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1.
Gac. méd. espirit ; 25(3)dic. 2023.
Artículo en Español | LILACS-Express | LILACS | ID: biblio-1528634

RESUMEN

Fundamento: En la carrera de Medicina es necesario formar profesionales con pensamiento creativo que permita la solución de problemas vinculados con el ejercicio de su profesión. La Genética Médica aporta la posibilidad de reflexionar y crear soluciones creativas. Objetivo: Proponer actividades que posibiliten el aprendizaje creativo en estudiantes de Medicina desde la Genética Médica. Metodología: Se emplearon métodos teóricos, empíricos y matemático-estadístico, con una muestra de 34 estudiantes y 3 profesores que imparten la asignatura. Resultados: Los docentes reconocen que, a pesar de hacer intentos para alcanzar el aprendizaje creativo, desconocen algunas vías y manifiestan no contar con el tiempo suficiente para su logro. El accionar didáctico no favorece el conocimiento, aplicación y disposición de estudiantes para un aprendizaje creativo. Se propusieron actividades sustentadas en procederes en Genética Médica, como parte de la estrategia didáctica de los docentes, asimismo contribuir al perfeccionamiento del aprendizaje creativo en los estudiantes. Las mismas centradas en métodos problémicos y el uso de recursos tecnológicos. Conclusiones: La formación de los médicos necesita expresar un aprendizaje creativo vinculado a un desempeño eficiente en la solución de problemas de la comunidad, lo cual se puede facilitar mediante la utilización de actividades en la asignatura Genética Médica.


Background: In the Medicine career it is necessary to form professionals with creative thoughts that allow the solution of problems linked to their professional practice. Medical Genetics provides the possibility to reflect and create creative solutions. Objective: To propose activities that allow creative learning in Medical students from the Medical Genetics perspective. Methodology: Theoretical, empirical and mathematical-statistical methods were applied, with a sample of 34 students and 3 teachers who teach the subject. Results: Teachers recognize that, despite making attempts to achieve creative learning, they are unaware of some ways and declare that they do not have enough time to achieve it. The didactic action does not favor the knowledge, application and disposition of students for creative learning. Activities supported by procedures in Medical Genetics were proposed as part of the didactic strategy of the teachers, likewise contribute to the improvement of creative learning in students. The same ones are focused on problem-solving methods and the use of technological resources. Conclusions: Physician education needs to express creative learning coupled with efficient performance in solving community problems, which may be facilitated through the use of activities in Medical Genetics Medical subject.

2.
Molecules ; 26(13)2021 Jun 25.
Artículo en Inglés | MEDLINE | ID: mdl-34202296

RESUMEN

TASK channels belong to the two-pore-domain potassium (K2P) channels subfamily. These channels modulate cellular excitability, input resistance, and response to synaptic stimulation. TASK-channel inhibition led to membrane depolarization. TASK-3 is expressed in different cancer cell types and neurons. Thus, the discovery of novel TASK-3 inhibitors makes these bioactive compounds very appealing to explore new cancer and neurological therapies. TASK-3 channel blockers are very limited to date, and only a few heterofused compounds have been reported in the literature. In this article, we combined a pharmacophore hypothesis with molecular docking to address for the first time the rational design, synthesis, and evaluation of 5-(indol-2-yl)pyrazolo[3,4-b]pyridines as a novel family of human TASK-3 channel blockers. Representative compounds of the synthesized library were assessed against TASK-3 using Fluorometric imaging plate reader-Membrane Potential assay (FMP). Inhibitory properties were validated using two-electrode voltage-clamp (TEVC) methods. We identified one active hit compound (MM-3b) with our systematic pipeline, exhibiting an IC50 ≈ 30 µM. Molecular docking models suggest that compound MM-3b binds to TASK-3 at the bottom of the selectivity filter in the central cavity, similar to other described TASK-3 blockers such as A1899 and PK-THPP. Our in silico and experimental studies provide a new tool to predict and design novel TASK-3 channel blockers.


Asunto(s)
Simulación del Acoplamiento Molecular , Bloqueadores de los Canales de Potasio , Canales de Potasio de Dominio Poro en Tándem , Piridinas , Humanos , Bloqueadores de los Canales de Potasio/síntesis química , Bloqueadores de los Canales de Potasio/química , Canales de Potasio de Dominio Poro en Tándem/antagonistas & inhibidores , Canales de Potasio de Dominio Poro en Tándem/química , Piridinas/síntesis química , Piridinas/química
3.
Comput Biol Chem ; 74: 218-229, 2018 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-29655025

RESUMEN

Given the wide spectrum of biological uses of pyrazolo[1,5-c]quinazoline and spiro-quinazoline derivatives as anticancer, anti-inflammatory analgesic agents, and their therapeutic applications in neurodegenerative disorders, it is compulsory to find easy, efficient, and simple methods to obtain and chemically diversify these families of compounds, thereby improving their biological applications. In this paper, we report the design and eco-friendly two-step synthesis of novel, fused spiro-pyrazolo[1,5-c]quinazoline derivatives as cholinesterase inhibitors. In addition, we studied their protein-ligand interactions via molecular docking and MM/GBSA calculations for a further rational design of more potent inhibitors. In first step, 2-(1H-pyrazol-5-yl)anilines were obtained through microwave (MW) assisted solvent-free/catalyst-free conditions and the second step involved the synthesis of the spiro-pyrazolo[1,5-c]quinazolines by a cyclocondensation reaction between 2-(1H-pyrazol-5-yl)anilines and cyclic ketones, or acetophenones, using stirring at room temperature. The compounds were obtained in high purity, good yields (50-97%), and at varying reaction times. The spiro-compounds were evaluated as acetylcholinesterase and butyrylcholinesterase inhibitors (AChEIs/BuChEIs) respectively, and the most potent compound exhibited a moderate AChE inhibitory activity (5f: IC50 = 84 µM). Molecular docking studies indicated that the binding mode of the compound 5f share common characteristics with the galantamine/donepezil-AChE complexes. Moreover, free binding energy (ΔG) calculations showed a good agreement with the experimental biological activity values. Our theoretical results indicated that halogen bond interactions could be involved with differential potency of these compounds and provide a new starting point to design novel pyrazolo[1,5-c]quinazolines as new anti-Alzheimer agents.


Asunto(s)
Inhibidores de la Colinesterasa/farmacología , Diseño de Fármacos , Simulación del Acoplamiento Molecular , Pirazoles/farmacología , Teoría Cuántica , Quinazolinas/farmacología , Compuestos de Espiro/farmacología , Acetilcolinesterasa/metabolismo , Butirilcolinesterasa/metabolismo , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/química , Relación Dosis-Respuesta a Droga , Humanos , Microondas , Estructura Molecular , Pirazoles/síntesis química , Pirazoles/química , Quinazolinas/síntesis química , Quinazolinas/química , Compuestos de Espiro/síntesis química , Compuestos de Espiro/química , Relación Estructura-Actividad
4.
MEDICC Rev ; 20(4): 27-34, 2018 10.
Artículo en Inglés | MEDLINE | ID: mdl-31242169

RESUMEN

INTRODUCTION The consequences of de novo balanced structural chromosome aberrations diagnosed antenatally are unpredictable, and, as a result, they introduce uncertainty into genetic counseling decisions. OBJECTIVE Describe de novo balanced structural aberrations present at antenatal diagnosis in samples from pregnant women in five Latin American countries and determine their effect on carrier individuals. METHODS This was a retrospective observational study based on analysis of 109,011 antenatal tests conducted from January 1981 to December 2016 in Cuba, Uruguay, Costa Rica, Mexico, and Colombia. Thirteen cytogenetic laboratories provided information that included the cases analyzed during the study period; number of de novo balanced structural aberrations diagnosed antenatally; number of diagnoses with de novo balanced structural aberrations that resulted in termination of pregnancy; detailed descriptions of the karyotypes of de novo balanced structural aberration carriers, and descriptions of the form of diagnosis, including types of samples used (amniotic fluid, chorionic villus or fetal blood). Each laboratory also provided pathology reports and genetic counseling at time of diagnosis. Postnatal followup for pregnancies carried to term continued for at least two years. RESULTS Of the 109,011 antenatal tests studied, 72 (0.07%) showed de novo balanced structural aberrations. These events primarily involved chromosomes 1, 2, 7, 14, 18, and 20. Of the 79 breakpoints identified, the most common were 5p15.3, 7q11.2, 7q22, and 14q24. We identified three breakpoints corresponding to 3.8% (3q13.1, 3q13.2, and 9p12) that were not reported in other studies of de novo balanced structural aberrations diagnosed antenatally in patients from other geographic regions or in studies of chromosomal fragile sites. Two of these breakpoints (3q13.1 and 3q13.2) were associated with high risk of phenotypic abnormalities. Information on antenatal or postnatal followup was available for 62 (86%) of de novo balanced structural aberration carriers; of the 44 carriers with postnatal followup, 10 had phenotypic abnormalities. CONCLUSIONS Three new de novo breakpoints were identified, presumably related to genetic admixture characteristics in Latin America. Since some diseases associated with de novo balanced structural aberrations detected antenatally have a late onset, followup for at least two years is recommended for carriers of these aberrations. The information in this study is useful in genetic counseling for pregnant women in Latin America.


Asunto(s)
Aberraciones Cromosómicas , Diagnóstico Prenatal , Puntos de Rotura del Cromosoma , Colombia , Costa Rica , Cuba , Femenino , Asesoramiento Genético , Humanos , Cariotipificación/métodos , México , Embarazo , Diagnóstico Prenatal/métodos , Uruguay
5.
Dialnet ; 30(4)2018.
Artículo en Español | CUMED | ID: cum-73649

RESUMEN

Método Se estudiaron prospectivamente 157 pacientes que ingresaron de forma consecutiva con diagnóstico de infarto agudo de miocardio con elevación del segmento ST y clase Killip > I, de enero de 2013 a diciembre de 2016, en el Hospital General Docente Camilo Cienfuegos. Se recogieron datos clínicos, de laboratorio y ecocardiográficos en relación con la presencia de síndrome cardiorrenal y se determinó la implicación pronóstica del mismo en la mortalidad intrahospitalaria a través de la regresión logística binaria(AU)


Method An analysis was performed on 157 consecutive patients admitted to the Coronary Care Unit of the Camilo Cienfuegos Hospital due to an ST-segment elevation myocardial infarction and heart failure, from January 2013 to December 2016. An analysis was made of the presence of cardiorenal syndrome and its relationship with epidemiological, clinical, and analytical variables, as well as complementary explorations. The relationship between cardiorenal syndrome and in-hospital mortality was assessed using binary logistical regression(AU)


Asunto(s)
Humanos , Síndrome Cardiorrenal/complicaciones , Síndrome Coronario Agudo/complicaciones , Mortalidad Hospitalaria , Estudios Prospectivos
6.
Biol Lett ; 12(8)2016 08.
Artículo en Inglés | MEDLINE | ID: mdl-27484648

RESUMEN

Mainly owing to their high diversity and abundance, ants are formidable as predators and defenders of foliage. Consequently, ants can exclude both invertebrate and vertebrate activity on plants via direct and indirect interactions as already shown in many previous studies. Here we present empirical evidence that objects resembling ant shape on dummy caterpillars were able to repel visually oriented predators. Moreover, we also show that rubber ants on dummy fruits can repel potential fruit dispersers. Our results have direct implications on the ecological and evolutionary dynamics of interactions in ant-based systems, as ant presence could affect the fitness of its partners. In short, our study highlights the importance of visual cues in interspecific interactions and opens a new way to study the effects of ant presence to test ecological and evolutionary hypotheses.


Asunto(s)
Frutas , Animales , Insectos , Plantas , Simbiosis
7.
Molecules ; 17(10): 12072-85, 2012 Oct 15.
Artículo en Inglés | MEDLINE | ID: mdl-23085657

RESUMEN

(E)-2-(benzo[d]thiazol-2-yl)-3-heteroarylacrylonitriles are described as a new class of selective inhibitors of acetylcholinesterase (AChE). The most potent compound in the series exhibited good AChE inhibitory activity (IC50 = 64 µM). Compound 7f was found to be more selective than galanthamine in inhibiting AChE and it showed a moderate selectivity index. Kinetic studies on AChE indicated that a competitive type of inhibition pattern exist for these acrylonitrile derivates. Molecular docking models of the ligand-AChE complexes suggest that compound 7 g is located on the periphery of the AChE active site.


Asunto(s)
Acrilonitrilo/síntesis química , Inhibidores de la Colinesterasa/síntesis química , Acetilcolinesterasa/química , Acetilcolinesterasa/metabolismo , Acrilonitrilo/análogos & derivados , Acrilonitrilo/química , Inhibidores de la Colinesterasa/química , Concentración 50 Inhibidora , Cinética , Simulación del Acoplamiento Molecular , Unión Proteica
8.
Gac méd espirit ; 14(2)mayo-ago. 2012. ilus
Artículo en Español | CUMED | ID: cum-51423

RESUMEN

Fundamento: Las inversiones cromosómicas pueden provocar un fenotipo afectado debido a la interrupción de genes o a la variación en la actividad de estos. Ellas son relativamente comunes, pero por debajo del 1 porciento. Las inversiones pericéntricas consisten en rupturas y reparaciones invertidas del segmento cromosómico, que involucran al centrómero. Presentación de caso: la amniocentesis se le realizó a una paciente de 38 años de edad a las 17, 2 semanas de gestación; la muestra se cultivó y se procesó según las técnicas estandarizadas en nuestro laboratorio. Conclusión: el estudio cromosómico del propósito evidenció una inversión pericéntrica del cromosoma 2: 46, XX, inv (2)(p21::q24). Es la primera vez que se reporta en Cuba este tipo de aberración cromosómica, siendo el padre portador de la misma(AU)


Background: The chromosomic inversions may provoke a phenotype affected due to genes interruption or to a variation of activity in them. They are relatively common but under 1 percent. The pericentric inversions consist of a ruptura and repair invertid in the chromosomic segment which involve the centrometer. Case presentation: The amniocentesis was performed to a 38 year old patient at 17.2 weeks gestation; the sample was cultured and processed according to standard techniques in our laboratory. Conclusion: The chromosomic study of the objective proved a pericentric inversion of the chromosome 2: 46, XX, inv (2)(p21::q24). This is the first time reported in Cuba this type of chromosomic aberration, being the father the carrier(AU)


Asunto(s)
Humanos , Cromosomas Humanos Par 2/genética , Amniocentesis/instrumentación
9.
Rev. cuba. med. trop ; 35(3): 238-241, sept.-dic. 1983. tab
Artículo en Español | CUMED | ID: cum-31836

RESUMEN

Se infestaron experimentalmente 12 hámsteres con 6 y 10 larvas infestivas de angiostrongylus cantonensis. Se observó un promedio de sobrevivencia inferior a 30,3 días,y que los parásitos alcanzaron los pulmones antes que en su hospedero habitual. En ningún caso se encontraron larvas en las heces(AU)


Asunto(s)
Animales , Cricetinae , Angiostrongylus cantonensis/patogenicidad , Infecciones por Strongylida
10.
Rev. cuba. med. trop ; 27(2): 151-157, may. -ago.1975. graf
Artículo en Español | CUMED | ID: cum-30574

RESUMEN

Se realiza un estudio de la incidencia de helmintiasis en 60 ratas blancas, machos, Wistard, encontrándose 4 tipos fundamentales de helmintos: H (H) nana (35(`por ciento); S obvelata (32(por ciento); C fasciolaris (25(por ciento); H (H) diminuta (4(por ciento). El índice de parasitosis entre los animales autopsiados fue el 69(por ciento). Se analiza la proporción de parasitismo concurrente y el número de distintos tipos de parásitos en cada rata. Se discuten brevemente los resultados obtenidos y se señala la necesidad...(AU)


Asunto(s)
Helmintiasis Animal/clasificación
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