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1.
Eur J Pharm Sci ; 199: 106820, 2024 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-38821248

RESUMO

Obesity is a global public health problem and is related with fatal diseases such as cancer and cardiovascular and metabolic diseases. Medical and lifestyle-related strategies to combat obesity have their limitations. White adipose tissue (WAT) browning is a promising strategy for increasing energy expenditure in individuals with obesity. Uncoupling protein 1 (UCP1) drives WAT browning. We previously screened natural products that enable induction of Ucp1 and demonstrated that these natural products induced WAT browning and increased energy expenditure in mice with diet-induced obesity. In this study, we aimed to extensively optimise the structure of compound 1, previously shown to promote WAT browning. Compound 3 s exhibited a significantly higher ability to induce Ucp1 in white and brown adipocytes than did compound 1. A daily injection of compound 3 s at 5 mg/kg prevented weight gain by 13.6 % in high-fat diet-fed mice without any toxicological observation. In addition, compound 3 s significantly improved glucose homeostasis, decreased serum triacylglycerol levels, and reduced total cholesterol and LDL cholesterol levels, without altering dietary intake or physical activity. Pharmaceutical properties such as solubility, lipophilicity, and membrane permeability as well as metabolic stability, half-life (T1/2), and blood exposure ratio of i.p to i.v were significantly improved in compound 3 s when compared with those in compound 1. Regarding the mode of action of WAT browning, the induction of Ucp1 and Prdm4 by compounds 1 and 3 s was dependent on Akt1 in mouse embryonic fibroblasts. Therefore, this study suggests the potential of compound 3 s as a therapeutic agent for individuals with obesity and related metabolic diseases, which acts through the induction of WAT browning as well as brown adipose tissue activation.


Assuntos
Dieta Hiperlipídica , Metabolismo Energético , Resistência à Insulina , Camundongos Endogâmicos C57BL , Obesidade , Proteína Desacopladora 1 , Animais , Dieta Hiperlipídica/efeitos adversos , Obesidade/tratamento farmacológico , Obesidade/metabolismo , Metabolismo Energético/efeitos dos fármacos , Masculino , Camundongos , Proteína Desacopladora 1/metabolismo , Tecido Adiposo Branco/efeitos dos fármacos , Tecido Adiposo Branco/metabolismo , Chalconas/farmacologia , Camundongos Obesos , Fármacos Antiobesidade/farmacologia , Células 3T3-L1
2.
J Pain Symptom Manage ; 37(2): 156-67, 2009 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-18687571

RESUMO

The Hospice Quality of Life Scale (HQLS) for Korean cancer patients was developed as follows: 1) item generation by semi-structured interviews and review of existing scales, 2) item reduction by the Delphi method, and 3) reliability and validity test. The final HQLS consisted of 40 questions within 13 domains and the internal consistency was 0.41-0.93. The domain "Family and Economy" was uniquely separated from the general social issues, which reflects the family-oriented Asian culture. For construct validity, the HQLS scores differed significantly according to their Eastern Cooperative Oncology Group Performance Status (known-group validity). Convergent and discriminant success rates were optimal in nine and four subscales, respectively. Total and subscale scores were significantly correlated with the related subscales in the European Organization for Research and Treatment of Cancer QLQ-C30 and the McMaster Quality of Life Scale, which supported the concurrent validity. HQLS was approved as an efficient tool for assessing the quality of life of Korean cancer patients who were receiving hospice and palliative care.


Assuntos
Indicadores Básicos de Saúde , Cuidados Paliativos na Terminalidade da Vida/estatística & dados numéricos , Neoplasias/epidemiologia , Neoplasias/enfermagem , Satisfação do Paciente/estatística & dados numéricos , Qualidade de Vida , Inquéritos e Questionários , Feminino , Humanos , Coreia (Geográfico)/epidemiologia , Masculino , Pessoa de Meia-Idade , Neoplasias/diagnóstico , Cuidados Paliativos/estatística & dados numéricos , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Resultado do Tratamento
3.
J Pain Symptom Manage ; 31(6): 553-62, 2006 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-16793495

RESUMO

Appropriate pain assessment is very important for managing cancer pain. This study was designed to evaluate the utility of the Korean Cancer Pain Assessment Tool (KCPAT) by assessing changes in the management of cancer pain. The changes in pain intensity, the pattern of drug prescriptions, and the patients' satisfaction with pain control were analyzed after using the KCPAT. The results indicated that pain medicine prescriptions were changed in 194 (51.5%) cases after using the KCPAT, and 69.5% of these changes were affected by the KCPAT. After using the KCPAT, pain intensity as assessed by the Visual Analogue Scale (VAS, 0-10cm) decreased (4.31+/-2.35 vs. 3.60+/-2.45, P<0.0001), and the presence of associated symptoms and psychosocial items was significantly reduced. The patients' satisfaction with pain control was improved. Forty-four physicians (89.8%) thought that the KCPAT was useful. The KCPAT improved patients' satisfaction with pain control and was a useful tool for evaluating and managing cancer pain.


Assuntos
Idioma , Neoplasias/complicações , Medição da Dor , Dor/diagnóstico , Dor/tratamento farmacológico , Satisfação do Paciente , Idoso , Analgésicos/administração & dosagem , Feminino , Humanos , Coreia (Geográfico) , Masculino , Pessoa de Meia-Idade , Dor/etiologia , Resultado do Tratamento
4.
J Korean Med Sci ; 20(5): 877-82, 2005 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-16224166

RESUMO

The Korean Cancer Pain Assessment Tool (KCPAT), which was developed in 2003, consists of questions concerning the location of pain, the nature of pain, the present pain intensity, the symptoms associated with the pain, and psychosocial/spiritual pain assessments. This study was carried out to evaluate the reliability and validity of the KCPAT. A stratified, proportional-quota, clustered, systematic sampling procedure was used. The study population (903 cancer patients) was 1% of the target population (90,252 cancer patients). A total of 314 (34.8%) questionnaires were collected. The results showed that the average pain score (5 point on Likert scale) according to the cancer type and the at-present average pain score (VAS, 0-10) were correlated (r=0.56, p<0.0001), and showed moderate agreement (kappa=0.364). The mean satisfaction score was 3.8 (1-5). The average time to complete the questionnaire was 8.9 min. In conclusion, the KCPAT is a reliable and valid instrument for assessing cancer pain in Koreans.


Assuntos
Coleta de Dados/normas , Neoplasias/diagnóstico , Neoplasias/epidemiologia , Avaliação de Resultados em Cuidados de Saúde/métodos , Medição da Dor/métodos , Dor/diagnóstico , Dor/epidemiologia , Adulto , Idoso , Idoso de 80 Anos ou mais , Causalidade , Comorbidade , Coleta de Dados/métodos , Feminino , Humanos , Coreia (Geográfico)/epidemiologia , Masculino , Pessoa de Meia-Idade , Reprodutibilidade dos Testes , Sensibilidade e Especificidade , Índice de Gravidade de Doença
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