Lupinus mutabilis Extract Exerts an Anti-Diabetic Effect by Improving Insulin Release in Type 2 Diabetic Goto-Kakizaki Rats.

Lupinus mutabilis (LM) is a legume part of Bolivian traditional diet that has a nutraceutical property reducing blood glucose levels. The prevalence of type 2 diabetes is increasing worldwide thus; the search for novel anti-diabetic drugs is needed. Based on its traditional use, we evaluated the anti-diabetic effect of LM in the spontaneously diabetic Goto-Kakizaki (GK) rat, a model of type 2 diabetes and in Wistar (W) rats as healthy control. LM seeds hydroethanolic extract, analyzed by gas chromatography-mass spectrometry and high-performance liquid chromatography-high resolution mass spectrometry, is a complex mixture of volatile and non-volatile components. A single oral administration of LM extract (2000 mg/kg b.w.) improved glucose tolerance during the oral glucose tolerance test (OGTT) (30⁻120 min) in GK and W rats (p < 0.0001). The long-term treatment with LM (1000 mg/kg b.w.), for 21 days, improved the area under the curve (AUC) of glucose during OGTT at day 20, in both GK (p < 0.01) and W rats (p < 0.01). The HbA1c (GK rats, p < 0.05 and W rats, p < 0.0001) and the non-fasting glucose (GK rats, p < 0.05) were also reduced. LM increased both serum insulin levels (2.4-fold in GK rats and 2.5-fold W rats), and the glucose-induced (16.7 mM glucose) insulin release in isolated islets from treated animals (6.7-fold in GK rats, and 6.6-fold in W rats). Moreover, LM (10 mg/mL) stimulated in vitro glucose induced (16.7 mM glucose) insulin release in batch incubated GK and W rat islets (p < 0.0001). In perifused GK rat islets, insulin release in 16.7 mM glucose was increased 95.3-fold compared to untreated islets (p < 0.0001), while no significant differences were found in perifused W rat islets. The LM mechanism of action, evaluated using inhibitory compounds of the insulin secretion pathway, showed that LM-dependent insulin secretion was reduced 42% by diazoxide (p < 0.001), 70% by nifedipine (p < 0.001), 86.7% by H89 (p < 0.0001), 70.8% by calphostine-C (p < 0.0001) and 93% by pertussis toxin (p < 0.0001). A similar effect was observed in W rats islets. Our findings provide evidence that LM has an anti-diabetic effect through stimulation of insulin release. The effect is-dependent on L-type calcium channel, protein kinase A and C systems, and G protein-coupled exocytosis and is partially mediated by K-ATP channels.

Amaranthus caudatus Stimulates Insulin Secretion in Goto-Kakizaki Rats, a Model of Diabetes Mellitus Type 2.

Diabetes Mellitus Type 2 prevalence is increasing worldwide; thus efforts to develop novel therapeutic strategies are required. Amaranthus caudatus (AC) is a pseudo-cereal with reported anti-diabetic effects that is usually consumed in food preparations in Bolivia. This study evaluated the anti-diabetic nutraceutical property of an AC hydroethanolic extract that contains mainly sugars and traces of polyphenols and amino acids (as shown by nalysis with liquid chromatography-mass spectrometry (LC-MS) and nuclear magnetic resonance (NMR)), in type 2 diabetic Goto-Kakizaki (GK) rats and healthy Wistar (W) rats. A single oral administration of AC extract (2000 mg/kg body weight) improved glucose tolerance during Oral Glucose Tolerance Tests (OGTT) in both GK rats and in W rats. Long-term treatment (21 days) with AC (1000 mg/kg b.w.) improved the glucose tolerance evaluated by the area under the curve (AUC) of glucose levels during the OGTT, in both GK and W rats. The HbA1c levels were reduced in both GK (19.83%) and W rats (10.7%). This effect was secondary to an increase in serum insulin levels in both GK and W rats and confirmed in pancreatic islets, isolated from treated animals, where the chronic AC exposure increased the insulin production 4.1-fold in GK and 3.7-fold in W rat islets. Furthermore, the effect of AC on in vitro glucose-dependent insulin secretion (16.7 mM glucose) was concentration-dependent up to 50 mg/mL, with 8.5-fold increase in GK and 5.7-fold in W rat islets, and the insulin secretion in perifused GK and W rat islets increased 31 and nine times, respectively. The mechanism of action of AC on insulin secretion was shown to involve calcium, PKA and PKC activation, and G-protein coupled-exocytosis since the AC effect was reduced 38% by nifedipine (L-type channel inhibitor), 77% by H89 (PKA inhibitor), 79% by Calphostine-C (PKC inhibitor) and 20% by pertussis toxin (G-protein suppressor).

Extract of Clinopodium bolivianum protects against E. coli invasion of uroepithelial cells.

ETHNOPHARMACOLOGICAL RELEVANCE: Clinopodium bolivianum is a South American plant with anti-inflammatory and anti-infective activities. The increasing antibiotic resistance urges for alternative therapy. Based on its use in traditional medicine, we investigated the effect of C. bolivianum on the ability to defend bladder epithelial cells from E. coli infection. MATERIALS AND METHODS: The extract was analyzed by LC-MS. Bladder epithelial cell lines T24 and 5637 and uropathogenic E. coli No. 12, its isogenic mutant WE16 csgBA bscA::Cm and CFT073 were used to investigate the effect of C. bolivianum on uroepithelial infection. Bacterial adherence and invasion to cells treated with C. bolivianum were analyzed. Expression of uroplakin 1a, ß1 integrin, caveolin-1, IL-8 and antimicrobial peptides in response to C. bolivianum treatment was assessed using RT-PCR. Protein expression was confirmed by Western blot analysis or ELISA. The antimicrobial effects of C. bolivianum on bacteria and fungus were investigated using minimum inhibitory concentration. Furthermore, the formation of biofilm was investigated with crystal violet assay. RESULTS: C. bolivianum extract consisted of more than 70 different types of phytochemicals including sugars and phenolic compounds. The extract decreased the uroplakin 1a expression and E. coli adhesion and invasion of uroepithelial cells while up-regulated caveolin-1. In uninfected C. bolivianum treated cells, IL-8 was lower than in non-treated cells. In infected cells, however, no difference was observed between treated and non-treated cells. Further, C. bolivianum treatment reduced uropathogenic E. coli (UPEC) biofilms but did not inhibit bacterial growth. CONCLUSIONS: Our results show that C. bolivianum has a protective role on bladder epithelial cells against UPEC infection by decreasing the bacterial adhesion, invasion and biofilm formation.

Condições sanitárias das águas de piscinas públicas e particulares / Sanitary conditions of water from publics and privates swimming pools

As piscinas representam locais de recreação, porém podem colocar em risco a saúde dos usuários pela possibilidade de veicular agentes danosos. A norma técnica do Estado de São Paulo para o controle de qualidade das águas de piscina entrou em vigor em 1979, e requer revisão. Este trabalho avaliou as condições sanitárias das águas de piscinas do Município de Praia Grande/SP. Foram coletadas quatro amostras semanais por estabelecimento, sendo duas piscinas públicas e seis particulares, totalizando-se 32 amostras. Os exames microbiológicos foram realizados segundo a APHA, 2005, para coliformes totais, Escherichia coli, Enterococos, Pseudomonas aeruginosa, Staphylococcus aureus, bolores e leveduras. As análises físico-químicas de turbidez, cloreto, nitrato, nitrito, cor, condutividade, ferro, sulfato, dureza total, odor, temperatura, pH e cloro residual livre foram efetuadas, de acordo com a ANVISA/MS, 2005. Apenas duas amostras estavam de acordo com a legislação e 30 mostraram não conformidade, quanto aos parâmetros estabelecidos (cloro residual livre e pH). Houve presença de coliformes totais, Pseudomonas aeruginosa e Staphylococcus aureus, não previstos na norma. Além da necessidade de controle permanente da qualidade das águas de piscinas localizadas no mencionado município, esses achados oferecem subsídios para efetuar atualização da legislação em vigor no Estado de São Paulo.

This study aimed to assess the health conditions of water from public and private swimming pools locatedin Praia Grande, São Paulo State, Brazil, regarding the microbiological control and physical-chemicalcharacteristics. Four samples were collected weekly from each site, being two public swimming pools andsix private ones (sports academies), and a total of 32 samples were analyzed. The microbiological tests wereperformed according to APHA, 2005, for coliforms, Escherichia coli, Enterococos, Pseudomonas aeruginosa,Staphylococcus aureus, yeasts and molds. The physical and chemical analyses were carried out using themethodology described by ANVISA/MS, 2005. Turbidity, chloride, nitrate, nitrite, color, conductivity, iron,sulfate, total hardness and smell were determined; in the field, temperature, pH and free residual chlorinewere measured. Only two samples were approved, and 30 were in disagreement in the restricted free residualchlorine and pH parameters, and also coliforms group, Pseudomonas aeruginosa and Staphylococcus aureuswere isolated, which are not included in the specific legislation. A permanent control of water quality ofswimming pools located in the municipality should be monitored, as well as a review on the São PauloState legislation in force is required, and also the inclusion of new parameters.

An antibody against RANKL for the treatment of osteoporosis, inflammatory and malignant bone diseases.

Over the years, the importance of receptor activator of nuclear factor κB ligand (RANKL) in bone physiology and pathophysiology has been thoroughly documented. Denosumab, also known as AMG 162, is a fully human monoclonal antibody against RANKL which is being studied in the treatment of metabolic, inflammatory, and malignant bone diseases. The purpose of this review is to analyze the potential role of denosumab in osteoporosis, rheumatoid arthritis, bone metastases and multiple myeloma.

Screening of South American plants against human immunodeficiency virus: preliminary fractionation of aqueous extract from Baccharis trinervis.

Ethanolic and aqueous extracts of 14 South American medicinal plants were tested for inhibitory activity on human immunodeficiency virus (HIV). Both extracts were relatively non-toxic to human lymphocytic MT-2 cells, but only the aqueous extract of Baccharis trinervis exhibited potent anti-HIV activity in an in vitro MTT assay. To delineate the extract-sensitive phase, some studies of the antiviral properties of the active extract are described in this paper. Based on the results presented here, a separation scheme was devised, which permitted the preliminary fractionation of the extract, with the aim of finding an inhibitor of this virus.

Exame microscópico-comparativo das espécies popularmente designadas "cana-do-brejo" / Identification of the species popularly known as \"cana-do-brejo\"

Säo comparadas as principais características morfológicas e estruturais de três espécies da família Zingiberaceae empregadas medicinalmente sob a denominaçäo coletiva de "cana-do-brejo": Costus spiralis (Jacquim) Roscoe. Costus arabicus L. e Hedychium coronarium Koening. Säo de importância diganóstica os detalhes referentes à inserçäo das folhas, espessura das lígulas, estrutura do mesofilo, inclusöes celulares, anexos epidérmicos e espessamento de estrias de Caspary. Empregou-se microscopia ótica neste estudo.

Contribución al estudio de la plumbagina determinación de la dosis letal media / Contribution to the study of plumbagina lethal average dosis

La plumbagina utilizada en la experiencia fue aislada de la Pera benesis (EUPHORBIACEAE), compuesto que ha revelado presentar actividad antibacteriana, antimicótica, pesticida y contra la leishmaniasis. Los resultadosobtenidos de DL-50 a través del Método de Reed Muench y Spearman Karber fueron de 7,9 y 6,15 mg/Kg de peso corporal respectivamente, y 4,94 a 7,65 como límites de confianza, reportándose a la plumbagina como un compuesto tóxico

Estudio de la microflora intestinal en niños con diarrea aguda y persistente / Study of the intestinal microflora in children with acute diarrhea

En ocasiones la etiología de la diarrea persistente no puede ser identificada y su mecanismo de producción es complejo y no bien aclarado, por lo que se hace necesario conocer el estado de la flora entérica del intestino delgado para definir si la alteración de éste constituye un factor para la prolongación de la diarrea. Se estudian 30 niños con diarrea aguda y 30 con diarrea persistente menores de un año de edad, en el que se toma una muestra de contenido duodenal a través de una sonda de doble lumen radiopaca, procesándose microbiológicamente por métodos de siembra cuantitativa para la búsqueda de los microorganismos entéricos, anaeróbicos, así como miembros del género Cándida y correlacionándose dichos resultados microbiológicos de las heces. La presencia del sobrecrecimiento bacteriano y la identificación de enterobacterias en la microflora duodenal, es una factor importante a considerar en la persistencia de la diarrea. Se constató la alteración en la flora duodenal cualitativa y cuantitativamente en ambos grupos de estudio

Actividad anti-inflamatoria y antiulcerosa de la tusca(Acasia macracantha) / Antiinflammatory and antiulcer of the tusca (Acasia Macracantha)

La determinación de los efectos se realizó en la clasificada en el Herbario Nacional (Lic.Rossi de Michel) Acasía macracantha Willd (tusca), planta medicinal utilizada popularmente en la región de Tarija, para el tratamiento de afecciones a nivel de la mucosa gástrica. El efecto anti-inflamatoriofue determinado en ratones previamente tratados con el extracto acuoso(E.A.Ig/Kg.v.o) produciendo la reducción del edema de pata inducido por la carragenina en un 25 por ciento frente al 32.1 por ciento del observado por la indometacina(10 mg/Kg.v.o.). El efecto antiulceroso fue del 60 por ciento determinado en ratones previamente tratados con el extracto acuoso en base a la metodología descrita por Macaubas y col(1988), los resultados indican que la tusca puede presentar un gran potencial terapéutico para el tratamiento de afecciones anti-inflamatorias sin presentar efectos colaterales a nivel de la mucosa gástrica

Estandarización de un modelo biológico in vivo para la detección de actividad cicatrizante de extractos vegetales / Standarization of a in vivo biologic model for the detection of reading activity of vegetal extracts

Con el objeto de evaluar las propiedades biológicas de las plantas medicinales de nuestra región es que el Instituto de Investigaciones Farmacia-Bioquímicas, ha emprendido la estandarización de modelos biológicos parala determinación de actividades en extractos vegetales. Una de ellas es la referida a la actividad cicatrizante, la cual es de interés por el limitado número demedicamentos y su elevado costo que ellos presentan en el mercado