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1.
Chem Res Toxicol ; 25(7): 1462-71, 2012 Jul 16.
Artigo em Inglês | MEDLINE | ID: mdl-22690874

RESUMO

1,3,5-Tri-N-alkylcarbamylphloroglucinols (1-4) are synthesized as a new series of bulky inhibitors of acetylcholinesterase that may block the catalytic triad, the anionic substrate binding site, and the entrance of the enzyme simultaneously. Among three series of phloroglucinol-derived carbamates, tridentate inhibitors 1,3,5-tri-N-alkylcarbamylphloroglucinols (1-4), bidentate inhibitors 3,5-di-N-n-alkylcarbamyloxyphenols (5-8), and monodentate inhibitors 5-N-n-alkylcarbamyloxyresorcinols (9-12), tridentate inhibitors 1-4 are the most potent inhibitors of mouse acetylcholinesterase. When different n-alkylcarbamyl substituents in tridentate inhibitors 1-4 are compared, n-octylcarbamate 1 is the most potent inhibitor of the enzyme. All inhibitors 1-12 are characterized as the pseudo substrate inhibitors of acetylcholinesterase. Thus, tridentate inhibitors 1-4 are supposed to be hydrolyzed to bidentate inhibitors 5-8 after the enzyme catalysis. Subsequently, bidentate inhibitors 5-8 and monodentate inhibitors 9-12 are supposed to yield monodentate inhibitors 9-12 and phloroglucinol, respectively, after the enzyme catalysis. This means that tridentate inhibitors 1-4 may act as long period inhibitors of the enzyme. Therefore, inhibitors 1-4 may be considered as a new methodology to develop the long-acting drug for Alzheimer's disease. Automated dockings of inhibitor 1 into the X-ray crystal structure of acetylcholinesterase suggest that the most suitable configuration of inhibitor 1 to the enzyme binding is the (1,3,5)- (cis,trans,trans)-tricarbamate rotamer. The cis-carbamyl moiety of this rotamer does not bind into the acetyl group binding site of the enzyme but stretches out itself to the entrance. The other two trans-carbmayl moieties of this rotamer bulkily block the tryptophan 86 residue of the enzyme.


Assuntos
Acetilcolinesterase/química , Inibidores da Colinesterase/síntese química , Floroglucinol/química , Acetilcolinesterase/metabolismo , Animais , Sítios de Ligação , Biocatálise , Carbamatos/química , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacologia , Cristalografia por Raios X , Isomerismo , Camundongos , Floroglucinol/síntese química , Floroglucinol/farmacologia , Estrutura Terciária de Proteína
2.
Mitochondrial DNA B Resour ; 7(8): 1416-1417, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-35937904

RESUMO

Callerya dielsiana is a Chinese endemic tropical/subtropical liana. We sequenced the complete chloroplast genome with the Illumina Hiseq X-Ten platform. The genome is obtained with 132,301 bp in length, lacking an inverted repeat (IR) region, contains 4 rRNAs, 30 tRNAs genes, and 76 protein-coding genes. The overall GC content is 33.9%. Based on the whole chloroplast genomes of 14 legume species, a phylogenetic tree is constructed and indicated that C. dielsiana belongs to the well-supported tribe Wisterieae. The tribe is sister to Glycyrrhiza and nested within the IRLC (Inverted Repeat-Lacking Clade) group of the subfamily Papilionoideae (Fabaceae).

3.
J Nurs Res ; 11(2): 137-47, 2003 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-12820077

RESUMO

Critical thinking is essential for professional nursing practice. Promoting critical thinking with teaching strategies has been a focus of nursing education and nursing research. Reading and writing assignments are teaching strategies for fostering critical thinking ability. We developed a course with the emphasis on critical reading and writing. The purposes of this study were to explore the effect of the course and teaching strategies on promoting critical thinking and to understand the learning experience and perception of nursing students as part of the course assessment plan. Quasi-experimental design and purposive sampling were used. 170 students of a two-year nursing program were grouped into an experimental and a control group depending on whether or not they took the course. The change in critical thinking ability was evaluated and determined based on performance in an article critique test before and after the course. Data was collected with an assessment tool developed for the purposes of the research and was analyzed with descriptive statistics, paired t-test, and two-factor analysis of variance with repeated measures and content analysis. The findings were: (1) The scores on the critique test at the end of the course in both groups were significantly higher than before the course (p<.001). The improvement in score of the experimental group, however, was significantly higher than that of the control group (p<.001). (2) Changes in thinking pattern and learning attitude, as well as a feeling of growth and achievement, were found in content analysis of students' self-evaluation of their learning experience and perception. Critical thinking skills were applied while learning the course. The results not only provide evidence to support the positive effect of reading and writing assignments on critical thinking ability but also confirm the teaching and learning activity design for the course.


Assuntos
Competência Clínica/normas , Educação Técnica em Enfermagem/métodos , Armazenamento e Recuperação da Informação/métodos , Medicina na Literatura , Literatura de Revisão como Assunto , Estudantes de Enfermagem/psicologia , Ensino/métodos , Pensamento , Atitude do Pessoal de Saúde , Capacitação de Usuário de Computador , Análise Fatorial , Conhecimentos, Atitudes e Prática em Saúde , Humanos , Conhecimento , Pesquisa em Educação em Enfermagem , Publicações Periódicas como Assunto , Avaliação de Programas e Projetos de Saúde , Leitura , Redação
4.
J Nurs Res ; 12(3): 203-12, 2004 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-15362012

RESUMO

The purpose of this study was to examine factors affecting the development of nursing competence in the writing of N3 (clinical nurse level III) case reports. A cross-sectional survey was conducted in 13 hospitals in southern Taiwan from July to October, 2002. The subjects included 239 nurses who had passed N3 case report accreditation. The results show that (1) nurses rated their current competence at a fairly good level ( 5.57 +/- 0.74). There was no significant difference between nurses ' subjective self-evaluation and supervisors ' objective evaluation (5.57 +/- 0.74 vs 5.55 +/- 0.89; t = 0.162, p = 0.871). (2) The nurses ' self-rating, supervisors ', and colleagues ' evaluation all indicated moderate progress in nursing competence after writing N3 case reports. The progress scores rated by nurses themselves, supervisors and colleagues were not significantly different (4.89 +/- 1.35 vs. 4.84 +/- 1.57 vs. 4.84 + 1.26; F = 0.096, p =.909). This finding reveals that writing N3 case reports has a positive effect on nursing competence. (3) The results also indicate that ' Attitude toward N3 case report ', 'Writing difficulty ', ' Preparation for writing case report ' were the three predicting factors of progress in nursing competence, which accounted for 26.2 % of the total variance. Therefore we recommend that N3 advancement education should include guidance in alleviating writing difficulty and emphasis on implementing various types of preparation for writing case reports, as effective ways to improve nursing competence.


Assuntos
Mobilidade Ocupacional , Certificação , Competência Clínica/normas , Recursos Humanos de Enfermagem Hospitalar/educação , Recursos Humanos de Enfermagem Hospitalar/normas , Adulto , Análise de Variância , Atitude do Pessoal de Saúde , Estudos Transversais , Educação Continuada em Enfermagem/normas , Avaliação de Desempenho Profissional , Humanos , Pessoa de Meia-Idade , Avaliação das Necessidades , Enfermeiros Administradores/psicologia , Pesquisa em Educação em Enfermagem , Pesquisa em Avaliação de Enfermagem , Registros de Enfermagem , Recursos Humanos de Enfermagem Hospitalar/psicologia , Grupo Associado , Estudos Retrospectivos , Autoavaliação (Psicologia) , Inquéritos e Questionários , Taiwan , Redação
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