vol. 21, no. 04

Terapia antioxidante en la infección por el Virus de la Inmunodeficiencia Humana

2013-10-17T12:02:29Z

Articulo Antioxidant therapy in human immunodeficiency virus-infection Acta Farmacéutica Bonaerense; vol. 21, no. 4 El estrés oxidativo juega un papel importante como cofactor en la patogénesis del virus de la inmunodeficiencia humana (VIH). Los individuos infectados con VIH desarrollan además deficiencia en micronutrientes antioxidantes que recrudecen aún más el estado redox. En la era actual de la terapia antirretroviral altamente efectiva, nos propusimos una revisión del estado del conocimiento sobre los mecanismos moleculares oxidativos involucrados con la infección y el uso de los antioxidantes en estos individuos. Las combinaciones de suplementación de antioxidantes empleadas, resultan variadas, así como controvertidas en cuanto a los resultados sobre su eficacia. El empleo de los antioxidantes en individuos seropositivos al VIH resulta una alternativa terapéutica con reducido efecto tóxico, que pudiera repercutir en la supresión viral con restauración de las funciones inmunológicas.; Antioxidant therapy in human immunodeficiency virus-infection. Oxidative stress may play an important role as cofactor in human immunodeficiency virus (HIV) pathogenesis. HIV infected individuals are known to be deficient in antioxidant micronutrients that exacerbates the loose of redox status. At the actual date of highly active antiretroviral therapies era we propose the revision about knowledge of oxidative molecular mechanisms involved and the use of antioxidants in HIV-seropositive patients. The combinations for antioxidants supplementation used are diverse as much as controversial the results about its efficacy. The option for its use in HIV seropositive individuals could be an alternative that seeks to both suppresses HIV and restore immune functions with less toxic side effects.

Actividad fasciolicida in vitro de Portulaca oleracea L.

2013-10-17T12:02:29Z

Articulo Fasciolicide activity in vitro of Portulaca oleracea L. Acta Farmacéutica Bonaerense; vol. 21, no. 4 La fasciolosis es una enfermedad parasitaria distribuida mundialmente, causante de múltiples trastornos fisiológicos que pueden comprometer la vida, tanto del hombre como de los animales y de grandes pérdidas económicas que van desde el decomiso de los hígados de los animales infestados hasta disminución del peso, retraso del crecimiento, reducción de la producción de carne, leche o lana, descenso de la resistencia a otras enfermedades, inhibición de la reproducción, abortos e incluso la muerte. Se evaluó la actividad fascilicida in vitro del extracto seco Portulaca oleracea L. obtenido a partir de la liofilización del extracto acuoso al 10% de la planta completa y se emplearon varias concentraciones del mismo. Se utilizaron dos modelos experimentales in vitro: en placa de Petri frente a fasciola adulta y en placas multipozos frente al miracidio de Fasciola hepatica. Se demostró la efectividad del extracto estudiado como fasciolicida, obteniéndose los mejores resultados con el extracto seco al 1% en ambos casos. La actividad antiparasitaria observada fue dependiente de la concentración. Considerando que el extracto evaluado fue obtenido a partir de la liofilización de un extracto acuoso, podría pensarse que existen metabolitos con características polares responsables de la actividad biológica, pudiendo ser los alcaloides, aminoácidos y saponinas presentes en la planta los potenciales antihelmínticos.; The fasciolosis is a parasitic illness distributed worldwide, causing multiple physiologic dysfunctions that can commit the life, so much of the man as of the animals, and big economic losses that go from the seizure of animals infested livers until decrease of weight, delay of growth, reduction of meat production, milk or wool, descent of resistance to other illnesses, inhibition of reproduction, abortions and even death. The in vitro fasciolicide activity of the dry extract of Portulaca oleracea L. obtained by liophylization from the 10% aqueous extract of the whole plant was evaluated and several concentrations were used. Two in vitro experimental models were used: Petri dishes in the case of mature Fasciola and multiwells in the case of Fasciola miracidium. The fasciolicide effectiveness of the extract was demonstrated and best results were obtaind with 1% dry extract in both cases, being the antiparasitic activity dependent on concentration. Taking into account that the evaluated extract was obtained by liophylization of an aqueous extract, we could think that metabolites with polar characteristics, like the alkaloids, amino acids or saponines present in the plant, are responsible for the potential antihelmintic activity.

Efecto de melatonina exógena en procesos inflamatorios agudos y crónicos en ratas

2013-10-17T12:02:29Z

Articulo Effect of exogenous melatonin on acute and chronic inflammatory process in rats Acta Farmacéutica Bonaerense; vol. 21, no. 4 Se investigó la influencia de melatonina (4 mg/kg) en la inflamación aguda usando el modelo de edema de pata en rata y en la inflamación crónica mediante la prueba del granuloma y artritis inducida por adyuvante. Melatonina inhibió el edema producido por carragenina en el modelo agudo, pero no presentó acción inhibitoria en la fase proliferativa de la prueba del granuloma y en la fase aguda y crónica de la artritis inducida por adyuvante. Estos resultados sugieren que melatonina, a la misma dosis, muestra diferentes comportamientos en los modelos inflamatorios ensayados.; Melatonin influence (4 mg/kg) was investigated on acute inflammation using rat paw edema and on chronic inflammation through granuloma test and adjuvant arthritis. Melatonin inhibited the edema produced by carrageenan in acute model. However, failed to inhibit the proliferative phase in the granuloma test and the acute and chronic phase in the adjuvant arthritis. These results suggest melatonin shows different activity on the tested inflammatory models at the same doses.

Vibrational spectra of Bis(L-Methioninato)Copper(II)

2013-10-17T12:02:29Z

Articulo Espectro vibracional del Bis(L-metioninato)cobre(II) Acta Farmacéutica Bonaerense; vol. 21, no. 4 Se registraron los espectros de infrarojo y Raman del complejo del título y se los discutió brevemente en base a sus carcaterísticas estructurales. Se hacen algunas comparaciones con otros complejos de Cu (II)/amino ácidos relacionados.; The infrared and Raman spectra of the tittle complex were recorded and briefly discussed on the basis of its structural characteristics. Some comparisons with related Cu(II)/amino acid complexes were made.

Análise preliminar da atividade antiulcerogênica do extrato hidroalcoólico de Solanum cernuum Vell.

2013-10-17T12:02:29Z

Articulo Preliminar analysis of anti-ulcerative activity of Solanum cernuum Vell. hydroalcoholic extract Acta Farmacéutica Bonaerense; vol. 21, no. 4 No presente trabalho a atividade antiulcerogênica do extrato hidroalcoólico a 60% das partes aéreas do Solanum cernuum Vell. (SCV) foi investigada utilizando-se modelo de úlcera induzida pela indometacina. Ratos albinos Wistar, machos, foram aleatoriamente distribuídos em grupos 1, 2, 3 e 4 recebendo respectivamente per os, solução de NaCl 0,9% (10 mL.kg -1), solução aquosa de tween 80 a 12% (10 mL.kg 1), SCV (1000 mg.kg -1), e cimetidina (100 mg.kg -1), 1 hora antes da administração de indometacina (30 mg.kg -1), sub-cutâneamente. O índice médio das lesões ulcerativas (IMLU), foram calculados 4 horas após a administração de indometacina. As análises evidenciaram que o grupo 3 tratado com SCV exibiu uma inibição de 50,4% no IMLU, quando comparado ao grupo 2, revelando atividade antiulcerogênica significativa.; In this work the anti-ulcerative activity of the 60% hydroalcoholic extract of the aerial parts of Solanum cernuum Vell. (SCV) was investigated in a model of ulcer induced by indomethacin. Male albino Wistar rats were randomly distributed in groups numbered from 1 to 4, which received, per os, a 0.9% NaCl solution (10 mL.kg -1 ), a 12% solution of tween 80 in water (10 mL.kg -1), SCV (1000 g.kg -1 ) and cimetidine (100 mg.kg -1 ) respectively, one hour before the subcutaneous administration of indomethacin (30 mg.kg -1 ). The average index of ulcerative lesions (AIUL) was calculated 4 hours after administering indomethacin. Analysis evidenced that group 3, treated with SCV, showed a 50.4% inhibition of the AIUL parameter, when compared to group 2, indi-cating significant anti-ulcerative activity.

Efecto sobre la propulsión intestinal y análisis fitoquímico preliminar de Aster squamatus (Asteraceae)

2013-10-17T12:02:29Z

Articulo Effect on gastrointestinal propulsion and preliminary phytochemical analysis of Aster squamatus (Asteraceae) Acta Farmacéutica Bonaerense; vol. 21, no. 4 The aim of this study was to determine the effect of Aster squamatus on gastrointestinal propulsion. Phytochemical screening suggested that stalks and roots contain steroids, terpenes, flavonoids, phenols, substances that contain amino-groups, saponins and hydrolysable and condensed tannins. The decoctions of leaves, stalks and roots indicated the presence of caffeic, cinnamic, and sinapic acids. All A. squamatus infusions significantly reduced gastrointestinal propulsion compared to control, whereas the decoctions and ethanolic extracts did not alter this parameter. The effect of the infusions and the lack of activity of the decoctions and ethanolic extracts may be linked to the presence of unstable or volatile con-stituents in the plant.

Búsqueda de actividad citotóxica en metabolitos secundarios de líquenes

2013-10-17T12:02:29Z

Articulo Cytotoxic screening activity of secondary lichen metabolites Acta Farmacéutica Bonaerense; vol. 21, no. 4 Búsqueda de Actividad Citotóxica en Metabolitos Secundarios de Líquenes. Cinco dépsidos y nueve depsidonas fueron estudiados para determinar su actividad citotóxica. Ambos grupos de metabolitos fenólicos obtenidos de líquenes fueron probados en cultivos celulares de linfocitos midiendo su capacidad para incorporar timidina tritiada, utilizando colchicina como estándar. Se observó un considerable efecto citotóxico para la mayoría de los compuestos, en particular pannarina, 1- cloropannarina y sfaeroforina, que presentaron un efecto citotóxico aún superior que el de colchicina. Se propone que la estructura molecular y la posibilidad de establecer puentes de hidrógeno por parte de los sustituyentes de los anillos aromáticos podrían ser los factores responsables de las diferentes actividades biológicas observadas.; Five depsides and nine depsidones were studied for their cytotoxic activity. Both groups of specific phenolic lichen metabolites were tested in cell culture of lymphocytes to which tritiated tymidine was agregated, using colchicine as standard. A conciderable cytotoxic effect was observed for all the com-pounds, being pannarin, 1-chloropannarin and sphaerophorin superior to colchicine. It is proposed that the molecular structures involved and the possibility of establishing hydrogen bonds by the substituents on the aromatic rings, might be responsible for the different biological activities observed.

Estudo toxicológico pré-clínico (agudo e sub-agudo) do produto Propovit Plus® em roedores

2013-10-17T12:02:29Z

Articulo Pre-clinical (acute and sub-acute) toxicologic study of phytomedicinal Propovit Plus® in rodents Acta Farmacéutica Bonaerense; vol. 21, no. 4 Realizou-se a avaliação toxicológica do fitoterápico Propovit Plus® em roedores. Os testes agudos não produziram mortalidade, com DL50 acima de 5 g/kg (oral) e 2,5 g/kg (i.p.), mas encontrou-se diminuição no peso dos corações dos grupos 5 g/kg (oral) e 2,5; 1,5 e 1,0 g/kg (i.p.). No tratamento sub-agudo, ocorreram três mortes no grupo 1,5 g/kg, aumento no peso dos pulmões dos machos tratados com a dose de 1,5 g/kg, aumento no peso do fígado e diminuição no peso dos pulmões das fêmeas tratadas também com a maior dose. Os testes sangüíneos mostraram diversos resultados significativos, embora sem correlação dose-resposta, sem ocorrência em ambos os sexos e com vários parâmetros dentro de faixas de normalidade. A avaliação histopatológica evidenciou poucas alterações, ocorrentes em praticamente todos os grupos e não dependentes da dose. Demonstra-se que o produto Propovit Plus® apresenta baixa toxicidade, mais evidente na dose de 1,5 g/kg, cerca de sessenta vezes maior que a dose terapêutica.; We report the toxicological evaluation of the phytomedicinal Propovit Plus in rodents. The acute tests didn't produce mortality, with DL50 above 5 g/kg (oral) and 2,5 g/kg (i.p.), but it was decrease in the weight of the hearts in groups 5 g/kg (oral) and 2,5; 1,5 and 1,0 g/kg (i.p.). In the long-term treatment, it happened three deaths in the group 1,5 g/kg, increase in the weight of the lungs of the males treated with the dose of 1,5 g/kg, increase in the weight of the liver and decrease in the weight of the lungs of the females also treated with the largest dose. The blood tests showed several significant results, although without correlation dose-answer, occurrence in both sexes and with several parameters inside of normality strips. The histological evaluation evidenced few alterations in practically all of the groups and was no dose-dependent. It is demonstrated that the product Propovit Plus present low toxicity, more evident in the dosage of 1,5 g/kg, about sixty times larger than the therapeutic dosage.

Actividad antinociceptiva de extractos crudos y de atranorina obtenidos a partir del liquen Cladina dendroides (des Abb.) Ahti

2015-07-08T18:55:36Z

Articulo Antinociceptive activity of crude extracts and atranorin obtained from the Lichen Cladina dendroides (des Abb.) Ahti Acta Farmacéutica Bonaerense; vol. 21, no. 4 El objeto de este estudio fue el aislamiento y la caracterización de atranorina, uno de los principales constituyentes presentes en Cladina dendroides (des Abb.) y analizar su efecto antinociceptivo. La actividad antinociceptiva fue verificada por medio del ensayo en ratones de las contorsiones inducidas por ácido acético (1%, 10 ml/Kg; i.p.). Tanto los extractos crudos (50 mg/Kg; i.p.) como la atranorina (25 mg/Kg; i.p.) demostraron tener una actividad significativa contra la nocicepción inducida por ácido acético. El extracto etéreo fue el más activo y con el mayor contenido de atranorina (72,4%) y menor cantidad de ácido fumarproto-cetrárico (27,5%). El extracto acetónico contuvo 55,5% de atranorina y 44,5% de ácido fumarprotocetrárico y también mostró una destacada acción antinociceptiva. El extracto clorofórmico, que presentó similar contenido de atranorina que el extracto etéreo, pero no ácido fumarprotocetrárico en su composición, exhibió la menor actividad antinociceptiva, indicando que la presenecia de este ácido en el extracto parece ser importante para que se manifieste la actividad antinociceptiva. Todos los extractos y la atranorina exhibieron bajo potencial toxicológico y un efecto antinociceptivo más pronunciado que la aspirina (50 mg/Kg; i.p.). Los datos sugieren que la actividad antinociceptiva de los extractos crudos es debida principalmente a atranorina, aunque un rol facilitador del ácido fumarprotocetrárico no debería ser descartado.; The aim of this study was to isolate and characterize atranorin, one of the major constituents presents in Cladina dendroides (des Abb.) Ahti., and analyze its antinociceptive effect. The antinociceptive activity was verified in acetic acid-induced (1%, 10 ml/Kg; i.p.) writhing test with mice. Both crude ex-tracts (50 mg/Kg; i.p.) as well as atranorin (25 mg/Kg; i.p.) were found to have a significant activity against acetic acid-induced nociception. The ether extract was the most active, and with the highest content of atranorin (72.4%), and low amount of fumarprotocetraric acid (27.5%). The acetone extract that contained 55.5% atranorin and 44.5% fumarprotocetraric acid also showed a remarkable antinociceptive action. The chloroform extract that presented similar content of atranorin as of ether extract, but no fumarprotocetraric acid in its composition, exerted lowest antinociceptive activity indicating that the presence of this acid in the extract seem be important to antinociceptive activity. All the extracts and atranorin exhibited low toxicity potential, and an antinociceptive effect more pronounced than aspirin (50 mg/Kg; i.p.). Taken together, the data suggest that the antinociceptive activity of crude extracts are primarily due to atranorin. A facilitator role for fumarprotocetraric acid should not be ruled out.

Atividade antimicrobiana in vitro de extratos hidroalcoólicos de Psidium guajava L. sobre bactérias gram-negativas

2016-12-12T20:01:31Z

Articulo In vitro antimicrobial activity of hydro-alcoholic extracts of Psidium guajava L. against gram-negativebacteria Acta Farmacéutica Bonaerense; vol. 21, no. 4 Este estudio tiene como objetivo probar in vitro por los métodos de difusión en disco de papel las susceptibilidades de bacterias Gran-negativas (Escherichia Coli, Pseudomonas Aeruginosa, Shigella spp, Proteus spp, Klebsiella spp, Salmonella spp) a los extractos hidroalcohólicos de hojas y ramas de Psidium guajava (goiabeira vermelha) y determinar su CMI en medio sólido. Se verificó que, expeptuando Klebsiella spp, todas las bacterias testeadas fuero inhibidas por los dos extractos utilizados, siendo que los extractos de hoja presentaron menor actividad para la Salmonella spp (17,3mm) y los extractos de rama fueron mas activos para Proteus spp (18,3mm). La CMI varió de 1,8 a 2,4 mg/mL en extracto de hoja y de 1,2 a 2,4 mg/mL en el extracto de rama. Para la Shigella spp y Pseudomonas Aeruginosa, la CMI fue de 1,2/mL en el extracto de rama. No hubo diferencias estadísticamente significantes entre los dos tipos de extractos, tanto en los tets antimicrobianos como en los valores de CMI.; In vitro antimicrobial activity of hydro-alcoholic extracts of Psidium guajava L. against gram-negative bacteria. The aim of this study was to test in vitro by a standardized single disk method the susceptibility of gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Shigella spp, Proteus spp, Klebsiella spp, Salmonella spp) in relation to hydro-alcoholic extracts of leaf and branch of Psidium guajava L. (known as goiabeira vermelha). A second aim was to determine the Minimum Inhibitory Concentration (MIC) in a solid medium. Except for Klebsiella spp, all tested bacteria were inhibited by both extracts. Leaf extract proved to be more active against Salmonella spp (17.3 mm) while branch extract showed better results against Proteus spp 18.3 mm). Minimum Inhibitory Concentration varied from 1.8 up to 2.4 mg/mL of leaf extract whereas for branch extract it varied from 1.2 up to 2.4 mg/mL. For Shigella spp and Pseudomonas aeruginosa MIC values were 1.2 mg/mL of branch extract. In general, no statistically significant differences were observed between both extracts when testing antimicrobial activity and MIC.

Disposición farmacocinética y biodistribución del anticuerpo monoclonal ior EGF/R3 en ratas, conejos y perros

2013-10-17T12:02:29Z

Articulo Pharmacokinetic disposition and biodistribution of the monoclonal antibody ior EGF/r3 in rats, dogs and rabbits Acta Farmacéutica Bonaerense; vol. 21, no. 4 El anticuerpo monoclonal ior EGF/r3, por sus propiedades bloqueadoras del receptor al factor de crecimiento epidérmico, presenta propiedades relevantes en la terapia del cáncer. Se realizó su estudio de caracterización farmacocinética en ratas Wistar a tres niveles de dosis: 0,5, 1 y 2 mg, bolus i.v. Mediante un Análisis por Radiorreceptor se obtuvieron las concentraciones a diferentes intervalos, desde 30 min hasta 96 h, en réplicas de 5x. Las dosis mayores se ajustaron a un transcurso bi-exponencial, mientras que en la dosis de 0,5 mg sólo fue posible alcanzar un ajuste mono-exponencial. Se estimaron los parámetros característicos y se encontraron diferencias fundamentales en el t 1/2 ß (31,66-68,07 h, p<0,05) y en el CL (1,35-2,68 mL/h, p<0,05). Se reporta una conducta dosis-dependiente. No se reportan altas captaciones a órganos, con excepción del hígado y riñón, órganos asociados al aclaramiento del monoclonal, aunque sus valores no sobrepasan al 7,03% de radio-actividad/órgano. Se estudió también su farmacocinética en conejos y perros. Los datos fueron en ambos casos ajustados a transcursos bi-exponenciales. En ambos se demuestra una regularidad farmacocinética, sin notables diferencias entre animales, mostrando parámetros confiables para su aplicación clínica. El t 1/2 alcanzó valores de 35,31 y 34,99 h, respectivamente, lo cual ratifica su potencialidad para una administración terapéutica.; Pharmacokinetic Disposition and Biodistribution of the Monoclonal Antibody ior EGF/r3 in rats, dogs and rabbits. MoAb ior EGF/r3 is well known by its antitumoral properties due to its anti-EGFr action. This survey was focused on the pharmacokinetic analysis of this drug in three different species, i.e., Wistar rats (at three dosage: 0.5, 1 and 2 mg), F1 rabbits and Beagle dogs, by bolus iv administration. The serum MoAb concentrations in rats were measured by radiobinding assay at several time points ranging from 30 min to 96 h, as 5 replication. At higher doses the pharmacokinetic biexponential decay profiles were fitted according to bicompartmental analysis, but at lower 0.5 mg dose the data points were better fitted using a monocompartmental modeling approach. It was reported the pharmacokinetic parameters with significant differences for t 1/2 ß (31,66-68,07 h, p<0,05) and CL (1,35-2,68 mL/h, p<0,05). showing a dose- dependence disposition pattern. There no exist significant uptake of the 99m Tc- ior EGF/r3 into the organs, but liver and kidney, which are both associated with its elimination clearance, although their values were not higher than 7.03 percentage of radioactivity/total organ weight. The pharmacokinetically characterized drug in rabbits and dogs was better fitted to biexponential elimination pofiles. The regularity of the drug disposition time course was provided in both species, without significantly differences between animals. Finally, the elimination half-lives of 35.3 h (rabbits) and 35 h (dogs), supported its potential for further clinical administration.