Stability of Tilo® tablets formulation obtained from dry extract of Justice pectoralis Jacq.

Justicia pectoralis Jacq., Acanthaceae, is a herb known popularly in Cuba as Tilo and used traditionally as sedative. The development in a solid pharmaceutical (Tablets 100 mg) using dry extract of Justicia pectolaris aqueous extract is of interest for the development of phytomedicines, which uses this active raw material. The aim of the present study was to carry out chemical and biological stability studies to the formulation. A method of coumarin determination by High Performance Liquid Chromatography (HPLC) was used and validated. The stability studies during different periods of time (24 months) showed a stability of the product stored at 32 ± 2 °C, and protected of the light.Justicia pectoralis Jacq., Acanthaceae é uma erva conhecida popularmente em Cuba como Tilo e utilizada tradicionalmente como sedativo. O desenvolvimento de formas farmacêuticas sólidas (comprimido 100 mg) usando extrato aquoso seco de J. pectoralis é de interesse no desenvolvimento de fitoterápicos que empreguem esse princípio ativo. O objetivo do presente estudo foi realizar estudos de estabilidade químicos e biológicos da formulação. Um método de determinação de cumarinas por Cromatografia Líquida de Alta Eficiência (CLAE) foi usado e devidamente validado. Os estudos de estabilidade durante diferentes períodos de tempo (24 meses) mostraram a estabilidade do produto preservado a 32 ± 2 °C e protegido da luz

Therapeutic potential of the novel hybrid molecule JM-20 against focal cortical ischemia in rats

Context: Despite the great mortality and morbidity of stroke, treatment options remain limited. We previously showed that JM-20, a novel synthetic molecule, possessed a strong neuroprotective effect in rats subjected to transient middle cerebral artery occlusion. However, to verify the robustness of the pre-clinical neuroprotective effects of JM-20 to get good prognosis in the translation to the clinic, it is necessary to use other experimental models of brain ischemia. Aims: To evaluate the neuroprotective effects of JM-20 following the onset of permanent focal cerebral ischemia induced in rats by thermocoagulation of blood into pial blood vessels of cerebral cortices. Methods: Ischemic lesion was induced by thermocoagulation of blood into pial blood vessels of primary motor and somatosensory cortices. Behavioral performance was evaluated by the cylinder testing for a period of 2, 3 and 7 days after surgery, and was followed by histopathological study in brain cortex stained with hematoxylin- eosin. Results: Ischemic injury resulted in impaired function of the forelimb evidenced by high asymmetry punctuation, and caused histopathological alterations indicative of tissue damage at cerebral cortex. JM-20 treatment (4 and 8 mg/kg) significantly decreased asymmetry scores and histological alterations with a marked preservation of cortical neurons. Conclusions: The effects of permanent brain ischemia were strongly attenuated by JM-20 administration, which expands and improves the current preclinical data of JM-20 as neuroprotector against cerebral ischemia, and strongly support the examination of its translation to the clinic to treat acute ischemic stroke

Stability of Tilo® tablets formulation obtained from dry extract of Justice pectoralis Jacq.

Justicia pectoralis Jacq., Acanthaceae, is a herb known popularly in Cuba as Tilo and used traditionally as sedative. The development in a solid pharmaceutical (Tablets 100 mg) using dry extract of Justicia pectolaris aqueous extract is of interest for the development of phytomedicines, which uses this active raw material. The aim of the present study was to carry out chemical and biological stability studies to the formulation. A method of coumarin determination by High Performance Liquid Chromatography (HPLC) was used and validated. The stability studies during different periods of time (24 months) showed a stability of the product stored at 32 ± 2 °C, and protected of the light

Preclinical anti-inflammatory effects of dry powder of Caléndula officinalis

Para demostrar la actividad antiinflamatoria del polvo seco Caléndula officinalis secado por atomización se emplearon dosis de 50, 150 y 450 mg/Kg y se evaluó el efecto sobre la inflamación aguda provocada por carragenina, dextrán, histamina y serotonina y granuloma inducido por discos de algodón en ratas y edema auricular inducido por aceite de crotón en ratones. El polvo seco mostró efecto inhibitorio sobre los diferentes modelos empleados sin afectar el peso del timo y las glándulas suprarrenales. Estos resultados muestran que el método de secado por atomización permite la obtención de una materia prima de Caléndula officinalis activa frente a procesos inflamatorios de naturaleza diversa.With the objective to demonstrate the anti-inflammatory effect of Calendula officinalis dry powder, doses of 50, 150 and 450 were used on inflammation induced by carragenin, dextran, histamine and serotonine, the granulome induced by cotton pellets in rats and ear inflammation induced by croton oil in mice. The spray dried powder of Calendula officinalis inhibited the inflammatory process in all animal model employed without affecting tymus's and adrenal's weight. These results show that the powder of Calendula officinalis obtained by spray drying is active in inflammatory processes of diverse nature.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Effect of the liophilized aqueous extract of Boerhavia erecta L. on passive cutaneous anaphylaxis, spasm and bronchial tonitity

Con el objetivo de demostrar las propiedades antialérgicas conferidas a Boerhavia erecta L., se estudió la posible influencia de la misma sobre los mediadores anafilácticos, espasmo y tonicidad bronquial inducido por histamina y sobre la musculatura lisa intestinal en cobayos. Como resultado final de este trabajo podemos concluir que el extracto acuoso liofilizado de Boerhavia erecta L. inhibe la anafilaxia pasiva cutánea y el espasmo bronquial inducido por histamina. También pudimos apreciar que la dosis de 100 mg/Kg por vía intravenosa aumenta en un 46% la contracción provocada por histamina 15 µg/Kg y a concentraciones superiores a 1 mg/mL provoca contracción de la musculatura lisa intestinal.To study the anti-allergy properties conferred to Boerhavia erecta L. on the anaphylactic mediators and H1 receptors at bronchial level, the tests of passive cutaneous anaphylaxis in rats and bronchial spasm and tonicity on the intestinal flat musculature in guinea pigs were carried out. After our results we can affirm that the extract watery of Boerhavia erecta L. inhibits the passive cutaneous anaphylaxis and the bronchial spasm induced by histamina. We could also appreciate that the dose of 100 mg/Kg of Boerhavia erecta L. after intravenous administration the contraction increases in 46% caused by histamina 15 µg/Kg and to superior concentrations to 1 mg/mL causes contraction of the intestinal flat musculature.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Effect of the liophilized aqueous extract of Boerhavia erecta L. on passive cutaneous anaphylaxis, spasm and bronchial tonitity

Con el objetivo de demostrar las propiedades antialérgicas conferidas a Boerhavia erecta L., se estudió la posible influencia de la misma sobre los mediadores anafilácticos, espasmo y tonicidad bronquial inducido por histamina y sobre la musculatura lisa intestinal en cobayos. Como resultado final de este trabajo podemos concluir que el extracto acuoso liofilizado de Boerhavia erecta L. inhibe la anafilaxia pasiva cutánea y el espasmo bronquial inducido por histamina. También pudimos apreciar que la dosis de 100 mg/Kg por vía intravenosa aumenta en un 46% la contracción provocada por histamina 15 µg/Kg y a concentraciones superiores a 1 mg/mL provoca contracción de la musculatura lisa intestinal.To study the anti-allergy properties conferred to Boerhavia erecta L. on the anaphylactic mediators and H1 receptors at bronchial level, the tests of passive cutaneous anaphylaxis in rats and bronchial spasm and tonicity on the intestinal flat musculature in guinea pigs were carried out. After our results we can affirm that the extract watery of Boerhavia erecta L. inhibits the passive cutaneous anaphylaxis and the bronchial spasm induced by histamina. We could also appreciate that the dose of 100 mg/Kg of Boerhavia erecta L. after intravenous administration the contraction increases in 46% caused by histamina 15 µg/Kg and to superior concentrations to 1 mg/mL causes contraction of the intestinal flat musculature.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Antioxidant and neuroprotective effects of gossypitrin, a flavonoid from Talipariti elatum, against chemical hypoxia-induced PC12 cell death

Context: Some flavonoids have been described as neuroprotectors. Gossypitrin (Gos) is a natural occurring flavonoid and the main bioactive substance from the flowers of Talipariti elatum Sw. (Majagua azul), traditionally used in Cuba as expectorant and antiasthmatic. Only few reports have documented its antioxidant properties. Aims: To evaluate the antioxidant and cytoprotective effects of Gos against cyanide-induced oxidative stress and cell death in PC12 cells. Methods: Gos effects on DPPH/ ABTS radical scavenging, ferric reducing power and lipid peroxidation were examined. The ischemia/reperfusion neuronal damage was produced by exposing PC12 cells to KCN in glucose-free medium. Gos was added to the incubation medium 30 min before chemical hypoxia induction. The neuroprotective potential of Gos was assessed by measuring cell viability by the MTT assay, the antioxidant enzymes SOD and CAT, and GSH and lipid peroxidation levels. Rutin (Rut), the well-known antioxidant, was used as a reference compound. Results: Gos showed a potent intrinsic antioxidant capacity evidenced by low IC50 and EC50 values for DPPH/ABTS/malondialdehyde and ferric reducing power, respectively. Pre-treatment of PC12 cells with Gos, significantly increased their survival against KCN, restored the levels of GSH and the SOD and CAT enzymes activities, as well as reduced the level of lipid peroxidation. Its antioxidant effects were higher than those elicited by Rut. Conclusions: The results show for the first time the neuroprotective potential of Gos against hypoxic cell damage, probably associated to its antioxidant effects

Estandarización de un modelo de isquemia por oclusión de la arteria cerebral media en ratas

El desarrollo y estandarización de biomodelos de isquemia cerebral para evaluar compuestos neuroprotectores es una necesidad imperante en numerosos grupos de investigación. La oclusión de la arteria cerebral media en ratas ha sido uno de los más empleados, sin embargo, este biomodelo es fuente de gran variabilidad ocasionada por diferentes factores. El presente trabajo establece las condiciones experimentales óptimas para lograr respuestas confiables y repetibles en nuestro laboratorio, y pueden facilitar a otros grupos la estandarización de este valioso modelo. Las mejores condiciones establecidas fueron 2 h de oclusión de la arteria cerebral media y 48 h de reperfusión, obteniendo una lesión isquémica caracterizada por evaluaciones conductuales, macroscópicas e histopatológicas.The development of animal models in stroke to evaluate neuroprotective agents is a serious need for many research groups. The middle cerebral artery occlusion in rats has been one of the most employed, although this model is associated with a great variability in the results. The present research establishes the optimum experimental conditions to obtain good experimental results in our model, and it can facilitate to other groups the standardization of this valuable model. The better conditions established were 2 h of the middle cerebral artery occlusion and 48 h of reperfusion, obtaining an ischemic injury characterized by behaviour test, macroscopic and histopathological evaluations.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Potential uses of Swiss albins mice as model of permanent unilateral brain ischemia

La elevada incidencia de las enfermedades cerebrovasculares y sus consecuencias, unida a la ausencia de tratamientos efectivos hace necesario desarrollar biomodelos sencillos, que permitan seleccionar moléculas neuroprotectoras. La inducción de isquemia unilateral permanente (IUP) en gerbil de Mongolia ha sido empleado desde los años 70; sin embargo presenta elevada mortalidad y disfunciones cognitivas que aparecen alrededor de los 7 días. El presente trabajo empleó ratones albinos suizos obteniéndose el 100 % de sobrevivencia y el daño cognitivo apareció 48 h después de inducida la lesión. La combinación de determinaciones seriadas de conducta exploratoria con IUP en ratones albinos suizos podría constituir un modelo sencillo para evaluar la influencia de nuevos fármacos sobre la plasticidad neuronal.The high incidence of cerebrovascular diseases and their consequences, together to the absence of effective treatments makes necessary to develop simple biomodels that allow to select new neuroprotective compounds. The induction of permanent unilateral brain ischemia (IUP) in Mongolian gerbil has been used from the seventies; however it presents high mortality and cognitive impairments that appear around the 7 days. The present work used swiss albins mices, obtaining 100% of survival and the cognitive impairments appeared 48 h after IUP-induced. The combination of repeated determinations of open field behavior in swiss albins mices after IUP-induced could be a simple model to evaluate the effects of new drugs on the neuronal plasticity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Potential uses of Swiss albins mice as model of permanent unilateral brain ischemia

La elevada incidencia de las enfermedades cerebrovasculares y sus consecuencias, unida a la ausencia de tratamientos efectivos hace necesario desarrollar biomodelos sencillos, que permitan seleccionar moléculas neuroprotectoras. La inducción de isquemia unilateral permanente (IUP) en gerbil de Mongolia ha sido empleado desde los años 70; sin embargo presenta elevada mortalidad y disfunciones cognitivas que aparecen alrededor de los 7 días. El presente trabajo empleó ratones albinos suizos obteniéndose el 100 % de sobrevivencia y el daño cognitivo apareció 48 h después de inducida la lesión. La combinación de determinaciones seriadas de conducta exploratoria con IUP en ratones albinos suizos podría constituir un modelo sencillo para evaluar la influencia de nuevos fármacos sobre la plasticidad neuronal.The high incidence of cerebrovascular diseases and their consequences, together to the absence of effective treatments makes necessary to develop simple biomodels that allow to select new neuroprotective compounds. The induction of permanent unilateral brain ischemia (IUP) in Mongolian gerbil has been used from the seventies; however it presents high mortality and cognitive impairments that appear around the 7 days. The present work used swiss albins mices, obtaining 100% of survival and the cognitive impairments appeared 48 h after IUP-induced. The combination of repeated determinations of open field behavior in swiss albins mices after IUP-induced could be a simple model to evaluate the effects of new drugs on the neuronal plasticity.Colegio de Farmacéuticos de la Provincia de Buenos Aire