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1.
Scand J Psychol ; 63(5): 476-483, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-35604020

RESUMO

The COVID-19 pandemic has affected nearly every aspect of our lives and has caused a considerable rise in psychological complaints such as anxieties and depression. The majority of studies so far has focused on outcomes of the COVID-19 pandemic. To augment current knowledge, we focus on the antecedents of COVID-19 rumination. Specially, we examine how negative and positive work events prior to the outbreak influence individuals' coping capacity with regard to COVID-19 (i.e., the extent to which individuals have recurrent negative thoughts about COVID-19). Drawing on Conservation of Resources Theory (COR), we maintain that positive and negative work events prior to the pandemic can affect one's self-efficacy experiences and in turn can impact recurrent negative thoughts about COVID-19. Alongside exploring the proposed theoretical mediation model, we test one of the key assumptions of the COR theory: the notion of primacy of negative over positive affect that results from negative (vs. positive) work events. Three-waved data was collected among Dutch employees (T1 = 302; T2 = 199; T3 = 171); two prior to the pandemic and one at the onset of the outbreak. Results showed that positive work events increased self-efficacy, which in turn reduced COVID-19 rumination. Contrary to the expectation of primacy of the effects of negative work events, we found no significant impact of negative work events on individuals' COVID-19 rumination.


Assuntos
COVID-19 , Adaptação Psicológica , Ansiedade/psicologia , Humanos , Pandemias
2.
Int J Health Plann Manage ; 36(4): 1166-1177, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33817832

RESUMO

OBJECTIVES: Starting with the spring of 2020, COVID-19 pandemic has impacted nearly every aspect of our lives. Due to its threatening nature, along with the rapid rise in contamination and mortality figures, the spread of the virus has caused a considerable rise in individuals' anxieties. To enable the assessment of the COVID-19-triggered individual rumination, we developed and tested a COVID-19 Rumination Scale (C-19RS). DESIGN AND METHODS: Demographics (i.e., gender, age and education) and several items assessing the proximity of one's exposure to the virus (i.e., whether one's family and close friends are affected) were evaluated as antecedents of C-19RS that provided evidence for the criterion validity of the scale. A sample of 523 Dutch employees working in different companies and sectors completed the online survey in March 2020. RESULTS: Results showed that women, older individuals and workers with lower educational level ruminated considerably more about COVID-19. In keeping with prior theoretical and empirical work on stress and coping, we established that COVID-19 ruminative thoughts can unlock withdrawal coping reactions (i.e., self-handicapping) and drain individual's energy (i.e., causing emotional exhaustion), whereby providing evidence for the predictive validity of the new instrument. In addition, we examined how the COVID-19 rumination evolved during the nearly 3-week period of the data collection, a time-frame that coincided with the introduction of the national restrictive measures in the Netherlands. Results showed a drop in the level of rumination, which might be indicative of potential habituation with the stressor. CONCLUSIONS: The results supported the sound psychometric qualities of the scale.


Assuntos
COVID-19/psicologia , Escalas de Graduação Psiquiátrica , Ruminação Cognitiva , Adaptação Psicológica , Adolescente , Adulto , Fatores Etários , Idoso , Escolaridade , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Países Baixos/epidemiologia , Psicometria , Reprodutibilidade dos Testes , Fatores de Risco , Fatores Sexuais , Inquéritos e Questionários , Adulto Jovem
3.
Faraday Discuss ; 189: 529-46, 2016 07 18.
Artigo em Inglês | MEDLINE | ID: mdl-27115034

RESUMO

We developed a model (CiTTy-Street-UFP) of traffic-related particle behaviour in a street canyon and in the nearby downwind urban background that accounts for aerosol dynamics and the variable vapour pressure of component organics. The model simulates the evolution and fate of traffic generated multicomponent ultrafine particles (UFP) composed of a non-volatile core and 17 Semi-Volatile Organic Compounds (SVOC, modelled as n-alkane proxies). A two-stage modelling approach is adopted: (1) a steady state simulation inside the street canyon is achieved, in which there exists a balance between traffic emissions, condensation/evaporation, deposition, coagulation and exchange with the air above roof-level; and (2) a continuing simulation of the above-roof air parcel advected to the nearby urban park during which evaporation is dominant. We evaluate the component evaporation and associated composition changes of multicomponent organic particles in realistic atmospheric conditions and compare our results with observations from London (UK) in a street canyon and an urban park. With plausible input conditions and parameter settings, the model can reproduce, with reasonable fidelity, size distributions in central London in 2007. The modelled nucleation-mode peak diameter, which is 23 nm in the steady-state street canyon, decreases to 9 nm in a travel time of just 120 s. All modelled SVOC in the sub-10 nm particle size range have evaporated leaving behind only non-volatile material, whereas modelled particle composition in the Aitken mode contains SVOC between C26H54 and C32H66. No data on particle composition are available in the study used for validation, or elsewhere. Measurements addressing in detail the size resolved composition of the traffic emitted UFP in the atmosphere are a high priority for future research. Such data would improve the representation of these particles in dispersion models and provide the data essential for model validation. Enhanced knowledge of the chemical composition of nucleation-mode particles from diesel engine exhaust is needed to predict both their atmospheric behaviour and their implications for human health.

4.
J Nurs Manag ; 24(7): 915-922, 2016 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-27237454

RESUMO

AIM: This study investigated whether Nigerian nurses' emotional exhaustion and active learning were predicted by job demands, control and social support. BACKGROUND: Limited research has been conducted concerning nurses' work stress in developing countries, such as Nigeria. Accordingly, it is not clear whether work interventions for improving nurses' well-being in these countries can be based on work stress models that are developed in Western countries, such as the job demand control support model, as well as on empirical findings of job demand control support research. METHOD: Nurses from Nurses Across the Borders Nigeria were invited to complete an online questionnaire containing validated scales; 210 questionnaires were fully completed and analysed. Multiple regression analysis was used to test the hypotheses. RESULTS: Emotional exhaustion was higher for nurses who experienced high demands and low supervisor support. Active learning occurred when nurses worked under conditions of high control and high supervisor support. CONCLUSION: The findings suggest that the job demand control support model is applicable in a Nigerian nursing situation; the model indicates which occupational stressors contribute to poor well-being in Nigerian nurses and which work characteristics may boost nurses' active learning. IMPLICATIONS FOR NURSING MANAGEMENT: Job (re)design interventions can enhance nurses' well-being and learning by guarding nurses' job demands, and stimulating job control and supervisor support.


Assuntos
Satisfação no Emprego , Aprendizagem , Enfermeiras e Enfermeiros/psicologia , Carga de Trabalho/normas , Adulto , Atitude do Pessoal de Saúde , Feminino , Humanos , Liderança , Masculino , Pessoa de Meia-Idade , Nigéria , Análise de Regressão , Apoio Social , Estresse Psicológico/etiologia , Inquéritos e Questionários , Carga de Trabalho/psicologia
5.
Biotechnol Biotechnol Equip ; 28(1): 160-163, 2014 Jan 02.
Artigo em Inglês | MEDLINE | ID: mdl-26019502

RESUMO

Galantamine hydrobromide (GAL) is a reversible acetylcholinesterase inhibitor, with properties to increase the concentration of acetylcholine in several brain structures. The aim of this study is to determine the effect of new galantamine peptide esters: 3,4-dichlorophenyl-alanil-leucil-glycine-galantamine (GAL-LEU) and 3,4-dichlorophenyl-alanil-valil-glycine-galantamine (GAL-VAL), on locomotor activity in mice and cognitive processes in experimental model of learning and memory in rats. The results showed that per oral administration of GAL-LEU in a dose of 3 mg per kg improved the cognitive processes by increasing the conditional avoidances and learning ability after the 5th day of application and preserved the memory at the 12th day of the study.

6.
Biotechnol Biotechnol Equip ; 28(2): 360-365, 2014 Mar 04.
Artigo em Inglês | MEDLINE | ID: mdl-26019521

RESUMO

The marketing management includes analysis of market opportunities, selection of target markets, planning, developing and implementing of marketing strategies, monitoring and result control. The object of the present study was to analyse the marketing approaches applied for non-steroidal anti-inflammatory drugs (NSAIDs) in Bulgaria. The performed SWOT(planning method used to evaluate the strengths, weaknesses, opportunities, and threats) analysis for one of the leading Bulgarian manufacturers marked the complex corporative strategy for stimulating the sales of NSAIDs. The study results show that the legislation frame in the country gives an opportunity for regulation of the NSAID market in order that incorrect marketing approaches such as disloyal competition are avoided.

7.
Pharmaceuticals (Basel) ; 17(4)2024 Mar 23.
Artigo em Inglês | MEDLINE | ID: mdl-38675372

RESUMO

Sambucus nigra L. (S. nigra, SN) or black elder is a traditional medicinal plant widely used worldwide for therapeutic and dietary purposes. The aim of the current study was to investigate the anti-inflammatory and antinociceptive activities of black elder fruit and flower extracts (SNFrE and SNFlE, respectively). The primary polyphenol constituents in the flower extract were flavonoids and phenolic acids, while anthocyanins were the main components in the fruit extract. SNFrE revealed pronounced and dose-dependent in vivo anti-inflammatory activity assessed by the cotton pellet-induced granuloma test. Doses of 10, 20, and 50 mg/kg BW of SNFrE reduced the weight of induced granuloma in rats by 20.3%, 20.5%, and 28.4%, respectively. At the highest dose (50 mg/kg BW), SNFrE had significant (p < 0.01) anti-inflammatory activity comparable to that of diclofenac, the reference compound used (10 mg/kg BW). In addition, the in vivo antinociceptive activity of the extracts in mice was estimated using the acetic-acid-induced writhing test. Both extracts at doses of 50 mg/kg BW inhibited the abdominal contractions induced by the acetic acid significantly comparing to the control group (p < 0.01). Our findings indicate that black elder extracts and particularly SNFrE possess anti-inflammatory and antinociceptive activities, providing experimental evidence for the use of S. nigra in traditional medicine.

8.
Pak J Pharm Sci ; 26(6): 1103-7, 2013 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-24191313

RESUMO

Lozenges (tablets intended to be dissolved slowly in the mouth) were evaluated as delivery system for polysaccharides extract from Althaea officinalis L. (marshmallow) root. The aim of investigation was to improve of the efficacy of convenient preparations for the treatment of irritated oropharyngeal mucosa and associated dry irritable cough. The formulations studied were prepared with water extract of roots of Althaea officinalis L. The polysaccharides extract was obtained by ultrasonification. Acute oral toxicity (LD 50 p.o.) of the obtained extract was estimated in mice. Four models of lozenges based on different excipients were formulated. The characteristics of the preparations: resistance to crushing, friability testing, disintegration time and drug release properties were evaluated.


Assuntos
Althaea , Tosse/tratamento farmacológico , Extratos Vegetais/uso terapêutico , Animais , Química Farmacêutica , Excipientes , Masculino , Camundongos , Raízes de Plantas , Comprimidos
9.
Antibiotics (Basel) ; 12(8)2023 Aug 09.
Artigo em Inglês | MEDLINE | ID: mdl-37627722

RESUMO

BACKGROUND: Klebsiella pneumoniae is among the most common Gram-negative bacteria isolated to neonatal intensive care units (NICU) and one of the leading causes of morbidity and mortality. The ceftazidime/avibactam (CAZ-AVI) combination is approved for infections caused by aerobic Gram-negative organisms. It is licensed for use in infants over 3 months old. There are no safety and efficacy data regarding the administration of CAZ-AVI to infants younger than 3 months, except for a few case reports. CASE PRESENTATION: This report describes a severely intoxicated 24-day-old, full-term, male neonate transferred to NICU level III from a secondary maternity hospital due to the deterioration of his general condition. On day four of admission, blood culture revealed the pan-drug-resistant (PDR) K. pneumoniae ss. pneumoniae, susceptible only to CAZ-AVI, which thus represented the only treatment option. Off-label CAZ-AVI was administered intravenously as a salvage therapy. CONCLUSIONS: In healthcare settings, treating resistant K. pneumoniae presents serious challenges, especially in NICU patients. The off-label treatment with CAZ-AVI for 17 days was safe and effective in this one-month-old patient. A year later, the patient was healthy with normal cognitive development.

10.
Pharmaceutics ; 15(12)2023 Nov 21.
Artigo em Inglês | MEDLINE | ID: mdl-38139994

RESUMO

Off-label prescribing is widespread among pediatricians, and it is unlikely that this trend will soon be bound by a uniform legal framework. This is necessitated by the fact that there are four variables: the patient's health condition, the physician's experience and knowledge, the legislative measures (laws, directives, guidelines, and recommendations), and finally, the pharmaceutical industry. There is considerable concern worldwide about the use of off-label medicines in children. We may call it an enormous global problem that is much talked about and written about; however, we should not forget that the goal around which everyone should unite is the patient's life. For healthcare providers, the most important thing will always be the health and preservation of the patient's life, particularly when it comes to children with life-threatening conditions in neonatal and pediatric intensive care units (NICU and PICU). The study aimed to examine the prevalence of off-label drug use in pediatrics. Literature research was conducted, and we included studies from 2012 to 2022 that evaluated off-label drug prevalence in various pediatric patient populations.

12.
Artigo em Inglês | MEDLINE | ID: mdl-33802094

RESUMO

The main goal of this study was to develop a scale for measuring Disengaging Leader-ship (DEL) behaviors and to provide preliminary evidence for the validity of this new instrument. Developing such new measures is needed given current concepts that tap into negative leadership behaviors are rarely based on a sound theoretical framework. Drawing on the core premises of Self-Determination Theory (SDT) regarding employees' basic needs and, more specifically, building on its more recent extended framework, including employees' needs frustration, we derived four dimensions that constitute Disengaging Leadership behaviors (coercive disengaging leadership, isolating disengaging leadership, eroding disengaging leadership, and demotivating disengaging leadership). To examine the factor structure and psychometric properties of the new Disengaging Leadership Scale (DLS), Exploratory Factor Analysis (EFA), Confirmatory Factor Analysis (CFA), and reliability analyses were conducted. Results supported the hypothesized four-factor structure of the DLS and showed that this factorial structure remained invariant across employees occupying blue-collar, white-collar, or managerial positions. Finally, we successfully tested convergent, divergent, and construct validity of DLS. We established that DEL is associated with employees' needs frustration and with their experiences of emotional exhaustion. It is concluded that the DLS has sound psychometric properties and can be used in future research on the dark side of leadership.


Assuntos
Frustração , Liderança , Análise Fatorial , Psicometria , Reprodutibilidade dos Testes
13.
Environ Pollut ; 266(Pt 3): 115223, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32731052

RESUMO

Traffic-generated ultrafine particles (UFPs) in the urban atmosphere have a high proportion of their composition comprised of semi-volatile compounds (SVOCs). The evaporation/condensation processes of these SVOCs can alter UFP number size distributions and play an important role in determining the fate of UFPs in urban areas. The neighbourhood-scale dispersion (over distances < 1 km) and evolution of traffic-generated UFPs for a real-world street network in central London was simulated by using the WRF-LES model (the large eddy simulation mode of the Weather Research and Forecasting modelling system) coupled with multicomponent microphysics. The neighbourhood scale dispersion of UFPs was significantly influenced by the spatial pattern of the real-world street emissions. Model output indicated the shrinkage of the peak diameter from the emitted profile to the downwind profile, due to an evaporation process during neighbourhood-scale dispersion. The dilution process and the aerosol microphysics interact with each other during the neighbourhood dispersion of UFPs, yielding model output that compares well with measurements made at a location downwind of an intense roadside source. The model captured the total SVOC concentrations well, with overestimations for gas concentrations and underestimations for particle concentrations, particularly of the lighter SVOCs. The contribution of the intense source, Marylebone Road (MR) in London, to concentrations at the downwind location (as estimated by a model scenario with emissions from MR only) is comparable with that of the rest of the street network (a scenario without emissions from MR), implying that both are important. An appreciable level of non-linearity is demonstrated for nucleation mode UFPs and medium range carbon SVOCs at the downwind receptor site.


Assuntos
Poluentes Atmosféricos/análise , Material Particulado/análise , Monitoramento Ambiental , Londres , Tamanho da Partícula , Emissões de Veículos/análise
14.
Artigo em Inglês | MEDLINE | ID: mdl-31126157

RESUMO

Prior research indicates that workplace changes can have both positive and negative consequences for employees. To explore the mechanisms that trigger these different outcomes, we propose and test a mediation model, which builds on the premises of the challenge-hindrance model of work stress. Specifically, we suggest that whereas workplace changes can engender positive outcomes (e.g., learning outcomes) through an increase in learning demands, they can also enhance negative outcomes (e.g., emotional exhaustion) through increased perceptions of qualitative job insecurity. While we made these specific assumptions, we also analyzed the reversed causation relationships. Two-wave data obtained from 1366 Dutch employees were used to test the study hypotheses. The results showed that the reciprocal causation model had the best fit for the data. However, whereas emotional exhaustion was only mediated by qualitative job insecurity, no mediation was found by learning demands. In addition to the hypothesized effects, several reversed causation effects emerged from the analyses, indicating that the relationships between workplace changes and employee learning and strain are not unidirectional. This underscores the need for a broader view on the causes and effects of workplace changes, as the traditional causation relationships (i.e., perceptions of workplace changes impacting employee learning and strain experiences) are insufficient to explain the complex dynamics between the studied phenomena.


Assuntos
Estresse Ocupacional , Inovação Organizacional , Local de Trabalho/psicologia , Adulto , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Inquéritos e Questionários
15.
Environ Pollut ; 238: 186-195, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29554566

RESUMO

This study implements a two-box model coupled with ultrafine particle (UFP) multicomponent microphysics for a compartmentalised street canyon. Canyon compartmentalisation can be described parsimoniously by three parameters relating to the features of the canyon and the atmospheric state outside the canyon, i.e. the heterogeneity coefficient, the vortex-to-vortex exchange velocity, and the box height ratio. The quasi-steady solutions for the two compartments represent a balance among emissions, microphysical aerosol dynamics (i.e. evaporation/condensation of semi-volatiles, SVOCs), and exchange processes, none of which is negligible. This coupled two-box model can capture significant contrasts in UFP number concentrations and a measure of the volatility of the multi-SVOC-particles in the lower and upper canyon. Modelled ground-level UFP number concentrations vary across nucleation, Aitken, and accumulation particle modes as well-defined monotonic functions of canyon compartmentalisation parameters. Compared with the two-box model, a classic one-box model (without canyon compartmentalisation) leads to underestimation of UFP number concentrations by several tens of percent typically. By quantifying the effects of canyon compartmentalisation, this study provides a framework for understanding how canyon geometry and the presence of street trees, street furniture, and architectural features interact with the large-scale atmospheric flow to determine ground-level pollutant concentrations.


Assuntos
Poluentes Atmosféricos/análise , Monitoramento Ambiental , Modelos Químicos , Material Particulado/análise , Aerossóis , Cidades , Árvores , Emissões de Veículos/análise
16.
Proc Math Phys Eng Sci ; 474(2220): 20180492, 2018 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30602933

RESUMO

Diesel engine emissions are by far the largest source of nanoparticles in many urban atmospheres, in which they dominate the particle number count, and may present a significant threat to public health. This paper reviews knowledge of the composition and atmospheric properties of diesel exhaust particles, and exemplifies research in this field through a description of the FASTER project (Fundamental Studies of the Sources, Properties and Environmental Behaviour of Exhaust Nanoparticles from Road Vehicles) which studied the size distribution-and, in unprecedented detail, the chemical composition-of nanoparticles sampled from diesel engine exhaust. This information has been systematized and used to inform the development of computational modules that simulate the behaviour of the largely semi-volatile content of the nucleation mode particles, including consequent effects on the particle size distribution, under typical atmospheric conditions. Large-eddy model studies have informed a simpler characterization of flow around the urban built environment, and include aerosol processes. This modelling and engine-laboratory work have been complemented by laboratory measurements of vapour pressures, and the execution of two field measurement campaigns in London. The result is a more robust description of the dynamical behaviour on the sub-kilometre scale of diesel exhaust nanoparticles and their importance as an urban air pollutant.

17.
Acta Pharm ; 57(3): 361-70, 2007 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-17878115

RESUMO

The synthesis of some aliphatic and arylaliphatic amides of caffeine-8-thioglycolic acid was studied. The structures of synthesized compounds were proved by micro-analyses, IR- and 1H NMR data. Values of acute p.o. and i.p. toxicity in mice show lower toxicity compared to caffeine. Declines in spontaneous locomotor activity support the idea of depressive CNS activity of the compounds. Two compounds exhibited brain antihypoxic activity (5a and 5b against haemic and circulatory hypoxia, respectively).


Assuntos
Cafeína/síntese química , Cafeína/farmacologia , Hipóxia-Isquemia Encefálica/prevenção & controle , Tioglicolatos/síntese química , Administração Oral , Animais , Cafeína/análogos & derivados , Cafeína/química , Hipóxia-Isquemia Encefálica/tratamento farmacológico , Injeções Intraperitoneais , Espectroscopia de Ressonância Magnética , Camundongos , Estrutura Molecular , Atividade Motora/efeitos dos fármacos , Tioglicolatos/química , Tioglicolatos/farmacologia , Testes de Toxicidade Aguda/métodos
18.
Postgrad Med ; 128(8): 790-796, 2016 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-27700189

RESUMO

OBJECTIVES: The purpose of this study was to reveal different subgroups of patients with at least moderate risk of developing diabetes in the next 10 years, based on clustering of cardiovascular risk factors. METHODS: We performed a one-center cross-sectional study of adult patients (n = 109, median age 45 years) with Findrisc score of above 11 out of 26 maximum. We included in the cluster analysis anthropometrics, lipid and carbohydrate parameters obtained in oral glucose tolerance test (OGTT), insulin, C-peptide, creatinine, C-reactive protein, liver enzymes, beta-cell function, insulin sensitivity and insulin resistance (HOMA calculations). We also evaluated the atherogenic index of plasma (AIP). RESULTS: We identified three metabolic phenotypes of patients with at least moderate Findrisc score-one 'male' (cluster AM, n = 24), and two 'female' phenotypes (cluster AW, n = 9 and cluster BW, n = 76). Men were almost homogenous for their metabolic phenotype, with lower fat percentage than women (p < .05). Most of the women (cluster BW, n = 76) presented with better metabolic pattern i.e. lower insulin resistance, lower C-reactive protein, lower degree of obesity and visceral fat rating (p < .05), despite the higher fat percentage (p < .05). Some of the women, however, (cluster AW, n = 9) presented with parameters very similar to that of men (cluster AM) and significantly higher than in cluster BW. Despite the lack of significant differences in lipid parameters among clusters, AIP was significantly lower in cluster BW (p < .05). CONCLUSION: Most of the women presented with clearly less unfavorable atherogenic risk than men. Two different phenotypes of obese women with at least moderate Findrisc score were revealed, and the level of inflammation seems to be the main discriminant factor. Larger prospective studies are required to elucidate whether those are really two different pathogenically phenotypes or if they belong to the same phenotype's continuum.


Assuntos
Doenças Cardiovasculares/epidemiologia , Obesidade/epidemiologia , Adulto , Idoso , Aterosclerose/epidemiologia , Glicemia , Pesos e Medidas Corporais , Proteína C-Reativa , Estudos Transversais , Diabetes Mellitus Tipo 2/epidemiologia , Dieta , Exercício Físico , Feminino , Teste de Tolerância a Glucose , Humanos , Hipertensão/epidemiologia , Resistência à Insulina , Lipídeos/sangue , Masculino , Pessoa de Meia-Idade , Estudos Prospectivos , Fatores de Risco
19.
Protein Pept Lett ; 22(10): 913-22, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26129719

RESUMO

New derivatives of galanthamine containing peptide fragments with ß-secretase inhibitor activity were synthesized. In position 6 of the galanthamine new shortened analogues of ß-secretase inhibitor OM 99-2 (Boc-Val-Asn-Leu-Ala-OH and Boc-Val-Asn-Leu-Ala-Val-OH) were included. The new derivatives of the galanthamine in position 11 including Boc and norgalanthamine in P3 or P4 positions, Val in P2' position and benzylamin in P3'-position were also synthesized. All new peptides were investigated on mice for acute toxicity. The test compounds were administered to mice via intraperitoneal (i.p.) route. They have low toxicity (LD50>1000 mg/kg) after i.p. The compound 11-N-demethyl-11-N-N-[Boc-Asp(Asp-Leu-Ala-Val-NH-Bzl)]-Galanthamine was investigated by two way active avoidance method. The compound has good influence on the conditioned reflexes, which improved the processes of learning and memory. Inhibition activity of newly synthesized compounds was monitored against BuChE and IC50 values are determined. All compounds show activity in micromolar concentration. Compounds 5 and 6 have around 10 times higher activity than galanthamine. Compounds 4 and 9 also show good activity. All newly synthesized compounds show low acute toxicity.


Assuntos
Doença de Alzheimer/prevenção & controle , Galantamina/química , Galantamina/síntese química , Peptídeos/química , Peptídeos/síntese química , Animais , Galantamina/uso terapêutico , Humanos , Camundongos , Peptídeos/uso terapêutico
20.
Acta Pharm ; 54(2): 151-6, 2004 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-15274758

RESUMO

Dry ethyl acetate extract containing flavonoids was obtained from above-ground parts of Astragalus corniculatus Bieb. Seven flavonoids were isolated and identified as rutin, hyperoside, isoquercitrin, narcissin, quercetin, kaempferol and isorhamnetin for the first time. The extract was found to be practically non-toxic (acute oral toxicity > 5 g kg(-1) in mice). The extract was investigated for antihypoxic activity in two models of experimental hypoxia--haemic and circulatory. Antihypoxic activity was especially pronounced in the model of circulatory hypoxia. This effect may be attributed, at least in part, to the presence of flavonoids in the extract.


Assuntos
Acetatos/análise , Acetatos/uso terapêutico , Astrágalo , Hipóxia Encefálica/tratamento farmacológico , Animais , Hipóxia Encefálica/metabolismo , Masculino , Camundongos , Extratos Vegetais/análise , Extratos Vegetais/uso terapêutico
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