Hypokinetic Activity of Menthofuran on the Gastrointestinal Tract in Rodents.

The acute toxicity and hypokinetic activity induced by menthofuran on the gastrointestinal tract of rodents were investigated in the present study. An absence of acute toxicity was observed. Menthofuran delayed gastric emptying at oral doses of 25, 50, and 100 mg/kg in the experimental model of phenol red, as well as it reduced the intestinal transit at oral doses of 50 and 100 mg/kg. Interestingly, a scopolamine-similar hypokinetic effect was observed for menthofuran. In the experimental model of castor oil-induced intestinal hypermotility, menthofuran (50 and 100 mg/kg) reduced the number of loose stools as observed for the normal group. Additionally, menthofuran induced a marked concentration-dependent relaxation in rat ileum segments precontracted with KCl (EC50 = 0.059 ± 0.008 µg/mL) or carbachol (EC50 = 0.068 ± 0.007 µg/mL). These results suggest the possible decrease of calcium influx underlying the effects of menthofuran on the gastrointestinal tract, which opens the door for further study regarding this potential application for the treatment of gastrointestinal disorders, noting possible limitations of its use due to adverse effects in children.

Effects of consumption of mauritia flexuosa fruits on renal and hepatic functions in growing rats

INTRODUCTION: Previous studies have reported that buriti (Mauritia flexuosa L. f.) is a typical fruit from the Brazilian cerrado ecosystem and an important food source for low-income populations. Its composition is rich in carotenoid polyphenols, monounsaturated fatty acids, and ascorbic acid. However, studies on the biological effects resulting from the consumption of this fruit are scarce. OBJECTIVE: To evaluate the effects of a diet supplemented with buriti (Mauritia flexuosa L. f.) on kidney and liver functions in growing rats. METHODS: Determination of centesimal composition, carotenoids, and fatty acids content for buriti pulp, standard chow, and butiti-supplemented chow were performed. Then, Wistar rats of both sexes were fed a standard diet or supplemented with buriti pulp. Blood samples were collected at the end of the experiment to determine biochemical parameters. The unpaired t-test was applied, and differences were considered significant when p<0.05. RESULTS: A diet enriched with buriti pulp did not interfere with kidney function and most markers of liver function in animals. Alkaline phosphatase showed significantly higher plasma concentration in female rats, and albumin and uric acid showed lower concentrations in male rats in both experimental groups. CONCLUSION: The changes observed in biochemical markers did not provide evidence of adverse effects of buriti pulp supplementation on liver function. Thus, the intake of buriti pulp can be encouraged as it is a low-cost food source for the general population.

Inhibition of neutrophil migration and reduction of oxidative stress by ethyl p-coumarate in acute and chronic inflammatory models.

BACKGROUND: It is well known that medicinal plants and their products are relevant candidates for the treatment of inflammatory conditions. Ethyl p-coumarate is a phenylpropanoid that has similar structure to others anti-inflammatory and antioxidant substances. However, these activities have never been tested. PURPOSE: The aim of this study was to investigate the effect of ethyl p-coumarate on inflammatory and oxidative stress parameters. STUDY DESIGN: This is an experimental study to evaluate the anti-inflammatory and antioxidant activities of ethyl p-coumarate in acute and chronic models of inflammation. METHODS: The anti-inflammatory effect of ethyl p-coumarate was evaluated in Swiss mice by carrageenan-induced paw edema model (1%, 50 µl), followed by histological analysis, and edema induced by compound 48/80 (12 µg/paw), histamine (100  µg/paw), serotonin (100 µg/paw) and prostaglandin E2 (3 nmol/paw) in comparison to indomethacin treatment (10 mg/kg, p.o.). In addition, peritonitis was induced by carrageenan (500 µg/cavity) to neutrophil and total leukocytes counting, myeloperoxidase (MPO), interleukin 6 (IL-6) and 8 (IL-8), nitrite (NO2-), glutathione (GSH) and malondialdehyde (MDA) measurements. The arthritis model was induced with Freund's complete adjuvant (id. 0.1 ml) in female Wistar rats, with measurement of joint diameter and X-ray. Changes in gastric tissue of Swiss mice were analyzed in comparison to indomethacin (20  mg/kg, p.o.). RESULTS: After treatment with ethyl p-coumarate, the animals had no apparent toxic effects, and significantly inhibited paw edema induced by edematogenic agents, neutrophil (p < 0.001) and total leukocyte (p < 0.001) migration, MPO (p < 0.01), IL-6 (p < 0.05) and IL-8 (p < 0.5), MDA (p < 0.5), GSH (p < 0.5), NO2- (p < 0.001), joint thickness and bones changes. Furthermore, were not observed significant formation of gastric lesions. CONCLUSION: Taken together, these results suggest that ethyl p-coumarate exhibits anti-inflammatory activity through the inhibition of inflammatory mediators and leukocyte migration without causing gastric lesions.

Pharmaceutical development of tablets containing a spray-dried optimized extract from Lippia origanoides H. B. K.: influence of excipients and toxicological assessment

ABSTRACT Lippia origanoides is a honey shrub which has showed hypotensive potential assessed by in vivo studies. The aim of this work is the development of a pharmaceutical formulation composed by an optimized extract obtained from aerial parts of L. origanoides. The quantification of the naringenin marker in the dry extract and tablets developed was performed, as well as the assessment of the oral acute toxicity in rats. The hydroalcoholic extract of L. origanoides was spray-dried with the addition of colloidal silicon dioxide (Lo-HAE/CSD), and then applied in the preparation of eight different lots of tablets. The influence of the diluent (cellulose or babassu mesocarp), the presence of binder, and the percentage of lubricant, as well as organoleptic and physicochemical characteristics were screened. For the quantification of the marker content both in Lo-HAE/CSD and in the tablets, an analytical curve of the naringenin standard was fitted, and the samples were then analyzed in UFLC. The toxicological assessment was performed in female Wistar rats according to the Acute Toxic Class Method from OECD. The developed tablets produced meet acceptable macroscopic characteristics, and the presence of babassu as diluent provided improved physicochemical properties. The best content of Lo-HAE/CSD in the tablet (100.27%) was identified for the lot containing babassu, composed by 1.0% magnesium stearate, without PVP binder in its formulation. Moreover, Lo-HAE/CSD showed no signs of toxicity. Therefore, the babassu mesocarp powder is a promising pharmaceutical excipient for the development of herbal tablets containing the Lippia origanoides extract.

Hepatic function and antioxidant activity in diabetic rats subjected to diet supplemented with multimixture / Función hepática y actividad antioxidante en ratas diabéticas con dieta suplementada con multimezcla

Introduction: Food and dietetic components have received considerable attention as auxiliary feeding resources on controlling of chronic non-transmissible diseases, among them diabetes. This study evaluated the effect of supplementary diet with multimixture based on linseed, sesame, oats and sunflower seeds on the hepatic function and antioxidant activity of diabetic rats. Methods: Male rats were distributed on groups of seven animals: diabetic control (DC), diabetics subject to multimixture diet (DM), diabetic with insulin (DI), and normal control (NC). The treatment was started on the 5th day after diabetes induction with 40 mg/kg i.v. streptozotocin on tampon citrate and kept during 50 days. Results: The ethereal extract of the supplemented diet showed a higher content of phenolics (p < 0.05) compared to other extracts of the supplemented diet and the ethereal extract of the standard diet. There was no difference in antioxidant in vitro activity of the utilized diets. Concerning to transaminases, signifi cant bigger ALT levels (p < 0.05) were present on diabetic groups compared to NC. The relative liver weight on diabetic groups was significantly higher (p < 0.001) compared to NC group. Non-proteic sulfhydryl group levels were significantly higher (p < 0.05) on DM and I groups when compared to DM and NC. Only the treatment with insulin resulted in an improvement of antioxidant activity concerning to hepatic catalase. The supplementation with multimixture did not improve the metabolic control of diabetes. Conclusion: The multimixture treatment showed an isolated improvement on antioxidant activity in the hepatic tissue, evidenced by the increasing on non-proteic sulfhydryl group levels (AU)

Introducción: alimentos y componentes de la dieta han recibido considerable atención como recursos auxiliares en el control de las enfermedades crónicas, como la diabetes. Este estudio evaluó el efecto de la dieta suplementada con base de linaza multimezcla, sésamo, avena y semillas de girasol en la función hepática y la actividad antioxidante de ratas diabéticas. Métodos: las ratas macho fueron divididas en grupos de siete animales: control de la diabetes (CD), diabéticos sometidos a dieta multimezcla (DM), diabéticos con insulina (DI), y control normal (CN). El tratamiento se inició en el quinto día después de la inducción de la diabetes con estreptozotocina 40 mg/kg i.v. en tampón citrato y se mantuvo durante 50 días. Resultados: la dieta extracto etéreo complementado tenía el contenido fenólico más alto (p < 0,05) que los otros extractos de la suplementación de la dieta y el extracto de éter de la comida estándar. No hubo diferencia en la actividad antioxidante in vitro de la alimentación usada. A medida que las transaminasas, los niveles de ALT significativamente mayor (p < 0,05) estuvieron presentes en el grupo de diabéticos en comparación con CN, el peso relativo del hígado en el grupo de diabéticos fue significativamente mayor (p < 0,001) en comparación con el grupo CN. Los grupos sulfhidrilo de los niveles de proteína no fueron significativamente mayores (p < 0,05) en los grupos F e I comparados con CN y CD. El tratamiento con insulina resultó en una mejora de la actividad antioxidante con respecto a la catalasa hepática. Conclusión: la suplementación con multimezcla no mejora el control metabólico de la diabetes. El tratamiento con multimezcla aislado mostró una mejora en la actividad antioxidante en el tejido hepático, como se evidencia por el aumento de los niveles de grupos sulfhidrilo no proteicos (AU)

Ferulic acid ethyl ester diminished Complete Freund's Adjuvant-induced incapacitation through antioxidant and anti-inflammatory activity.

Ferulic acid ethyl ester (FAEE) is a derivate from ferulic acid which reportedly has antioxidant effect; however, its role on inflammation was unknown. In this study, we investigated the orally administered FAEE anti-inflammatory activity on experimental inflammation models and Complete Freund's Adjuvant (CFA)-induced arthritis in rats. CFA-induced arthritis has been evaluated by incapacitation model and radiographic knee joint records at different observation time. FAEE (po) reduced carrageenan-induced paw edema (p < 0.001) within the 1st to 5th hours at 50 and 100 mg/kg doses. FAEE 50 and 100 mg/kg, po inhibited leukocyte migration into air pouch model (p < 0.001), and myeloperoxidase, superoxide dismutase, and catalase activities (p < 0.001) increased total thiol concentration and decreased the TNF-α and IL-1ß concentrations, NO, and thiobarbituric acid reactive species. In the CFA-induced arthritis, FAEE 50 and 100 mg/kg significantly reduced the edema and the elevation paw time, a joint disability parameter, since second hour after arthritis induction (p < 0.001). FAEE presented rat joint protective activity in radiographic records (p < 0.001). The data suggest that the FAEE exerts anti-inflammatory activity by inhibiting leukocyte migration, oxidative stress reduction, and pro-inflammatory cytokines.

Chest and neck mobilization effects on spirometric responses in healthy subjects.

OBJECTIVES: In this observational study, we evaluated the effects of chest and neck mobilization on spirometric parameters in healthy subjects. METHODS: We conducted an observational, quantitative, and experimental study in a sample of 100 healthy subjects. We evaluated spirometric parameters before and after pompage mobilization techniques. Three techniques were used, and each technique was performed 6 times. RESULTS: Forced vital capacity (3.4 ± 0.1 L vs 3.5 ± 0.1 L), forced expiratory volume at the first second (3.2 ± 0.09 L vs 3.3 ± 0.09 L), and peak expiratory flow (6.4 ± 0.27 L/s vs 6.6 ± 0.25 L/s) were significantly increased after mobilization (P < .0001), whereas Tiffeneau index (94% ± 1% vs 6% ± 0.2%) was decreased (P < .0001). CONCLUSION: Chest and neck mobilization techniques used in this study improved spirometric parameters in a group of young and healthy subjects.