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1.
Molecules ; 28(21)2023 Nov 02.
Article in English | MEDLINE | ID: mdl-37959813

ABSTRACT

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.


Subject(s)
Acetylcholinesterase , Alzheimer Disease , Animals , Mice , Humans , Acetylcholinesterase/metabolism , Molecular Docking Simulation , Oxazolone , Cholinesterase Inhibitors/chemistry , Disease Models, Animal , Cognition , Structure-Activity Relationship
3.
ACS Omega ; 7(23): 19640-19647, 2022 Jun 14.
Article in English | MEDLINE | ID: mdl-35721970

ABSTRACT

Silicon carbide (SiC) has become an extraordinary photonic material. Achieving reproducible self-formation of silicon quantum dots (SiQDs) within SiC matrices could be beneficial for producing electroluminescent devices operating at high power, high temperatures, or high voltages. In this work, we use a remote plasma-enhanced chemical vapor deposition system to grow SiC thin films. We identified that a particular combination of 20 sccm of CH4 and a range of 58-100 sccm of H2 mass flow with 600 °C annealing allows the abundant and reproducible self-formation of SiQDs within the SiC films. These SiQDs dramatically increase the photoluminescence-integrated intensity of our SiC films. The photoluminescence of our SiQDs shows a normal distribution with positive skewness and well-defined intensity maxima in blue regions of the electromagnetic spectrum (439-465 nm) and is clearly perceptible to the naked eye.

4.
Rev. enferm. Inst. Mex. Seguro Soc ; 30(2): 37-42, 01-abr-2022. tab
Article in Spanish | LILACS, BDENF - Nursing | ID: biblio-1378934

ABSTRACT

Introducción: la intervención de enfermería en pacientes sometidos a cateterismo cardiaco constituye el eje articular de las acciones de planeación, desarrollo y evaluación; lo que permite atender el proceso de aprendizaje. Objetivo: evaluar la relación entre el nivel de conocimiento y ansiedad de los pacientes sometido a cateterismo cardiaco, antes y después de aplicar una intervención educativa. Metodología: investigación con enfoque cuantitativo, descriptivo, transversal y exploratorio a 70 pacientes sometidos a cateterismo cardiaco por primera vez, se aplicaron dos instrumentos validados para medir el nivel de conocimiento y ansiedad con un Alfa de Cronbach de 0.90; la recolección fue en dos fases, pretest y postest, la primera antes de la cirugia; la segunda posterior al procedimiento y se compararon los resultados de ambos test en búsqueda de mejores resultados. Resultados: media de edad de 60 - 79 años; 68.6% hombres y 31.4% mujeres; el nivel de conocimientos del pretest fue de 52.9% regular y postest, excelente con un 50%; en cuanto a la ansiedad el pretest el 97.1% reportó grave, mientras que en el postest, el 80% reportó moderado. Conclusiones: el aporte de conocimientos por parte del personal de enfermería a través del rol educador, favorece a los pacientes que son sometidos a un cateterismo cardiaco, que se refleja en disminución de ansiedad e incremento de calidad de vida.


Introduction:The nursing intervention in patients undergoing cardiac catheterization constitutes the articular axis of planning, development and evaluation actions; which allows to attend the learning process. Objective: To evaluate the relationship between the level of knowledge and anxiety of the patient undergoing cardiac catheterization, before and after applying an educational intervention. Methodology: Investigation with a quantitative, descriptive, cross-sectional and exploratory approach to 70 patients undergoing cardiac catheterization for the first time. Two validated instruments were applied to measure the level of knowledge and anxiety with a Cronbach's Alpha of 0.90; the collection was in two phases, pre and post test, the first before surgery; the second after the procedure, the results of both tests were compared in search of better results. Results: Average age of 60-79 years, 68.6% men and 31.4% women; the level of knowledge of the pre-test was 52.9% regular and post-test, excellent with 50%; regarding anxiety, the pre-test 97.1% serious, post-test, 80% moderate. Conclusions: The contribution of knowledges by the nursing staff through the educator role, favors patients who undergo cardiac catheterization, which is reflected in the reduction of seniority and the increase in the quality of life.


Subject(s)
Humans , Male , Female , Cardiac Catheterization/instrumentation , Professional Training , Nursing Staff/education , Epidemiology, Descriptive , Cross-Sectional Studies , Mexico
5.
Rev. ADM ; 79(1): 20-27, ene.-feb. 2022. ilus, tab
Article in Spanish | LILACS | ID: biblio-1361506

ABSTRACT

Los sistemas cementantes han mejorado notablemente, los objetivos que persiguen los nuevos cementos es que la adhesión sea duradera y conseguir siempre que sea posible una interface cerrada con un sellado perfecto. Se han podido desarrollar nuevas técnicas y nuevos materiales de cementación que han ido perfeccionando la unión del material restaurador al diente. En el presente estudio se compara la fuerza de adhesión a dentina de cementos de autograbado y cementos de grabado total para comprobar los efectos positivos en el grabado de la dentina. Para el estudio se utilizaron dos cementos a base de resina (RelyX U200 Clicker 3M y RelyX Ultimate 3M). Se encapsularon 40 molares en acrílico en dos grupos de 20 muestras para la aplicación de dos sistemas cementantes de autograbado (grupo 1) y de grabado total (grupo 2), respectivamente, se desgastaron hasta descubrir la dentina; siguiendo las especificaciones del fabricante se colocó el cemento en cada grupo, y después se sometieron a pruebas de cizalla en una máquina de ensayo universal Instron. La medida expresada en megapascales (MPa) fue: grupo 1 = 7.5569 y grupo 2 = 12.6444. En este caso fueron analizados dos grupos, tomándose la primera significancia bilateral. Se realiza la prueba en t de Student, con 95% de intervalo de confianza en la diferencia, demostrando así que el cemento RelyX Ultimate 3M tiene mayor fuerza de adhesión que el cemento RelyX U200 Clicker 3M. Nuestra investigación fue factible y llegamos a nuestro propósito, en el cual comprobamos la mayor adhesión de cementos de grabado total, los cuales son sometidos a un previo tratamiento del diente (AU)


Subject(s)
Humans , Adolescent , Adult , Acid Etching, Dental , Cementation , Dentin-Bonding Agents , Resin Cements , Shear Strength , Tensile Strength , Dentin/drug effects
6.
Asia Pac J Clin Nutr ; 30(4): 602-613, 2021 Dec.
Article in English | MEDLINE | ID: mdl-34967189

ABSTRACT

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.


Subject(s)
Bariatric Surgery , Obesity, Morbid , Cognitive Dissonance , Dietary Supplements , Folic Acid , Humans , Micronutrients , Vitamins
7.
Am J Health Behav ; 45(6): 1091-1102, 2021 11 15.
Article in English | MEDLINE | ID: mdl-34969419

ABSTRACT

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.


Subject(s)
Metabolic Syndrome , Blood Pressure , Body Mass Index , Cross-Sectional Studies , Ghrelin , Glucose , Humans , Hydrocortisone , Mediation Analysis , Metabolic Syndrome/epidemiology , Students , Triglycerides , Universities , Waist Circumference
8.
Healthcare (Basel) ; 9(11)2021 Oct 25.
Article in English | MEDLINE | ID: mdl-34828482

ABSTRACT

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.

9.
Chem Biodivers ; 18(8): e2100369, 2021 Aug.
Article in English | MEDLINE | ID: mdl-34138517

ABSTRACT

A decoction prepared from the aerial parts of Melampodium divaricatum showed antinociceptive and antihyperalgesic responses when tested in the formalin model in mice. From the CH2 Cl2 fraction of the decoction, two non-previously reported secondary metabolites, 3-O-ß-D-glucopyranosyl-16α-hydroxy-ent-kaurane (1) and melampodiamide (2) [(2'R*,4'Z)-2'-hydroxy-N-[(2S*,3S*,4R*)-1,3,4-trihydroxyoctadec-2-yl]tetracos-4-enamide] were separated and characterized by spectroscopic, spectrometric, and computational techniques. The flavonoids isoquercitrin and hyperoside, which possessed noted antinociceptive properties, were obtained from the active AcOEt fraction of the decoction. The chemical composition of the essential oil of the plant was also analyzed by gas chromatography-mass spectrometry. The major constituents were (E)-caryophyllene, germacrene D, ß-elemene, δ-elemene, γ-patchoulene, and 7-epi-α-selinene. Headspace solid-phase microextraction analysis detected (E)-caryophyllene as the main volatile compound of the plant.


Subject(s)
Analgesics/chemistry , Asteraceae/chemistry , Oils, Volatile/chemistry , Plant Extracts/chemistry , Analgesics/isolation & purification , Analgesics/therapeutic use , Animals , Asteraceae/metabolism , Diterpenes, Kaurane/chemistry , Diterpenes, Kaurane/isolation & purification , Diterpenes, Kaurane/therapeutic use , Gas Chromatography-Mass Spectrometry , Male , Mice , Mice, Inbred ICR , Molecular Conformation , Neuralgia/chemically induced , Neuralgia/drug therapy , Neuralgia/pathology , Plant Components, Aerial/chemistry , Plant Components, Aerial/metabolism , Plant Extracts/therapeutic use , Solid Phase Microextraction , Stereoisomerism
10.
Arch Microbiol ; 203(4): 1807-1823, 2021 May.
Article in English | MEDLINE | ID: mdl-33491161

ABSTRACT

Heavy-metal (HM) contamination is a huge environmental problem in many countries including Mexico. Currently, microorganisms with multiple heavy-metal resistance and/or plant-promoting characteristics have been widely used for bioremediation of HM-contaminated soils. The aim of the study was isolated bacteria with multiple heavy-metal resistance and to determinate the resistance mechanism developed by these organisms. A total of 138 aerobic bacteria were isolated from soil and sediments surrounding the Lerma-Chapala basin located in the boundary of the States of Michoacán and Jalisco states of Mexico. One hundred and eight strains showed at least 1 plant growth-promoting features. The Lerma-Chapala basin bacteria were also resistant to high concentrations of HMs including the metalloid arsenic. Sequence analysis of 16S RNA genes reveled that these bacteria were mainly affiliated to the phyla Proteobacteria (38%), Firmicutes (31%) and Actinobacteria (25%), covering 21 genera with Bacillus as the most abundant one. Among them, at least 27 putative novel species were detected in the genera Acinetobacter, Arthrobacter, Bacillus, Agrobacterium, Dyadobacter, Enterobacter, Exiguobacterium, Kluyvera, Micrococcus, Microbacterium and Psychrobacter. In addition, these bacteria developed various heavy-metal-resistance mechanisms, such as biosorption/bioaccumulation, immobilization and detoxification. Therefore, the bacteria isolated from soils and sediments of Lerma-Chapala basin could be used in bioremediation strategies.


Subject(s)
Bacteria/metabolism , Biodegradation, Environmental , Drug Resistance, Bacterial/genetics , Metals, Heavy/analysis , Metals, Heavy/metabolism , Arsenic/analysis , Bacteria/genetics , Bacteria/isolation & purification , Mexico , Plant Development , Soil/chemistry , Soil Microbiology , Soil Pollutants/analysis
11.
Invest New Drugs ; 39(2): 426-441, 2021 04.
Article in English | MEDLINE | ID: mdl-33200242

ABSTRACT

Intraocular retinoblastoma treatment has changed radically over the last decade, leading to a notable improvement in ocular survival. However, eyes that relapse remain difficult to treat, as few alternative active drugs are available. More challenging is the scenario of central nervous system (CNS) metastasis, in which almost no advancements have been made. Both clinical scenarios represent an urgent need for new drugs. Using an integrated multidisciplinary approach, we developed a decision process for prioritizing drug selection for local (intravitreal [IVi], intrathecal/intraventricular [IT/IVt]), systemic, or intra-arterial chemotherapy (IAC) treatment by means of high-throughput pharmacological screening of primary cells from two patients with intraocular tumor and CNS metastasis and a thorough database search to identify clinical and biopharmaceutical data. This process identified 169 compounds to be cytotoxic; only 8 are FDA-approved, lack serious toxicities and available for IVi administration. Four of these agents could also be delivered by IT/IVt. Twelve FDA-approved drugs were identified for systemic delivery as they are able to cross the blood-brain barrier and lack serious adverse events; four drugs are of oral usage and six compounds that lack vesicant or neurotoxicity could be delivered by IAC. We also identified promising compounds in preliminary phases of drug development including inhibitors of survivin, antiapoptotic Bcl-2 family proteins, methyltransferase, and kinesin proteins. This systematic approach may be applied more broadly to prioritize drugs to be repurposed or to identify novel hits for use in retinoblastoma treatment.


Subject(s)
Drug Discovery/organization & administration , Retinal Neoplasms/drug therapy , Retinoblastoma/drug therapy , Cell Line, Tumor , Drug Discovery/methods , High-Throughput Screening Assays/methods , Humans , Infusions, Intraventricular , Injections, Spinal , Intravitreal Injections , Neoplasm Metastasis , Neoplasm Recurrence, Local , Retinal Neoplasms/pathology , Retinoblastoma/pathology
12.
Salud ment ; 43(6): 253-261, Nov.-Dec. 2020. tab, graf
Article in English | LILACS-Express | LILACS | ID: biblio-1156871

ABSTRACT

Abstract Introduction Preventive measures taken during periods of health crisis, specifically in pandemics, have consistently been associated with detrimental effects on mental health. Isolation and loneliness are indirect effects of these preventive measures. Given these premises, monitoring the behavior of the population in the face of these eventualities becomes important. Worry as an indirect measure of anxiety and stress enables one to recognize subjects who are vulnerable to phenomena of high uncertainty, since measures taken to avoid excessive contagion can have high costs for this population. This phenomenon has been consistently observed in other pandemics such as H1/N1 influenza. Objective To determine the prevalence of worry and perceived risk of contagion in the Guadalajara population during the COVID-19 quarantine and to identify differentiating effects. Method A total of 255 people from western Mexico (Guadalajara, Jalisco) voluntarily participated by answering the Penn State Worry Questionnaire (PSWQ) adapted to Mexican population. The average age of the respondents, aged between 18 and 70 years, was 31.71 (± 5.19). A total of 170 women and 85 men participated in the study. Results 40.12% of the population scored high levels of worry, making them vulnerable to mental health conditions. Subjects favored the prevention of a contagion regardless of whether they were self-isolated. The only variable that had a differential effect was sex (p < .05), and there were no differences in educational attainment, occupational demandingness, and isolation between the groups. Discussion and conclusion A preventive attitude was observed among the participants, and so it is important to implement strategies that will prevent mental health costs in those who express excessive worry to avoid saturating mental health services.


Resumen Introducción Las medidas preventivas tomadas durante periodos de crisis de salud, específicamente en las pandemias, se han asociado constantemente a efectos perjudiciales en la salud mental. El aislamiento y la soledad son efectos indirectos de estas medidas preventivas. Dadas estas premisas, monitorear la conducta de la población ante estas eventualidades cobra importancia. La preocupación como medida indirecta de la ansiedad y el estrés puede permitir reconocer aquellos sujetos que se encuentren en una situación de vulnerabilidad ante fenómenos de alta incertidumbre, por lo que las medidas tomadas para evitar contagios excesivos pueden tener un costo alto para dicha población. Este fenómeno se ha observado consistentemente en otras pandemias como la de la influenza H1/N1. Objetivo Determinar la prevalencia de preocupación y riesgo de contagio percibido en población tapatía durante la cuarentena por COVID-19 e identificar efectos diferenciadores. Método Un total de 255 personas del occidente de México (Guadalajara, Jalisco) participaron voluntariamente contestando el Cuestionario de Preocupación del Pensilvania (PWSQ) adaptado a la población mexicana. La edad promedio fue de 31.71 (± 5.19) de entre los 18 y los 70 años. Un total de 170 mujeres y 85 hombres participaron en la encuesta. Resultados El 40.12% de la población alcanzó puntajes altos de preocupación, que los vuelven vulnerables a los padecimientos de salud mental. Se expresaron datos favorables en pro de la prevención de un contagio independientemente de si se estaba en situación de aislamiento o no. Por otro lado, la única variable que tuvo un efecto diferencial fue la del sexo (p < .05), mientras que la escolaridad, la exigencia ocupacional y el aislamiento no mostraron diferencias entre grupos. Discusión y conclusión Se observa una actitud de prevención en los participantes; es importante realizar estrategias que eviten que haya costes a razón de la salud mental en aquellos que muestra preocupación excesiva para evitar la saturación de los servicios de salud mental.

13.
Rev chil anest ; 48(5): 465-469, 2019. ilus
Article in Spanish | UY-BNMED, BNUY, LILACS | ID: biblio-1370907

ABSTRACT

La patología coronaria no es frecuente dentro de la población joven. El diagnóstico en la paciente obstétrica no es fácil dado los cambios fisiológicos que esta población presenta. La disección espontánea de una arteria coronaria es una afección muy poco frecuente que puede ser causa de isquemia miocárdica y asociarse a un síndrome coronario agudo. Se trata del caso de una paciente de sexo femenino de 38 años cursando 33 semanas de gestación, la cual presentó un síndrome coronario agudo con elevación del segmento ST, por una disección coronaria, desprendimiento prematuro de placenta normo inserta (DPPNI) y óbito fetal.


Coronary disease is infrequent among young population. Diagnosis in the obstetric population is not easy, due to the physiological changes that this population presents. Spontaneous coronary artery dissection, not a frequent medical condition, can be a cause of myocardial ischemia and be associated with and acute coronary syndrome. We present the case of a 38-year-old female patient, at 33 weeks gestation, who presented an acute coronary syndrome with ST segment elevation, caused by coronary artery dissection. This syndrome was accompanied with abruptio placentae and fetal death.


Subject(s)
Humans , Female , Pregnancy , Adult , Cesarean Section , Abruptio Placentae , Fetal Death , ST Elevation Myocardial Infarction/diagnostic imaging , Coronary Artery Disease/complications , Emergencies , ST Elevation Myocardial Infarction/etiology , ST Elevation Myocardial Infarction/drug therapy
14.
Rev Lat Am Enfermagem ; 26: e3055, 2018 Sep 06.
Article in English, Portuguese, Spanish | MEDLINE | ID: mdl-30208161

ABSTRACT

OBJECTIVE: to review the most relevant evidence on the nurses' attitudes towards witnessed resuscitation, in the inpatient and out-of-hospital spheres. METHOD: integrative literature review, covering the period from 2008 till 2015, using the databases PubMed, Lilacs and SciELO; in Spanish, English and Portuguese. The pediatric context was excluded from the study. RESULTS: the synthesis of the data resulted in the inclusion of 10 articles, categorized as: positive attitudes and negative attitudes. CONCLUSIONS: discrepancies exist among the nurses from different contexts and geographical regions towards the concept; protocols need to be established for this situation, in view of the advantages evidenced in the literature, for the nursing professionals as well as the relatives. Witnessed resuscitation can represent an opportunity to understand and cope with the rational and irrational in the situation in a shared manner, as well as mitigate or dignify the mourning.


Subject(s)
Family/psychology , Nursing Staff, Hospital/psychology , Resuscitation/nursing , Attitude of Health Personnel , Emergency Service, Hospital , Humans , Resuscitation/psychology
15.
Oncotarget ; 9(41): 26527-26542, 2018 May 29.
Article in English | MEDLINE | ID: mdl-29899874

ABSTRACT

Breast cancer can be classified into molecular subtypes. Tumors overexpressing HER2 protein are more aggressive and metastatic; hence, patients have a poor prognosis. Anti-HER2 strategies, such as the monoclonal antibody Trastuzumab (Tz), have therefore been developed. Despite this progress, not all patients respond to the treatment. Retinoic acid (RA) has been proposed as an adjuvant treatment of breast carcinoma because of its ability to inhibit cell growth. We evaluated the effect of Tz in combination with RA on the viability, adhesion, migration, invasion and expression of migration-related proteins in SKBR3 and BT-474 human breast cancer cells. MTT, pharmacological interaction analysis, immunofluorescence, adhesion/migration/invasion and Western blot assays were performed. The coadministration of both drugs synergistically decreased cell survival. Tz+RA significantly decreased adhesion/migration/invasion in both cell types. Tz+RA strongly reduced FAK and HER2 expression and induced nuclear FAK translocation. In addition, a granular distribution of HER2 receptor was observed after the combined treatment. In conclusion, the coadministration of both drugs in patients with this type of cancer could contribute to the improvement of their prognosis and reduce the adverse effects of therapy because the applied Tz doses would be lower due to the adjuvant effect of RA.

16.
Biomed Pharmacother ; 101: 553-562, 2018 May.
Article in English | MEDLINE | ID: mdl-29514128

ABSTRACT

The aim of this work was to design, synthesize and characterize the potential anti-nociceptive and anti-inflammatory activities of a new series of bioisosteres and hybrids from known non-steroidal anti-inflammatory drugs (NSAIDs). The compounds 4-(acetylamino)phenyl (2S)-2-(6-methoxy-2-naphthyl)propanoate (GUF-1) and 4-(acetylamino)phenyl 2-(R,S)-(4-isobutylphenyl)propanoate (GUF-2) were synthesized as hybrids (also known as heterodimers); whereas those named 2-(R,S)-(4-isobutylphenyl)-N-1H-tetrazol-5-ylpropanamide (GUF-3), (2S)-2-(6-methoxy-2-naphthyl)-N-1H-tetrazol-5-ylpropanamide (GUF-4), [2-(R,S)-N-hydroxy-2-[4-(2-methylpropyl)phenyl]propanamide] (GUF-5), and (2S)-N-hydroxy-2-(6-methoxy-2-naphthyl)propanamide (GUF-6) were synthesized as bioisosteres of the NSAIDs paracetamol, ibuprofen, and naproxen, respectively. All these compounds were characterized by spectroscopic and spectrometric analysis. Antinociceptive activity of GUF-1 to GUF-6 was evaluated using the formalin test in rats. Pharmacological responses of GUF-1, GUF-2 (hybrids), and GUF-5 (bioisostere) demonstrated significant antinociceptive effects; thus these compounds were assayed in an inflammation test like carrageenan-induced paw oedema in rats. Complete molecular docking of cyclooxygenase and the GUF-1 and GUF-2 hybrids showed high docking scores, compared to the reference drugs. Our data demonstrate that compounds GUF-1, GUF-2, and GUF-5 possesses antinociceptive and antiinflammatory activities resembling and improving those known for the traditional NSAIDs, paracetamol, naproxen and ibuprofen.


Subject(s)
Acetaminophen/chemical synthesis , Anti-Inflammatory Agents, Non-Steroidal/chemical synthesis , Ibuprofen/chemical synthesis , Molecular Docking Simulation/methods , Naproxen/chemical synthesis , Pain Measurement/drug effects , Acetaminophen/metabolism , Acetaminophen/pharmacology , Animals , Anti-Inflammatory Agents, Non-Steroidal/metabolism , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Binding Sites/physiology , Cyclooxygenase Inhibitors/chemical synthesis , Cyclooxygenase Inhibitors/metabolism , Cyclooxygenase Inhibitors/pharmacology , Drug Evaluation, Preclinical/methods , Female , Ibuprofen/metabolism , Ibuprofen/pharmacology , Imaging, Three-Dimensional/methods , Naproxen/metabolism , Naproxen/pharmacology , Pain Measurement/methods , Rats , Rats, Wistar
17.
Rev. latinoam. enferm. (Online) ; 26: e3055, 2018. graf
Article in English | LILACS, BDENF - Nursing | ID: biblio-961170

ABSTRACT

ABSTRACT Objective: to review the most relevant evidence on the nurses' attitudes towards witnessed resuscitation, in the inpatient and out-of-hospital spheres. Method: integrative literature review, covering the period from 2008 till 2015, using the databases PubMed, Lilacs and SciELO; in Spanish, English and Portuguese. The pediatric context was excluded from the study. Results: the synthesis of the data resulted in the inclusion of 10 articles, categorized as: positive attitudes and negative attitudes. Conclusions: discrepancies exist among the nurses from different contexts and geographical regions towards the concept; protocols need to be established for this situation, in view of the advantages evidenced in the literature, for the nursing professionals as well as the relatives. Witnessed resuscitation can represent an opportunity to understand and cope with the rational and irrational in the situation in a shared manner, as well as mitigate or dignify the mourning.


RESUMO Objetivo: revisar a evidência mais relevante sobre as atitudes das enfermeiras quanto à reanimação presenciada nos âmbitos intra e extra-hospitalar. Metodologia: revisão integrativa da literatura, abrangendo os anos 2008 a 2015, utilizando-se as bases de dados PubMed, Lilacs e SciELO; em espanhol, inglês e português. Exclui-se do estudo o âmbito pediátrico. Resultados: a síntese dos dados deu como resultado a inclusão de 10 artigos categorizados em: atitudes positivas e atitudes negativas. Conclusões: discrepâncias entre as enfermeiras de diferentes áreas e zonas geográficas diante de dito conceito. A necessidade de protocolar essa situação, dadas as vantagens que a literatura evidencia, tanto para profissionais enfermeiros como para familiares. A reanimação presenciada pode ser uma oportunidade de entender e enfrentar de forma compartilhada os lados racional e irracional da situação e atenuar ou dignificar o luto.


RESUMEN Objetivo: revisar la evidencia más relevante acerca de las actitudes de las enfermeras en cuanto a la reanimación presenciada en el ámbito tanto intra como extrahospitalario. Metodología: revisión integradora de la literatura, abarcando los años de 2008 a 2015, utilizando las bases de datos PubMed, Lilacs y SciELO; en español, inglés y portugués. Se excluyen del estudio el ámbito pediátrico. Resultados: la síntesis de los datos dio como resultado la inclusión de 10 artículos, categorizándolos en: actitudes positivas y actitudes negativas. Conclusiones: existen discrepancias entre las enfermeras de diferentes ámbitos y zonas geográficas ante dicho concepto; hay necesidad de protocolizar dicha situación dadas las ventajas que la literatura evidencia tanto para los profesionales enfermeros como para los familiares. La reanimación presenciada puede ser una oportunidad de entender y afrontar de forma compartida lo racional y lo irracional de la situación y atenuar o dignificar el duelo.


Subject(s)
Humans , Attitude of Health Personnel , Emergency Nursing , Cardiopulmonary Resuscitation , Family Relations , Heart Arrest
18.
J Nat Prod ; 80(1): 190-195, 2017 01 27.
Article in English | MEDLINE | ID: mdl-28060505

ABSTRACT

From an extract prepared from the grain-based culture of Malbranchea flavorosea two new polyketides, namely, 8-chloroxylarinol A (1) and flavoroseoside (2), along with the known compounds xylarinol A (3), xylarinol B (4), massarigenins B and C (5 and 6), and clavatol (7), were isolated. The structures of 1 and 2 were elucidated using spectroscopic methods and corroborated by single-crystal X-ray diffraction analysis. In the case of compound 2 the absolute configuration at the stereogenic centers was established according to the method of Flack. In addition, the X-ray structure of compound 6 is reported for the first time. Compounds 3, 4, and 6 significantly inhibited yeast α-glucosidase. Compound 6 also inhibited the postprandial peak during an oral sucrose tolerance assay when tested in vivo, using normal and NA/STZ-induced hyperglycemic mice.


Subject(s)
Benzoxepins/isolation & purification , Benzoxepins/pharmacology , Glycoside Hydrolase Inhibitors/isolation & purification , Glycoside Hydrolase Inhibitors/pharmacology , Hypoglycemic Agents/metabolism , Lactones/isolation & purification , Lactones/pharmacology , Polyketides/isolation & purification , Polyketides/pharmacology , Spiro Compounds/isolation & purification , Spiro Compounds/pharmacology , Animals , Benzoxepins/chemistry , Glycoside Hydrolase Inhibitors/chemistry , Hypoglycemic Agents/chemistry , Lactones/chemistry , Magnetic Resonance Spectroscopy , Mice , Molecular Structure , Polyketides/chemistry , Spiro Compounds/chemistry , X-Ray Diffraction
19.
Planta Med ; 83(6): 534-544, 2017 Apr.
Article in English | MEDLINE | ID: mdl-27824405

ABSTRACT

The purpose of this research was to examine the preclinical efficacy of a decoction from the roots of Acourtia thurberi as a hypoglycemic, antihyperglycemic, and antihyperalgesic agent using well-known experimental models in mice. Acute oral administration of A. thurberi decoction did not produce toxic effects in mice, according to the Lorke procedure. A. thurberi decoction (31.6-316.2 mg/kg, p. o.) decreased blood glucose levels during acute hypoglycemic and the oral glucose tolerance and oral sucrose tolerance tests, both in normoglycemic and hyperglycemic animals. Phytochemical analysis of A. thurberi roots led to the isolation of perezone (1), a mixture of α-pipitzol (2) and ß-pipitzol (3), and 8-ß-D-glucopyranosyloxy-4-methoxy-5-methyl-coumarin (4). A pharmacological evaluation of compounds 1-4 (3.2-31.6 mg/kg) using the same assays revealed their hypoglycemic and antihyperglycemic actions. Finally, local administration of A. thurberi decoction (31.6-316.2 µg/paw) and compounds 1-4 (3.2-31.6 µg/paw) produced significant inhibition on the licking time during the formalin test in healthy and hyperglycemic mice, demonstrating their antinociceptive and antihyperalgesic potential, respectively. Altogether, these results could be related to the use of A. thurberi for treating diabetes and painful complaints in contemporary Mexican folk medicine. A suitable UPLC-ESI/MS method was developed and successfully applied to quantify simultaneously compounds 1 and 4 in A. thurberi decoction.


Subject(s)
Asteraceae/chemistry , Diabetes Mellitus, Experimental/drug therapy , Hypoglycemic Agents/isolation & purification , Hypoglycemic Agents/pharmacology , Plant Extracts/pharmacology , Sesquiterpenes/pharmacology , Animals , Blood Glucose/drug effects , Diabetes Mellitus, Experimental/chemically induced , Disease Models, Animal , Humans , Male , Medicine, Traditional , Mexico , Mice , Mice, Inbred ICR , Niacinamide/adverse effects , Phytotherapy , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plants, Medicinal , Sesquiterpenes/chemistry , Sesquiterpenes/isolation & purification , Streptozocin/adverse effects
20.
Planta Med ; 82(14): 1286-94, 2016 Sep.
Article in English | MEDLINE | ID: mdl-27399232

ABSTRACT

Benzomalvin A (1), quinolactacins A1 (2), A2 (3) and B (4), quinolonimide (5), asperphenamate (6), and a new halogenated polyhydroxyanthraquinone, namely 2-chloro-6-[2'(S)-hydroxypropyl]-1,3,8-trihydroxy-anthraquinone (7), were isolated from an organic extract obtained from the solid culture of Penicillium spathulatum B35. Compounds 2 and 3 were isolated as an epimeric mixture, and compound 4 as a racemate. The structure of 7 was elucidated using 1D and 2D NMR, combined with computational methods (density functional theory). Compound 1, the mixture of 2 and 3, racemate 4, and compound 6 inhibited the yeast α-glucosidase in a concentration-dependent fashion with IC50 values of 383.2, 273.3, 57.3, and 8.3 µM, respectively. The α-glucosidase inhibitory properties of 1 were confirmed in vivo with an oral sucrose tolerance test in normal and hyperglycemic mice (p < 0.05). Furthermore, docking studies predicted that the most stable conformers of 1 bind to yeast and mammalian α-glucosidases with a higher affinity than acarbose. Finally, 1 also showed antihyperalgesic activity when tested in the formalin assay in hyperglycemic mice (p < 0.05).


Subject(s)
Alkaloids/isolation & purification , Glycoside Hydrolase Inhibitors/isolation & purification , Penicillium/chemistry , alpha-Glucosidases/metabolism , Alkaloids/chemistry , Alkaloids/pharmacology , Animals , Cell Survival/drug effects , Fibroblasts/drug effects , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Humans , Male , Mice, Inbred ICR , Models, Molecular , Molecular Structure
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