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1.
Molecules ; 28(21)2023 Nov 02.
Artículo en Inglés | MEDLINE | ID: mdl-37959813

RESUMEN

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.


Asunto(s)
Acetilcolinesterasa , Enfermedad de Alzheimer , Animales , Ratones , Humanos , Acetilcolinesterasa/metabolismo , Simulación del Acoplamiento Molecular , Oxazolona , Inhibidores de la Colinesterasa/química , Modelos Animales de Enfermedad , Cognición , Relación Estructura-Actividad
2.
Invest New Drugs ; 39(2): 426-441, 2021 04.
Artículo en Inglés | MEDLINE | ID: mdl-33200242

RESUMEN

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.


Asunto(s)
Descubrimiento de Drogas/organización & administración , Neoplasias de la Retina/tratamiento farmacológico , Retinoblastoma/tratamiento farmacológico , Línea Celular Tumoral , Descubrimiento de Drogas/métodos , Ensayos Analíticos de Alto Rendimiento/métodos , Humanos , Infusiones Intraventriculares , Inyecciones Espinales , Inyecciones Intravítreas , Metástasis de la Neoplasia , Recurrencia Local de Neoplasia , Neoplasias de la Retina/patología , Retinoblastoma/patología
3.
Arch Microbiol ; 203(4): 1807-1823, 2021 May.
Artículo en Inglés | MEDLINE | ID: mdl-33491161

RESUMEN

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.


Asunto(s)
Bacterias/metabolismo , Biodegradación Ambiental , Farmacorresistencia Bacteriana/genética , Metales Pesados/análisis , Metales Pesados/metabolismo , Arsénico/análisis , Bacterias/genética , Bacterias/aislamiento & purificación , México , Desarrollo de la Planta , Suelo/química , Microbiología del Suelo , Contaminantes del Suelo/análisis
4.
Chem Biodivers ; 18(8): e2100369, 2021 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-34138517

RESUMEN

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.


Asunto(s)
Analgésicos/química , Asteraceae/química , Aceites Volátiles/química , Extractos Vegetales/química , Analgésicos/aislamiento & purificación , Analgésicos/uso terapéutico , Animales , Asteraceae/metabolismo , Diterpenos de Tipo Kaurano/química , Diterpenos de Tipo Kaurano/aislamiento & purificación , Diterpenos de Tipo Kaurano/uso terapéutico , Cromatografía de Gases y Espectrometría de Masas , Masculino , Ratones , Ratones Endogámicos ICR , Conformación Molecular , Neuralgia/inducido químicamente , Neuralgia/tratamiento farmacológico , Neuralgia/patología , Componentes Aéreos de las Plantas/química , Componentes Aéreos de las Plantas/metabolismo , Extractos Vegetales/uso terapéutico , Microextracción en Fase Sólida , Estereoisomerismo
5.
Asia Pac J Clin Nutr ; 30(4): 602-613, 2021 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-34967189

RESUMEN

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.


Asunto(s)
Cirugía Bariátrica , Obesidad Mórbida , Disonancia Cognitiva , Suplementos Dietéticos , Ácido Fólico , Humanos , Micronutrientes , Vitaminas
6.
J Nat Prod ; 80(1): 190-195, 2017 01 27.
Artículo en Inglés | MEDLINE | ID: mdl-28060505

RESUMEN

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.


Asunto(s)
Benzoxepinas/aislamiento & purificación , Benzoxepinas/farmacología , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Inhibidores de Glicósido Hidrolasas/farmacología , Hipoglucemiantes/metabolismo , Lactonas/aislamiento & purificación , Lactonas/farmacología , Policétidos/aislamiento & purificación , Policétidos/farmacología , Compuestos de Espiro/aislamiento & purificación , Compuestos de Espiro/farmacología , Animales , Benzoxepinas/química , Inhibidores de Glicósido Hidrolasas/química , Hipoglucemiantes/química , Lactonas/química , Espectroscopía de Resonancia Magnética , Ratones , Estructura Molecular , Policétidos/química , Compuestos de Espiro/química , Difracción de Rayos X
7.
Planta Med ; 83(6): 534-544, 2017 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-27824405

RESUMEN

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.


Asunto(s)
Asteraceae/química , Diabetes Mellitus Experimental/tratamiento farmacológico , Hipoglucemiantes/aislamiento & purificación , Hipoglucemiantes/farmacología , Extractos Vegetales/farmacología , Sesquiterpenos/farmacología , Animales , Glucemia/efectos de los fármacos , Diabetes Mellitus Experimental/inducido químicamente , Modelos Animales de Enfermedad , Humanos , Masculino , Medicina Tradicional , México , Ratones , Ratones Endogámicos ICR , Niacinamida/efectos adversos , Fitoterapia , Extractos Vegetales/química , Extractos Vegetales/aislamiento & purificación , Plantas Medicinales , Sesquiterpenos/química , Sesquiterpenos/aislamiento & purificación , Estreptozocina/efectos adversos
8.
Planta Med ; 82(14): 1286-94, 2016 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-27399232

RESUMEN

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).


Asunto(s)
Alcaloides/aislamiento & purificación , Inhibidores de Glicósido Hidrolasas/aislamiento & purificación , Penicillium/química , alfa-Glucosidasas/metabolismo , Alcaloides/química , Alcaloides/farmacología , Animales , Supervivencia Celular/efectos de los fármacos , Fibroblastos/efectos de los fármacos , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/farmacología , Humanos , Masculino , Ratones Endogámicos ICR , Modelos Moleculares , Estructura Molecular
9.
Rev Invest Clin ; 67(2): 122-9, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25938846

RESUMEN

BACKGROUND: PAI-1 is the main inhibitor of fibrinolysis. Increase in PAI-1 levels has been associated with the risk of coronary disease; however, there are few studies on the relationship between subclinical atherosclerosis and PAI-1 levels. OBJECTIVE: The aim of this study was to analyze the relationship between PAI-1 level and carotid intima-media thickness in premenopausal and postmenopausal women without apparent cardiovascular disease. MATERIAL AND METHODS: A cross-sectional study was conducted in 142 women aged 45 to 60 years with no history of cardiovascular disease. Anthropometric and laboratory measurements were performed, including PAI-1 levels. All participants underwent a B-Mode ultrasound to measure intima-media thickness. Subclinical atherosclerosis was considered when intima-media thickness was ≥ 0.7 mm and/or an atheromatous plaque was observed. RESULTS: Postmenopausal women had greater intima-media thickness than premenopausal women (0.688 ± 0.129 vs. 0.621 ± 0.113 mm; p < 0.05). Compared to women with normal intima-media thickness, women with subclinical atherosclerosis had higher PAI-1 levels (23.2 ± 13.7 vs. 30.4 ± 20.7 ng/ml; p < 0.05). In all participants, intima-media thickness correlated with PAI-1 (r = 0.302; p = 0.01) and with age (r = 0.358; p = 0001). CONCLUSIONS: An increase in intima-media thickness was observed in postmenopausal women compared with premenopausal women. Asymptomatic women with increased intima-media thickness had higher PAI-1 levels. These findings suggest that fibrinolytic activity is low in the subclinical stage of atherosclerosis.


Asunto(s)
Aterosclerosis/patología , Grosor Intima-Media Carotídeo , Inhibidor 1 de Activador Plasminogénico/sangre , Posmenopausia , Aterosclerosis/epidemiología , Estudios Transversales , Femenino , Fibrinólisis/fisiología , Humanos , Persona de Mediana Edad , Premenopausia
10.
ACS Omega ; 7(23): 19640-19647, 2022 Jun 14.
Artículo en Inglés | MEDLINE | ID: mdl-35721970

RESUMEN

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.

11.
Healthcare (Basel) ; 9(11)2021 Oct 25.
Artículo en Inglés | MEDLINE | ID: mdl-34828482

RESUMEN

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.

12.
Am J Health Behav ; 45(6): 1091-1102, 2021 11 15.
Artículo en Inglés | MEDLINE | ID: mdl-34969419

RESUMEN

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.


Asunto(s)
Síndrome Metabólico , Presión Sanguínea , Índice de Masa Corporal , Estudios Transversales , Ghrelina , Glucosa , Humanos , Hidrocortisona , Análisis de Mediación , Síndrome Metabólico/epidemiología , Estudiantes , Triglicéridos , Universidades , Circunferencia de la Cintura
13.
Neuropharmacology ; 56(2): 564-71, 2009 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-19027760

RESUMEN

Tilia species are well known around the world for their properties in traditional medicine. Antinociceptive activity of hexane, methanol and aqueous extracts from Tilia americana var. mexicana inflorescences was evaluated in the pain-induced functional impairment model in rats (PIFIR). A preliminar 300 mg/kg dosage of aqueous extracts i.p., but not the same dose of methanol or hexane extract, produced an antinociceptive response in rats similar to that of tramadol (17.8 mg/kg i.p.). A dose-response curve from aqueous extract allowed the determination of ED(50) = 364.97 mg/kg in comparison to ED(50) = 10.35 mg/kg for tramadol in this model. A previous HPLC-DAD analysis corroborated by an HPLC-MS technique in this study demonstrated the flavonoid composition in this Tilia aqueous extract revealing the presence of glycosides mainly derived from quercetin. Thus, Tilia aqueous extract and quercetin were tested at 30 and/or 100 mg/kg dosages i.p. in the PIFIR and formalin models producing a significant and dose-dependent antinociceptive response resembling that produced by a total and a partial agonist of 5-HT(1A) receptors like 8-OH-DPAT (0.1 mg/kg, s.c.) and buspirone (5 mg/kg, i.p.), respectively. In all the treatments, antinociceptive response was inhibited in the presence of WAY 100635 (0.12 mg/kg, i.p.). Our results support the analgesic activity of T. americana var. mexicana inflorescences attributed by folk medicine; they also indicate that quercetin is partly responsible for this pharmacological activity that is likely mediated by serotonin 5-HT(1A) receptors.


Asunto(s)
Dimensión del Dolor/métodos , Dolor/tratamiento farmacológico , Fitoterapia/métodos , Extractos Vegetales/uso terapéutico , Quercetina/uso terapéutico , Tilia , Animales , Área Bajo la Curva , Artritis/diagnóstico , Artritis/etiología , Conducta Animal/efectos de los fármacos , Cromatografía Líquida de Alta Presión/métodos , Modelos Animales de Enfermedad , Relación Dosis-Respuesta a Droga , Interacciones Farmacológicas , Masculino , Dolor/etiología , Piperazinas/farmacología , Piridinas/farmacología , Ratas , Ratas Wistar , Antagonistas de la Serotonina/farmacología
14.
Rev Lat Am Enfermagem ; 26: e3055, 2018 Sep 06.
Artículo en Inglés, Portugués, Español | MEDLINE | ID: mdl-30208161

RESUMEN

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.


Asunto(s)
Familia/psicología , Personal de Enfermería en Hospital/psicología , Resucitación/enfermería , Actitud del Personal de Salud , Servicio de Urgencia en Hospital , Humanos , Resucitación/psicología
16.
Biomed Pharmacother ; 101: 553-562, 2018 May.
Artículo en Inglés | MEDLINE | ID: mdl-29514128

RESUMEN

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.


Asunto(s)
Acetaminofén/síntesis química , Antiinflamatorios no Esteroideos/síntesis química , Ibuprofeno/síntesis química , Simulación del Acoplamiento Molecular/métodos , Naproxeno/síntesis química , Dimensión del Dolor/efectos de los fármacos , Acetaminofén/metabolismo , Acetaminofén/farmacología , Animales , Antiinflamatorios no Esteroideos/metabolismo , Antiinflamatorios no Esteroideos/farmacología , Sitios de Unión/fisiología , Inhibidores de la Ciclooxigenasa/síntesis química , Inhibidores de la Ciclooxigenasa/metabolismo , Inhibidores de la Ciclooxigenasa/farmacología , Evaluación Preclínica de Medicamentos/métodos , Femenino , Ibuprofeno/metabolismo , Ibuprofeno/farmacología , Imagenología Tridimensional/métodos , Naproxeno/metabolismo , Naproxeno/farmacología , Dimensión del Dolor/métodos , Ratas , Ratas Wistar
17.
Oncotarget ; 9(41): 26527-26542, 2018 May 29.
Artículo en Inglés | MEDLINE | ID: mdl-29899874

RESUMEN

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.

18.
Rev. ADM ; 79(1): 20-27, ene.-feb. 2022. ilus, tab
Artículo en Español | LILACS | ID: biblio-1361506

RESUMEN

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)


Asunto(s)
Humanos , Adolescente , Adulto , Grabado Ácido Dental , Cementación , Recubrimientos Dentinarios , Cementos de Resina , Resistencia al Corte , Resistencia a la Tracción , Dentina/efectos de los fármacos
19.
Rev. enferm. Inst. Mex. Seguro Soc ; 30(2): 37-42, 01-abr-2022. tab
Artículo en Español | LILACS, BDENF - enfermagem (Brasil) | ID: biblio-1378934

RESUMEN

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.


Asunto(s)
Humanos , Masculino , Femenino , Cateterismo Cardíaco/instrumentación , Capacitación Profesional , Personal de Enfermería/educación , Epidemiología Descriptiva , Estudios Transversales , México
20.
Salud ment ; 43(6): 253-261, Nov.-Dec. 2020. tab, graf
Artículo en Inglés | LILACS-Express | LILACS | ID: biblio-1156871

RESUMEN

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.

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