Base de dados : LILACS
Pesquisa : A11.284.835.540 [Categoria DeCS]
Referências encontradas : 31 [refinar]
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  1 / 31 LILACS  
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Id: biblio-839390
Autor: Dube, Aman K; Kumar, Maushmi S.
Título: Biotransformation of bromhexine by Cunninghamella elegans, C. echinulata and C. blakesleeana
Fonte: Braz. j. microbiol;48(2):259-267, April.-June 2017. tab, graf.
Idioma: en.
Resumo: Abstract Fungi is a well-known model used to study drug metabolism and its production in in vitro condition. We aim to screen the most efficient strain of Cunninghamella sp. among C. elegans, C. echinulata and C. blakesleeana for bromhexine metabolites production. We characterized the metabolites produced using various analytical tools and compared them with mammalian metabolites in Rat liver microsomes (RLM). The metabolites were collected by two-stage fermentation of bromhexine with different strains of Cunninghamella sp. followed by extraction. Analysis was done by thin layer chromatography, high performance thin layer chromatography, Fourier transform infrared spectroscopy, high performance liquid chromatography and Liquid chromatography–mass spectrometry. The role of Cytochrome P3A4 (CYP3A4) enzymes in bromhexine metabolism was studied. Fungal incubates were spiked with reference standard – clarithromycin to confirm the role of CYP3A4 enzyme in bromhexine metabolism. Three metabolites appeared at 4.7, 5.5 and 6.4 min retention time in HPLC. Metabolites produced by C. elegans and RLM were concluded to be similar based on their retention time, peak area and peak response of 30.05%, 21.06%, 1.34%, and 47.66% of three metabolites and bromhexine in HPLC. The role of CYP3A4 enzyme in metabolism of bromhexine and the presence of these enzymes in Cunninghamella species was confirmed due to absence of peaks at 4.7, 5.4 and 6.7 min when RLM were incubated with a CYP3A4 enzyme inhibitor – clarithromycin.
Descritores: Bromoexina/metabolismo
Cunninghamella/metabolismo
-Espectrometria de Massas
Biotransformação
Cromatografia Líquida de Alta Pressão
Cromatografia em Camada Delgada
Espectroscopia de Infravermelho com Transformada de Fourier
Citocromo P-450 CYP3A/metabolismo
Microssomos/metabolismo
Limites: Animais
Ratos
Responsável: BR1.1 - BIREME


  2 / 31 LILACS  
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Ribeiro, Lúcia Regina
Mantovani, Mário Sérgio
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Id: lil-555819
Autor: Tsuboy, Marcela Stefanini; Marcarini, Juliana Cristina; Ferreira, Dalva Trevisan; Ferraz, Elisa Raquel Anastácio; Chequer, Farah Maria Drumond; Oliveira, Danielle Palma de; Ribeiro, Lúcia Regina; Mantovani, Mário Sérgio.
Título: Evaluation of extracts from Coccoloba mollis using the Salmonella/microsome system and in vivo tests
Fonte: Genet. mol. biol;33(3):542-548, 2010. graf, tab.
Idioma: en.
Resumo: The common everyday use of medicinal plants is an ancient, and still very widespread practice, whereby the need for studies on their possible toxicity and mutagenic properties. The species Coccoloba mollis has been much used in phytotherapy, mainly in cases involving loss of memory and stress. In order to investigate its genotoxic and mutagenic potential, ethanolic extracts from the leaves and roots underwent Salmonella/microsome assaying (TA98 and TA100 strains, with and without exogenous metabolism - S9), besides comet and micronucleus tests in vivo.There was no significant increase in the number of revertants/plate of Salmonella strains in any of the analyzed root-extract concentrations, although the extract itself was extremely toxic to the Salmonella TA98 strain in the tests carried out with S9 (doses varying from 0.005 to 0.5 µg/plate). On the other hand, the leaf-extract induced mutations in the TA98 strain in the absence of S9 in the highest concentration evaluated, although at very low mutagenic potency (0.004 rev/µg). Furthermore, there was no statistically significant increase in the number of comets and micronuclei, in treatments involving Swiss mice. It was obvious that extracts of Coccoloba mollis, under the described experimental conditions, are not mutagenic.
Descritores: Microssomos
Plantas Medicinais
Salmonella
-Ensaio Cometa
Testes para Micronúcleos
Testes de Mutagenicidade
Polygonaceae
Limites: Animais
Responsável: BR26.1 - Biblioteca Central


  3 / 31 LILACS  
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Id: lil-535636
Autor: Yeyati, N. L; Altuna, M. E; Damasco, M. C; Mac Laughlin, M. A.
Título: Role of 11â-hydroxysteroid dehydrogenase 2 renal activity in potassium homeostasis in rats with chronic renal failure
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;43(1):52-56, Jan. 2010. tab, ilus.
Idioma: en.
Projeto: CONICET.
Resumo: Aldosterone concentrations vary in advanced chronic renal failure (CRF). The isozyme 11â-hydroxysteroid dehydrogenase 2 (11â-HSD2), which confers aldosterone specificity for mineralocorticoid receptors in distal tubules and collecting ducts, has been reported to be decreased or normal in patients with renal diseases. Our objective was to determine the role of aldosterone and 11â-HSD2 renal microsome activity, normalized for glomerular filtration rate (GFR), in maintaining K+ homeostasis in 5/6 nephrectomized rats. Male Wistar rats weighing 180-220 g at the beginning of the study were used. Rats with experimental CRF obtained by 5/6 nephrectomy (N = 9) and sham rats (N = 10) were maintained for 4 months. Systolic blood pressure and plasma creatinine (Pcr) concentration were measured at the end of the experiment. Sodium and potassium excretion and GFR were evaluated before and after spironolactone administration (10 mg·kg-1·day-1 for 7 days) and 11â-HSD2 activity on renal microsomes was determined. Systolic blood pressure (means ± SEM; Sham = 105 ± 8 and CRF = 149 ± 10 mmHg) and Pcr (Sham = 0.42 ± 0.03 and CRF = 2.53 ± 0.26 mg/dL) were higher (P < 0.05) while GFR (Sham = 1.46 ± 0.26 and CRF = 0.61 ± 0.06 mL/min) was lower (P < 0.05) in CRF, and plasma aldosterone (Pald) was the same in the two groups. Urinary sodium and potassium excretion was similar in the two groups under basal conditions but, after spironolactone treatment, only potassium excretion was decreased in CRF rats (sham = 0.95 ± 0.090 (before) vs 0.89 ± 0.09 µEq/min (after) and CRF = 1.05 ± 0.05 (before) vs 0.37 ± 0.07 µEq/min (after); P < 0.05). 11â-HSD2 activity on renal microsomes was lower in CRF rats (sham = 0.807 ± 0.09 and CRF = 0.217 ± 0.07 nmol·min-1·mg protein-1; P < 0.05), although when normalized for mL GFR it was similar in both groups. We conclude that K+ homeostasis is ...
Descritores: /fisiologia
ABELSON MURINE LEUKEMIA VIRUS-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE TEMEFOS/fisiologia
Homeostase/fisiologia
Falência Renal Crônica/metabolismo
Microssomos/enzimologia
Potássio/metabolismo
-/metabolismo
ABELSON MURINE LEUKEMIA VIRUS-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE TEMEFOS/metabolismo
Aldosterona/sangue
Pressão Sanguínea/fisiologia
Falência Renal Crônica/enzimologia
Nefrectomia
Ratos Wistar
Limites: Animais
Masculino
Ratos
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME


  4 / 31 LILACS  
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Id: lil-518688
Autor: González-Mujica, Freddy.
Título: Glucosa-6-fosfatasa de envoltura nuclear de hígado de rata / Glucose-6-phosphatase from nuclear envelope in rat liver
Fonte: Invest. clín;49(2):169-180, jun. 2008. tab.
Idioma: es.
Resumo: Se comparó la actividad de la glucosa-6-fosfatasa (G-6-Pasa) de envoltura nuclear (EN) con la microsomal. Los microsomas intactos fueron incapaces de hidrolizar manosa-6-fosfato (M-6-P); por el contrario, la EN intacta fue capaz de hidrolizar dicho substrato. La galactosa-6-fosfato mostró ser un buen substrato tanto para la enzima de EN como microsomal, con una latencia similar a la obtenida para M-6-P utilizando microsomas, por lo cual galactosa-6-fosfato fue usado para medir el porcentaje de EN intactas. Los parámetros cinéticos (Kii y Kis) de la inhibición por floricina de la G-6-Pasa de EN intactas, utilizando glucosa-6-fosfato (G-6-P) y M-6-P como substrato, fueron aproximadamente iguales. El transportador T1 de EN fue más sensible a la amiloride que el microsomal. Por el contrario, el sistema microsomal fue más sensible al efecto de N-etilmaleimida (NEM) que el de EN y este último, fue prácticamente insensible a los inhibidores de transporte aniónico DIDS y SITS, los cuales afectan fuertemente la enzima microsomal. Los resultados anteriores permiten sugerir que en la EN existe un transportador de hexosas-6-fosfato, capaz de transportar G-6-P y M-6-P y quizás otras hexosas-6-fosfato y que, o es diferente al T1 microsomal, o si es igual es influenciado por las características del sistema membranoso en el cual está incluido. La capacidad superior de hidrólisis de PPi de la G-6-Pasa de EN intacta, en comparación con la de microsomas intactos, sugiere diferencias en el transportador de Pi/PPi (T2) de ambos sistemas. La menor sensibilidad de la G-6-Pasa de EN al NEM sugiere que la subunidad catalítica de este sistema también podría tener algunas diferencias con la isoforma microsomal.
Descritores: GLUCOSA-ABDOMEN, ACUTE-FOSFATASA
Microssomos
Membrana Nuclear
Florizina
-Bioquímica
Limites: Animais
Ratos
Tipo de Publ: Estudo Comparativo
Revisão
Responsável: VE1.1 - Biblioteca Humberto Garcia Arocha


  5 / 31 LILACS  
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Id: lil-506485
Autor: Remigio Montero, Antonia C; Vega Hurtado, Yamilé; Piloto Ferrer, Janet; Rodríguez Chanfrau, Jorge.
Título: Genotoxicidad de Justicia pectoralis Jacq: (tilo) / Genotocixity of Justicia pectoralis Jacq: (tilo)
Fonte: Rev. cuba. plantas med;13(2), abr.-jun. 2008. tab.
Idioma: es.
Resumo: Objetivo: determinar el efecto genotóxico del extracto hidroalcohólico 30 por ciento de partes aéreas de Justicia pectoralis Jacq. (variedad pectoralis) secado por spray dryer. Métodos: se empleó el ensayo Salmonella/microsomas con las líneas TA 1535, TA 1537, TA 98 y TA 100 con un rango de concentraciones de 50 a 5 000 mg de polvo/placa (± S9) según el protocolo de incorporación en placas; para el ensayo de micronúcleos en médula ósea se utilizaron ratones Cenp: NMRI de los 2 sexos, que recibieron dosis isovolumétricas (10 mL/kg) de 500, 1 000 y 2 000 mg de polvo/kg, por vía intragástrica, separadas 24 h, con sacrificio 24 h después de la última aplicación. Resultados: no se encontró efecto genotóxico con ninguna de las cepas en el ensayo de Salmonella/microsomas y el extracto no causó un aumento estadísticamente significativo en la frecuencia de eritrocitos policromáticos micronucleados en los ratones tratados y no mostró relación dosis respuesta positiva. Conclusiones: el polvo no reveló efecto genotóxico en las condiciones experimentales de este estudio.

Objective: to detemine the genotoxic effect of the hydroalcoholic extract 30 of aerial parts of Justicia pectoralis Jacq. (variety pectoralis) dried by spray drier. Methods: the Salmonella/microsomes with lines TA 1535, TA 1537, TA 98 and TA 100 with a concentration range from 50 to 5 000 ìg of powder/plaque (± S9) was used according to the protocol of incorporation in plaques; for the bone marrow micronucleus assay there were used Cenp mice: NMRI of both sexes that received isovolumetric doses (10 mL/kg) of 500, 1 000 y 2 000 mg of powder/kg by intragastric route at intervals of 24 h and were sacrificed 24 h after the last application. Results: no genotoxic effect was found with any of the strains in the assay of Salmonella/microsomes. The extract did not cause a statistically significant increase in the frequency of micronucleated polychromatic erythrocytes in the mice treated. No dose/positive response relation was observed. Conclusions: the powder did not reveal genotoxic effect under the experimental conditions of this.
Descritores: Microssomos/microbiologia
Salmonella typhimurium/isolamento & purificação
Tilia/genética
Tilia/toxicidade
Limites: Animais
Camundongos
Responsável: CU1.1 - Biblioteca Médica Nacional


  6 / 31 LILACS  
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Id: lil-495743
Autor: Mecca, María Montalto de; Bartel, Laura C; Castro, Carmen Rodríguez de; Castro, José A.
Título: Benznidazole biotransformation in rat heart microsomal fraction without observable ultrastructural alterations: comparison to Nifurtimox-induced cardiac effects
Fonte: Mem. Inst. Oswaldo Cruz;103(6):549-553, Sept. 2008. ilus, tab.
Idioma: en.
Projeto: FONCyT; . UNSAM.
Resumo: Benznidazole (Bz) and Nifurtimox (Nfx) have been used to treat Chagas disease. As recent studies have de-monstrated cardiotoxic effects of Nfx, we attempted to determine whether Bz behaves similarly. Bz reached the heart tissue of male rats after intragastric administration. No cytosolic Bz nitroreductases were detected, although microsomal NADPH-dependent Bz nitroreductase activity was observed, and appeared to be mediated by P450 reductase. No ultrastructurally observable deleterious effects of Bz were detected, in contrast to the overt cardiac effects previously reported for Nfx. In conclusion, when these drugs are used in chagasic patients, Bz may pose a lesser risk to heart function than Nfx when any cardiopathy is present.
Descritores: Coração/efeitos dos fármacos
Miocárdio/metabolismo
Nifurtimox/farmacocinética
Nitroimidazóis/farmacocinética
Tripanossomicidas/farmacocinética
-Biotransformação
Avaliação Pré-Clínica de Medicamentos
Microscopia Eletrônica de Transmissão
Microssomos/enzimologia
Nifurtimox/efeitos adversos
Nitroimidazóis/efeitos adversos
Nitrorredutases/análise
Ratos Sprague-Dawley
Fatores de Tempo
Tripanossomicidas/efeitos adversos
Limites: Animais
Masculino
Ratos
Tipo de Publ: Estudo Comparativo
Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME


  7 / 31 LILACS  
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Id: lil-387949
Autor: Aiub, Claudia Alessandra Fortes; Pinto, Luis Felipe Ribeiro; Felzenszwalb, Israel.
Título: Standardization of conditions for the metabolic activation of N-nitrosodiethylamine in mutagenicity tests
Fonte: Genet. mol. res. (Online);3(2):264-272, jun. 2004.
Idioma: en.
Resumo: Like all nitrosamines, N-nitrosodiethylamine (NDEA) requires metabolic activation in order to exert its carcinogenic effects. This activation involves cytochrome P450s (CYP), which generates unstable metabolites that react with the DNA of cells in the immediate vicinity of metabolite formation. Although NDEA is carcinogenic, it has been considered a weak mutagen in classic genotoxicity assays. We used optimized Salmonella/mammalian microsome genotoxicity assays to assess the mutagenicity and toxicity of low concentrations of NDEA. Using a fixed concentration of NDEA (36.5 mg/ml), we varied the length of preincubation in the presence of different concentrations of an S9 metabolic activation mixture. Salmonella typhimurium strains TA97 and TA102 were resistant to NDEA-induced mutagenesis, even after a preincubation of up to 120 min and the use of different concentrations of the S9 mix. Strain TA98 was susceptible to mutagenesis by NDEA in the absence of the S9 mix and after preincubation with NDEA for 90 min. When bacteria of this strain were preincubated with NDEA for 60 min, mutagenesis was detected at an S9 mix concentration >9.55 mg/ml. NDEA also induced mutagenesis in strain TA100 after preincubation for 90 or 120 min, and this effect was dependent on the S9 concentration. E. coli strain BH990 also showed a concentration-dependent response, with only 60% of the cells surviving after a 120-min preincubation with NDEA in the presence of 19.1 mg S9 mix/ml.
Descritores: Alquilantes
Dietilnitrosamina
Escherichia coli
Salmonella typhimurium
-Alquilantes
Biotransformação
Dietilnitrosamina
Relação Dose-Resposta a Droga
Escherichia coli
Microssomos
Testes de Mutagenicidade
Salmonella typhimurium
Fatores de Tempo
Responsável: BR1.1 - BIREME


  8 / 31 LILACS  
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Id: lil-364989
Autor: Vecino, Maria C; Czepielewski, Mauro; Freitas, Daniel M. O; Vettori, Daniela V; Perla, Alexandre da Silveira; Haussen, Diogo C; Haussen, Sérgio R.
Título: Prevalência de anticorpos antimicrossomais em pacientes com esclerose múltipla / Prevalence of antimicrosomal antibodies in patients with multiple sclerosis
Fonte: Arq. neuropsiquiatr;62(3A):674-677, set. 2004. tab.
Idioma: pt.
Resumo: O objetivo deste estudo consiste em avaliar a prevalência de anticorpos antimicrossomais (AAM), a função tireóidea e a ocorrência de sintomas relacionados ao hipotireoidismo em pacientes com esclerose multipla (EM). Em um grupo de 21 pacientes com EM, foi realizado exameclínico, foram dosados o TSH, T4 e T4 livre e pesquisados AAM. A média de idade foi 41,05 anos e a média de tempo de doença foi 85,9 meses. Os sintomas relacionados ao hipotireoidismo foram fadiga, fraqueza, letargia e parestesias. Os AAM foram encontrados em 4 pacientes (19 por cento). O tempo de doença foi dividido em três períodos: <60 meses (3 pacientes AAM+/7AAM-), 60-120 meses (8 pacientes AAM-) e >120 meses (1 paciente AAM+/2 AAM-). Dois pacientes apresentaram níveis de T4 livre diminuídos, porém com T4 e TSH normais. Em 1 paciente, constatou-se hipotireoidismo subclínico, e em outro, hipotireoidismo clássico. Conclui-se que na avaliação dos pacientes com EM, em vista da falta de precisão na avaliação clínica do hipotireoidismo ocasionada pela sobreposição de sintomas referentes à EM, devam ser incorporadas as dosagens das provas de função tireóidea (PFT) e dos AAM.
Descritores: Autoanticorpos/sangue
Hipotireoidismo/imunologia
Microssomos/imunologia
Esclerose Múltipla/imunologia
Tireoidite Autoimune/imunologia
Tiroxina/sangue
-Testes de Função Tireóidea
Glândula Tireoide/imunologia
Tireoidite Autoimune/diagnóstico
Tireotropina/sangue
Limites: Seres Humanos
Masculino
Feminino
Adulto
Meia-Idade
Responsável: BR1.1 - BIREME


  9 / 31 LILACS  
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Id: lil-360936
Autor: Vargas, A. M; Barros, R. P. A; Zampieri, R. A; Okamoto, M. M; De Carvalho Papa, P; Machado, U. F.
Título: Abnormal subcellular distribution of GLUT4 protein in obese and insulin-treated diabetic female dogs
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;37(7):1095-1101, July 2004. ilus, tab, graf.
Idioma: en.
Projeto: FAPESP.
Resumo: The GLUT4 transporter plays a key role in insulin-induced glucose uptake, which is impaired in insulin resistance. The objective of the present study was to investigate the tissue content and the subcellular distribution of GLUT4 protein in 4-to 12-year-old control, obese and insulin-treated diabetic mongrel female dogs (4 animals per group). The parametrial white adipose tissue was sampled and processed to obtain both plasma membrane and microsome subcellular fractions for GLUT4 analysis by Western blotting. There was no significant difference in glycemia and insulinemia between control and obese animals. Diabetic dogs showed hyperglycemia (369.9 ± 89.9 mg/dl). Compared to control, the plasma membrane GLUT4, reported per g tissue, was reduced by 55 percent (P < 0.01) in obese dogs, and increased by 30 percent (P < 0.05) in diabetic dogs, and the microsomal GLUT4 was increased by approximately 45 percent (P < 0.001) in both obese and diabetic animals. Considering the sum of GLUT4 measured in plasma membrane and microsome as total cellular GLUT4, percent GLUT4 present in plasma membrane was reduced by approximately 65 percent (P < 0.001) in obese compared to control and diabetic animals. Since insulin stimulates GLUT4 translocation to the plasma membrane, percent GLUT4 in plasma membrane was divided by the insulinemia at the time of tissue removal and was found to be reduced by 75 percent (P < 0.01) in obese compared to control dogs. We conclude that the insulin-stimulated translocation of GLUT4 to the cell surface is reduced in obese female dogs. This probably contributes to insulin resistance, which plays an important role in glucose homeostasis in dogs.
Descritores: Adipócitos
Diabetes Mellitus Experimental
Insulina
Obesidade
-Transporte Biológico
Western Blotting
Membrana Celular
Modelos Animais de Doenças
Microssomos
Limites: Animais
Feminino
Cães
Responsável: BR1.1 - BIREME


  10 / 31 LILACS  
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Id: lil-255046
Autor: Ojeda, M. S; Gómez, N. N; Gil, E; Scardapane, L; Gimenez, M. S.
Título: Morphologic and biochemical changes in male rat lung after surgical and pharmacological castration
Fonte: Braz. j. med. biol. res = Rev. bras. pesqui. méd. biol;33(3):279-85, Mar. 2000. ilus, tab.
Idioma: en.
Resumo: The morphology of the rat lung was studied by light microscopy in different situations: after surgical and pharmacological castration and after administration of testosterone to the castrated rat to determine if the androgen is required to maintain the normal morphology of the lung. We also determined the effect of flutamide on the phospholipid composition of both the surfactant and microsomes of the lung. Rats were separated into five groups: I - control non-castrated rats, II - castrated rats sacrificed 21 days after castration, III - castrated rats that received testosterone daily from day 2 to day 21 after castration, IV - castrated rats that received testosterone from day 15 to day 21 after castration, and V - control rats injected with flutamide for 7 days. The amount of different phospholipids in the surfactant and microsomes of the lung was measured in group I and V rats. At the light microscopy level, the surgical and pharmacological castration provoked alterations in the morphology of the lung, similar to that observed in human lung emphysema. The compositions of surfactant and microsomes of the lung were similar to those previously reported by us for the surgically castrated rats. These results indicate that androgens are necessary for the normal morphology as well as for some metabolic aspects of the lung.
Descritores: Antagonistas de Androgênios/farmacologia
Flutamida/farmacologia
Hormônios Esteroides Gonadais/farmacologia
Pulmão/citologia
Microssomos/efeitos dos fármacos
Orquiectomia
Surfactantes Pulmonares/efeitos dos fármacos
Testosterona/farmacologia
-Pulmão/metabolismo
Microssomos/química
Orquiectomia/efeitos adversos
Fosfolipídeos/análise
Surfactantes Pulmonares/química
Ratos Wistar
Limites: Animais
Masculino
Ratos
Tipo de Publ: Research Support, Non-U.S. Gov't
Responsável: BR1.1 - BIREME



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