Inhibitory Activity of 4-Benzylidene Oxazolones Derivatives of Cinnamic Acid on Human Acetylcholinesterase and Cognitive Improvements in a Mouse Model.

We synthesized seven (Z)-benzylidene-2-(E)-styryloxazol-5(4H)-ones derivatives of cinnamic acid and evaluated the ability of these compounds to inhibit human acetylcholinesterase (hAChE). The most potent compound was evaluated for cognitive improvement in short-term memory. The seven compounds reversibly inhibited the hAChE between 51 and 75% at 300 µM, showed an affinity (Ki) from 2 to 198 µM, and an IC50 from 9 to 246 µM. Molecular docking studies revealed that all binding moieties are involved in the non-covalent interactions with hAChE for all compounds. In addition, in silico pharmacokinetic analysis was carried out to predict the compounds' blood-brain barrier (BBB) permeability. The most potent inhibitor of hAChE significantly improved cognitive impairment in a modified Y-maze test (5 µmol/kg) and an Object Recognition Test (10 µmol/kg). Our results can help the rational design of hAChE inhibitors to work as potential candidates for treating cognitive disorders.

Memantine as a neuroprotective agent in ischemic stroke: Preclinical and clinical analysis.

The primary mechanism for neuron death after an ischemic stroke is excitotoxic injury. Excessive depolarization leads to NMDA-mediated calcium entry to the neuron and, subsequently, cellular death. Therefore, the inhibition of the NMDA channel has been proposed as a neuroprotective measure in ischemic stroke. The high morbimortality associated with stroke warrants new therapies that can improve the functional prognosis of patients. Memantine is a non-competitive NMDA receptor antagonist which has gained attention as a potential drug for ischemic stroke. Here we analyze the available preclinical and clinical evidence concerning the use of memantine following an ischemic stroke. Preclinical evidence shows inhibition of the excitotoxic cascade, as well as improved outcomes in terms of motor and sensory function with the use of memantine. The available clinical trials of high-dose memantine in patients poststroke have found that it can improve patients' NIHSS and Barthel index and help patients with poststroke aphasia and intracranial hemorrhage. These results suggest that memantine has a clinically relevant neuroprotective effect; however, small sample sizes and other study shortcomings limit the impact of these findings. Even so, current studies show promising results that should serve as a basis to promote future research to conclusively determine if memantine does improve the outcomes of patients' post-ischemic stroke. We anticipate that future trials will fill current gaps in knowledge, and these latter results will broaden the therapeutic arsenal for clinicians looking to improve the prognosis of patients poststroke.

Hybrid Systems of Nanofibers and Polymeric Nanoparticles for Biological Application and Delivery Systems.

Nanomedicine is a new discipline resulting from the combination of nanotechnology and biomedicine. Nanomedicine has contributed to the development of new and improved treatments, diagnoses, and therapies. In this field, nanoparticles have notable importance due to their unique properties and characteristics, which are useful in different applications, including tissue engineering, biomarkers, and drug delivery systems. Electrospinning is a versatile technique used to produce fibrous mats. The high surface area of the electrospun mats makes them suitable for applications in fields using nanoparticles. Electrospun mats are used for tissue engineering, wound dressing, water-treatment filters, biosensors, nanocomposites, medical implants, protective clothing materials, cosmetics, and drug delivery systems. The combination of nanoparticles with nanofibers creates hybrid systems that acquire properties that differ from their components' characteristics. By utilizing nanoparticles and nanofibers composed of dissimilar polymers, the two synergize to improve the overall performance of electrospinning mats and nanoparticles. This review summarizes the hybrid systems of polymeric nanoparticles and polymeric nanofibers, critically analyzing how the combination improves the properties of the materials and contributes to the reduction of some disadvantages found in nanometric devices and systems.

Micronutrient Deficiency Pre- and Post-bariatric Metabolic Surgery in Latin America: a Systematic Review.

BACKGROUND: Persons submitted to bariatric metabolic surgery present micronutrient deficiency before and after surgery, due to the lack of proper supplementation. The aim of this study is to establish the prevalence of micronutrient deficiency in people before and after bariatric metabolic surgery in Latin America. METHODS: This review was conducted in accordance with the 2020 PRISMA Guidelines. RESULTS: Twenty-seven studies and 2135 participants were included. The highest prevalence of deficiency before surgery was reported for vitamin D (74%), zinc (71%), and hemoglobin (62%); after surgery, they were vitamin A (90.6%), vitamin D (90%), and zinc (68%). CONCLUSIONS: There is a high prevalence of micronutrient deficiency before and after bariatric metabolic surgery from Latin American persons; the micronutrients with the highest deficiency prevalence were vitamin D before and vitamin A after bariatric metabolic surgery.

Self-care model and body image in adults after a bariatric surgery. / Modelo de autocuidado e imagem corporal em adultos pós cirurgia bariátrica.

OBJECTIVE: the aim of the present article was to test a self-care model explained by the relationship between self-efficacy, body image, obsessive-compulsive disorder, and depression in people with bariatric surgery in the city of Tijuana, Baja California, Mexico. METHOD: this was a correlational cross-sectional study carried out between August and December 2020. Validated instruments were administered to 102 participants to measure their self-care capacity, general self-efficacy, psychopathological symptoms, and body image perception and satisfaction. The variables of interest were analyzed using descriptive statistics and the Pearson and Spearman correlation coefficients were used to develop a model using path analysis. RESULT: a significant model was obtained with adequate goodness-of-fit indicators (chi-square χ2 (8) = 11.451, p = .177; root mean square error of approximation (RMSEA)= 0.000; goodness-of-fit index (GFI)= 0.965; comparative fit index (CFI)= 0.985; parsimonious normed fit index (PNFI)= 0.509, and Akaike information criterion (AIC)= 37.451). Self-efficacy (Zß=0.294) and body image dissatisfaction (So= -0.376) were shown to influence self-care abilities while psychopathological symptoms influenced body dissatisfaction: obsessive-compulsive disorder (Zß=0.370) and depression (Zß=0.320). CONCLUSION: adequate levels of self-efficacy and body satisfaction predict a high capacity for self-care.

Modelo de autocuidado e imagem corporal em adultos pós cirurgia bariátrica / Self-care model and body image in adults after a bariatric surgery / Modelo de autocuidado e imagen corporal en adultos post-cirugía bariátrica

Resumo Objetivo: testar um modelo de autocuidado explicado pela relação entre autoeficácia, imagem corporal, transtorno obsessivo-compulsivo e depressão em pessoas com cirurgia bariátrica na cidade de Tijuana, no México. Método: estudo transversal correlacional realizado entre agosto e dezembro de 2020. Instrumentos validados foram aplicados a 102 participantes para medir sua capacidade de autocuidado, autoeficácia geral, sintomas psicopatológicos, e percepção e satisfação com a imagem corporal. As variáveis de interesse foram analisadas utilizando estatísticas descritivas e correlações de Pearson e Spearman para finalmente desenvolver um modelo utilizando a análise de caminho (path analysis). Resultados: foi obtido um modelo significativo com bons indicadores de bondade de ajuste (qui-quadrado χ 2 (8)= 11,451, p = 0,177; raiz quadrada da média do erro de aproximação (RMSEA)= 0,000; índice de bondade de ajuste (GFI)= 0,965; índice de ajuste comparativo (CFI)= 0,985; índice de ajuste normalizado parcimonioso (PNFI)= 0,509 e critério de informação de Akaike (AIC)= 37,451). A autoeficácia (Zβ= 0,294) e a insatisfação com a imagem corporal (Zβ= -0,376) demonstraram ter um efeito sobre as capacidades de autocuidado, enquanto os sintomas psicopatológicos influenciam a insatisfação corporal: transtorno obsessivo-compulsivo (Zβ= 0,370) e depressão (Zβ= 0,320). Conclusão: níveis adequados de autoeficácia e satisfação corporal predizem uma alta capacidade de autocuidado.

Abstract Objective: the aim of the present article was to test a self-care model explained by the relationship between self-efficacy, body image, obsessive-compulsive disorder, and depression in people with bariatric surgery in the city of Tijuana, Baja California, Mexico. Method: this was a correlational cross-sectional study carried out between August and December 2020. Validated instruments were administered to 102 participants to measure their self-care capacity, general self-efficacy, psychopathological symptoms, and body image perception and satisfaction. The variables of interest were analyzed using descriptive statistics and the Pearson and Spearman correlation coefficients were used to develop a model using path analysis. Result: a significant model was obtained with adequate goodness-of-fit indicators (chi-square χ2 (8) = 11.451, p = .177; root mean square error of approximation (RMSEA)= 0.000; goodness-of-fit index (GFI)= 0.965; comparative fit index (CFI)= 0.985; parsimonious normed fit index (PNFI)= 0.509, and Akaike information criterion (AIC)= 37.451). Self-efficacy (Zβ=0.294) and body image dissatisfaction (So= -0.376) were shown to influence self-care abilities while psychopathological symptoms influenced body dissatisfaction: obsessive-compulsive disorder (Zβ=0.370) and depression (Zβ=0.320). Conclusion: adequate levels of self-efficacy and body satisfaction predict a high capacity for self-care.

Resumen Objetivo: probar un modelo de autocuidado explicado por la relación entre autoeficacia, imagen corporal, obsesión-compulsión y depresión en personas con cirugía bariátrica de la ciudad de Tijuana, B.C. Método: estudio transversal correlacional realizado entre agosto y diciembre de 2020. Se aplicaron instrumentos validados a 102 participantes para medir su capacidad de autocuidado, autoeficacia general, síntomas psicopatológicos, percepción y satisfacción de la imagen corporal. Las variables de interés fueron analizadas mediante estadística descriptiva y correlaciones de Pearson y Spearman para finalmente elaborar un modelo mediante análisis de ruta (Path Analysis). Resultados: se obtuvo un modelo significativo con buenos indicadores de bondad de ajuste (chi-cuadrado χ 2 (8)= 11.451, p = .177; error de aproximación raíz-media-cuadrada (RMSEA)= 0.000; índice de bondad de ajuste (GFI)= 0.965; índice de ajuste comparativo (CFI)= 0.985; índice de ajuste normado parsimonioso (PNFI)= 0.509 y criterio de información de Akaike (AIC)= 37.451). Se demostró que la autoeficacia (Zβ= 0.294) y la insatisfacción de la imagen corporal (Zβ= -0.376) tienen un efecto sobre las capacidades de autocuidado mientras que los síntomas psicopatológicos influyen sobre la insatisfacción corporal: obsesión-compulsión (Zβ= 0.370) y depresión (Zβ= 0.320). Conclusión: los niveles adecuados de autoeficacia y satisfacción corporal predicen una alta capacidad de autocuidado.

Efficacy of a multivitamin adherence program based on cognitive dissonance for bariatric patients: A randomized controlled trial.

BACKGROUND AND OBJECTIVES: Micronutrient deficiencies are common among bariatric patients; this study aimed to determine whether a cognitive dissonance-based virtual program improved adherence to multivitamin use in bariatric patients from northern Mexico. METHODS AND STUDY DESIGN: A randomized controlled trial of the supplementation strategy was conducted over three months. The participants were randomized to an intervention or waitlisted control group and received two psycho-educative and four cognitive dissonance virtual sessions. Multiple linear regression was used to determine standardized estimates of associations between the intervention and dependent variables. Two path analyses were evaluated considering baseline and post-test measurements. RESULTS: Intervention was associated with higher concentrations of Hb (ß=0.758, p<0.001), vitamin D (ß=0.577, p<0.001), iron (ß=0.523, p<0.001), folate (ß=0.494, p<0.01), calcium (ß=0.452, p<0.01), higher adherence (ß=0.467, p<0.001), and level of knowledge (ß=0.298, p<0.05. CONCLUSIONS: The dissonance-based intervention potentiated the level of supplementation adherence. A higher level of adherence was reflected in micronutrient concentrations, thus providing confirmation of intervention. Thus, support is found for a multidisciplinary clinical practice that enhances nutrition status after bariatric surgery for obesity.

Association between Stress and Metabolic Syndrome and its Mediating Factors in University Students.

OBJECTIVES: In this study, we evaluated the association between perceived stress and indicators of metabolic syndrome and how this association is mediated by sleep problems, unhealthy eating habits, and night eating syndrome, in addition to serum levels of ghrelin and cortisol in university students. METHODS: We recruited 192 students from a public university in Mexico. Weight, height, waist circumference and blood pressure were taken in accordance with standard protocols. Validated questionnaires were used to assess perceived stress, sleep quality and eating habits. Fasting blood samples were taken to measure ghrelin, cortisol, triglycerides, glucose and HDL-C. RESULTS: Path Analysis indicated direct positive effects of stress over PSQI (ß = 0.341) and NES (ß = 0.443); PSQI over NES (ß = 0.233) and NES over glucose (ß = 0.170), triglycerides over LDL-C (ß = 0.215), waist circumference over SBP (ß = 0.259). Likewise, standardized negative regression weights of PSQI over Diet Quality Index (ß = -0.239) and ghrelin concentrations (ß = -0.132), ghrelin over Diet Quality Index (ß = -0.188) and waist circumference (ß = -0.147). Diet Quality Index over triglycerides (ß = -0.184); sleep duration over systolic blood pressure (ß = -0.242); waist circumference over HDL-C (ß = -0.256). CONCLUSION: Psychological stress leads to increased indicators of MetS via decreased sleep quality, inadequate eating habits and eating behavior in university students.

Body Image, Anxiety, and Bulimic Behavior during Confinement Due to COVID-19 in Mexico.

BACKGROUND: The potential impact of the COVID-19 pandemic on weight, shape-related appearance behaviors (body image dissatisfaction), and bulimic symptoms in nonclinical participants is poorly evaluated. This study aimed to identify the relationship between labor status, confinement degree due to COVID-19, dissatisfaction with body image, and anxiety and to discover its effect on bulimic behavior in Mexican adults. METHODS: A cross-sectional study was conducted with a non-probabilistic sample of 276 participants via an online survey. Questions addressed their anxiety, body image dissatisfaction, and bulimic behavior. RESULTS: The path analysis showed direct effects on the confinement degree (ß = -0.157); of the labor situation (ß = -0.147) and gender (ß = 0.129) on anxiety; of dissatisfaction on bulimic behavior (ß = 0.443) and anxiety about bulimic behavior (ß = 0.184); and dissatisfaction (ß = 0.085). CONCLUSIONS: The confinement, gender, and labor status are predictors of anxiety, while anxiety and body dissatisfaction directly influence bulimic behavior.

Epicatechin and quercetin exhibit in vitro antioxidant effect, improve biochemical parameters related to metabolic syndrome, and decrease cellular genotoxicity in humans.

Metabolic syndrome is a condition whose incidence has been increasing around the world. It promotes a metabolic state of chronic systemic inflammation, correlated to cellular stress and genetic mutations, and subsequently with deadly chronic diseases, such as type 2 diabetes mellitus, cardiovascular diseases, and cancer. A randomized placebo-controlled study (n = 156) was conducted to determine the effects of consuming an enriched bread with 0.05% of a 1:1 mixture of (-)-epicatechin and quercetin on anthropometric and biochemical parameters of the participants. As a result, total cholesterol, LDL-cholesterol, total triglycerides, and fasting plasma glucose significantly decreased after three months of daily enriched bread consumption. Nuclear abnormalities in buccal epithelium cells also decreased (15.8 ± 3.2 down to 8.3 ± 1.0), showing a genoprotective effect. The antioxidant properties of these compounds were observed by monitoring changes in the cytoplasmic redox tone of intact Caco-2 cells expressing HyPer, a fluorescent redox biosensor. The combination of (-)-epicatechin and quercetin changes the cytoplasmic redox ambient in living cells and significantly improves biochemical parameters related to metabolic syndrome, and decreases the number of cell abnormalities in buccal epithelium cells of patients.

Impact of Spirulina maxima Intake and Exercise (SIE) on Metabolic and Fitness Parameters in Sedentary Older Adults with Excessive Body Mass: Study Protocol of a Randomized Controlled Trial.

Life expectancy has increased unprecedentedly in recent decades, benefiting the longevity of the world's population. The most frequent pathological conditions presented in this age group include excessive body fat, frailty, and hypercholesterolemia. These pathological characteristics condition general health and autonomy in adults to carry out their usual activities. In this sense, the search for a healthy lifestyle is necessary, consisting in a healthy diet that includes supplementation with nutraceuticals and the daily practice of physical activity. This study protocol aims to evaluate the independent and synergistic effect of 12 weeks of Spirulina maxima intake (5 g/day), with or without an exercise program on metabolic and fitness parameters of 52 sedentary older adults with excessive body mass in a double-blind, randomized, crossover, controlled trial design. The main findings from this trial will provide novel evidence for future interventions designed for the elderly population and the result will be disseminated through peer-reviewed journals and international meetings. ClinicalTrials.gov identification number: NCT04658875 (Effect of Spirulina maxima and Exercise on General Fitness and Blood Lipids in Older Adults).

Adverse drug reactions' reporting in a Mexican hospital.

OBJECTIVES: To summarize the procedure for reporting adverse drug reactions (ADRs) in a Mexican hospital, with the purpose of promoting and facilitating the report of ADRs by the heath team. We outline the relevance of pharmacists in performing these activities in Mexican hospitals. METHODS: A pharmacovigilance study was carried out following the establishment of the Pharmacovigilance Unit of a Mexican hospital on January 2014 through March 2019. KEY FINDINGS: There is an undernotification rate of ADRs, since only 137 ADRs were notified in a five-year period, mostly by biopharmaceutical chemists holding bachelor's degrees that were acting as pharmacists. CONCLUSIONS: To improve the safety of medications, it is necessary to improve ADR notifications in Mexico's health system. One important step in this direction is to establish a Pharmacy degree with training for promoting and performing ADR notifications.

Radiation Grafting of a Polymeric Prodrug onto Silicone Rubber for Potential Medical/Surgical Procedures.

Silicone rubber (SR) is a material used for medical procedures, with a common example of its application being in implants for cosmetic or plastic surgeries. It is also an essential component for the development of medical devices. SR was functionalized with the polymeric prodrug of poly(2-methacryloyloxy-benzoic acid) (poly(2MBA)) to render the analgesic anti-inflammatory drug salicylic acid by hydrolysis. The system was designed by functionalizing SR films (0.5 cm × 1 cm) with a direct grafting method, using gamma irradiation (60Co source) to induce the polymerization process. The absorbed dose (from 20 to 100 kGy) and the monomer concentration (between 0.4 and 1.5 M) were critical in controlling the surface and the bulk modifications of SR. Grafting poly(2MBA) onto SR (SR-g-2MBA) were characterized by attenuated total reflectance Fourier transform infrared spectroscopy, thermogravimetric analysis, scanning electron microscopy/energy-dispersive X-ray spectrometry, fluorescence microscopy, the contact angle, and the swelling. SR-g-2MBA demonstrated the drug's sustained and pH-dependent release in simulated physiological mediums (pH = 5.5 and 7.4). The drug's release was quantified by high-performance liquid chromatography and confirmed by gas chromatography-mass spectrometry. Finally, cytocompatibility was demonstrated in murine fibroblast and human cervical cancer cell lines. The developed systems provide new polymeric drug release systems for medical silicone applications.

Mucoadhesive electrospun nanofibers for drug delivery systems: applications of polymers and the parameters' roles.

Electrospun nanofibers have been widely studied for many medical applications. They can be designed with specific features, including mucoadhesive properties. This review summarizes the polymeric scaffolds obtained by the electrospinning process that has been applied for drug release in different mucosal sites such as oral, ocular, gastroenteric, vaginal, and nasal. We analyzed the electrospinning parameters that have to be optimized to create reproducible and efficient mucoadhesive nanofibers, among them are: electrical field, polymer concentration, viscosity, flow rate, needle-collector distance, solution conductivity, solvent, environmental parameters, and electrospinning setup. We also revised the mucoadhesive theories as well as the mucoadhesive properties of the polymers used. This review shows that the most studied mucosal site is the oral cavity, because it is accessible and easy to evaluate, while the rest are uncomfortable for the patient and difficult to assess in vivo. We found problems that need to be solved for mucoadhesive electrospun nanofibers, such as improving adhesion strength and mucosal permanence time, and the design of unidirectional release, multilayer systems for the treatment of several pathologies, to ensure the drug concentration in the tissue or target organ.

Drugs Loaded into Electrospun Polymeric Nanofibers for Delivery.

The electrospinning technique is a useful and versatile approach for conversion of polymeric solutions into continuous fibers, ranging from a few micrometers (10-100 µm) to the scale of nanometers (10- 100 nm) in diameters. This technique can be used in a vast number of polymers, in some cases after modifying them to the required properties. The high surface-to-volume ratio of the fibers can improve some processes like cell binding and proliferation, drug loading, and mass transfer processes. One of the most important and studied areas of electrospinning is in the drug delivery field, for the controlled release of active substances ranging from antibiotics and anticancer agents, to macromolecules such as proteins and DNA. The advantage of this method is that a wide variety of low solubility drugs can be loaded into the fibers to improve their bioavailability or to attain controlled release. This review presents an overview of the reported drugs loaded into electrospun polymeric nanofibers to be used as drug delivery systems. These drugs are classified by their applications in pharmacy.

Neuropsychiatric Disorders in Farmers Associated with Organophosphorus Pesticide Exposure in a Rural Village of Northwest México.

This study aims to determine the degree of acetylcholinesterase inhibition and neurological symptoms for each of the psychiatric disorders diagnosed in the farm workers of a rural population in the state of Baja California, Mexico. We conducted a cross-sectional study on 140 agricultural workers (exposed participants). The study was run using the Mini International Neuropsychiatric Interview Diagnostic Test (MINI), a pre-established questionnaire to diagnose the mental state of each agricultural worker. Analysis of enzymatic activity was carried out using the modified Ellman method. The results showed that, among agricultural workers with slightly inhibited enzymatic activity, 25% met the criteria for the diagnosis of major depression with suicidal attitudes, 23.9% with inhibited enzymatic activity showed generalized anxiety, 23.5% showed combined depression⁻anxiety, and 22% met the criteria for major depression and no psychiatric diagnosis disorder. These results suggest the need for the development of effective public-health strategies to inform farm workers about integrated pesticide management in order to prevent serious health complications.

A Summary of Electrospun Nanofibers as Drug Delivery System: Drugs Loaded and Biopolymers Used as Matrices.

Recently, electrospun polymeric nanofibers have proven to be an interesting strategy for drug delivery systems application. The high surface-to-volume ratio of the fibers can improve some processes, such as cell binding and proliferation, drug loading, and mass transfer processes. One of the most important and studied areas of electrospinning is in the drug delivery field, for the controlled release of active substances ranging from antibiotics and anticancer agents to macromolecules such as proteins and DNA. The advantage of this method is that a wide variety of low solubility drugs can be loaded into the fibers to improve their bioavailability or to attain controlled release. This review presents an overview of the reported drugs loaded into polymeric nanofibers, to be used as drug delivery systems. For instance, it presents the reports on drugs with different bioactivities such as antiinflammatory, anti-microbial, anticancer, cardiovascular, anti-histamine, gastrointestinal, palliative and contraceptive drugs, etc. It also analyzes the electrospinning techniques used in each system, as well as the polymers used as matrices for the preparation of the nanofibers; unfolding the advantages of electrospun polymeric nanofibers over other drug delivery systems. This review intends to enlist and summarize the reported literature concerning this topic. In addition, it proposes future research in the field.

Hydrophobic weak acid polymers as controlled release carriers.

Poly(carboxyalkyl methacrylates) were studied as a cationic-drug delivery system, at pH 6.8 and 8.0. Different polymer/drug complexes were used to prepare compressed tablets. By kinetics experiments, we have found that drug release is dependent on both the hydrophobicity of the whole complex and the pH of the environment. Furthermore, a mechanism of dissociation/erosion clearly describes the drug release from a complex formed by a polymer soluble at target pH; otherwise, a mechanism of dissolution/diffusion is depicted. Additionally, we have observed that hydrophilic fillers increase the drug release rate. Since our results using different polymer/drug complexes exhibit pH-sensitive drug release, we propose that the poly(carboxyalkyl methacrylates) have potential as a colon-specific drug-delivery system.