Spray dried extract of Calophyllum brasiliense Cambés produces a potent hypoglycemic effect and improves total serum cholesterol and triglycerides in diabetic rats / El extracto secado por pulverización de Calophyllum brasiliense cambés produce un potente efecto hipoglucémico y mejora el colesterol sérico total y los triglicéridos en ratas diabéticas / O extrato seco por aspersão de Calophyllum brasiliense Cambés produz um potente efeito hipoglicemiante e melhora o colesterol total e triglicérideos em ratos diabéticos

SUMMARY Introduction: The species Calophyllum brasiliense Cambés (Calophyllaceae) is widespread throughout Central and South America. The stem bark infusion is used for lowering blood glucose. Aim: To optimize the spray dry extract ofthis plant using a D-optimal experimental design. Materials and methods: As factors were used the air-drying speed (3.5-4.5 m3/h), the feed flow rate of the suspension (5-11 mL/ min), and the inlet air temperature (90-130 °C). The dried extract was characterized by measuring the phenolics and flavonoids content, moisture, the water activity, apparent densities, flowability, and compressibility. The antioxidant activity, the inhibitory activity of lipase and alpha-glycosidase, and the antiglycant activity of the spray dried extract (SDE) were evaluated. Subsequently, the hypoglycemic activity was evaluated in rats by monitoring the blood glucose level, triglycerides, and cholesterol. Results: Inlet air temperature and feed flow rate were the factors that most affected the yield and phenolic content. SDE showed a potent antioxidant effect (IC50 1.83 μg/mL), a potent a-glycosidase (IC50 74.45 μg/mL) and pancreatic lipase (IC50 27.33 μg/mL) inhibition. A potent antiglycation effect (IC50 9.45^g/mL) was also observed. Conclusion: the SDE showed a potent hypoglycemic effect at 100 mg/kg. These results suggest that SDE could activate four important pathways that can contribute to diabetes control.

Resumen Introducción: la especie Calophyllum brasiliense (Calophyllaceae) está muy extendida en Centro y Suramérica. La infusión del tronco reduce los niveles de glucosa en sangre. bjetivo: optimizar el extracto seco por aspersión (SDE) de esta planta utilizando un diseño experimental D-óptimal. Materiales y métodos: como factores se utilizaron la velocidad del gas secante (aire, 3,5-4,5 m3/h), la temperatura de entrada del aire fue 90-130 °C y la velocidad de alimentación, 5-11 mL/min. Se determinó el contenido de fenoles y flavonoides en el extracto seco, la humedad residual, la actividad del agua, las densidades aparentes, fluidez y compresibilidad. Se evaluó la actividad antioxidante e inhibidora de lipasa y alfa-glicosidasa y la actividad antiglicante. También se evaluó la actividad hipoglicemiante midiendo glucosa en sangre, triglicéridos y colesterol. Resultados: la temperatura del aire de entrada y la velocidad de alimentación afectaron, significativamente, el rendimiento y contenido de fenoles. El SDE mostró un potente efecto antioxidante (IC50 1,83 μg/mL), una potente inhibición de a-glicosidasa (IC50 74,45 μg/mL) y de lipasa pancreática (IC50 27,33 μg/ mL). Se observó un fuerte efecto antiglicante (IC50 9,45 μg/mL). Conclusiones: el SDE mostró un potente efecto hipoglicemiante a 100 mg/kg. Estos resultados sugieren que el SDE podría actuar activando cuatro vías importantes para el control de la diabetes.

RESUMO Introdução: a espécie Calophyllum brasiliense (Calophyllaceae) é amplamente distribuída na América do Sul e Central. A infusão da casca do caule reduz os níveis de glicose no sangue. Objetivo: otimizar o extrato seco por pulverização (SDE) desta planta usando um planejamento experimental D-ótimo. Materiais e métodos: a velocidade do gás de secagem ar (3,5-4,5 m3/h), a temperatura de entrada do ar (90-130 °C) e a taxa de alimentação (5-11 mL/min) foram usados como fatores. Foi determinado o teor de fenóis e flavonóides no extrato seco, a umidade residual, a atividade de água, as densidades aparentes, a fluidez e a compressibilidade. Avaliou-se a atividade antioxidante e a atividade inibitória de lipase e alfa-glicosidase, e a atividade antiglicante do extrato seco. A atividade hipoglicêmica foi avaliada em ratos diabeticos, medindo a glicose no sangue, triglicerídeos e colesterol. Resultados: a temperatura de entrada do ar e a taxa de alimentação afetaram significativamente o desempenho e o conteúdo de fenois. O SDE mostrou um potente efeito antioxidante (IC50 1,83 μg/mL), uma significativa inibição de a-glicosidase (IC50 74,45 ig/mL) e da lipase pancreática (IC50 27,33 μg/mL). Um forte efeito antiglicante também foi observado (IC50 9,45 μg/mL). O SDE mostrou um forte efeito hipogli-cemiente à concentração de 100 mg/kg. Conclusões: Esses resultados sugerem que o SDE poderia atuar ativando quatro vias importantes para o controle do diabetes.

Cnidoscolus aconitifolius: therapeutic use and phytochemical properties. Literature review / Cnidoscolus aconitifolius: usos terapéuticos y propiedades fitoquímicas. Revisión de la literatura

Abstract Introduction: Medicinal plants have been traditionally used to cure or alleviate infectious and non-infectious diseases. They are widely accepted due to their low cost and low toxicity indexes. These plants are frequently used in cases involving skin irritation, superficial wounds, insect bites, and snake bites. Objective: To compile available evidence on the main therapeutic uses and phytochemical components of Cnidoscolus aconitifolius (popularly known as chaya), a plant that grows in tropical regions of Mexico and Central America. Materials and methods: A literature review of studies on C. aconitifolius published until 2017 was conducted in the BIREME, PubMed/Medline, Elsevier and SciELO databases. Descriptors "Cnidoscolus" and "aconitifolius" were used for the literature search, and no language restrictions were applied. Results: 82 articles were retrieved after completing the initial search. Once the studies were filtered by title (descriptors in the title) and duplicates were removed, 18 articles were reviewed. Based on the information found, it was possible to confirm that this plant has multiple health benefits. Conclusions: The traditional therapeutic use of Cnidoscolus aconitifolius is backed by scientific evidence. Therefore, further research aimed at identifying new phytochemical properties of this plant should be conducted to establish alternative therapies for treating different conditions.

Resumen Introducción. El uso tradicional de plantas medicinales para tratar diferentes enfermedades, ya sean infecciosas o no, es ampliamente aceptado debido a su bajo costo y sus bajos índices de toxicidad. Estas plantas son frecuentemente usadas en casos que involucran irritaciones de la piel, heridas superficiales, picaduras de insectos y mordeduras de víboras. Objetivo. Recopilar la información disponible sobre los principales usos terapéuticos y los componentes fitoquímicos de Cnidoscolus aconitifolius, una planta conocida popularmente como chaya y que crece en regiones tropicales de México y Centroamérica. Materiales y métodos. Se realizó una revisión de la literatura sobre C. aconitifolius publicada hasta 2017 en las bases de datos BIREME, PubMed/Medline, Elsevier y SciELO. Para la búsqueda se emplearon los descriptores "Cnidoscolus" y "aconitifolius", y no se aplicaron filtros de idioma. Resultados. Se identificaron 82 artículos luego de completar la búsqueda inicial. Después de filtrar los estudios por título (presencia de descriptores de búsqueda en el título) y remover duplicados, se incluyeron 18 artículos en la revisión. De acuerdo a la información encontrada, fue posible confirmar que esta planta ofrece diversos beneficios para la salud. Conclusiones. El uso terapéutico tradicional de la chaya está sustentado por evidencia científica, por lo que se sugiere realizar más investigaciones centradas en la identificación de nuevas propiedades fitoquímicas de esta planta y, así, establecer alternativas terapéuticas para distintas afecciones.

Hypoglycemic effect of formulation containing hydroethanolic extract of Calophyllum brasiliense in diabetic rats induced by streptozotocin

ABSTRACT Diabetes mellitus is a chronic and severe metabolic dysfunction, it's slow and progressive evolution interferes directly in the metabolism of carbohydrates, fats and proteins, causing hyperglycemia, glycosuria, polydipsia, hyperlipidaemia, among others. The aim of this study was to evaluate the antidiabetic effect of hydroethanolic extract and granulated of Calophyllum brasiliense Cambess., Clusiaceae, species in diabetic rats as well as it's biochemical parameters. The results demonstrated that both the pharmaceutical forms, hydroethanolic extract and granulated, were able to reduce significantly (p < 0.001) hyperglycemia and glycosuria, in addition to improve polydipsia, polyuria, and weight loss. Treatments using hydroethanolic extract and granulated were also able to reduce significantly levels of triacylglycerides, cholesterol and low-density lipoprotein, as well as the transaminases, urea and creatinine levels. Therefore, it is concluded that these pharmaceutical forms have anti-diabetic effect and act improving the biochemical parameters, this effect is probably due to the high content of polyphenolic compounds found in the formulations.

Toxicidad aguda oral e irritabilidad de la mucosa oral con una formulación de tabletas de Tamarindus indica L / Acute oral toxicity and irritability of the oral mucosa with a tablet formulation of Tamarindus indica L

In this study, the possible preclinical toxic effects of the Tamarindus indica L tablets were evaluated by the acute oral toxicity (AOT) and oral mucosa irritation (OMI), adapting guideline OECD 423 and ISO 10993-10, respectively. The AOT was evaluated, using the Class Toxocity Method in Sprague Dawley females rats and the OMI was assessed in sirian hamsters, according to the acute exposure method. Any sign of toxicity were not observed in the study. No animal death was occurring and the body weight increase in the two experimental groups was not statistically different. Slight irritation of the oral mucosa of the animals was observed, but this fact didn't impede them to feed appropriately and they body weight increase normally during the assay. Tamarind tablets were framed as non toxic substance and they produce a “light irritability” of the oral mucosa.

En este trabajo se evaluó a nivel preclínico, los posibles efectos tóxicos de las tabletas de Tamarindus indica L. Se ensayó la toxicidad aguda oral, por el método de las clases de toxicidad, en ratas hembras de la línea Sprague Dawley y la irritabilidad de la mucosa oral en Hamster sirio, según las normas OECD 423 y ISO 10993-10, respectivamente. Durante el estudio de toxicidad aguda, no se observaron signos de toxicidad, ni muerte. El peso corporal en ambos grupos experimentales aumentó y no fue diferente estadísticamente. En el estudio de irritabilidad, se observó una ligera irritación en la mucosa de los biomodelos. Esto no les impidió alimentarse adecuadamente y se observó un incremento del peso corporal de ambos grupos experimentales. Se determinó que las tabletas producen una irritabilidad “leve” de la mucosa oral y no clasifican como tóxicas según las normas internacionales de referencia.