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1.
Braz. j. med. biol. res ; 47(3): 231-236, 03/2014. graf
Artigo em Inglês | LILACS | ID: lil-704623

RESUMO

Studies have shown that edaravone may prevent liver injury. This study aimed to investigate the effects of edaravone on the liver injury induced by D-galactosamine (GalN) and lipopolysaccharide (LPS) in female BALB/c mice. Edaravone was injected into mice 30 min before and 4 h after GalN/LPS injection. The survival rate was determined within the first 24 h. Animals were killed 8 h after GalN/LPS injection, and liver injury was biochemically and histologically assessed. Hepatocyte apoptosis was measured by TUNEL staining; proinflammatory cytokines [tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6)] in the liver were assayed by ELISA; expression of caspase-8 and caspase-3 proteins was detected by Western blot assay; and caspase-3 activity was also determined. Results showed that GalN/LPS induced marked elevations in serum aspartate aminotransferase (AST) and alanine aminotransferase (ALT). Edaravone significantly inhibited elevation of serum AST and ALT, accompanied by an improvement in histological findings. Edaravone lowered the levels of TNF-α and IL-6 and reduced the number of TUNEL-positive cells. In addition, 24 h after edaravone treatment, caspase-3 activity and mortality were reduced. Edaravone may effectively ameliorate GalN/LPS-induced liver injury in mice by reducing proinflammatory cytokines and inhibiting apoptosis.


Assuntos
Animais , Feminino , Antipirina/análogos & derivados , Apoptose/efeitos dos fármacos , Citocinas/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Sequestradores de Radicais Livres/farmacologia , Alanina Transaminase/sangue , Antipirina/farmacologia , Aspartato Aminotransferases/sangue , /análise , /metabolismo , /análise , Doença Hepática Induzida por Substâncias e Drogas/fisiopatologia , Ensaio de Imunoadsorção Enzimática , Endotoxinas/toxicidade , Galactosamina/toxicidade , Hepatócitos/efeitos dos fármacos , Marcação In Situ das Extremidades Cortadas , /análise , Lipopolissacarídeos/toxicidade , Camundongos Endogâmicos BALB C , Distribuição Aleatória , Fator de Necrose Tumoral alfa/análise
2.
Egyptian Journal of Chemistry. 2008; 51 (3): 373-388
em Inglês | IMEMR | ID: emr-99644

RESUMO

Mixtures of malononitrile, aromatic aIdeyde, and 4-nitrosoantipyrine [5] were interacted in ethanolic piperidine solutions, in one-pot reaction to give the corresponding 6-aryl-1-methyl-3-oxo-2-phenyl-2, 3-dihydro-1H-pyrazolo [4, 3-b] pyridine-5 carbonitriles [3] or their corresponding 6-alkyl-4-hydroxy- 1-methyl-3-oxo-2-phenyl- 1, 2, 3, 4-tetrahydro-SH-pyrazolo [4,-3-b] pyridine-5, 5-dicarbonitrile [4] depending on reaction temperature. However, carrying out the above reaction using 3-methyl-4-oximmno-1-phenyl-1H-pyrazolin-5-one [15b] instead of compound [5], the corresponding 6-aryl-7a-hydroxy-3-methyl-1-phenyl- 1, 7a-dihydro-pyrazolo [4, 3-c] [1, 2] oxazine-7-carbonitrile [17] were obtained. Chalcones [9] were reacted also with compounds [5] and [15b], to afford the corresponding 5-aroyl-6-aryl-1-methel-2phenyl-1, 2-dihydro-3H-pyrazolo [4, 3-b] pyridine-3 ones [12], and aryl [6-aryl-3-methyl-1-phenyl-1, 4-dihydropyrazolo [4, 3-c] [1, 2] oxazin-5-yl] methan-ones [20]. Aniline hydrochloride was condensed with compounds [3] in acetic acid to give the corresponding N-phenyl-2, 3-dihydro-1 H-pyrazolo [4, 3-b] pyridine-5-carboximidamides 6, which were converted into the corresponding 1-phenyl-1 H-imidazole-4, 5-diones [7] by their reaction with oxaly 1 chloride. However, on reaction of ethylenediamine with compounds [3] in the presence of p-toluenesulfonic acid, the corresponding 6-aryl-5-[4, 5-dihydro-1 H-imidazol-2-y1]-1-methyl-2-phenyl-1, 2-dihydropyrazolo [4, 3-b] pyridin-3-ones [8] were obtained


Assuntos
Piridinas/síntese química , Oxazinas/síntese química , Antipirina/análogos & derivados
4.
Invest. med. int ; 12(4): 321-5, feb 1986. tab, ilus
Artigo em Espanhol | LILACS | ID: lil-45898

RESUMO

Se estudiaron 20 pacientes de ambos sexos con cefalea de origen diverso a quienes se administró la combinación analgésica dihidroergotamina, propifenazona y cafeína en una solo gragea, en dosis de dos grageas iniciales y cada seis horas hasta alcanzar el efecto terapéutico o la dosis máxima de seis grageas. La edad promedio de los pacientes fue de 31.7 ñ 11.6 años. Se observaron efectos indeseables graves en dos casos; sin embargo no fue necesario suspender el tratamiento en ninguno. Finalmente la combinación analgésica estudiada demostró ser eficaz en el tratamiento de cefalea de origen diverso y fue bien tolerada en dosis terapéuticas


Assuntos
Adolescente , Adulto , Pessoa de Meia-Idade , Humanos , Masculino , Feminino , Antipirina/análogos & derivados , Antipirina/uso terapêutico , Cafeína/uso terapêutico , Di-Hidroergotamina/uso terapêutico , Cefaleia/tratamento farmacológico , Quimioterapia Combinada
5.
Invest. med. int ; 12(4): 254-9, feb 1986. tab, ilus
Artigo em Espanhol | LILACS | ID: lil-46865

RESUMO

En un estudio doble ciego comparativo contra placebo, se incluyó a 37 pacientes con cefalea de origen diverso; 17 de ellos recibieron una combinación analgésica de mesilato de dehidroergotamina (0.5 mg), butalbital (45 mg), propifenazona (125 mg) y cafeína (40 mg) en dosis de dos grageas cada seis horas, hasta un máximo de seus grageas por día, quedando 20 pacientes que recibieron placebo, en presentación idéntica al medicamento estudiado. El origen de la cefalea fue diverso tanto en el grupo que recibió el principio activo como en el grupo placebo; la localización y evolución de las cefaleas fueron similares en ambos grupos. Mediante el tratamiento, que tuvo una duración de cinco días, la intensidad del dolor de acuerdo a una escala de valoración previamente establecida, descendió de 3.23 ñ 0.90 a 0.82 ñ 1.28 en el grupo tratado, mientras que en el grupo placebo el descenso no fue estadísticamente significativo. Se analizó también el número de grageas requeridas, tiempo de instalación del efecto terapéutico y su duración, así como los efectos indeseables que se presentaron en cada grupo. Se concluye que la combinación analgésica demostró ser útil en el tratamiento de la cefalea de diverso origen


Assuntos
Adolescente , Adulto , Pessoa de Meia-Idade , Masculino , Feminino , Antipirina/análogos & derivados , Barbitúricos/uso terapêutico , Cafeína/uso terapêutico , Di-Hidroergotamina/uso terapêutico , Cefaleia/tratamento farmacológico , Ensaios Clínicos como Assunto , Método Duplo-Cego , Quimioterapia Combinada
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