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1.
Bioorg Med Chem Lett ; 49: 128264, 2021 10 01.
Artículo en Inglés | MEDLINE | ID: mdl-34280408

RESUMEN

In the present study we synthesized new methoxy derivatives of trans 2,3-diaryl-2,3-dihydrobenzofurans, starting from suitable trans 2,3-diaryloxiranes, using regio- and stereoselective nucleophilic oxiranyl ring-opening reactions. The compounds were tested as anti-inflammatories in U937 cells. All compounds showed a significant role in inhibiting the NF-κB pathway and were able to restore normal ROS and NO level upon LPS activation. Moreover, regarding inhibition of ACLY, enantioenriched (50% ee) 7a50 showed more potency than the racemic counterpart 7arac, together with a higher reduction of prostaglandin E2 production, thus suggesting a stereoselective interaction in this pathway.


Asunto(s)
Antiinflamatorios/farmacología , Benzofuranos/farmacología , ATP Citrato (pro-S)-Liasa/antagonistas & inhibidores , Antiinflamatorios/síntesis química , Benzofuranos/síntesis química , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/farmacología , Humanos , Estructura Molecular , Óxido Nítrico/metabolismo , Especies Reactivas de Oxígeno/metabolismo , Transducción de Señal/efectos de los fármacos , Factor de Transcripción ReIA/metabolismo , Células U937
2.
J Dairy Sci ; 102(10): 8587-8603, 2019 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-31400903

RESUMEN

Yogurt is a good source of probiotics, calcium, and proteins, but its content of vitamin D is low. Therefore, yogurt could be a good choice for vitamin D fortification to improve the positive health outcomes associated with its consumption. The primary aim of this systematic review and meta-analysis was to investigate the effect of vitamin D-fortified yogurt compared with plain yogurt on levels of serum 25-hydroxy vitamin D (25OHD). The secondary aim was to evaluate the effect of fortified yogurt on parathyroid hormone, anthropometric parameters, blood pressure, glucose metabolism, and lipid profile. We searched PubMed, Scopus, and Google Scholar for eligible studies; that is, randomized controlled trials (RCT) that compared vitamin D-fortified yogurt with control treatment without any additional supplement. Random-effects models were used to estimate pooled effect sizes and 95% confidence intervals. Findings from 9 RCT (n = 665 participants) that lasted from 8 to 16 wk are summarized in this review. The meta-analyzed mean differences for random effects showed that vitamin D-fortified yogurt (from 400 to 2,000 IU) increased serum 25OHD by 31.00 nmol/L. In addition, vitamin D-fortified yogurt decreased parathyroid hormone by 15.47 ng/L, body weight by 0.92 kg, waist circumference by 2.01 cm, HOMA-IR by 2.18 mass units, fasting serum glucose by 22.54 mg/dL, total cholesterol by 13.38 mg/dL, and triglycerides by 30.12 mg/dL compared with the controlled treatments. No publication bias was identified. Considerable between-study heterogeneity was observed for most outcomes. Vitamin D-fortified yogurt may be beneficial in improving serum 25OHD, lipid profile, glucose metabolism, and anthropometric parameters and decreasing parathyroid hormone level in pregnant women and adult and elderly subjects with or without diabetes, prediabetes, or metabolic syndrome.


Asunto(s)
Alimentos Fortificados , Valor Nutritivo , Vitamina D/administración & dosificación , Vitaminas/administración & dosificación , Yogur , Suplementos Dietéticos , Humanos , Ensayos Clínicos Controlados Aleatorios como Asunto , Vitamina D/análogos & derivados , Vitamina D/sangre , Vitamina D/farmacología , Vitaminas/farmacocinética
3.
Adv Gerontol ; 32(6): 1023-1033, 2019.
Artículo en Inglés | MEDLINE | ID: mdl-32160444

RESUMEN

We compare bioimpedance analysis (BIA) with dual-energy X-ray absorptiometry (DXA) in the assessment of free fat mass (FFM), fat mass (FM) and percentage of body fat under different conditions in relation to age categories, hydration parameters, body mass index (BMI) and sarcopenia. A cross-sectional analysis of body composition was estimated by BIA and DXA in 379 hospitalized elderly patients. In addition, estimates of FFM, FM and percentage of body fat were investigated across different conditions. Paired t-tests, Bland-Altman plot and intraclass correlation coefficient analysis were used to compare methods. Data showed an underestimation of means (BIA versus DXA) of FFM (women: 0,97 kg, p<0,01; men: 1,99 kg; p<0,01), and an overestimation of both the FM (women: +1,11 kg; p<0,01; men: +1,67 kg; p<0,01) and percentage of body fat (women: +2,07 %, p<0,01; men: +2,82 %, p<0,01). BIA underestimated FFM and overestimated FM and percentage of body fat in patients from the age group of 75 to 85 years, in patients with a total body water content <60%, in underweight and normal weight patients and in patients with sarcopenia (p<0,01). The intraclass coefficient results were indicative of poor reproducibility between BIA and DXA for FFM (women: +0,197; men: +0,250) and FM (women: +0,141; men +0,144). BIA is a good alternative for estimation of FFM and FM only in overweight or obese patients or in patients with good hydration status. BIA, on the other hand, is not an accurate method for assessing FFM in sarcopenic patients.


Asunto(s)
Absorciometría de Fotón , Composición Corporal , Impedancia Eléctrica , Anciano , Anciano de 80 o más Años , Estudios de Cohortes , Estudios Transversales , Femenino , Humanos , Masculino , Reproducibilidad de los Resultados
5.
Acta Ortop Mex ; 35(2): 142-152, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-34731914

RESUMEN

INTRODUCTION: In case of zinc (Zn) deficiency, this mineral becomes a nutrient limiting muscle and bone synthesis. The study in humans on zinc and bone health are few and no reviews have been published on this topic. So, the aim of this narrative review was to consider the state of the art on the correlation between blood zinc, daily zinc intake, zinc supplementation and bone mineral density. MATERIAL AND METHODS: A narrative review was performed. RESULTS: This review included 16 eligible studies: eight studies concern Zn blood; three studies concern Zn intake and five studies concern Zn supplementation. CONCLUSION: Blood zinc levels seem to be lower in subjects with pathology related to bone metabolism. Regarding daily zinc intake, a high proportion of the population, more than 20%, seems to be at risk of having inadequate zinc intake. The literature suggests that an insufficient zinc intake (less than 3 mg/day) could be a risk factor for fractures and for development of osteopenia and osteoporosis. Zinc supplementation (40-50 g/day) could have beneficial effects on bone health in terms of maintaining bone mineral density and faster healing in the event of fractures, with even better results in situations of reduced intake zinc through food.


INTRODUCCIÓN: En caso de deficiencia de zinc, se limitará la síntesis muscular y ósea. Los estudios en humanos sobre zinc y salud ósea son pocos y no se han publicado comentarios sobre este tema. Por lo tanto, el objetivo de esta revisión narrativa es considerar el estado de la técnica sobre la correlación entre el zinc en la sangre, la ingesta diaria de zinc, la suplementación de zinc y la densidad mineral ósea. MATERIAL Y MÉTODOS: Se realizó una revisión narrativa. RESULTADOS: Esta revisión incluyó 16 estudios elegibles: ocho se refieren al zinc en sangre; tres estudios se refieren a la ingesta de Zn y cinco estudios se refieren a la suplementación de Zn. CONCLUSIÓN: Los niveles de zinc en sangre parecen ser más bajos en sujetos con patología relacionada con el metabolismo óseo. En cuanto a la ingesta diaria de zinc, una alta proporción de la población, más de 20%, parece estar en riesgo de tener una ingesta inadecuada de zinc. La literatura sugiere que una ingesta insuficiente de zinc (menos de 3 mg/día) podría ser un factor de riesgo de fracturas y para el desarrollo de osteopenia y osteoporosis. La suplementación con zinc (40-50 g/día) podría tener efectos beneficiosos sobre la salud ósea para mantener la densidad mineral ósea y una curación más rápida en caso de fracturas, con resultados aún mejores en situaciones de reducción de la ingesta de zinc a través de los alimentos.


Asunto(s)
Enfermedades Óseas Metabólicas , Osteoporosis , Densidad Ósea , Suplementos Dietéticos , Humanos , Zinc
6.
Acta ortop. mex ; 35(2): 142-152, mar.-abr. 2021. tab, graf
Artículo en Inglés | LILACS-Express | LILACS | ID: biblio-1374160

RESUMEN

Abstract: Introduction: In case of zinc (Zn) deficiency, this mineral becomes a nutrient limiting muscle and bone synthesis. The study in humans on zinc and bone health are few and no reviews have been published on this topic. So, the aim of this narrative review was to consider the state of the art on the correlation between blood zinc, daily zinc intake, zinc supplementation and bone mineral density. Material and methods: A narrative review was performed. Results: This review included 16 eligible studies: eight studies concern Zn blood; three studies concern Zn intake and five studies concern Zn supplementation. Conclusion: Blood zinc levels seem to be lower in subjects with pathology related to bone metabolism. Regarding daily zinc intake, a high proportion of the population, more than 20%, seems to be at risk of having inadequate zinc intake. The literature suggests that an insufficient zinc intake (less than 3 mg/day) could be a risk factor for fractures and for development of osteopenia and osteoporosis. Zinc supplementation (40-50 g/day) could have beneficial effects on bone health in terms of maintaining bone mineral density and faster healing in the event of fractures, with even better results in situations of reduced intake zinc through food.


Resumen: Introducción: En caso de deficiencia de zinc, se limitará la síntesis muscular y ósea. Los estudios en humanos sobre zinc y salud ósea son pocos y no se han publicado comentarios sobre este tema. Por lo tanto, el objetivo de esta revisión narrativa es considerar el estado de la técnica sobre la correlación entre el zinc en la sangre, la ingesta diaria de zinc, la suplementación de zinc y la densidad mineral ósea. Material y métodos: Se realizó una revisión narrativa. Resultados: Esta revisión incluyó 16 estudios elegibles: ocho se refieren al zinc en sangre; tres estudios se refieren a la ingesta de Zn y cinco estudios se refieren a la suplementación de Zn. Conclusión: Los niveles de zinc en sangre parecen ser más bajos en sujetos con patología relacionada con el metabolismo óseo. En cuanto a la ingesta diaria de zinc, una alta proporción de la población, más de 20%, parece estar en riesgo de tener una ingesta inadecuada de zinc. La literatura sugiere que una ingesta insuficiente de zinc (menos de 3 mg/día) podría ser un factor de riesgo de fracturas y para el desarrollo de osteopenia y osteoporosis. La suplementación con zinc (40-50 g/día) podría tener efectos beneficiosos sobre la salud ósea para mantener la densidad mineral ósea y una curación más rápida en caso de fracturas, con resultados aún mejores en situaciones de reducción de la ingesta de zinc a través de los alimentos.

7.
Am J Med Sci ; 307(3): 228-32, 1994 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-8160715

RESUMEN

Modulation of the hypothalamic-pituitary-adrenal axis in major depression is thought to depend on the hypothalamus and other areas of the central nervous system, or both. Hypothalamic over-activity may be responsible for the hypercortisolism observed in 50% of depressed subjects. To investigate the relation between psychosocial factors and cardiovascular disease, morning (8 AM) plasma concentrations of cortisol and thromboxane B2 (the stable metabolite of thromboxane A2, an eicosanoid closely linked to thrombotic disorders) were measured by radioimmunoassay in 32 patients with major depression (DSM III) triggered by psychosocial events and in 9 nondepressed volunteers. The depressed patients were studied in two groups, 16 with cortisol levels under 90 ng/mL and 16 with levels over 90 ng/mL. All the healthy non-depressed subjects had cortisol values over 100 ng/mL. The depressed patients with high cortisol had significantly higher plasma TxB2 concentrations than the other two groups. In addition, plasma cortisol and TxB2 concentrations correlated significantly over the whole group of depressed patients and in the high cortisol sub-group but not in the low-cortisol sub-group or in the nondepressed subjects. These findings appear to support the recently proposed role of the hypothalamic dysfunction associated with affective disorders in the pathogenesis of cardiovascular disease.


Asunto(s)
Depresión/sangre , Hidrocortisona/sangre , Tromboxano B2/sangre , Adulto , Anciano , Anciano de 80 o más Años , Femenino , Humanos , Masculino , Persona de Mediana Edad
8.
Eur Neuropsychopharmacol ; 23(8): 978-87, 2013 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-22959654

RESUMEN

The use of clozapine and other antipsychotic drugs is known to be associated with a number of adverse metabolic side effects, including diabetes mellitus. These side effects could be, at least in part, the result of impaired islet cell function and abnormal insulin secretion, although the underlying mechanisms are unknown. The aim of this study is the identification of targets for clozapine related to the abnormal insulin secretion. We identify a specific activation of the transcriptional factor FOXA1, but not FOXA2 and FOXA3, by clozapine in HepG2 cells. Clozapine enhances FOXA1 DNA-binding and its transcriptional activity, increasing mitochondrial citrate carrier gene expression, which contains a FOXA1 site in its promoter. Haloperidol, a conventional antipsychotic drug, does not determine any increase of FOXA1 gene expression. We also demonstrate that clozapine upregulates FOXA1 and CIC gene expression in INS-1 cells only at basal glucose concentration. In addition, we find that abnormal insulin secretion in basal glucose conditions could be completely abolished by FOXA1 silencing in INS-1 cells treated with clozapine. The identification of FOXA1 as a novel target for clozapine may shed more light to understand molecular mechanism of abnormal insulin secretion during clozapine treatment.


Asunto(s)
Proteínas de Transporte de Anión/agonistas , Antipsicóticos/farmacología , Clozapina/farmacología , Factor Nuclear 3-alfa del Hepatocito/agonistas , Células Secretoras de Insulina/efectos de los fármacos , Insulina/metabolismo , Proteínas Mitocondriales/agonistas , Regulación hacia Arriba/efectos de los fármacos , Proteínas de Transporte de Anión/biosíntesis , Proteínas de Transporte de Anión/genética , Proteínas de Transporte de Anión/metabolismo , Antipsicóticos/efectos adversos , Línea Celular , Clozapina/administración & dosificación , Diabetes Mellitus/inducido químicamente , Regulación de la Expresión Génica/efectos de los fármacos , Silenciador del Gen , Glucosa/metabolismo , Haloperidol/efectos adversos , Haloperidol/farmacología , Células Hep G2 , Factor Nuclear 3-alfa del Hepatocito/antagonistas & inhibidores , Factor Nuclear 3-alfa del Hepatocito/genética , Factor Nuclear 3-alfa del Hepatocito/metabolismo , Humanos , Secreción de Insulina , Células Secretoras de Insulina/metabolismo , Proteínas Mitocondriales/biosíntesis , Proteínas Mitocondriales/genética , Proteínas Mitocondriales/metabolismo , Transportadores de Anión Orgánico , Regiones Promotoras Genéticas/efectos de los fármacos , ARN Mensajero/metabolismo , ARN Interferente Pequeño , Proteínas Recombinantes/biosíntesis , Proteínas Recombinantes/química , Proteínas Recombinantes/metabolismo , Elementos de Respuesta/efectos de los fármacos
9.
J Med Chem ; 56(1): 60-72, 2013 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-23171045

RESUMEN

The preparation of a series of 2-(aryloxy)-3-phenylpropanoic acids, resulting from the introduction of different substituents into the biphenyl system of the previously reported peroxisome proliferator-activated receptor α/γ (PPARα/γ) dual agonist 1, allowed the identification of new ligands with higher potency on PPARα and fine-tuned moderate PPARγ activity. For the most promising stereoisomer (S)-16, X-ray and calorimetric studies in PPARγ revealed, at high ligand concentration, the presence of two molecules simultaneously bound to the receptor. On the basis of these results and docking experiments in both receptor subtypes, a molecular explanation was provided for its different behavior as a full and partial agonist of PPARα and PPARγ, respectively. The effects of (S)-16 on mitochondrial acylcarnitine carrier and carnitine-palmitoyl-transferase 1 gene expression, two key components of the carnitine shuttle system, were also investigated, allowing the hypothesis of a more beneficial pharmacological profile of this compound compared to the less potent PPARα agonist fibrates currently used in therapy.


Asunto(s)
Carnitina O-Palmitoiltransferasa/metabolismo , Proteínas de Transporte de Membrana/metabolismo , Proteínas Mitocondriales/metabolismo , PPAR alfa/agonistas , PPAR gamma/agonistas , Propionatos/síntesis química , Calorimetría , Carnitina O-Palmitoiltransferasa/genética , Línea Celular Tumoral , Cristalografía por Rayos X , Humanos , Proteínas de Transporte de Membrana/genética , Proteínas Mitocondriales/genética , Simulación del Acoplamiento Molecular , Propionatos/química , Propionatos/farmacología , Conformación Proteica , Estereoisomerismo , Relación Estructura-Actividad , Termodinámica , Activación Transcripcional , Regulación hacia Arriba
10.
G Batteriol Virol Immunol ; 77(7-12): 208-14, 1984.
Artículo en Italiano | MEDLINE | ID: mdl-6545800

RESUMEN

By the end of the year 1979 and the beginning of 1980 in the departments of babies and obstetrics of our hospital, we registered an epidemic episode of umbilical and ocular infection for hospitality by Pseudomonas aeruginosa and Staphylococcus aureus (about the 85% of the umbilical and conjunctival tampons sent to laboratory turned out be positive of these germs). At once we disposed a series of environmental checks; the result was that the cause of infection was originated in the wash bowl of these departments and, above all the ones fit to bath babies in the department of obstetrics. After timely measures of disinfection, further environmental checks proved the disappearing of these germs, only keeping a light positivity for the Pseudomonas in a wash bowl of the department of babies. We didn't have serious or mortal cases and all the strains by us isolated proved a good sensibility towards the antibiotics.


Asunto(s)
Infección Hospitalaria/microbiología , Oftalmopatías/epidemiología , Departamentos de Hospitales , Neonatología , Servicio de Ginecología y Obstetricia en Hospital , Infecciones por Pseudomonas/epidemiología , Infecciones Estafilocócicas/epidemiología , Ombligo/microbiología , Adulto , Brotes de Enfermedades , Contaminación de Equipos , Oftalmopatías/microbiología , Femenino , Humanos , Recién Nacido , Italia , Embarazo
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