In Vivo, In Vitro and In Silico Anticancer Activity of Ilama Leaves: An Edible and Medicinal Plant in Mexico.

Ilama leaves are an important source of secondary metabolites with promising anticancer properties. Cancer is a disease that affects a great number of people worldwide. This work aimed to investigate the in vivo, in vitro and in silico anticancer properties of three acyclic terpenoids (geranylgeraniol, phytol and farnesyl acetate) isolated from petroleum ether extract of ilama leaves. Their cytotoxic activity against U-937 cells was assessed using flow cytometry to determine the type of cell death and production of reactive oxygen species (ROS). Also, a morphological analysis of the lymph nodes and a molecular docking study using three proteins related with cancer as targets, namely, Bcl-2, Mcl-1 and VEGFR-2, were performed. The flow cytometry and histomorphological analysis revealed that geranylgeraniol, phytol and farnesyl acetate induced the death of U-937 cells by late apoptosis and necrosis. Geranylgeraniol and phytol induced a significant increase in ROS production. The molecular docking studies showed that geranylgeraniol had more affinity for Bcl-2 and VEGFR-2. In the case of farnesyl acetate, it showed the best affinity for Mcl-1. This study provides information that supports the anticancer potential of geranylgeraniol, phytol and farnesyl acetate as compounds for the treatment of cancer, particularly with the potential to treat non-Hodgkin's lymphoma.

Actividades para implementar el juego pre deportivo mediante la combinación balonmano - fútbol en estudiantes universitarios

Los juegos como actividades lúdicas constituyen un elemento importante en el desarrollo del proceso pedagógico de la Educación Física; se contribuye al trabajo en colectivo, formación de valores como: la valentía, la perseverancia, la disciplina, la honestidad, el compañerismo, la organización, el respeto a las reglas, entre otros, lo cual hace que contenga un gran valor biológico, psicológico, pedagógico, evidenciados en sus actividades y en los beneficios que reporta al ser humano. No obstante, a pesar de ser este planteamiento una fortaleza en el sistema educativo de Cuba, no se potencia desde el punto de vista científico y académico el juego pre deportivo para lograr estos componentes antes mencionados. Es por ello que se proyectó como objetivo caracterizar los juegos pre deportivos que implementan los profesores del departamento de Educación Física en los dos primeros años de la formación de profesionales en la Universidad de Oriente, Cuba. Como métodos empíricos se aplica una entrevista a los profesores y una guía de observación dedicada al proceso de enseñanza aprendizaje en la Educación Física. Se intenta conocer las potencialidades y debilidades que poseen los juegos pre deportivos para mejorar las habilidades físicas y deportivas de estos estudiantes, además de los valores en los que se pueden tributar a la formación integral desde estas prácticas. La inserción de este tipo de juegos ha contado con un nivel de opinión muy positivo por parte de los educandos y los profesores.

Os jogos como atividades lúdicas constituem um elemento importante no desenvolvimento do processo pedagógico da Educação Física; Contribui para o trabalho coletivo, formação de valores como: coragem, perseverança, disciplina, honestidade, camaradagem, organização, respeito às regras, entre outros, o que faz com que contenha grande valor biológico e psicológico. atividades e nos benefícios que traz ao ser humano. No entanto, apesar desta abordagem ser um ponto forte no sistema educativo cubano, o jogo pré-desportivo não é promovido do ponto de vista científico e académico para alcançar estes componentes acima mencionados. Por isso foi projetado o objetivo de caracterizar os jogos pré-desportivos implementados pelos professores do departamento de Educação Física nos primeiros dois anos de formação profissional da Universidade de Oriente, Cuba. Como métodos empíricos, são aplicados uma entrevista com professores e um roteiro de observação dedicado ao processo de ensino-aprendizagem em Educação Física. Procura-se conhecer as potencialidades e fragilidades que os jogos pré-desportivos apresentam para melhorar as competências físicas e desportivas destes alunos, bem como os valores em que pode contribuir uma formação integral a partir destas práticas. A inserção deste tipo de jogos tem tido uma opinião muito positiva por parte de alunos e professores.

Games as recreational activities constitute an important element in the development of the pedagogical process of Physical Education; tt contributes to collective work, formation of values such as: courage, perseverance, discipline, honesty, camaraderie, organization, respect for the rules, among others, which makes it contain great biological psychological and pedagogical value evidenced in its activities and in the benefits it brings to human beings. However, despite this approach being a strength in the Cuban educational system, the pre-sports game is not promoted from a scientific and academic point of view to achieve these aforementioned components. That is why the objective was projected to characterize the pre-sports games implemented by the teachers of the Physical Education department in the first two years of professional training at the Universidad de Oriente, Cuba. As empirical methods, an interview with teachers and an observation guide dedicated to the teaching-learning process in Physical Education are applied. An attempt is made to know the potential and weaknesses that pre-sports games have to improve the physical and sports skills of these students, in addition to the values in which comprehensive training can be contributed from these practices. The insertion of this type of games has had a very positive level of opinion from students and teachers.

Recomendaciones metodológicas para mitigar los efectos de las presiones ambientales en la gimnasia rítmica

Los gimnastas pueden recibir lesiones por sobrecarga, fatiga de segmentos y por inmadurez del aparato locomotor; todas pueden constituir presiones que, en determinado momento de la práctica deportiva, frenan el rendimiento sostenido en el deportista. Sn embargo, en un estudio exploratorio se pudo determinar que algunos atletas de gimnasia rítmica, representativos de la provincia Santiago de Cuba, se evidencian otras presiones ambientales que tienen mayor énfasis en lo psicológico. El objetivo de este trabajo consistió en proponer un grupo de recomendaciones metodológicas para evitar el efecto de las presiones ambientales en atletas de gimnasia rítmica. Dentro de los métodos empíricos utilizados se encuentran la observación, la encuesta y la entrevista. Se plantearon recomendaciones metodológicas, dirigidas a incidir en el rendimiento deportivo, ellas son: presión cuerpo de jueces, cumplimiento de elementos de dificultad en los ejercicios y participación en eventos, en correspondencia con las demás gimnastas. La propuesta se incorpora a una serie de estudios que tratan el seguimiento de la preparación del deportista de manera general y, en particular, el de gimnasia rítmica.

Ginastas podem sofrer lesões por sobrecarga, fadiga segmentar e imaturidade do sistema musculoesquelético; Todas elas podem constituir pressões que, em determinado momento da prática desportiva, retardam o desempenho sustentado do atleta. Porém, num estudo exploratório foi determinado que alguns atletas de ginástica rítmica, representativos da província de Santiago de Cuba, apresentam outras pressões ambientais que têm maior ênfase no psicológico. O objetivo deste trabalho foi propor um conjunto de recomendações metodológicas para evitar o efeito das pressões ambientais sobre atletas de ginástica rítmica. Entre os métodos empíricos utilizados estão a observação, o levantamento e a entrevista. Foram propostas recomendações metodológicas que visam influenciar o desempenho esportivo, são elas: pressão corporal dos juízes, cumprimento de elementos de dificuldade nos exercícios e participação em eventos, em correspondência com as demais ginastas. A proposta está incorporada a uma série de estudos que abordam o acompanhamento da preparação de atletas em geral e, em particular, da ginástica rítmica.

Gymnasts can receive injuries due to overload, segment fatigue and due to immaturity of the musculoskeletal system; all of them can constitute pressures that, at a certain point in sports practice, slow down the athlete's sustained performance. However, in the exploratory study it was determined that some rhythmic gymnastics athletes, representative of the Santiago de Cuba province, show other environmental pressures that have greater emphasis on the psychological. The objective of this work was to propose a group of methodological recommendations to mitigate the effect of environmental pressures on rhythmic gymnastics athletes. Among the empirical methods used are observation, survey and interview. Methodological recommendations were proposed, aimed at influencing sports performance, they are: pressure from the judges' body, compliance with elements of difficulty in the exercises and participation in events, in correspondence with the other gymnasts. The proposal is incorporated into a series of studies that address the monitoring of athlete preparation in general and, in particular, rhythmic gymnastics.

Consideraciones sobre las presiones ambientales que influyen en el rendimiento del tenis de mesa

El trabajo que se presenta forma parte de una de las investigaciones contenidas en el proyecto institucional "El tenis de mesa para el desarrollo integral del ser humano, sistematización desde la materia Actividad física, deporte y recreación: masificación deportiva escolar". Esta investigación tiene como objetivo valorar, mediante un estudio diagnóstico, si las presiones ambientales afectan la práctica del tenis de mesa en estudiantes de la Universidad Técnica "Luis Vargas Torres", de Esmeraldas. Después de realizar un análisis teórico sobre algunos antecedentes referidos a las presiones ambientales en el deporte, se aplicó un grupo de encuestas, entrevistas, revisión documental y test, para constatar la presencia de presiones ambientales en relación directa con las presiones psicológicas y físicas. Se concluyó que las presiones referentes al público, al límite de tiempo y el marcador fueron las más significativas y como consecuencia, se deben tomar medidas para la prevención de sus impactos, así como ponderar su inclusión en las orientaciones metodológicas para el entrenamiento del tenis de mesa.

O trabalho apresentado faz parte de uma das investigações contidas no projeto institucional "Tênis de mesa para o desenvolvimento integral do ser humano, sistematização a partir da disciplina Atividade física, esporte e recreação: massificação do esporte escolar". Esta pesquisa tem como objetivo avaliar, por meio de um estudo diagnóstico, se as pressões ambientais afetam a prática do tênis de mesa em estudantes da Universidade Técnica "Luis Vargas Torres", Esmeraldas. Depois de realizar uma análise teórica de algumas informações básicas sobre as pressões ambientais no esporte, foi aplicado um conjunto de pesquisas, entrevistas, revisão documental e testes para confirmar a presença de pressões ambientais em relação direta com as pressões psicológicas e físicas. Concluiu-se que as pressões relacionadas ao público, ao limite de tempo e ao placar foram as mais significativas e, como consequência, devem ser tomadas medidas para prevenir seus impactos, bem como considerar sua inclusão nas diretrizes metodológicas para o treinamento de tênis de mesa.

The work presented is part of one of the researches contained in the institutional project "Table tennis for the integral development of the human being, systematization from the subject Physical activity, sport and recreation: school sports massification". This research aims to assess, through a diagnostic study, if environmental pressures affect the practice of table tennis in students of the Technical University "Luis Vargas Torres" in Esmeraldas. After carrying out a theoretical analysis on some background related to environmental pressures in sport, a group of surveys, interviews, documentary review and tests were applied to verify the presence of environmental pressures in direct relation to psychological and physical pressures. It was concluded that the pressures related to the public, the time limit and the scoreboard were the most significant and as a consequence, measures must be taken to prevent their impacts, as well as considering their inclusion in the methodological guidelines for tennis training. table.

Formación deportiva en estudiantes con discapacidades, una experiencia en la escuela especial "28 de Enero"

El deporte adaptado, referido al término de actividad física con niños que presentan algún tipo de discapacidad, tiene una evolución histórica relevante, pues desde sus orígenes enfrenta altos retos. Es reconocido que en escuelas de nivel internacional y específicamente en Cuba, se realizan esfuerzos por potenciar la inclusión en el deporte; sin embargo, se considera que todavía son insuficientes las propuestas que, desde el punto de vista científico y metodológico, sustentan el aprovechamiento de las competencias y el desarrollo de habilidades en las personas con discapacidad. Es por ello, que se propone como objetivo de este trabajo visualizar la captación de niños con potencialidades para practicar deportes, desde la Educación Física, en la escuela especial "28 de Enero". En esta investigación, se aplicó una encuesta a los estudiantes sobre sus gustos en materia de deporte y se realizó una caracterización, a partir de aplicación de test que midió la discapacidad intelectual y la discapacidad físico-motor en ellos. Los datos, de forma general, revelaron que con dedicación, superación y trabajo en equipo se pueden obtener resultados satisfactorios no solo en el rendimiento deportivo, sino en la autoestima y calidad de vida en estos estudiantes.

O esporte adaptado, referente ao termo de atividade física com crianças que apresentam algum tipo de deficiência, tem uma evolução histórica relevante, pois desde suas origens tem enfrentado grandes desafios. Reconhece-se que nas escolas, em nível internacional e especificamente em Cuba, estão sendo feitos esforços para promover a inclusão no esporte; no entanto, considera-se que as propostas que, do ponto de vista científico e metodológico, apoiam o uso de competências e o desenvolvimento de habilidades em pessoas com deficiência ainda são insuficientes. É por essa razão que o objetivo deste trabalho é visualizar o recrutamento de crianças com potencial para a prática esportiva, a partir da Educação Física, na escola especial "28 de Enero". Nessa pesquisa, foi aplicado um questionário aos alunos sobre seus gostos pelo esporte e realizada uma caracterização, a partir da aplicação de um teste que mediu a deficiência intelectual e a deficiência físico-motora neles. Os dados, em geral, revelaram que, com dedicação, autoaperfeiçoamento e trabalho em equipe, é possível obter resultados satisfatórios não só no desempenho esportivo, mas também na autoestima e na qualidade de vida desses alunos.

Adapted sport, referred to as the term physical activity with children who have some type of disability, has a relevant historical evolution, since from its origins it has faced high challenges. It is recognized that in international level schools and specifically in Cuba, efforts are made to promote inclusion in sport; however, it is considered that the proposals that, from the scientific and methodological point of view, support the use of skills and the development of skills in people with disabilities are still insufficient. For this reason, the objective of this work is to visualize the recruitment of children with the potential to practice sports, from Physical Education, in the special school "28 de Enero". In this research, a survey was applied to students about their likes in sports and a characterization was carried out, based on the application of a test that measured intellectual disability and physical-motor disability in them. The data, in general, revealed that with dedication, improvement and teamwork, satisfactory results can be obtained not only in sports performance, but also in self-esteem and quality of life in these students.

Annona cherimola Miller and Its Flavonoids, an Important Source of Products for the Treatment of Diabetes Mellitus: In Vivo and In Silico Evaluations.

The antihyperglycemic activity of ethanolic extract from Annona cherimola Miller (EEAch) and its products were evaluated using in vivo and in silico assays. An α-glucosidase inhibition was evaluated with oral sucrose tolerance tests (OSTT) and molecular docking studies using acarbose as the control. SGLT1 inhibition was evaluated with an oral glucose tolerance test (OGTT) and molecular docking studies using canagliflozin as the control. Among all products tested, EEAc, the aqueous residual fraction (AcRFr), rutin, and myricetin reduced the hyperglycemia in DM2 mice. During the carbohydrate tolerance tests, all the treatments reduced the postprandial peak such as the control drugs. In the molecular docking studies, rutin showed more affinity in inhibiting α-glucosidase enzymes and myricetin in inhibiting the SGLT1 cotransporter, showing ∆G values of -6.03 and -3.32 kcal/mol-1, respectively, in α-glucosidase enzymes. In the case of the SGLT1 cotransporter, molecular docking showed ∆G values of 22.82 and -7.89 in rutin and myricetin, respectively. This research sorts in vivo and in silico pharmacological studies regarding the use of A. cherimola leaves as a source for the development of new potential antidiabetic agents for T2D control, such as flavonoids rutin and myricetin.

Antidiabetic and Toxicological Effects of the Tea Infusion of Summer Collection from Annona cherimola Miller Leaves.

Annona cherimola Miller (Ac) is a plant used in Mexican traditional medicine for the treatment of diabetes. In this work, the tea infusion extracts obtained from 1.5 g of leaf powder from Ac collected in May (AcMa), June (AcJun), July (AcJul), and August (AcAu) were evaluated on streptozocin-induced diabetic (STID) mice and for subchronic toxicity in STID and non-diabetic (ND) mice. In addition, extracts were subjected to high-performance liquid chromatography with diode array detection (HPLC-DAD). Results showed that the tea infusion extract of the sample collected in August (AcAu) exhibited the most significant antihyperglycemic activity during all acute assays. The analysis of the extracts (AcMa, AcJu, AcJul, and AcAu) by HPLC-DAD revealed that flavonoid glycosides, rutin, narcissin, and nicotiflorin were the major components. In addition, the sample AcAu contained the best concentration of flavonoids. In the case of subchronic oral toxicity, the AcAu sample did not cause mortality in STID mice, and histopathological analysis revealed significant improvement in the changes associated with diabetes in the liver and kidneys. These findings suggest that the Ac leaves collected in August may be a source of flavonoids such as rutin, with antidiabetic potential. In addition, these findings support the use of Ac to treat diabetes in traditional medicine.

Prevalencia de sobrepeso y obesidad. Problema de salud en la comunidad universitaria y politécnica ecuatoriana / Prevalence of overweight and obesity. Health problem in the Ecuadorian university and polytechnic community

RESUMEN Objetivo: Analizar investigaciones relacionados con la prevalencia de bajo peso, sobrepeso y obesidad en el ámbito universitario para determinar los indicadores de la determinación de este problema de salud. Método: Revisión descriptiva, la búsqueda bibliográfica se realizó a partir de las bases de datos como Scielo, Dialnet, Lilacs, Scopus. PubMed y Portal Regional de la BVS. Que permitió seleccionar 33 artículos científicos. Resultados y conclusiónes: A partir de las investigaciones consultadas los investigadores determinar que, en la mayoría de estas, se da a conocer resultados sobre la prevalencia de obesidad y sobrepeso, sin tener en cuenta el bajo peso y normopeso. Además, en las investigaciones abordadas para determinar la prevalencia de la obesidad y sobrepeso, se realiza a partir del IMC con los datos de la talla y peso corporal de los sujetos investigados y factores los factores sociodemográficos de la población investigada.

ABSTRACT Objective: To analyze research related to the prevalence of underweight, overweight and obesity in the university setting in order to determine the indicators of the determination of this health problem. Method: Descriptive review, the bibliographic search was carried out using databases such as Scielo, Dialnet, Lilacs, Scopus. PubMed and Regional Portal of the VHL. Which allowed the selection of 33 scientific articles. Results and conclusions: From the researches consulted, the researchers determined that, in most of these, results on the prevalence of obesity and overweight are reported, without taking into account underweight and normal weight. In addition, in the researches approached to determine the prevalence of obesity and overweight, it is done from the BMI with the data of the height and body weight of the investigated subjects and the sociodemographic factors of the investigated population.

The addition of different oils in the diet regulates the expression of adipocytokine signaling genes in sheep longissimus dorsi muscle.

Nutrition is an important factor that regulates the expression of several genes. The aim of this work was to analyze the effects of diets containing additions of different oils on the regulation of the adipocytokine signaling gene expressions in sheep longissimus dorsi muscle. Forty males and non-neutered sheep were kept in individual cages and fed under four different treatments: control treatment (concentrate and forage) and the other three treatments containing the concentrate and forage plus 4% oil (yellow grease, soybean and palm oils). After slaughter, samples of the longissimus dorsi muscle were collected. RNA extraction followed by Real Time PCR for five adipocytokine signaling genes. ANOVA was performed followed by the Dunnett's test (0.01). The normalized expressions of the ACLY gene were not significant between treatments to control, but for the ALDOC gene, all oil-supplemented treatments were significantly downregulated relative to the control treatment. The DUSP gene was not significantly expressed between the oil-supplemented treatments to control treatment. The ENPP1 gene was significantly upregulated with the addition of palm oil and yellow grease and the FASN gene was only significantly expressed in soybean oil-supplemented treatment to control treatment. It was concluded that the addition of different oils in the sheep diet regulated the expression of most genes for up or down, which can influence the metabolic pathways responsible for the fatty acid biosynthesis in the sheep longissimus dorsi muscle.

Linearolactone Induces Necrotic-like Death in Giardia intestinalis Trophozoites: Prediction of a Likely Target.

Linearolactone (LL) is a neo-clerodane type diterpene that has been shown to exert giardicidal effects; however, its mechanism of action is unknown. This work analyzes the cytotoxic effect of LL on Giardia intestinalis trophozoites and identifies proteins that could be targeted by this active natural product. Increasing concentrations of LL and albendazole (ABZ) were used as test and reference drugs, respectively. Cell cycle progression, determination of reactive oxygen species (ROS) and apoptosis/necrosis events were evaluated by flow cytometry (FCM). Ultrastructural alterations were analyzed by transmission electron microscopy (TEM). Ligand-protein docking analyses were carried out using the LL structure raised from a drug library and the crystal structure of an aldose reductase homologue (GdAldRed) from G. intestinalis. LL induced partial arrest at the S phase of trophozoite cell cycle without evidence of ROS production. LL induced pronecrotic death in addition to inducing ultrastructural alterations as changes in vacuole abundances, appearance of perinuclear and periplasmic spaces, and deposition of glycogen granules. On the other hand, the in silico study predicted that GdAldRed is a likely target of LL because it showed a favored change in Gibbs free energy for this complex.

Cognitive function and blood pressure control in elderly hypertensive individuals. / Função cognitiva e controle da pressão arterial em idosos hipertensos.

This article aims to estimate the prevalence of cognitive impairment and analyze its association with blood pressure control in elderly hypertensive individuals. Cross-sectional study of 383 elderly hypertensive individuals in the state of Piauí, Brazil. The authors collected sociodemographic and clinical data, performed blood pressure measurement, and assessed cognitive function using the Montreal Cognitive Assessment (MoCA) test. Poisson regression with robust variance was used. Overall prevalence of cognitive impairment was 74.4%, higher in the age group 80 years and over and among older persons with less schooling. Prevalence of uncontrolled blood pressure was 61.6%, with a higher proportion in the elderly with cognitive impairment. An association was observed between cognitive impairment and uncontrolled blood pressure (aPR: 3.98; 95%CI = 2.51-6.33). The significant association between cognitive function and blood pressure control suggest that cognitive impairment is an important risk factor for uncontrolled blood pressure in older persons. The inclusion of screening measures for possible cognitive deficits may be useful for better monitoring blood pressure levels among elderly hypertensive individuals.

O objetivo deste artigo é estimar a prevalência de comprometimento cognitivo e analisar sua associação com o controle da pressão arterial em idosos hipertensos. Trata-se de um estudo transversal realizado com 383 idosos hipertensos no estado do Piauí, Brasil. Foram coletados dados sociodemográficos, clínicos, realizada aferição da pressão arterial e avaliação da função cognitiva utilizando o teste Montreal Cognitive Assessment (MoCA). Utilizou-se regressão de Poisson com variância robusta. A prevalência de comprometimento cognitivo foi de 74,4%, sendo maior na faixa etária entre 80 anos ou mais de idade e naqueles com menor escolaridade. A prevalência de pressão arterial não controlada foi de 61,6%, com maior proporção entre os idosos com comprometimento cognitivo. Observou-se associação entre o comprometimento cognitivo e pressão arterial não controlada (RPAjustada: 3,98; IC95% = 2,51-6,33). A associação significativa entre função cognitiva e controle pressórico sugere que comprometimento cognitivo é um importante fator de risco para pressão arterial não controlada em pessoas idosas. A inclusão de medidas de rastreamento para possíveis déficits cognitivos podem ser úteis para melhor monitoramento da elevação dos níveis pressóricos entre idosos hipertensos.

Função cognitiva e controle da pressão arterial em idosos hipertensos / Cognitive function and blood pressure control in elderly hypertensive individuals

Resumo O objetivo deste artigo é estimar a prevalência de comprometimento cognitivo e analisar sua associação com o controle da pressão arterial em idosos hipertensos. Trata-se de um estudo transversal realizado com 383 idosos hipertensos no estado do Piauí, Brasil. Foram coletados dados sociodemográficos, clínicos, realizada aferição da pressão arterial e avaliação da função cognitiva utilizando o teste Montreal Cognitive Assessment (MoCA). Utilizou-se regressão de Poisson com variância robusta. A prevalência de comprometimento cognitivo foi de 74,4%, sendo maior na faixa etária entre 80 anos ou mais de idade e naqueles com menor escolaridade. A prevalência de pressão arterial não controlada foi de 61,6%, com maior proporção entre os idosos com comprometimento cognitivo. Observou-se associação entre o comprometimento cognitivo e pressão arterial não controlada (RPAjustada: 3,98; IC95% = 2,51-6,33). A associação significativa entre função cognitiva e controle pressórico sugere que comprometimento cognitivo é um importante fator de risco para pressão arterial não controlada em pessoas idosas. A inclusão de medidas de rastreamento para possíveis déficits cognitivos podem ser úteis para melhor monitoramento da elevação dos níveis pressóricos entre idosos hipertensos.

Abstract This article aims to estimate the prevalence of cognitive impairment and analyze its association with blood pressure control in elderly hypertensive individuals. Cross-sectional study of 383 elderly hypertensive individuals in the state of Piauí, Brazil. The authors collected sociodemographic and clinical data, performed blood pressure measurement, and assessed cognitive function using the Montreal Cognitive Assessment (MoCA) test. Poisson regression with robust variance was used. Overall prevalence of cognitive impairment was 74.4%, higher in the age group 80 years and over and among older persons with less schooling. Prevalence of uncontrolled blood pressure was 61.6%, with a higher proportion in the elderly with cognitive impairment. An association was observed between cognitive impairment and uncontrolled blood pressure (aPR: 3.98; 95%CI = 2.51-6.33). The significant association between cognitive function and blood pressure control suggest that cognitive impairment is an important risk factor for uncontrolled blood pressure in older persons. The inclusion of screening measures for possible cognitive deficits may be useful for better monitoring blood pressure levels among elderly hypertensive individuals.

The association between diabetes mellitus and incidence of depressive episodes is different based on sex: insights from ELSA-Brasil.

Objective: To investigate the association between diabetes mellitus (DM) and incidence of depressive episodes among men and women. Methods: Data were used from 12,730 participants (5866 men and 6864 women) at baseline (2008-2010) and follow-up 1 (2012-2014) of the Longitudinal Study of Adult Health (ELSA-Brasil), a multicenter cohort of Brazilian civil servants. Participants were classified for diabetes using self-reported and clinical information, and evaluated for presence of depressive episodes by the Clinical Interview Schedule-Revised (CIS-R). Associations were estimated by means of logistic regression models (crude and adjusted for socio-demographic variables). Results: Women classified as with DM prior to the baseline were at 48% greater risk (95% confidence interval (CI) = 1.03-2.07) of depressive episodes in the crude model and 54% greater risk (95% CI = 1.06-2.19) in the final adjusted model compared to women classified as non-DM. No significant associations were observed for men. The regression models for duration of DM and incidence of depressive episodes (n = 2143 participants; 1160 men and 983 women) returned no significant associations. Conclusion: In women classified as with prior DM, the greater risk of depressive episodes suggests that more frequent screening for depression may be beneficial as part of a multi-factorial approach to care for DM.

Antihyperglycemic Effects of Salvia polystachya Cav. and Its Terpenoids: α-Glucosidase and SGLT1 Inhibitors.

The antihyperglycemic activity of ethanolic extract from Salvia polystachya (EESpS) and its products was evaluated using in vivo, ex vivo and in silico assays; additionally, an acute toxicity assay was evaluated. EESpS was classified as a nontoxic class 5 drug. EESpS, ethyl acetate fraction (EtOAcFr), secondary-6-fraction (SeFr6), ursolic acid (UA), and oleanolic acid (OA) reduced the hyperglycemia in DM2 mice. α-glucosidase inhibition was evaluated with oral sucrose and starch tolerance tests (OSuTT and OStTT), an intestinal sucrose hydrolysis (ISH) assay and molecular docking studies using acarbose as control. SGLT1 inhibition was evaluated with oral glucose and galactose tolerance tests (OGTT and OGaTT), an intestinal glucose absorption (IGA) assay and molecular docking studies using canagliflozin as the control. During the carbohydrate tolerance tests, all the treatments reduced the postprandial peak, similar to the control drugs. During the ISH, IC50 values of 739.9 and 726.3 µM for UA and OA, respectively, were calculated. During the IGA, IC50 values of 966.6 and 849.3 for UA, OA respectively, were calculated. Finally, during the molecular docking studies, UA and OA showed ∆G values of -6.41 and -5.48 kcal/mol-1, respectively, on α-glucosidase enzymes. During SGLT1, UA and OA showed ∆G values of -10.55 and -9.65, respectively.

Expanding the Study of the Cytotoxicity of Incomptines A and B against Leukemia Cells.

Heliangolide-type sesquiterpene lactones (HTSLs) are phytocompounds with several pharmacological activities including cytotoxic and antitumor activity. Both bioactivities are related to an α-methylene-γ-lactone moiety and an ester group on carbon C-8 in the sesquiterpene lactone (SL) structure. Two HTSLs, incomptines A (AI) and B (IB) isolated from Decachaeta incompta, were evaluated for their cytotoxic activity on three leukemia cell lines: HL-60, K-562, and REH cells. Both compounds were subjected to a molecular docking study using target proteins associated with cancer such as topoisomerase IIα, topoisomerase IIß, dihydrofolate reductase, methylenetetrahydrofolate dehydrogenase, and Bcl-2-related protein A1. Results show that IA and IB exhibit cytotoxic activity against all cell lines used. The CC50 value of IA was 2-4-fold less than etoposide and methotrexate, two anticancer drugs used as positive controls. The cytotoxic activity of IB was close to that of etoposide and methotrexate. The molecular docking analysis showed that IA and IB have important interaction on all targets used. These findings suggest that IA and IB may serve as scaffolds for the development of new treatments for different types of leukemia.

Understanding the Anti-Diarrhoeal Properties of Incomptines A and B: Antibacterial Activity against Vibrio cholerae and Its Enterotoxin Inhibition.

Incomptines A (IA) and B (IB) are two sesquiterpene lactones with antiprotozoal, antibacterial, cytotoxic, antitumor, spermicidal, and phytotoxic properties. The antibacterial activity of IA and IB against bacteria causing diarrhoea have been reported; however, no information is available regarding their antibacterial activity on Vibrio cholerae. In this work, both compounds were evaluated for their anti-diarrhoeal potential using the bacterium V. cholerae, sodium dodecyl sulphate-polyacrylamide gel electrophoresis (SDS-PAGE) analysis on cholera toxin, and a cholera toxin-induced diarrhoea model in male Balb/c mice. In addition, a molecular docking study was carried out to understand the interaction of IA and IB with cholera toxin. In terms of antibacterial activity, IB was three times more active than IA on V. cholerae. In the case of SDS-PAGE analysis and the in silico study, IA was most effective, revealing its potential binding mode at a molecular level. In terms of anti-diarrhoeal activity, IA was 10 times more active than IB and racecadotril, an antisecretory drug used as positive control; the anti-diarrheal activity of IB was also closer than racecadotril. The results obtained from in vitro, in vivo, and computational studies on V. cholerae and cholera toxin support the potential of IA and IB as new anti-diarrhoeal compounds.

Antitumor Potential of Annona muricata Linn. An Edible and Medicinal Plant in Mexico: In Vitro, In Vivo, and Toxicological Studies.

Annona muricata (Am) is a plant used in traditional Mexican medicine to treat cancer. In this study, ethanol extracts of Am collected in Acapulco and Tecpan from Guerrero state were evaluated orally on Balb/c mice inoculated with 4T1 cells, for cytotoxic activity (CA) on 4T1 cells, in brine shrimp lethality assay (BSLA), and for acute oral toxicity in mice. In addition, ethanol extracts were subjected to high-performance liquid chromatography (HPLC) with diode array detection. Results showed that the extracts collected in December in Acapulco (AcDe) and Tecpan (TeDe) exhibited the most significant antitumor and cytotoxic activity. In the BSLA, the most important effect was observed in the extracts from Acapulco and Tecpan collected in June (AcJu) and August (TeAg), respectively. The samples from Acapulco (AcJu, and AcAg) and Tecpan (TeJu and TeAg) showed the highest toxicity. The analysis of the extracts, AcDe and TeDe, by HPLC revealed that flavonoids, rutin, narcissin, and nicotinflorin were the major components. These findings suggest that extracts from Am collected in Acapulco and Tecpan in the month of December may be an important source to obtain flavonoid glycosides with anticancer potential specifically against breast cancer. This also supports the use of Am to treat cancer in Mexican traditional medicine.

Antilymphoma Effect of Incomptine A: In Vivo, In Silico, and Toxicological Studies.

Incomptine A (IA) is a sesquiterpene lactone isolated from Decachaeta incompta that induces apoptosis, reactive oxygen species production, and a differential protein expression on the U-937 (diffuse histiocytic lymphoma) cell line. In this work, the antitumor potential of IA was investigated on Balb/c mice inoculated with U-937 cells and through the brine shrimp lethality (BSL) test. Furthermore, IA was subjected to molecular docking study using as targets proteins associated with processes of cancer as apoptosis, oxidative stress, and glycolytic metabolism. In addition to determining the potential toxicity of IA in human, its acute toxicity was performed in mice. Results reveals that IA showed high antilymphoma activity and BSL with an EC50 of 2.4 mg/kg and LC50 16.7 µg/mL, respectively. The molecular docking study revealed that IA has strong interaction on all targets used. In the acute oral toxicity, IA had a LD50 of 149 mg/kg. The results showed that the activities of IA including antilymphoma activity, BSL, acute toxicity, and in silico interactions were close to the methotrexate, an anticancer drug used as positive control. These findings suggest that IA may serve as a candidate for the development of a new drug to combat lymphoma.

Incomptine A Induces Apoptosis, ROS Production and a Differential Protein Expression on Non-Hodgkin's Lymphoma Cells.

Sesquiterpene lactones are of pharmaceutical interest due their cytotoxic and antitumor properties, which are commonly found within plants of several genera from the Asteraceae family such as the Decachaeta genus. From Decachaeta incompta four heliangolide, namely incomptines A-D have been isolated. In this study, cytotoxic properties of incomptine A (IA) were evaluated on four lymphoma cancer cell lines: U-937, Farage, SU-DHL-2, and REC-1. The type of cell death induced by IA and its effects on U-937 cells were analyzed based on its capability to induce apoptosis and produce reactive oxygen species (ROS) through flow cytometry with 4',6-diamidino-2-phenylindole staining, dual annexin V/DAPI staining, and dichlorofluorescein 2',7'-diacetate, respectively. A differential protein expression analysis study was carried out by isobaric tags for relative and absolute quantitation (iTRAQ) through UPLC-MS/MS. Results reveal that IA exhibited cytotoxic activity against the cell line U-937 (CC50 of 0.12 ± 0.02 µM) and the incubation of these cells in presence of IA significantly increased apoptotic population and intracellular ROS levels. In the proteomic approach 1548 proteins were differentially expressed, out of which 587 exhibited a fold-change ≥ 1.5 and 961 a fold-change ≤ 0.67. Most of these differentially regulated proteins are involved in apoptosis, oxidative stress, glycolytic metabolism, or cytoskeleton structuration.

Antihyperglycemic and Antilipidemic Properties of a Tea Infusion of the Leaves from Annona cherimola Miller on Streptozocin-Induced Type 2 Diabetic Mice.

The antihyperglycemic and antilipidemic effects of the tea infusion extracts of leaves from Annona cherimola Miller (IELAc-0.5, IELAc-1.5, and IELAc-3.0) were evaluated on normoglycemic (NG) and streptozocin-induced diabetic (STID) mice. In the acute test, IELAc-1.5 at 300 mg/kg bodyweight (bw) exhibited antihyperglycemic activity on STID mice since the first hour of treatment. Then, its antidiabetic potential was analyzed in a subchronic evaluation. IELAc-1.5 was able to reduce the blood glucose level, glycated hemoglobin (HbA1c), cholesterol (CHO), and triglycerides (TG); high-density lipoprotein (HDL) showed an increase at the end of treatment. IELAc-1.5 did not modify the urine profile at the end of the evaluation, and neither toxicity nor macroscopic organ damage were observed in acute and subchronic assays. In addition, a major flavonol glycoside present in the tea infusion extracts was identified using high-performance liquid chromatography with diode array detection (HPLC-DAD). The analysis of the tea infusion extracts by HPLC revealed that rutin was the major component. This study supports the use of tea infusions from Annona cherimola for the treatment of diabetes and suggests that rutin could be responsible, at least in part, for their antidiabetic properties.