Anti-Inflammatory Activity of Babassu Oil and Development of a Microemulsion System for Topical Delivery.

Babassu oil extraction is the main income source in nut breakers communities in northeast of Brazil. Among these communities, babassu oil is used for cooking but also medically to treat skin wounds and inflammation, and vulvovaginitis. This study aimed to evaluate the anti-inflammatory activity of babassu oil and develop a microemulsion system with babassu oil for topical delivery. Topical anti-inflammatory activity was evaluated in mice ear edema using PMA, arachidonic acid, ethyl phenylpropiolate, phenol, and capsaicin as phlogistic agents. A microemulsion system was successfully developed using a Span® 80/Kolliphor® EL ratio of 6 : 4 as the surfactant system (S), propylene glycol and water (3 : 1) as the aqueous phase (A), and babassu oil as the oil phase (O), and analyzed through conductivity, SAXS, DSC, TEM, and rheological assays. Babassu oil and lauric acid showed anti-inflammatory activity in mice ear edema, through inhibition of eicosanoid pathway and bioactive amines. The developed formulation (39% A, 12.2% O, and 48.8% S) was classified as a bicontinuous to o/w transition microemulsion that showed a Newtonian profile. The topical anti-inflammatory activity of microemulsified babassu oil was markedly increased. A new delivery system of babassu microemulsion droplet clusters was designed to enhance the therapeutic efficacy of vegetable oil.

The influence of aerobic fitness status on ventilatory efficiency in patients with coronary artery disease.

OBJECTIVE: To test the hypotheses that 1) coronary artery disease patients with lower aerobic fitness exhibit a lower ventilatory efficiency and 2) coronary artery disease patients with lower initial aerobic fitness exhibit greater improvements in ventilatory efficiency with aerobic exercise training. METHOD: A total of 123 patients (61.0±0.7 years) with coronary artery disease were divided according to aerobic fitness status into 3 groups: group 1 (n = 34, peak VO2<17.5 ml/kg/min), group 2 (n = 67, peak VO2>17.5 and <24.5 ml/kg/min) and group 3 (n = 22, peak VO2>24.5 ml/kg/min). All patients performed a cardiorespiratory exercise test on a treadmill. Ventilatory efficiency was determined by the lowest VE/VCO2 ratio observed. The exercise training program comprised moderate-intensity aerobic exercise performed 3 times per week for 3 months. Clinicaltrials.gov: NCT02106533 RESULTS: Before intervention, group 1 exhibited both lower peak VO2 and lower ventilatory efficiency compared with the other 2 groups (p<0.05). After the exercise training program, group 1 exhibited greater improvements in aerobic fitness and ventilatory efficiency compared with the 2 other groups (group 1: ▵ = -2.5±0.5 units; group 2: ▵ = -0.8±0.3 units; and group 3: ▵ = -1.4±0.6 units, respectively; p<0.05). CONCLUSIONS: Coronary artery disease patients with lower aerobic fitness status exhibited lower ventilatory efficiency during a graded exercise test. In addition, after 3 months of aerobic exercise training, only the patients with initially lower levels of aerobic fitness exhibited greater improvements in ventilatory efficiency.

The influence of aerobic fitness status on ventilatory efficiency in patients with coronary artery disease

OBJECTIVE: To test the hypotheses that 1) coronary artery disease patients with lower aerobic fitness exhibit a lower ventilatory efficiency and 2) coronary artery disease patients with lower initial aerobic fitness exhibit greater improvements in ventilatory efficiency with aerobic exercise training. METHOD: A total of 123 patients (61.0±0.7 years) with coronary artery disease were divided according to aerobic fitness status into 3 groups: group 1 (n = 34, peak VO2<17.5 ml/kg/min), group 2 (n = 67, peak VO2>17.5 and <24.5 ml/kg/min) and group 3 (n = 22, peak VO2>24.5 ml/kg/min). All patients performed a cardiorespiratory exercise test on a treadmill. Ventilatory efficiency was determined by the lowest VE/VCO2 ratio observed. The exercise training program comprised moderate-intensity aerobic exercise performed 3 times per week for 3 months. Clinicaltrials.gov: NCT02106533 RESULTS: Before intervention, group 1 exhibited both lower peak VO2 and lower ventilatory efficiency compared with the other 2 groups (p<0.05). After the exercise training program, group 1 exhibited greater improvements in aerobic fitness and ventilatory efficiency compared with the 2 other groups (group 1: ▵ = -2.5±0.5 units; group 2: ▵ = -0.8±0.3 units; and group 3: ▵ = -1.4±0.6 units, respectively; p<0.05). CONCLUSIONS: Coronary artery disease patients with lower aerobic fitness status exhibited lower ventilatory efficiency during a graded exercise test. In addition, after 3 months of aerobic exercise training, only the patients with initially lower levels of aerobic fitness exhibited greater improvements in ventilatory efficiency. .

Structure and rheological properties of a xyloglucan extracted from Hymenaea courbaril var. courbaril seeds.

Hymenaea courbaril var courbaril seed xyloglucan was efficiently extracted with 0.1M NaCl, followed by ethanol precipitation (yield=72±5% w/w). Its amorphous structure was identified by the pattern of X-ray diffraction. The monosaccharide composition was determined by GC/MS analysis of the alditol acetates and showed the occurrence of glucose:xylose:galactose:arabinose (40:34:20:6). One-(1D) and two-dimensional-(2D) NMR spectra confirmed a central backbone composed by 4-linked ß-glucose units partially branched at position 6 with non-reducing terminal units of α-xylose or ß-galactose-(1→2)-α-xylose disaccharides. The xyloglucan solution was evaluated by dynamic light scattering and presents a polydisperse and practically neutral profile, and at 0.5 and 1.0% (w/v) the solutions behave as a viscoelastic fluid. The polysaccharide did not show significant antibacterial or hemolytic activities. Overall our results indicate that xyloglucan from H. courbaril is a promising polysaccharide for food and pharmaceutical industries.

Effect of continuous and interval exercise training on the PETCO2 response during a graded exercise test in patients with coronary artery disease.

OBJECTIVE: The purpose of this study was to evaluate the following: 1) the effects of continuous exercise training and interval exercise training on the end-tidal carbon dioxide pressure (PETCO2) response during a graded exercise test in patients with coronary artery disease; and 2) the effects of exercise training modalities on the association between PETCO2 at the ventilatory anaerobic threshold (VAT) and indicators of ventilatory efficiency and cardiorespiratory fitness in patients with coronary artery disease. METHODS: Thirty-seven patients (59.7 + 1.7 years) with coronary artery disease were randomly divided into two groups: continuous exercise training (n = 20) and interval exercise training (n = 17). All patients performed a graded exercise test with respiratory gas analysis before and after three months of the exercise training program to determine the VAT, respiratory compensation point (RCP) and peak oxygen consumption. RESULTS: After the interventions, both groups exhibited increased cardiorespiratory fitness. Indeed, the continuous exercise and interval exercise training groups demonstrated increases in both ventilatory efficiency and PETCO2 values at VAT, RCP, and peak of exercise. Significant associations were observed in both groups: 1) continuous exercise training (PETCO2VAT and cardiorespiratory fitness r = 0.49; PETCO2VAT and ventilatory efficiency r = -0.80) and 2) interval exercise training (PETCO2VAT and cardiorespiratory fitness r = 0.39; PETCO2VAT and ventilatory efficiency r = -0.45). CONCLUSIONS: Both exercise training modalities showed similar increases in PETCO2 levels during a graded exercise test in patients with coronary artery disease, which may be associated with an improvement in ventilatory efficiency and cardiorespiratory fitness.

Effect of continuous and interval exercise training on the PETCO2 response during a graded exercise test in patients with coronary artery disease

OBJECTIVE: The purpose of this study was to evaluate the following: 1) the effects of continuous exercise training and interval exercise training on the end-tidal carbon dioxide pressure (PETCO2) response during a graded exercise test in patients with coronary artery disease; and 2) the effects of exercise training modalities on the association between PETCO2 at the ventilatory anaerobic threshold (VAT) and indicators of ventilatory efficiency and cardiorespiratory fitness in patients with coronary artery disease. METHODS: Thirty-seven patients (59.7 + 1.7 years) with coronary artery disease were randomly divided into two groups: continuous exercise training (n = 20) and interval exercise training (n = 17). All patients performed a graded exercise test with respiratory gas analysis before and after three months of the exercise training program to determine the VAT, respiratory compensation point (RCP) and peak oxygen consumption. RESULTS: After the interventions, both groups exhibited increased cardiorespiratory fitness. Indeed, the continuous exercise and interval exercise training groups demonstrated increases in both ventilatory efficiency and PETCO2 values at VAT, RCP, and peak of exercise. Significant associations were observed in both groups: 1) continuous exercise training (PETCO2VAT and cardiorespiratory fitness r = 0.49; PETCO2VAT and ventilatory efficiency r = -0.80) and 2) interval exercise training (PETCO2VAT and cardiorespiratory fitness r = 0.39; PETCO2VAT and ventilatory efficiency r = -0.45). CONCLUSIONS: Both exercise training modalities showed similar increases in PETCO2 levels during a graded exercise test in patients with coronary artery disease, which may be associated with an improvement in ventilatory efficiency and cardiorespiratory fitness.

Augmented muscle vasodilatory responses in obese children with Glu27 beta-2-adrenoceptor polymorphism.

This study examined forearm vasodilatation during mental challenge and exercise in 72 obese children (OC; age = 10 +/- 0.1 years) homozygous with polymorphism in the allele 27 of the beta-2-adrenoceptors: Gln27 (n = 61) and Glu27 (n = 11). Forearm blood flow was recorded during 3 min of each using the Stroop color-word test (MS) and handgrip isometric exercise. Baseline hemodynamic and vascular measurements were similar. During the MS, peak forearm vascular conductance was significantly greater in group Glu27 (Delta = 0.35 +/- 0.4 vs. 0.12 +/- 0.1 units, respectively, p = .042). Similar results were found during exercise (Delta = 0.64 +/- 0.1 vs. 0.13 +/- 0.1 units, respectively, p = .035). Glu27 OC increased muscle vasodilatory responsiveness upon the MS and exercise.

[Obese children lipid profile: effects of hypocaloric diet and aerobic physical exercise]. / Perfil lipídico em crianças obesas: efeitos de dieta hipocalórica e atividade física aeróbica.

UNLABELLED: Diet and exercise help improve obese adults' lipid profile. However, their effect on obese children, the aim of the present study, is poorly known. Fifty obese children were studied into 2 paired groups: Group D (1,500 - 1,800 kcal diet: 55% carbohydrate, 30% fat, 15% protein), and Group DE (same diet + aerobic physical activity 1 hour/day 3 times a week). After 5 months BMI, triglycerides, total cholesterol (TC) and fractions were assessed. No change in triglycerides, TC and low-density lipoprotein cholesterol (LDL-C) levels were reported in both groups. However, high-density lipoprotein cholesterol (HDL-C) increased (+10.3%; p< 0.01) only in DE Group. Screening patients with TC > 170 mg/dL, LDL-C > 110 mg/dL and HDL-C < 35 mg/dL we had: similar reduction for TC in both groups (-6.0% x -6.0%; p= ns), LDL-C reduction in both groups (-14.2% x -13.5%; p= ns), and HDL-C increase only in DE Group (+10.0%; p< 0.05). CONCLUSIONS: 1) Hypocaloric diet (HD) + exercise, rather than diet only, increase obese children's HDL-C levels irrespective of baseline levels; 2) HD only and HD + exercise lead to TC and LDL-C reduction in obese children with TC and LDL-C above normal values.

Perfil lipídico em crianças obesas: efeitos de dieta hipocalórica e atividade física aeróbica / Obese children lipid profile: effects of hypocaloric diet and aerobic physical exercise

Dieta hipocalórica e atividade física aeróbia promovem perda de peso e melhora do perfil lipídico de adultos obesos, entretanto pouco se conhece em crianças obesas, sendo este o objetivo do trabalho. Estudamos cinqüenta crianças obesas e dividimos em dois grupos pareados: Grupo D (dieta com 55 por cento de carboidrato, 30 por cento de gordura e 15 por cento de proteína - 1.500 e 1.800 kcal) e Grupo DE (mesma dieta + atividade física aeróbia 1 hora por dia, três vezes por semana). Após cinco meses, avaliamos: índice de massa corpórea (IMC), triglicerídeos, colesterol total (CT) e frações. Nenhuma modificação foi observada nos triglicerídeos, CT e lipoproteína de baixa-densidade colesterol (LDL-C) em ambos os grupos. Houve, porém, aumento da lipoproteína de alta-densidade colesterol (HDL-C) apenas no grupo DE (+10,3 por cento, p< 0,01). Selecionando pacientes com CT > 170 mg/dL, LDL-C > 110 mg/dL e HDL-C < 35 mg/dL, observou-se redução semelhante do CT nos dois grupos (-6,0 por cento x -6,0 por cento; p= ns), assim como da LDL-C de ambos (-14,2 por cento x -13,5 por cento; p= ns), e um acréscimo da HDL-C apenas no grupo DE (+10,0 por cento; p< 0,05). Conclusões: 1) Dieta hipocalórica (DH) e atividade física aeróbia promovem aumento da HDL-C, independente do valor basal, em crianças obesas quando comparado à DH isoladamente; 2) DH isoladamente ou associada a exercício aeróbio reduz CT e LDL-C, quando estes estão em níveis acima do valor normal, em crianças obesas.

Synthesis and vasodilatory activity of new N-acylhydrazone derivatives, designed as LASSBio-294 analogues.

Conventional therapy to treat hypertension often involves arterial vasodilation. Decrease of blood pressure by vasodilators is normally associated with adverse effects because of their low vascular selectivity. This is of interest to develop new molecules with potential for clinical use and fewer side effects. Recently, a new bioactive compound of the N-acylhydrazone class, LASSBio-294, was shown to produce a cardioinotropic effect and vasodilation. In this report, new derivatives of LASSBio-294 were designed and tested on the contractile response of vascular smooth muscle from Wistar rats. Phenylephrine-induced contracture in the aorta was inhibited by the derivatives LASSBio-785 and LASSBio-788. The concentrations necessary to cause 50% reduction of the maximal vascular response (IC50) were 10.2 +/- 0.5 and 67.9 +/- 6.5 microM. Vasodilation induced by both derivatives is likely to be mediated by a direct effect on smooth muscle because it was not dependent on the integrity of vascular endothelium. LASSBio-785 was seven times more potent than the reference compound LASSBio-294 (IC50 = 74 microM) in producing an endothelium-independent vasodilator effect.

Diet and exercise training restore blood pressure and vasodilatory responses during physiological maneuvers in obese children.

BACKGROUND: The effects of diet and diet plus exercise training on muscle vasodilatation during physiological maneuvers in obese children are unknown. We tested the hypothesis that (1) blood pressure (BP) and forearm vascular conductance (FVC) responses during handgrip exercise and mental stress would be altered in obese children and (2) diet plus exercise training would restore BP and FVC responses during exercise and mental stress in obese children. METHODS AND RESULTS: Thirty-nine obese children (aged 10+/-0.2 years) were randomly divided into 2 groups: diet plus exercise training (n=21; body mass index [BMI]=28+/-0.5 kg/m2) and diet (n=18; BMI=30+/-0.4 kg/m2). Ten age-matched lean control children (BMI=17+/-0.5 kg/m2) were also studied. Forearm blood flow was measured by venous occlusion plethysmography. BP was monitored noninvasively. Handgrip exercise was performed at 30% maximal voluntary contraction for 3 minutes. Stroop color word test was performed for 4 minutes. Baseline BP was significantly higher and FVC was significantly lower in obese children. During exercise and mental stress, BP responses were significantly higher and FVC responses were significantly lower in obese children. Diet and diet plus exercise training significantly reduced body weight. Diet and diet plus exercise training significantly decreased BP levels during exercise and mental stress. Diet plus exercise training, in contrast to diet alone, significantly increased FVC responses during exercise (3.7+/-0.3 versus 5.6+/-0.4 U; P=0.01) and mental stress (3.5+/-0.5 versus 4.5+/-0.4 U; P=0.02). After diet plus exercise training, BP and FVC responses during exercise and mental stress were similar between obese children and the control group. CONCLUSIONS: Obesity exacerbates BP responses and impairs FVC responses during exercise and mental stress in children. Diet and exercise training restore BP and FVC responses in obese children.