Anti-Diabetic Activity of Glycyrrhetinic Acid Derivatives FC-114 and FC-122: Scale-Up, In Silico, In Vitro, and In Vivo Studies.

Type 2 diabetes (T2D) is one of the most common diseases and the 8th leading cause of death worldwide. Individuals with T2D are at risk for several health complications that reduce their life expectancy and quality of life. Although several drugs for treating T2D are currently available, many of them have reported side effects ranging from mild to severe. In this work, we present the synthesis in a gram-scale as well as the in silico and in vitro activity of two semisynthetic glycyrrhetinic acid (GA) derivatives (namely FC-114 and FC-122) against Protein Tyrosine Phosphatase 1B (PTP1B) and α-glucosidase enzymes. Furthermore, the in vitro cytotoxicity assay on Human Foreskin fibroblast and the in vivo acute oral toxicity was also conducted. The anti-diabetic activity was determined in streptozotocin-induced diabetic rats after oral administration with FC-114 or FC-122. Results showed that both GA derivatives have potent PTP1B inhibitory activity being FC-122, a dual PTP1B/α-glucosidase inhibitor that could increase insulin sensitivity and reduce intestinal glucose absorption. Molecular docking, molecular dynamics, and enzymatic kinetics studies revealed the inhibition mechanism of FC-122 against α-glucosidase. Both GA derivatives were safe and showed better anti-diabetic activity in vivo than the reference drug acarbose. Moreover, FC-114 improves insulin levels while decreasing LDL and total cholesterol levels without decreasing HDL cholesterol.

Green Synthesis of Magnetic Nanoparticles of Iron Oxide Using Aqueous Extracts of Lemon Peel Waste and Its Application in Anti-Corrosive Coatings.

Lately, the development of green chemistry methods with high efficiency for metal nanoparticle synthesis has become a primary focus among researchers. The main goal is to find an eco-friendly technique for the production of nanoparticles. Ferro- and ferrimagnetic materials such as magnetite (Fe3O4) exhibit superparamagnetic behavior at a nanometric scale. Magnetic nanoparticles have been gaining increasing interest in nanoscience and nanotechnology. This interest is attributed to their physicochemical properties, particle size, and low toxicity. The present work aims to synthesize magnetite nanoparticles in a single step using extracts of green lemon Citrus Aurantifolia residues. The results produced nanoparticles of smaller size using a method that is friendlier to health and the environment, is more profitable, and can be applied in anticorrosive coatings. The green synthesis was carried out by a co-precipitation method under variable temperature conditions. The X-ray Diffraction (XRD) and Transmission Electron Microscopy (TEM) characterization showed that magnetite nanoparticles were successfully obtained with a very narrow particle size distribution between 3 and 10 nm. A composite was produced with the nanoparticles and graphene to be used as a surface coating on steel. In addition, the coating's anticorrosive behavior was evaluated through electrochemical techniques. The surface coating obtained showed good anticorrosive properties and resistance to abrasion.

Eco-Friendly Reduction of Graphene Oxide by Aqueous Extracts for Photocatalysis Applications.

In the present work, reduced graphene oxide was obtained by green synthesis, using extracts of Larrea tridentata (gobernadora) and Capsicum Chinense (habanero). Graphene oxide was synthesized by the modified Hummers' method and subsequently reduced using natural extracts to obtain a stable and environmentally friendly graphene precursor. Consequently, the gobernadora aqueous extract was found to have a better reducing power than the habanero aqueous extract. This opportunity for green synthesis allows the application of RGO in photocatalysis for the degradation of the methylene blue dye. Degradation efficiencies of 60% and 90% were obtained with these materials.

[Predictive ability of baseline frailty and handgrip strength at admission on outcomes at discharge in a geriatric functional recovery unit]. / Capacidad predictiva de fragilidad basal y fuerza de prensión al ingreso en resultados al alta en una unidad geriátrica de recuperación funcional.

OBJECTIVE: To evaluate the predictive capacity of different frailty scales, as well as the strength of the handgrip, and to determine their relationship with clinical favourable outcomes. PATIENTS AND METHOD: Prospective study of patients admitted to the Geriatric Functional Recovery Unit (GFRU) of the Hospital Central Cruz Roja. The «FRAIL¼ scale, «Clinical Frailty Scale¼ (CFS) and «Fragil-VIG¼ index, and handgrip strength by hydraulic dynamometer were completed on admission. A functional gain was assumed as 20 or more points in the Barthel Index and return to home, as good outcomes at discharge. The discriminative capacity of favourable outcomes for each frailty scale and handgrip strength was analysed by means of ROC curves, calculating the C statistic (area under the curve = AUC). RESULTS: The analysis included 74 patients (median age 82 years; 48.5% women), admitted for stroke recovery (65%), orthopaedic pathology (16%), and other causes (19%). The prevalence of frailty varied between 31% (FRAIL scale), 40% (CFS), and 57.5% («Fragil-VIG¼). Median handgrip strength was 15 Kg in males (interquartile range 11-21), and 9 Kg in females (interquartile range 7-12). At discharge, 51.5% of patients had a functional gain of 20 or more points in Barthel index, and 63% returned to their previous home. The discriminating ability to achieve acceptable functional gain at discharge was good for CFS (AUC = 0.72; 95% CI; 0.60-0.84) and «Fragil-VIG¼ (AUC = 0.72; 95% CI;0.58-0.82), and handgrip strength was the only tool related to return home (AUC = 0.68; 95% CI;0.56-0.81). CONCLUSION: To evaluate frailty on admission to a GFRU contributes to predicting favourable clinical outcomes, but the discriminating capacity of each scale is variable.

La prueba de la marcha de 6 minutos como factor pronóstico y de capacidad de ejercicio en pacientes con silicosis / The 6-Minute Walk Test as a Tool for Determining Exercise Capacity and Prognosis in Patients with Silicosis

Objetivo: Evaluar la capacidad de ejercicio, utilizando la prueba de la marcha de 6 minutos (6MWT), en pacientes con silicosis complicada, e identificar factores relacionados con dicho resultado, así como su valor pronóstico de hospitalización y mortalidad. Método: Estudio observacional prospectivo en 143 pacientes diagnosticados de silicosis complicada atendidos en consulta de neumología desde 2009 hasta diciembre 2016, sin limitación para hacer la 6MWT. Se evaluaron las pruebas de función pulmonar, los hallazgos de la tomografía computarizada y los parámetros de la 6MWT (distancia caminada y desaturación de oxígeno). Resultados: Los pacientes con silicosis complicada caminaban una media de 387 ± 92m. Los resultados fueron peores al aumentar la gravedad de la enfermedad; en silicosis A: 407 ± 97; B: 370 ± 88, y C: 357 ± 68 (p=0,022). La 6MWT mostraba una correlación positiva con la función pulmonar e inversa con la disnea (p < 0,001). Los pacientes con enfisema moderado/severo y un mayor tiempo con saturación nocturna de oxígeno por debajo del 90% presentaban resultados significativamente peores en la 6MWT. Los pacientes que caminaban < 350 m tenían más hospitalizaciones (3,7 ± 4,0) que los que caminaban>350 (1,1 ± 2,9). Los fallecidos al final del seguimiento caminaron 327,9 ± 73,0 frente a los que sobreviven, que caminaron 404,5 ± 89,7 m (p < 0,001). Conclusiones: Los valores de la espirometría y la categoría de la silicosis se relacionan con el resultado de la 6MWT, que resultó ser factor pronóstico para hospitalización y mortalidad. La 6MWT se perfila como una herramienta útil en salud ocupacional para el seguimiento de pacientes con silicosis

Objective: To evaluate exercise capacity using the 6-minute walk test (6MWT) in patients with complicated silicosis, and to determine how results shape the prognostic value of 6MWT for hospitalization and mortality. Method: Prospective observational study in 143 patients with complicated silicosis who performed the 6MWT in our outpatient pulmonology clinic between 2009 and the end of 2016. Lung function tests, computed tomography findings and 6MWT parameters (distance walked and oxygen desaturation) were evaluated. Results: Patients with complicated silicosis walked 387±92m. Results deteriorated as silicosis severity increased; category A: 407 ± 97m, B: 370±88m, and C: 357 ± 68m (P=.022). The 6MWT correlated positively with lung function and inversely with dyspnea determined by mMRC (P < .001). Patients with moderate/severe emphysema and greater CT90 presented a worse result on 6MWT. Patients who walked < 350m had more hospitalizations (3.7 ± 4.0) than those who walked > 350m (1.1 ± 2.9). There was an impact on survival: non-survivors walked 327.9 ± 73.0m, while survivors walked 404.5 ± 89.7m (P < .001). Conclusions: Spirometry values and category of complicated silicosis correlated with 6MWT and distance walked was a prognostic factor for hospitalization and mortality. The 6MWT is a useful tool in occupational health for monitoring patients with silicosis

The 6-Minute Walk Test as a Tool for Determining Exercise Capacity and Prognosis in Patients with Silicosis. / La prueba de la marcha de 6 minutos como factor pronóstico y de capacidad de ejercicio en pacientes con silicosis.

OBJECTIVE: To evaluate exercise capacity using the 6-minute walk test (6MWT) in patients with complicated silicosis, and to determine how results shape the prognostic value of 6MWT for hospitalization and mortality. METHOD: Prospective observational study in 143 patients with complicated silicosis who performed the 6MWT in our outpatient pulmonology clinic between 2009 and the end of 2016. Lung function tests, computed tomography findings and 6MWT parameters (distance walked and oxygen desaturation) were evaluated. RESULTS: Patients with complicated silicosis walked 387±92m. Results deteriorated as silicosis severity increased; category A: 407±97m, B: 370±88m, and C: 357±68m (P=.022). The 6MWT correlated positively with lung function and inversely with dyspnea determined by mMRC (P<.001). Patients with moderate/severe emphysema and greater CT90 presented a worse result on 6MWT. Patients who walked<350m had more hospitalizations (3.7±4.0) than those who walked>350m (1.1±2.9). There was an impact on survival: non-survivors walked 327.9±73.0m, while survivors walked 404.5±89.7m (P<.001). CONCLUSIONS: Spirometry values and category of complicated silicosis correlated with 6MWT and distance walked was a prognostic factor for hospitalization and mortality. The 6MWT is a useful tool in occupational health for monitoring patients with silicosis.

Validation of the portable Air-Smart Spirometer.

BACKGROUND: The Air-Smart Spirometer is the first portable device accepted by the European Community (EC) that performs spirometric measurements by a turbine mechanism and displays the results on a smartphone or a tablet. METHODS: In this multicenter, descriptive and cross-sectional prospective study carried out in 2 hospital centers, we compare FEV1, FVC, FEV1/FVC ratio measured with the Air Smart-Spirometer device and a conventional spirometer, and analyze the ability of this new portable device to detect obstructions. Patients were included for 2 consecutive months. We calculate sensitivity, specificity, positive and negative predictive value (PPV and NPV) and likelihood ratio (LR +, LR-) as well as the Kappa Index to evaluate the concordance between the two devices for the detection of obstruction. The agreement and relation between the values of FEV1 and FVC in absolute value and the FEV1/FVC ratio measured by both devices were analyzed by calculating the intraclass correlation coefficient (ICC) and the Pearson correlation coefficient (r) respectively. RESULTS: 200 patients (100 from each center) were included with a mean age of 57 (± 14) years, 110 were men (55%). Obstruction was detected by conventional spirometry in 73 patients (40.1%). Using a FEV1/FVC ratio smaller than 0.7 to detect obstruction with the Air Smart-Spirometer, the kappa index was 0.88, sensitivity (90.4%), specificity (97.2%), PPV (95.7%), NPV (93.7%), positive likelihood ratio (32.29), and negative likelihood ratio (0.10). The ICC and r between FEV1, FVC, and FEV1 / FVC ratio measured by the Air Smart Spirometer and the conventional spirometer were all higher than 0.94. CONCLUSION: The Air-Smart Spirometer is a simple and very precise instrument for detecting obstructive airway diseases. It is easy to use, which could make it especially useful non-specialized care and in other areas.

Conocimientos, actitudes y prácticas en adolescentes universitarios entre 15 y 20 años sobre VIH/SIDA en Medellín, Colombia 2013 / Knowledge, Attitudes and Practices about HIV/AIDS in university adolescents in Medellín, Colombia 2013

Introducción: el Plan Nacional de respuesta ante el VIH/SIDA en Colombia enfatiza la necesidad de fomentar conocimientos, actitudes, comportamientos y prácticas que propendan por el desarrollo de una sexualidad autónoma, responsable y placentera. Objetivo: analizar los conocimientos, actitudes y prácticas sobre VIH/SIDA en adolescentes universitarios de Medellín según aspectos sociodemográficos. Materiales y métodos: estudio transversal en 210 adolescentes universitarios de Medellín. Los datos fueron almacenados y analizados en SPSS 21.0®. Para la descripción de la población se realizaron medidas de resumen y frecuencias, para la identificación de factores asociados con el tema se usaron pruebas como la U de Mann-Whitney, H de Kruskal-Wallis y Coeficiente de Correlación de Spearman, y regresión lineal multivariante. Resultados: los conocimientos fueron regulares en el 14%, las actitudes en el 8% y las prácticas en el 41%; no se halló correlación significativa con el número de personas en el hogar, ni la edad y escolaridad de los padres. Los puntajes de Actitudes y Prácticas presentaron una correlación estadísticamente significativa con la edad y el semestre del estudiante. Los estudiantes de mayor edad y semestres más avanzados presentaron puntajes más altos en las Actitudes y más bajos en las Prácticas. Conclusión: los puntajes de conocimientos, actitudes y prácticas presentaron resultados desfavorables demostrando el riesgo de los jóvenes de adquirir VIH/SIDA y la necesidad de fortalecer los programas destinados a mejorar la salud sexual y reproductiva de este grupo. MÉD.UIS. 2014;27(3):35-45.

Introduction: the National Plan response to HIV/AIDS in Colombia emphasizes the need to promote knowledge, attitudes, behaviors and practices which foster the development of an autonomous, responsible and pleasurable sexuality. Objective: to assess the knowledge, attitudes and practices on HIV / AIDS among university adolescents in Medellin according to socio-demographics aspects. Materials and methods: cross-sectional study of 210 students. Data were stored and analyzed by SPSS 21.0®. The description of the subjects was realized with summary measures and frequencies, the identification of associated factors with the tests UMann-Whitney, Kruskal-Wallis, Spearman's correlation coefficient and multivariate linear regression were performed. Results: the knowledge was regular in the 14%, attitudes in the 8% and the practices in the 41%. The knowledge, attitudes and practices showed no significant correlation with the number of members of the house, parent's age nor theeducation level of the parents. The scores of attitudes and practices showed a statistically significant correlation with age and current semester of the student. Older students and those in more advanced semesters had higher scores on the attitudes and lower in the practices. Conclusion: the knowledge, attitudes and practices score showed unfavorable results demonstrating the risk of the adolescent of acquiring HIV/AIDS and the need to strengthen programs to improve sexual and reproductive health of this group. MÉD.UIS. 2014;27(3):35-45.

Especies promisorias para el ecoturismo en Campo Aventura Roca Madre, Toluviejo-Sucre, Colombia / Promising species for the development of ecotourism in Campo Aventura Roca Madre, Toluviejo-Sucre, Colombia

Objetivo. Determinar las especies de flora y fauna más importantes para el desarrollo del ecoturismo, en una localidad del departamento de Sucre, Colombia. Materiales y métodos. Se hizo un listado de las especies de flora y fauna observadas en el sendero ecológico de un centro de ecoturismo en Toluviejo, Sucre y se calculó su abundancia, importancia económica, estado de conservación y adaptaciones, que fueron evaluadas mediante un índice de importancia potencial para el ecoturismo, que suma los valores que se asignan a las variables consideradas de interés. Resultados. Se detectaron 18 especies promisorias de fauna, de 91 especies observadas y 16 especies vegetales de 53 observadas. Los animales de mayor potencial ecoturístico resultantes, fueron: Dendrobates truncatus y Saguinus oedipus, especies endémicas de Colombia, seguidas por Basiliscus basiliscus, Atta sp., Morpho peleides, Lycorea halia y Ara ararauna; todas estas con una alta abundancia y fácil detección. Dentro de las plantas, Anacardium excelsum obtuvo el mayor índice de importancia, como resultado de su endemismo y sus adaptaciones. Las especies Piper auritum, Matayba escrobiculata, Tabernaemontana cymosa y la comúnmente conocida como jazmín de monte, fueron fácilmente detectables y abundantes, además Brownea ariza y Tabebuia rosea resultaron las más representativas por la belleza de sus flores. Conclusiones. Se determinaron las especies que pueden ser de interés para los ecoturistas y esto hace posible mejorar el producto que se oferta a partir de profundizar en su conocimiento.

Objectives. To determine the species of flora and fauna relevant for development of ecotourism in a location of Sucre, Colombia. Materials and methods. A list of various species at the ecotourism center in the municipality of Toluviejo, Sucre, was studied which included abundance, economic and conservation relevance and adaptation data. The census was estimated and evaluated according to our index of potential importance for ecotourism, by adding the values assigned to each of the variables of interest. Results. 18 promising species of fauna and 16 promising species of plants were found. Animals with higher ecotourism potential were Dendrobates truncatus and Saguinus oedipus, endemic to Colombia, followed by Basiliscus basiliscus, Atta sp. Morpho peleides, Lycorea halia, Ara ararauna, all these of high abundance and easy detection. Regarding plants, Anacardium excelsum obtained the highest value as a result of endemism and their adaptations. Piper auritum, Matayba escrobiculata, Tabernaemontana cymosa and the specie commonly known as "jazmín de monte", were easily detectable and abundant. Brownea ariza and Tabebuia rosea were the best candidates because of the beauty of their flowers. Conclusions. The species that may be of interest to eco-tourists were determined and this makes it possible to improve the product offering from deepening their knowledge.

Radioguided surgery in brain tumors with thallium-201.

RATIONALE: Malignant astrocytomas show thallium uptake with a high target-to-background ratio, allowing the use of radioguided surgery. METHOD: We report on 6 patients (3 men) diagnosed with malignant astrocytoma. All patients signed informed consent documents. Previous thallium-201 SPECT was performed, showing uptake in tumors. In the operating room we injected 37 MBq (1 mCi) of thallium-201 at the same time the craniotomy was performed. With the gamma probe we confirmed the tumor uptake, and a biopsy sample was taken. After conventional tumor resection, we scanned the surgical bed with the gamma probe. All areas of abnormal uptake were evaluated by the surgeon and, if possible, removed. RESULTS: In all patients the biopsy confirmed a high-grade astrocytoma. In all cases we found residual uptake in the surgical bed that was confirmed as residual tumor by pathologic examination. In 3 cases it was not possible to remove all the sites of pathologic uptake because critical areas were involved. In the other 3 patients, only background activity was found after the procedure. CONCLUSION: Radioguided surgery in brain tumors with thallium-201 is a complex technique and expertise in radioguided surgery and neuroimaging is needed, but we think that it is promising.

Comportamiento de la respuesta a la fitohemaglutinina (PHA) de linfocitos humanos en presencia de Coralan / Behavior of response to phytohemagglutinin (PHA) of human lymphocytes in the presence of Coralan

La búsqueda de nuevos inmunomoduladores con actividad antitumoral es tarea priorizada de muchos laboratorios en el mundo. En el Instituto Nacional de Oncología y Radiobiología (INOR) se obtuvo un polisacárido de un coral blanco del Caribe, que produjo rechazo al transplante de hasta 100 por ciento del tumor ascítico de Ehrlich en ratones. Este producto evidenci ó actividad de los linfocitos T a diferentes niveles en donantes sanos, lo que podría permitir en el futuro separar los mismos por el grado de incremento de respuesta a la PHA

Comportamiento de la respuesta a la fitohemaglutinina (PHA) de linfocitos humanos en presencia de Coralan / Behavior of response to phytohemagglutinin (PHA) of human lymphocytes in the presence of Coralan

La búsqueda de nuevos inmunomoduladores con actividad antitumoral es tarea priorizada de muchos laboratorios en el mundo. En el Instituto Nacional de Oncología y Radiobiología (INOR) se obtuvo un polisacárido de un coral blanco del Caribe, que produjo rechazo al transplante de hasta 100 por ciento del tumor ascítico de Ehrlich en ratones. Este producto evidenci ó actividad de los linfocitos T a diferentes niveles en donantes sanos, lo que podría permitir en el futuro separar los mismos por el grado de incremento de respuesta a la PHA (AU)

Repuesta de los linfocitos de pacientes con cáncer a la fitohemaglutinina (PHA) en presencia de coralan / Response of lymphocytes of patients with cancer to phytohemaglutinin (PHA) in presence of coralan

En la terapia del cáncer se utilizan diferentes modalidades como son: cirugía, radiaciones, quimioterapia o inmunoterapia, solas o combinadas entre sí, que a menudo tienen efectos indeseables como por ejemplo la inmunosupresión. Cada día son más los laboratorios que dedican sus esfuerzos a encontrar productos capaces de elevar los índices del sistema inmunológico. En el INOR se extrajo una glicoproteína de un coral blando del Caribe capaz de elevar la respuesta a los linfocitos frente a la fitohemaglutinina y la actividad de las células NK, además de mostrar actividad potenciadora frente al test de establecimiento de metástasis pulmonares y hepáticas

Repuesta de los linfocitos de pacientes con cáncer a la fitohemaglutinina (PHA) en presencia de coralan / Response of lymphocytes of patients with cancer to phytohemaglutinin (PHA) in presence of coralan

En la terapia del cáncer se utilizan diferentes modalidades como son: cirugía, radiaciones, quimioterapia o inmunoterapia, solas o combinadas entre sí, que a menudo tienen efectos indeseables como por ejemplo la inmunosupresión. Cada día son más los laboratorios que dedican sus esfuerzos a encontrar productos capaces de elevar los índices del sistema inmunológico. En el INOR se extrajo una glicoproteína de un coral blando del Caribe capaz de elevar la respuesta a los linfocitos frente a la fitohemaglutinina y la actividad de las células NK, además de mostrar actividad potenciadora frente al test de establecimiento de metástasis pulmonares y hepáticas

Influencia del coralán sobre la respuesta in vitro de células inmunocompetentes / Coralan influence on the in vitro response of inmunocompetent cells

El coralán, aislado de la Pseudopterogorgia americana, un coral blando, es una glicoproteìna sulfatada que contiene 1% de sulfato, se ha informado que tienen influencia en el rechazo del trasplante del tumor ascìtico de Ehrlich. Diferentes concentraciones de esta sustancia se probaron en células mononucleares de sangre periférica (CMN) frente a la PHA, se observó un incremento significativo de la respuesta, lo que indica que una de las vías por las que este producto ajerce su actividad es por la vía de los linfocitos T. Tambièn se produce un ligero incremento de la actividad de las células NK frente a las células K 562 cuando las CMN son preincubadas con el producto 2 horas antes de realizarse el experimento, datos que en nuestras condiciones fueron comparables al procucido por el IFN, que se ha descrito que aumenta esta actividad.

Influencia del coralán sobre la respuesta in vitro de células inmunocompetentes / Coralan influence on the in vitro response of inmunocompetent cells

El coralán, aislado de la Pseudopterogorgia americana, un coral blando, es una glicoproteìna sulfatada que contiene 1

de sulfato, se ha informado que tienen influencia en el rechazo del trasplante del tumor ascìtico de Ehrlich. Diferentes concentraciones de esta sustancia se probaron en células mononucleares de sangre periférica (CMN) frente a la PHA, se observó un incremento significativo de la respuesta, lo que indica que una de las vías por las que este producto ajerce su actividad es por la vía de los linfocitos T. Tambièn se produce un ligero incremento de la actividad de las células NK frente a las células K 562 cuando las CMN son preincubadas con el producto 2 horas antes de realizarse el experimento, datos que en nuestras condiciones fueron comparables al procucido por el IFN, que se ha descrito que aumenta esta actividad.