; Maugeri F; Bucolo C
[Ad] Endereço:Dipartimento di Scienze Farmaceutiche, Università degli Studi di Catania, Viale A. Doria, 6, 95125 Catania, Italy. r.pignatello@unict.it
[Ti] Título:Enhancement of availability of cloricromene at brain level by a lipophilic prodrug.
[So] Source:J Pharm Pharmacol;58(7):1001-5, 2006 Jul.
[Is] ISSN:0022-3573
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:The pharmacokinetics of a lipophilic alkylamino acid (LAA) prodrug of cloricromene (AD6), name CLOR-C4, was studied in rat plasma and brain. In particular, we observed that the intraperitoneal administration of CLOR-C4 to rats was able to provide a slight but statistically significant higher concentration of the active drug metabolite (cloricromene acid) in the brain compared with the parent drug administered by the same way. The correlation between pharmacokinetic data and calculated partition (LogP) and brain distribution coefficients (LogBB) supported the hypothesis that the amphiphilic nature of the LAA promoiety could be responsible for a better penetration into the brain, more than the simple increase of lipophilicity gained with respect to the parent drug.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Cromonar/análogos & derivados
Portadores de Fármacos/química
Lipídeos/química
Pró-Fármacos/farmacocinética
[Mh] Termos MeSH secundário: Animais
Disponibilidade Biológica
Cromonar/sangue
Cromonar/química
Cromonar/farmacocinética
Masculino
Pró-Fármacos/química
Ratos
Ratos Sprague-Dawley
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Drug Carriers); 0 (Lipids); 0 (Prodrugs); B9454PE93C (cloricromen); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:0612
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:060630
[St] Status:MEDLINE


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[PMID]:16584158
[Au] Autor:Pignatello R; Ricupero N; Bucolo C; Maugeri F; Maltese A; Puglisi G
[Ad] Endereço:Dipartimento di Scienze Farmaceutiche, Università degli Studi di Catania; Città Universitaria, Viale A Doria, 6, 95125 Catania, Italy. r.pignatello@unict.it
[Ti] Título:Preparation and characterization of eudragit retard nanosuspensions for the ocular delivery of cloricromene.
[So] Source:AAPS PharmSciTech;7(1):E27, 2006 Mar 24.
[Is] ISSN:1530-9932
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The purpose of this study was to improve the stability of cloricromene (AD6) in ophthalmic formulations and its drug availability at the ocular level. To this end, AD6-loaded polymeric nanoparticle suspensions were made using inert polymer resins (Eudragit RS100 and RL100). We modified the quasi-emulsion solvent diffusion technique by varying some formulation parameters (the drug-to-polymer ratio, the total drug and polymer amount, and the stirring speed). The chemical stability of AD6 in the nanosuspensions was assessed by preparing some formulations using (unbuffered) isotonic saline or a pH 7 phosphate buffer solution as the dispersing medium. The formulations were stored at 4 degrees C, and the rate of degradation of AD6 was followed by high performance liquid chromatography (HPLC). The obtained nanosuspensions showed mean sizes and a positive surface charge (zeta-potential) that make them suitable for an ophthalmic application; these properties were maintained upon storage at 4 degrees C for several months. In vitro dissolution tests confirmed a modified release of the drug from the polymer matrixes. Nanosuspensions prepared with saline solution and no or lower amounts of surfactant (Tween 80) showed an enhanced stability of the ester drug for several months, with respect to an AD6 aqueous solution. Based on the technological results, AD6-loaded Eudragit Retard nanoparticle suspensions appear to offer promise as a means to improving the shelf life and bioavailability of this drug after ophthalmic application.
[Mh] Termos MeSH primário: Resinas Acrílicas/administração & dosagem
Cromonar/análogos & derivados
Olho/metabolismo
Nanoestruturas
[Mh] Termos MeSH secundário: Química Farmacêutica
Cromonar/administração & dosagem
Cromonar/química
Cromonar/farmacocinética
Estabilidade de Medicamentos
Tamanho da Partícula
Solubilidade
Suspensões
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acrylic Resins); 0 (Suspensions); 33434-24-1 (Eudragit RS); B9454PE93C (cloricromen); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:0604
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:060406
[St] Status:MEDLINE


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[PMID]:16572308
[Au] Autor:Muià C; Mazzon E; Zito D; Maiere D; Britti D; Crisafulli C; Oteri G; Cordasco G; Cuzzocrea S
[Ad] Endereço:Department of Clinical and Experimental Medicine and Pharmacology, Torre Biologica, Policlinico Universitario, 98123, Messina, Italy.
[Ti] Título:Cloricromene, a coumarine derivative, reduced the development of periodontitis in rats.
[So] Source:Naunyn Schmiedebergs Arch Pharmacol;373(1):51-9, 2006 Apr.
[Is] ISSN:0028-1298
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Recent studies have demonstrated that cloricromene, a coumarin derivative, exerts protective effects in models of inflammation and shock. Tumour necrosis factor plays a pivotal role in the induction of genes involved in physiological processes, as well as in the response to inflammation. We investigated the effect of cloricromene in a rat model of periodontitis. Periodontitis was induced in rats by placing a 2/0 braided silk ligature around the lower left first molar. At day 8 the gingivomucosal tissue encircling the mandibular first molar was removed for evaluation of tumour necrosis factor production, neutrophil infiltration, tissue permeability, nitrotyrosine formation, poly (ADP-ribose) polymerase activation, radiography and histology. Ligation significantly induced an increased tumour necrosis factor production, neutrophil infiltration and a positive staining for nitrotyrosine formation and poly (ADP-ribose) polymerase activation. Ligation significantly increased Evans blue extravasation in gingivomucosal tissue and alveolar bone erosion as evaluated by radiography analysis. Intraperitonal injection of cloricromene (10 mg/kg daily for 8 days) significantly decreased all of the parameters of inflammation as described above. This suggests that cloricromene treatment, which reduced tumour necrosis factor production, may be of benefit in the treatment of periodontitis.
[Mh] Termos MeSH primário: Cromonar/análogos & derivados
Periodontite/prevenção & controle
[Mh] Termos MeSH secundário: Animais
Permeabilidade Capilar/efeitos dos fármacos
Cromonar/farmacologia
Cromonar/uso terapêutico
Masculino
Infiltração de Neutrófilos
Periodontite/metabolismo
Periodontite/patologia
Poli(ADP-Ribose) Polimerases/metabolismo
Ratos
Ratos Sprague-Dawley
Fator de Necrose Tumoral alfa/análise
Fator de Necrose Tumoral alfa/antagonistas & inibidores
Fator de Necrose Tumoral alfa/biossíntese
Tirosina/análogos & derivados
Tirosina/biossíntese
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Tumor Necrosis Factor-alpha); 3604-79-3 (3-nitrotyrosine); 42HK56048U (Tyrosine); B9454PE93C (cloricromen); EC 2.4.2.30 (Poly(ADP-ribose) Polymerases); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:0811
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:060331
[St] Status:MEDLINE


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[PMID]:16126232
[Au] Autor:Ragazzi E; Costa CV; Comai S; Bertazzo A; Caparrotta L; Allegri G
[Ad] Endereço:Department of Pharmacology and Anaesthesiology, University of Padova, Largo E. Meneghetti 2, I-35131 Padova, Italy. eugenio.ragazzi@unipd.it
[Ti] Título:Cloricromene effect on the enzyme activities of the tryptophan-nicotinic acid pathway in diabetic/hyperlipidemic rabbits.
[So] Source:Life Sci;78(8):785-94, 2006 Jan 18.
[Is] ISSN:0024-3205
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Since alterations of tryptophan metabolism have been reported in diabetes and atherosclerosis, it was thought of interest to investigate any role of cloricromene through the influence on the oxidative metabolism of the amino acid by using diabetic/hyperlipidemic rabbits. Male 4-month-old New Zealand white rabbits, fed a diet enriched with 1% cholesterol and 10% corn oil, were made diabetic with alloxan. During the hyperlipidemic diet, a group of rabbits was treated with cloricromene (10 mg/kg/day subcutaneously plus 1.5 mg/kg/day intravenously, for 5 weeks). The other group received saline. Normometabolic New Zealand rabbits fed standard diet, treated or not with cloricromene, were used as control. The specific activities of liver tryptophan 2,3-dioxygenase and small intestine indole 2,3-dioxygenase were not significantly changed by the drug treatment. Also the specific activities of other enzymes of the kynurenine pathway in the liver and kidneys, specifically kynurenine 3-monooxygenase, kynureninase and kynurenine-oxoglutarate transaminase, did not show any significant difference in both tissues between the two groups of rabbits. On the contrary, 3-hydroxyanthranilate 3,4-dioxygenase activity in the liver of diabetic/hyperlipidemic rabbits and control rabbits treated with cloricromene showed a slight increase in comparison with untreated animals. Conversely, the specific activity of the enzyme in kidneys was not affected by the drug treatment in diabetic/hyperlipidemic animals but was reduced in controls. Aminocarboxymuconate-semialdehyde decarboxylase specific activity remained unchanged in the liver following cloricromene treatment, instead the specific activity of the enzyme in the kidneys of the diabetic/hyperlipidemic rabbits was significantly increased by the drug, with a value more than double in comparison to untreated animals. The activity of the scavenger enzyme Cu/Zn superoxide dismutase (Cu/Zn SOD) in the small intestine was also determined and found significantly increased of about twice as much in the group of diabetic/hyperlipidemic rabbits treated with cloricromene. In conclusion, in diabetic/hyperlipidemic rabbits, cloricromene appeared to influence the enzymes involved in the last steps of tryptophan oxidative metabolism through the kynurenine pathway. This, together with the antioxidant action through the activation of Cu/Zn SOD, might deserve further investigation for evaluating any link between the observed experimental findings at the level of the kynurenine pathway and the clinical effect of the drug.
[Mh] Termos MeSH primário: Cromonar/análogos & derivados
Diabetes Mellitus Experimental/enzimologia
Hiperlipidemias/enzimologia
Niacina/metabolismo
Oxigenases/metabolismo
Inibidores da Agregação de Plaquetas/farmacologia
Triptofano/metabolismo
[Mh] Termos MeSH secundário: Animais
Colesterol na Dieta/administração & dosagem
Cromonar/farmacologia
Diabetes Mellitus Experimental/tratamento farmacológico
Depuradores de Radicais Livres/metabolismo
Hiperlipidemias/tratamento farmacológico
Intestino Delgado/efeitos dos fármacos
Intestino Delgado/enzimologia
Fígado/efeitos dos fármacos
Fígado/enzimologia
Masculino
Oxirredução
Coelhos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Cholesterol, Dietary); 0 (Free Radical Scavengers); 0 (Platelet Aggregation Inhibitors); 2679MF687A (Niacin); 8DUH1N11BX (Tryptophan); B9454PE93C (cloricromen); EC 1.13.- (Oxygenases); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:0602
[Cu] Atualização por classe:151119
[Lr] Data última revisão:
151119
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:050830
[St] Status:MEDLINE


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[PMID]:15322736
[Au] Autor:Ianaro A; Maffia P; Grassia G; Di Meglio P; Sorrentino R; di Villa Bianca Rd; Di Rosa M; Ialenti A
[Ad] Endereço:Department of Experimental Pharmacology, University of Naples Federico II, Via Domenico Montesano 49, 80131 Naples, Italy.
[Ti] Título:Cloricromene in endotoxemia: role of NF-kappaB.
[So] Source:Naunyn Schmiedebergs Arch Pharmacol;370(2):140-5, 2004 Aug.
[Is] ISSN:0028-1298
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:In this study we investigated, for the first time in vivo, the effect of cloricromene, a cumarine derivative, on NF-kappaB activation in endotoxin-treated rats. Endotoxemia was induced in male rats by the intravenous injection of Salmonella typhosa lipopolysaccharide (LPS; 2 mg/kg/i.v.). In vivo treatment with cloricromene (2 mg/kg/i.v.) 30 min before lipopolysaccharide administration reversed the LPS-induced loss in tone of the aortic rings, improved their reactivity to phenylephrine, decreased both nitric oxide (NO) and TNF-alpha serum levels by inhibiting LPS-induced inducible NO synthase and TNF-alpha mRNA expression, and interestingly inhibited LPS-induced NF-kappaB activation. Our data suggest that cloricromene protects rats from LPS by blocking LPS-induced NF-kappaB activation, leading to inhibition of NO and TNF-alpha overproduction and thereby reversing the LPS-induced vascular hyporeactivity.
[Mh] Termos MeSH primário: Cromonar/análogos & derivados
Cromonar/uso terapêutico
Endotoxemia/tratamento farmacológico
NF-kappa B/antagonistas & inibidores
Salmonella typhi
[Mh] Termos MeSH secundário: Animais
Aorta Torácica/efeitos dos fármacos
Aorta Torácica/metabolismo
Aorta Torácica/fisiologia
Ensaio de Desvio de Mobilidade Eletroforética
Endotoxemia/metabolismo
Endotoxemia/fisiopatologia
Técnicas In Vitro
Masculino
Contração Muscular/efeitos dos fármacos
Músculo Liso Vascular/efeitos dos fármacos
Músculo Liso Vascular/fisiologia
NF-kappa B/genética
NF-kappa B/metabolismo
Nitratos/sangue
Óxido Nítrico Sintase/antagonistas & inibidores
Óxido Nítrico Sintase/genética
Óxido Nítrico Sintase Tipo II
Nitritos/sangue
Fenilefrina
RNA Mensageiro/antagonistas & inibidores
Ratos
Ratos Wistar
Reação em Cadeia da Polimerase Via Transcriptase Reversa
Fator de Necrose Tumoral alfa/antagonistas & inibidores
Fator de Necrose Tumoral alfa/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (NF-kappa B); 0 (Nitrates); 0 (Nitrites); 0 (RNA, Messenger); 0 (Tumor Necrosis Factor-alpha); 1WS297W6MV (Phenylephrine); B9454PE93C (cloricromen); EC 1.14.13.39 (Nitric Oxide Synthase); EC 1.14.13.39 (Nitric Oxide Synthase Type II); EC 1.14.13.39 (Nos2 protein, rat); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:0504
[Cu] Atualização por classe:170920
[Lr] Data última revisão:
170920
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:040824
[St] Status:MEDLINE


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[PMID]:15233861
[Au] Autor:Bucolo C; Maltese A; Maugeri F; Busà B; Puglisi G; Pignatello R
[Ad] Endereço:Bausch & Lomb Oftal, C. so Italia 141, I-95127, Catania, Italy.
[Ti] Título:Eudragit RL100 nanoparticle system for the ophthalmic delivery of cloricromene.
[So] Source:J Pharm Pharmacol;56(7):841-6, 2004 Jul.
[Is] ISSN:0022-3573
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:A Eudragit RL100 polymer nanoparticle system loaded with cloricromene was prepared and characterized on the basis of physicochemical properties, stability and drug release features. To investigate the ocular bioavailability of cloricromene after inclusion in the polymer matrix, the new nanoparticle system was topically administered in the rabbit eye and compared with an aqueous solution of the same drug. The nanoparticle system showed interesting size distribution and surface charge values, suitable for ophthalmic application. The results indicated that the dispersion of cloricromene within Eudragit RL100 polymer nanoparticles increased its ocular bioavailability and enhanced the biopharmaceutical profile. The new cloricromene-loaded nanoparticle system described here may be useful in clinical practice.
[Mh] Termos MeSH primário: Resinas Acrílicas/química
Cromonar/análogos & derivados
Cromonar/administração & dosagem
Cromonar/química
Inibidores da Agregação de Plaquetas/administração & dosagem
Inibidores da Agregação de Plaquetas/química
[Mh] Termos MeSH secundário: Animais
Área Sob a Curva
Cromatografia Líquida de Alta Pressão
Cromonar/farmacocinética
Vias de Administração de Medicamentos
Sistemas de Liberação de Medicamentos
Estabilidade de Medicamentos
Masculino
Nanotecnologia
Tamanho da Partícula
Inibidores da Agregação de Plaquetas/farmacocinética
Coelhos
Solubilidade
Propriedades de Superfície
Tecnologia Farmacêutica
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acrylic Resins); 0 (Platelet Aggregation Inhibitors); 33434-24-1 (Eudragit RS); B9454PE93C (cloricromen); R0C9NIE5JJ (Chromonar)
[Em] Mês de entrada:0411
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:040706
[St] Status:MEDLINE



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