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1.
Appl Physiol Nutr Metab ; 44(7): 791-795, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-30608872

RESUMO

The purpose of this study was to investigate the effect of 6 weeks of oral Echinacea purpurea supplementation on serum erythropoietin (EPO) and erythropoietic status. Twenty-four males (mean ± SE; age = 25.2 ± 1.4 years, height = 178.1 ± 1.4 cm, body mass = 78.1 ± 1.6 kg, body fat = 12.7 ± 0.9%, maximal oxygen uptake = 52.9 ± 0.9 mL·kg-1·min-1) were randomly grouped using a matched-pair, double-blind design and self-administered 8000 mg·day-1 of either E. purpurea (n = 12) or placebo (n = 12) for 42 consecutive days. Blood samples were collected prior to supplementation (day 0) and every 2 weeks during the supplementation period (days 14, 28, and 42) and were analyzed for EPO, red blood cell count, hemoglobin concentration, hematocrit, mean corpuscular volume, and mean corpuscular hemoglobin concentration. Separate 2 × 4 (group × time) factorial ANOVA with repeated measures on time were used to determine statistical differences with significance set at p ≤ 0.05. There were no significant interaction, group, or time effects observed for EPO or erythropoietic status markers for any of the measurement points (p ≤ 0.05). The present study indicated that 6 weeks of oral E. purpurea supplementation in recreationally active males with above average aerobic fitness did not enhance EPO or erythropoietic status. These findings are in contrast with previous reports of E. purpurea supplementation in untrained participants with average fitness levels, but consistent with observations in trained endurance athletes.


Assuntos
Aerobiose/fisiologia , Suplementos Nutricionais , Echinacea/química , Eritropoese/efeitos dos fármacos , Eritropoetina/sangue , Aptidão Física/fisiologia , Adulto , Limiar Anaeróbio/efeitos dos fármacos , Método Duplo-Cego , Contagem de Eritrócitos , Índices de Eritrócitos , Hematócrito , Hemoglobinas/análise , Humanos , Masculino , Adulto Jovem
2.
Org Biomol Chem ; 14(39): 9388-9405, 2016 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-27714195

RESUMO

The sigma-1 receptor (S1R) has attracted a great deal of attention as a prospective drug target due to its involvement in numerous neurological disorders and, more recently, for its therapeutic potential in neuropathic pain. As there was no crystal structure of this membrane-bound protein reported until 2016, ligand generation was driven by pharmacophore refinements to the general model suggested by Glennon and co-workers. The generalised S1R pharmacophore comprises a central region where a basic amino group is preferred, flanked by two hydrophobic groups. Guided by this pharmacophore, S1R ligands containing piperazines, piperazinones, and ethylenediamines have been developed. In the current work, we systematically deconstructed the piperazine core of a prototypic piperazine S1R ligand (vide infra) developed in our laboratories. Although we did not improve the affinity at the S1R compared to the lead, we identified several features important for affinity and selectivity. These included at least one basic nitrogen atom, conformational flexibility and, for S1R, a secondary or tertiary amine group proximal to the anisole. Furthermore, S2R selectivity can be tailored with functional group modifications of the N-atom proximal to the anisole.


Assuntos
Diaminas/química , Diaminas/metabolismo , Receptores sigma/metabolismo , Animais , Sítios de Ligação , Encéfalo/efeitos dos fármacos , Encéfalo/metabolismo , Avaliação Pré-Clínica de Medicamentos/métodos , Etilenodiaminas/química , Cobaias , Ligantes , Piperazina , Piperazinas/química , Ensaio Radioligante , Ratos , Receptores sigma/química , Relação Estrutura-Atividade , Receptor Sigma-1
3.
Eur J Appl Physiol ; 113(3): 743-52, 2013 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22941193

RESUMO

The aim of the present study was to examine the effects of sodium bicarbonate (NaHCO(3)) administration on lower-body, hypertrophy-type resistance exercise (HRE). Using a double-blind randomized counterbalanced design, 12 resistance-trained male participants (mean ± SD; age = 20.3 ± 2 years, mass = 88.3 ± 13.2 kg, height = 1.80 ± 0.07 m) ingested 0.3 g kg(-1) of NaHCO(3) or placebo 60 min before initiation of an HRE regimen. The protocol employed multiple exercises: squat, leg press, and knee extension, utilizing four sets each, with 10-12 repetition-maximum loads and short rest periods between sets. Exercise performance was determined by total repetitions generated during each exercise, total accumulated repetitions, and a performance test involving a fifth set of knee extensions to failure. Arterialized capillary blood was collected via fingertip puncture at four time points and analyzed for pH, [HCO(3)(-)], base excess (BE), and lactate [Lac(-)]. NaHCO(3) supplementation induced a significant alkaline state (pH: NaHCO(3): 7.49 ± 0.02, placebo: 7.42 ± 0.02, P < 0.05; [HCO(3)(-)]: NaHCO(3): 31.50 ± 2.59, placebo: 25.38 ± 1.78 mEq L(-1), P < 0.05; BE: NaHCO(3): 7.92 ± 2.57, placebo: 1.08 ± 2.11 mEq L(-1), P < 0.05). NaHCO(3) administration resulted in significantly more total repetitions than placebo (NaHCO(3): 139.8 ± 13.2, placebo: 134.4 ± 13.5), as well as significantly greater blood [Lac(-)] after the exercise protocol (NaHCO(3): 17.92 ± 2.08, placebo: 15.55 ± 2.50 mM, P < 0.05). These findings demonstrate ergogenic efficacy for NaHCO(3) during HRE and warrant further investigation into chronic training applications.


Assuntos
Desempenho Atlético/fisiologia , Suplementos Nutricionais , Músculo Esquelético/efeitos dos fármacos , Treinamento Resistido , Bicarbonato de Sódio/administração & dosagem , Adolescente , Adulto , Método Duplo-Cego , Humanos , Hipertrofia , Articulação do Joelho/efeitos dos fármacos , Articulação do Joelho/fisiologia , Perna (Membro) , Masculino , Músculo Esquelético/patologia , Levantamento de Peso/fisiologia , Adulto Jovem
4.
J Strength Cond Res ; 26(7): 1928-33, 2012 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-22728943

RESUMO

The purpose of this investigation was to determine the effects of 4 weeks of oral Echinacea (ECH) supplementation on erythropoietin (EPO), red blood cell (RBC) count, running economy (RE), and VO2max. Twenty-four men aged 24.9 ± 4.2 years, height 178.9 ± 7.9 cm, weight 87.9 ± 14.6 kg, body fat 19.3 ± 6.5% were grouped using a double-blind design and self-administered an 8,000-mg·d(-1) dosage of either ECH or placebo (PLA) in 5 × 400 mg × 4 times per day for 28 days. Blood samples were collected and analyzed for RBCs and EPO using automated flow cytometery and enzyme-linked immunosorbent assay. Maximal graded exercise tests (GXTs) were administered to measure VO2max, RE, and heart-rate responses. Analysis of variance was used to determine statistically significant differences (P ≤ 0.05). The EPO increased significantly in ECH at 7 days (ECH: 15.75 ± 0.64, PLA: 10.01 ± 0.73 mU·ml(-1)), 14 days (ECH: 18.88 ± 0.71, PLA: 11.02 ± 0.69 mU·ml(-1)), and 21 days (ECH: 16.06 ± 0.55, PLA: 9.20 ± 0.55 mU·ml(-1)). VO2max increased significantly in ECH (ECH: 1.47 ± 1.28, PLA: -0.13 ± 0.52%). Running economy improved significantly in ECH as indicated by a decrease in submaximal VO2max during the first 2 stages of the GXT (stage 1: ECH -1.50 ± 1.21, PLA 0.60 ± 1.95%; stage 2: ECH -1.67 ± 1.43, PLA 0.01 ± 1.03%). These data suggest that ECH supplementation results in significant increases in EPO, VO2max, and running economy.


Assuntos
Suplementos Nutricionais , Echinacea , Consumo de Oxigênio/efeitos dos fármacos , Preparações de Plantas/administração & dosagem , Corrida/fisiologia , Adulto , Análise de Variância , Método Duplo-Cego , Contagem de Eritrócitos , Eritropoetina/sangue , Teste de Esforço , Frequência Cardíaca/efeitos dos fármacos , Humanos , Masculino , Adulto Jovem
5.
Int J Sport Nutr Exerc Metab ; 17(4): 378-90, 2007 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-17962712

RESUMO

The purpose of this investigation was to determine whether echinacea supplementation results in alterations of erythroid growth factors and erythropoietic status. Twenty-four men age 24.9 +/- 4.2 y, height 1.7 +/- 0.8 m, weight 87.9 +/- 14.6 kg, and 19.3% +/- 6.5% body fat were grouped using a double-blind design and self- administered an 8000-mg/d dose of either echinacea (ECH) or placebo (PLA) in 5 x 400 mg x 4 times/d for 28 d. Blood samples were collected and analyzed for red blood cells (RBCs), hematocrit (Hct), hemoglobin (Hb), mean corpuscular volume, mean corpuscular hemoglobin content, prostaglandin E2, ferritin, erythropoietin (EPO), interleukin 3 (IL-3), and granulocyte-macrophage-colony-stimulating factor using automated flow cytometry and ELISA. ANOVA was used to determine significant differences (P ? 0.05). EPO was greater (P < 0.001) in ECH at Days 7, 14, and 21 and reflected a 44%, 63%, and 36% increase, respectively. IL-3 was greater (P = 0.011) in ECH at Days 14 and 21, which indicated a 65% and 73% increase, respectively. These data indicate that ECH supplementation resulted in an increase in EPO and IL-3 but did not significantly alter RBCs, Hb, or Hct.


Assuntos
Echinacea , Eritropoese/efeitos dos fármacos , Eritropoetina/sangue , Administração Oral , Adulto , Análise de Variância , Área Sob a Curva , Contagem de Células Sanguíneas , Suplementos Nutricionais , Método Duplo-Cego , Índices de Eritrócitos/efeitos dos fármacos , Eritropoese/imunologia , Eritropoese/fisiologia , Citometria de Fluxo , Humanos , Interleucina-3/sangue , Masculino , Fatores de Tempo
6.
Med Sci Sports Exerc ; 35(1): 150-6, 2003 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-12544649

RESUMO

PURPOSE: To compare glycerol and water hyperhydration and rehydration on tennis related skill and agility performance. METHODS: Eleven male subjects completed two counter-balanced, double-blind trials. Each trial consisted of three phases: 1). hyperhydration with or without glycerol (1.0 g.kg/(-1)) over 150 min, 2). 120 min of exercise-induced dehydration (EID), and 3) rehydration with or without glycerol (0.5 g.kg(-1)) over 90 min. After each phase, subjects performed 5- and 10-m sprint tests, a repeated-effort agility test, and tennis skill tests. RESULTS: Glycerol (G) hyperhydration significantly increased fluid retention by approximately 900 mL over the placebo (P) (P

Assuntos
Glicerol/uso terapêutico , Soluções para Reidratação , Corrida/fisiologia , Análise e Desempenho de Tarefas , Água , Adulto , Estudos Cross-Over , Desidratação/prevenção & controle , Método Duplo-Cego , Humanos , Masculino , Volume Plasmático , Tênis/fisiologia
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