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1.
Molecules ; 26(12)2021 Jun 17.
Artigo em Inglês | MEDLINE | ID: mdl-34204232

RESUMO

Folk experiences suggest natural products in Tetradium ruticarpum can be effective inhibitors towards diabetes-related enzymes. The compounds were experimentally isolated, structurally elucidated, and tested in vitro for their inhibition effects on tyrosine phosphatase 1B (PTP1B) and α-glucosidase (3W37). Density functional theory and molecular docking techniques were utilized as computational methods to predict the stability of the ligands and simulate interaction between the studied inhibitory agents and the targeted proteins. Structural elucidation identifies two natural products: 2-heptyl-1-methylquinolin-4-one (1) and 3-[4-(4-methylhydroxy-2-butenyloxy)-phenyl]-2-propenol (2). In vitro study shows that the compounds (1 and 2) possess high potentiality for the inhibition of PTP1B (IC50 values of 24.3 ± 0.8, and 47.7 ± 1.1 µM) and α-glucosidase (IC50 values of 92.1 ± 0.8, and 167.4 ± 0.4 µM). DS values and the number of interactions obtained from docking simulation highly correlate with the experimental results yielded. Furthermore, in-depth analyses of the structure-activity relationship suggest significant contributions of amino acids Arg254 and Arg676 to the conformational distortion of PTP1B and 3W37 structures overall, thus leading to the deterioration of their enzymatic activity observed in assay-based experiments. This study encourages further investigations either to develop appropriate alternatives for diabetes treatment or to verify the role of amino acids Arg254 and Arg676.


Assuntos
Evodia/metabolismo , Inibidores de Glicosídeo Hidrolases/química , Proteína Tirosina Fosfatase não Receptora Tipo 1/antagonistas & inibidores , Produtos Biológicos/química , Produtos Biológicos/farmacologia , Inibidores Enzimáticos/farmacologia , Simulação de Acoplamento Molecular , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Proteína Tirosina Fosfatase não Receptora Tipo 1/efeitos dos fármacos , Proteína Tirosina Fosfatase não Receptora Tipo 1/metabolismo , Relação Estrutura-Atividade , alfa-Glucosidases/efeitos dos fármacos , alfa-Glucosidases/metabolismo
2.
BMC Infect Dis ; 17(1): 493, 2017 07 12.
Artigo em Inglês | MEDLINE | ID: mdl-28701159

RESUMO

BACKGROUND: Bloodstream infections (BSIs) are associated with high morbidity and mortality worldwide. However their aetiology, antimicrobial susceptibilities and associated outcomes differ between developed and developing countries. Systematic data from Vietnam are scarce. Here we present aetiologic data on BSI in adults admitted to a large tertiary referral hospital for infectious diseases in Hanoi, Vietnam. METHODS: A retrospective study was conducted at the National Hospital for Tropical Diseases between January 2011 and December 2013. Cases of BSI were determined from records in the microbiology department. Case records were obtained where possible and clinical findings, treatment and outcome were recorded. BSI were classified as community acquired if the blood sample was drawn ≤48 h after hospitalization or hospital acquired if >48 h. RESULTS: A total of 738 patients with BSI were included for microbiological analysis. The predominant pathogens were: Klebsiella pneumoniae (17.5%), Escherichia coli (17.3%), Staphylococcus aureus (14.9%), Stenotrophomonas maltophilia (9.6%) and Streptococcus suis (7.6%). The overall proportion of extended spectrum beta-lactamase (ESBL) production among Enterobacteriaceae was 25.1% (67/267 isolates) and of methicillin-resistance in S. aureus (MRSA) 37% (40/108). Clinical data was retrieved for 477 (64.6%) patients; median age was 48 years (IQR 36-60) with 27.7% female. The overall case fatality rate was 28.9% and the highest case fatality was associated with Enterobacteriaceae BSI (34.7%) which accounted for 61.6% of all BSI fatalities. CONCLUSIONS: Enterobacteriaceae (predominantly K. pneumoniae and E. coli) are the most common cause of both community and hospital acquired bloodstream infections in a tertiary referral clinic in northern Vietnam.


Assuntos
Bacteriemia/tratamento farmacológico , Bacteriemia/microbiologia , Farmacorresistência Bacteriana , Adulto , Bacteriemia/epidemiologia , Infecção Hospitalar/epidemiologia , Infecção Hospitalar/microbiologia , Farmacorresistência Bacteriana/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Escherichia coli/patogenicidade , Feminino , Humanos , Klebsiella pneumoniae/isolamento & purificação , Klebsiella pneumoniae/patogenicidade , Masculino , Pessoa de Meia-Idade , Mortalidade , Estudos Retrospectivos , Infecções Estafilocócicas/tratamento farmacológico , Infecções Estafilocócicas/epidemiologia , Infecções Estafilocócicas/microbiologia , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/isolamento & purificação , Staphylococcus aureus/patogenicidade , Centros de Atenção Terciária , Resultado do Tratamento , Vietnã/epidemiologia , beta-Lactamases/genética
4.
Bioorg Med Chem Lett ; 25(23): 5597-600, 2015 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-26522953

RESUMO

A new series of vinca-alkaloids derivatives containing various α,ß-unsaturated aromatic side chains was synthesized. Four new vinca-alkaloids derivatives showed selective cytotoxicities against KB tumor cell lines with IC50 value below 0.1 µM, thus comparable with vinblastine.


Assuntos
Antineoplásicos Fitogênicos/síntese química , Antineoplásicos Fitogênicos/uso terapêutico , Neoplasias/tratamento farmacológico , Vimblastina/uso terapêutico , Antineoplásicos Fitogênicos/química , Linhagem Celular Tumoral , Humanos , Concentração Inibidora 50 , Estrutura Molecular , Vimblastina/química , Alcaloides de Vinca/química
6.
BMJ Open ; 14(6): e076763, 2024 Jun 10.
Artigo em Inglês | MEDLINE | ID: mdl-38858157

RESUMO

INTRODUCTION: Transurethral resection of bladder tumour (TURBT) is one of the more common procedures performed by urologists. It is often described as an 'incision-free' and 'well-tolerated' operation. However, many patients experience distress and discomfort with the procedure. Substantial opportunity exists to improve the TURBT experience. An enhanced recovery after surgery (ERAS) protocol designed by patients with bladder cancer and their providers has been developed. METHODS AND ANALYSIS: This is a single-centre, randomised controlled trial to investigate the effectiveness of an ERAS protocol compared with usual care in patients with bladder cancer undergoing ambulatory TURBT. The ERAS protocol is composed of preoperative, intraoperative and postoperative components designed to optimise each phase of perioperative care. 100 patients with suspected or known bladder cancer aged ≥18 years undergoing initial or repeat ambulatory TURBT will be enrolled. The change in Quality of Recovery 15 score, a measure of the quality of recovery, between the day of surgery and postoperative day 1 will be compared between the ERAS and control groups. ETHICS AND DISSEMINATION: The trial has been approved by the Johns Hopkins Institutional Review Board #00392063. Participants will provide informed consent to participate before taking part in the study. Results will be reported in a separate publication. TRIAL REGISTRATION NUMBER: NCT05905276.


Assuntos
Neoplasias da Bexiga Urinária , Humanos , Neoplasias da Bexiga Urinária/cirurgia , Procedimentos Cirúrgicos Ambulatórios/métodos , Recuperação Pós-Cirúrgica Melhorada , Cistectomia/métodos , Ensaios Clínicos Controlados Aleatórios como Assunto , Feminino , Masculino , Assistência Perioperatória/métodos
7.
JBJS Rev ; 11(8)2023 08 01.
Artigo em Inglês | MEDLINE | ID: mdl-37549236

RESUMO

The cost of surgical care accounts for almost one-third of all health care spending in the United States. Within health care spending, the operating room (OR) is one of the largest health care costs during a perioperative episode of care. Efficiency in the OR has been associated with increased productivity, safety, and quality of care. However, multiple sources of delays can contribute to inefficiency, and improving efficiency in the OR requires a systematic approach to identify and address each issue. We report on the case of a process improvement initiative implemented in a large academic institution to improve OR efficiency in outpatient orthopaedic cases, and we discuss the lessons learned through this program. Optimizing workflow in the OR requires a multidisciplinary team approach consisting of clinician leaders with common goals and open discussion regarding the needs of each team member, including circulating nurses, surgical nurses/technologists, and anesthesiologists. Our experience highlights the importance of practical, clinician-driven changes that are supported by administrative engagement, resources for staffing and equipment, and institutional flexibility, which are required to implement systemic changes to address and improve efficiency in the OR.


Assuntos
Salas Cirúrgicas , Ortopedia , Humanos , Estados Unidos , Anestesiologistas
8.
Zoolog Sci ; 26(1): 54-65, 2009 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-19267612

RESUMO

Gravitactic bioconvective patterns created by Tetrahymena pyriformis in a Hele-Shaw apparatus were realized and compared with theoretical results. There were found to be two thresholds for bio-convection development: the first indicates the transition from the diffusion to the steady convection state; the second corresponds to the transition from the steady to the unsteady convection state. The results showed that the Hele-Shaw apparatus may be used as a physical analogy of porous media to study 2D bioconvection, with possible extensions to larger scale biological systems where population growth and distribution are driven by similar bio-physical interactions.


Assuntos
Gravitropismo , Movimento , Tetrahymena pyriformis/fisiologia , Animais , Modelos Biológicos
9.
Breathe (Sheff) ; 15(1): 55-59, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30838060

RESUMO

Can you diagnose this case of a Vietnamese woman with a 2-week history of cough ? http://ow.ly/9cIG30n21Pu.

10.
Breathe (Sheff) ; 14(3): 225-228, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30186520

RESUMO

Can you diagnose this clinical case of a rare disease presenting as a very common disease? http://ow.ly/Trzu30kGzk6.

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