RESUMEN
Scheduled naps in the workplace are an effective countermeasure to drowsiness in safety-sensitive industries. This quasi-experimental study with a one-group, pre- and post-test design aimed to examine the effects of scheduled naps on nurses working 12-h shifts. Nurses in two pediatric intensive care units at a tertiary hospital were provided 30-min scheduled nap opportunities during their shifts. A total of 38 nurses completed pre- and post-test work diaries for sleepiness, fatigue, work demands and pace, and quality of nursing care at the end of each shift. The drowsiness of 13 nurses was continuously assessed during their shifts using infrared reflectance oculography. Nurses who reached naps reported improved levels of fatigue on the first night shift and better quality of nursing care the second night and day shifts post-test, while nurses who did not reach naps showed no significant improvements. The oculography successfully assessed drowsiness during 73% and 61% of the pre- and post-test total work hours, respectively. The total cautionary and cautionary or higher levels of drowsiness decreased. Nurse managers should consider scheduled naps in clinical settings to improve nurses' alertness during their shifts.
Asunto(s)
Trastornos del Sueño del Ritmo Circadiano , Somnolencia , Niño , Fatiga , Humanos , Sueño , Vigilia , Tolerancia al Trabajo ProgramadoRESUMEN
Quarantine often provokes negative psychological consequences. Thus, we aimed to identify the psychological and behavioral responses and stressors of caregivers quarantined with young patients after a close contact to a coronavirus disease 2019 case at a children's hospital. More than 90% of the caregivers reported feelings of worry and nervousness, while some of them reported suicidal ideations (4.2%), and/or homicidal ideations (1.4%). Fear of infection of the patient (91.7%) and/or oneself (86.1%) were most frequently reported stressors. A multidisciplinary team including infection control team, pediatrician, psychiatrist, nursing staff and legal department provided supplies and services to reduce caregiver's psychological distress. Psychotropic medication was needed in five (6.9%), one of whom was admitted to the psychiatry department due to suicidality. Quarantine at a children's hospital makes notable psychological impacts on the caregivers and a multidisciplinary approach is required.
Asunto(s)
Cuidadores/psicología , Infecciones por Coronavirus/psicología , Neumonía Viral/psicología , Cuarentena/psicología , Estrés Psicológico/psicología , Ansiedad/psicología , COVID-19 , Infecciones por Coronavirus/transmisión , Transmisión de Enfermedad Infecciosa/prevención & control , Hospitales Pediátricos , Humanos , Pandemias , Neumonía Viral/transmisiónRESUMEN
A quantitative structure-activity relationship (QSAR) study of aromatic inhibitors against aldose reductase (AR) activity was performed using variable selection from stepwise multiple linear regression (MLR) and genetic algorithm (GA)-MLR. As a result of variable selection, stepwise MLR and GA-MLR gave the same results with one, two, three and five descriptors and different results with four and six descriptors. GA-MLR produced higher values and was better in explanatory and predictive power than stepwise MLR in four variables. AR activity (pIC50) of aromatic derivatives was expressed with acceptable explanatory (74.6-81.2%) and predictive power (68.8-74.4%) in models 3 and 4. The resulting models with the given descriptors illustrate that hydrophobic and electrostatic interactions play a significant role in inhibition of AR activity. This study suggests that the QSAR models can be used as guidelines to predict improved aldose reductase inhibitory activity and to obtain reliable predictions in structurally diverse compounds.
Asunto(s)
Aldehído Reductasa/antagonistas & inhibidores , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Cristalino/enzimología , Modelos Biológicos , Animales , Activación Enzimática/efectos de los fármacos , Interacciones Hidrofóbicas e Hidrofílicas , Concentración 50 Inhibidora , Estructura Molecular , Relación Estructura-Actividad Cuantitativa , RatasRESUMEN
Simple synthesis of modafinil derivatives and their biological activity are described. The key synthetic strategies involve substitution and coupling reactions. We determined the anti-inflammatory effects of modafinil derivatives in cultured BV2 cells by measuring the inhibition of nitrite production and expression of iNOS and COX-2 after LPS stimulation. It was found that for sulfide analogues introduction of aliphatic groups on the amide part (compounds 11ad) resulted in lower anti-inflammatory activity compared with cyclic or aromatic moieties (compounds 11ek). However, for the sulfoxide analogues, introduction of aliphatic moieties (compounds 12ad) showed higher anti-inflammatory activity than cyclic or aromatic fragments (compounds 12ek) in BV-2 microglia cells.
Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Antiinflamatorios no Esteroideos/farmacología , Compuestos de Bencidrilo , Ciclooxigenasa 2/metabolismo , Óxido Nítrico Sintasa de Tipo II/metabolismo , Nitritos/antagonistas & inhibidores , Antiinflamatorios no Esteroideos/química , Antioxidantes/síntesis química , Antioxidantes/química , Antioxidantes/farmacología , Compuestos de Bencidrilo/química , Compuestos de Bencidrilo/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Humanos , Lipopolisacáridos/inmunología , Modafinilo , Óxido Nítrico/metabolismo , Safrol/análogos & derivados , Safrol/química , Sulfuros/químicaRESUMEN
The total synthesis and structure determination of cis- and trans-flocoumafen was described. The key synthetic steps involve Knoevenagel condensation with p-methoxybenzaldehyde, in situ decarboxylation and intramolecular ring cyclization to construct the tetralone skeleton. Stereospecific reduction of the O-alkylated ketone 13 afforded good yield of precusor alcohol 5. Final coupling of alcohol 5 with 4-hydroxy-coumarin yielded flocoumafen (1). Separation and structure determination of cis- and trans-flocoumafen through 2D NMR analyses-assisted computer simulation techniques for the evaluation of anticoagulant activities are reported for the first time. This method is useful for generating the core tetralone skeleton of 4-hydroxycoumarin derivatives and provides a generalized access to various warfarin type anticoagulants.
Asunto(s)
4-Hidroxicumarinas/química , 4-Hidroxicumarinas/síntesis química , Productos Biológicos/química , Productos Biológicos/síntesis química , Alquilación , Anticoagulantes/química , Benzaldehídos/química , Ciclización , DescarboxilaciónRESUMEN
Simple synthesis and biological activities of modafinil derivatives are described. The key reactions include condensation of acid and propargyl alcohol, subsequent 1,3-dipolar cycloaddition reaction of alkynes and (3-azido-propyl)cyclohexane or (4-azido-butyl)benzene in the presence of sodium ascorbate and CuSO4·5H2O in excellent yield. They were then evaluated for the suppression of LPS-induced NO generation in vitro. It was found that all compounds showed moderate effects for suppression of LPS-induced NO generation.
Asunto(s)
Compuestos de Bencidrilo/síntesis química , Compuestos de Bencidrilo/farmacología , Triazoles/síntesis química , Triazoles/farmacología , Animales , Compuestos de Bencidrilo/química , Línea Celular , Ésteres/síntesis química , Ésteres/química , Ésteres/farmacología , Ratones , Microglía/citología , Microglía/efectos de los fármacos , Microglía/metabolismo , Modafinilo , Óxido Nítrico/metabolismo , Triazoles/químicaRESUMEN
Dimethyl lithosermate B (DLB) is a highly potent natural antioxidant and antidiabetic polyphenol with unknown mode of action. To determine its cellular targets, a photochemical and fluorescent dimethyl lithopermate B probe was designed and efficiently synthesized. The dual-labeled chemical probe for biological application was evaluated by UV and fluorescence to determine its electrochemical absorption and emission properties. This probe could be valuable for investigating ligand-protein interactions and subcellular localization.
Asunto(s)
Medicamentos Herbarios Chinos/síntesis química , Sondas Moleculares/síntesis química , Etiquetas de Fotoafinidad/metabolismo , Procesos Fotoquímicos , Medicamentos Herbarios Chinos/química , Espectrometría de Fluorescencia , Espectrofotometría Ultravioleta , Rayos UltravioletaRESUMEN
Here, we describe the practical synthesis and biological properties of bergenin and its structural analogs. Synthetic bergenin compounds were prepared by acylation of bergenin. These compounds were then evaluated for suppression of lipopolysaccharide-induced nitric oxide (NO) generation in cultured cells and anti-narcotic effects on morphine-dependent mice. We found that bergenin derivatives showed potent anti-inflammatory activity (suppression of NO generation) at concentrations ranging from 20 to 30 µmin vitro, and bergenin derivatives (10-20 mg/kg) exhibited significant anti-narcotic effects on morphine dependence in mice. These results suggest the potential utility of bergenin and its analogs as anti-narcotic agents and the design of more potent anti-inflammatory compounds.
Asunto(s)
Antiinflamatorios/química , Antiinflamatorios/farmacología , Benzopiranos/química , Benzopiranos/farmacología , Dependencia de Morfina/tratamiento farmacológico , Óxido Nítrico/metabolismo , Acilación , Animales , Antiinflamatorios/síntesis química , Benzopiranos/síntesis química , Línea Celular , Técnicas de Química Sintética , Lipopolisacáridos/metabolismo , Ratones , Ratones Endogámicos C57BL , Microglía/citología , Trastornos Relacionados con SustanciasRESUMEN
Pedestrian safety is a serious concern at busy intersections and pedestrian campuses across the nation. Although crosswalks and signs inform pedestrians where to cross, there is no standard protocol for pedestrians to signal drivers that they wish to use the crosswalks, except to stand in or at the crosswalk. We examined the effects of two pedestrian prompts, a raised hand and extended arm, on motorist yielding at uncontrolled crosswalks. The two prompts were effective at increasing yielding.
Asunto(s)
Accidentes de Tránsito/prevención & control , Conducción de Automóvil/psicología , Conflicto Psicológico , Caminata/psicología , Accidentes de Tránsito/psicología , Accidentes de Tránsito/estadística & datos numéricos , HumanosRESUMEN
A convenient synthesis and the biological properties of new amides, esters and other derivatives of trans-stilbene are described. The key synthetic strategies involve the Wittig-Horner reaction of a phosphonium salt 9 and an aldehyde 10 to generate (E)- or (Z)-olefins and a coupling reaction of an acid 12 and various amines 13a-n to give trans-stilbene derivatives 15a-n in high yields. A amide derivative 15g showed three times more in vitro free radical-scavenging activity than resveratrol, while another 15d exhibited strong inhibitory activity against lipopolysaccharide (LPS)(a)-induced NO generation. Allylamide analogue 15a showed the most potent neuroprotective activity in glutamate-induced primary cortical neuron cells.
Asunto(s)
Diseño de Fármacos , Depuradores de Radicales Libres/síntesis química , Depuradores de Radicales Libres/farmacología , Fármacos Neuroprotectores/síntesis química , Fármacos Neuroprotectores/farmacología , Estilbenos/síntesis química , Estilbenos/farmacología , Animales , Línea Celular , Corteza Cerebral/citología , Depuradores de Radicales Libres/química , Cinética , L-Lactato Deshidrogenasa/metabolismo , Ratones , Ratones Endogámicos ICR , Microglía/citología , Microglía/efectos de los fármacos , Microglía/metabolismo , Neuronas/efectos de los fármacos , Neuronas/metabolismo , Fármacos Neuroprotectores/química , Óxido Nítrico/metabolismo , Estereoisomerismo , Estilbenos/químicaRESUMEN
A series of benzamide-containing stilbene derivatives was synthesized through the incorporation of short basic side-chains in the B-ring hydroxy position of resveratrol. Their antiplasmodial activity was evaluated in vitro against the chloroquine resistant Plasmodium falciparum D10 strain, showing IC(50) values between 1.5 and 80 microM, while their cytotoxicity was assessed using an human myeloid leukemia (U-937) cell line. With a selectivity ratio of > 51.02, the most selective of these derivatives, 29, also had the most lowest cytotoxic activity of the series.
Asunto(s)
Antimaláricos/química , Antimaláricos/farmacología , Estilbenos/química , Estilbenos/farmacología , Animales , Antimaláricos/síntesis química , Línea Celular Tumoral , Humanos , Concentración 50 Inhibidora , Plasmodium falciparum/efectos de los fármacos , Estilbenos/síntesis químicaRESUMEN
In the present study we report the simple synthesis and antitumour activity of novel stilbene derivatives 13-22. The key synthetic strategies involved Wadsworth-Horner-Emmons condensation and coupling reactions in high yields. All compounds showed significant growth inhibition on human tumour cell lines, with the most potent compound (19) exhibiting an IC(50) of 5.7 microM-11.4 microM in vitro.
Asunto(s)
Antineoplásicos Fitogénicos/síntesis química , Antineoplásicos Fitogénicos/farmacología , Estilbenos/química , Antineoplásicos Fitogénicos/química , Línea Celular Tumoral , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Concentración 50 Inhibidora , Resveratrol , Estilbenos/síntesis química , Estilbenos/farmacologíaRESUMEN
An efficient synthesis involving a key aldol reaction and biological properties of 1,3-diphenyl-2-propen-1-ones 8- 20 is described. The in vitro activity for 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging of 10 and 11 was 2 times higher than that for resveratrol. Compounds 9 and 11 were the strongest in suppression of in vitro nitric oxide (NO) generation and antiexcitotoxicity. Molecular modeling proposes an electron-donating group at the para position of acetophenones that leads to a dramatic increase in the suppression of NO production.
Asunto(s)
Chalcona/síntesis química , Chalcona/farmacología , Fármacos Neuroprotectores/síntesis química , Fármacos Neuroprotectores/farmacología , Aldehídos/química , Animales , Línea Celular , Supervivencia Celular/efectos de los fármacos , Chalcona/química , Glutaratos/farmacología , Lipopolisacáridos/farmacología , Ratones , Modelos Moleculares , Estructura Molecular , Neuronas/efectos de los fármacos , Neuronas/metabolismo , Fármacos Neuroprotectores/química , Óxido Nítrico/biosíntesis , Relación Estructura-Actividad , Técnicas de Cultivo de TejidosRESUMEN
Dihydroxy stilbene derivatives were designed based on lithospermic acid B and were prepared from 4-(chloromethyl)benzoic acid. The inhibitory activities of the novel compounds against protein tyrosine phosphatase 1B (PTP1B) were evaluated. 3,4-Dihydroxy stilbene carbonyl compounds (7, 11b, 27b) inhibited PTP1B with IC50 values comparable to molybdate, while the conjugation-extended compound (15b) showed inhibition 3-fold better than preclinical RK682. The introduction of electron withdrawing groups or amides into the second phenyl ring, or extension of the conjugation into the stilbene molecule may increase stability of the generated radicals.
Asunto(s)
Benzofuranos/química , Depsidos/química , Diseño de Fármacos , Proteína Tirosina Fosfatasa no Receptora Tipo 1/antagonistas & inhibidores , Estilbenos/síntesis química , Estilbenos/farmacología , Antioxidantes/química , Antioxidantes/farmacología , Benzofuranos/farmacología , Depsidos/farmacología , Modelos Moleculares , Estructura Molecular , Relación Estructura-ActividadRESUMEN
Hepatocellular cancer occurs more frequently among Koreans, Vietnamese, and Chinese than other racial/ethnic groups in the U.S. This excess risk can be attributed to high rates of chronic hepatitis B viral (HBV) infection and low rates of HBV vaccination among Asian immigrants. However, there is little available information regarding the hepatitis B knowledge, beliefs, and practices among Koreans, the fifth-largest Asian population in the U.S. This brief report summarizes results from 30 qualitative interviews and two focus groups investigating hepatitis and liver cancer prevention, behavior, and beliefs among first-generation Korean immigrant adults ages 18-64 years residing in the Seattle-Tacoma metropolitan area of Washington State. The report concludes with suggestions for future investigations to address the high rates of chronic HBV infection and hepatocellular cancer in this vulnerable population.