A new bianthron glycoside as inhibitor of Trypanosoma cruzi glyceraldehyde 3-phosphate dehydrogenase activity

A phytochemical investigation of the ethanolic extract of stalks of Senna martiana Benth. (Leguminoseae), native specie of northeast Brazil, resulted in the isolation and spectroscopic characterization of a new bianthrone glycoside, martianine 1 (10,10'-il-chrysophanol-10-oxi10,10'-bi-glucosyl). Its identification was established by HRMS, IR and 2D NMR experiments. The evaluation of martianine trypanocidal activity was carried out against gliceraldehyde 3-phosphate dehydrogenase enzyme from Trypanosoma cruzi. Its inhibitory constant (Ki) is in the low micromolar concentration and it was determined by isothermal titration calorimetry to be 27.3 ± 2.47 µmol L-1. The non-competitive mechanism is asserted to be putative of the mode of action martianine displays against T. cruzi GAPDH. Results show that martianine has a great potential to become new lead molecule by inhibiting this key enzyme and for the development of new drugs against Chagas disease.

Trypanosoma cruzi benznidazole susceptibility in vitro does not predict the therapeutic outcome of human Chagas disease

Therapeutic failure of benznidazole (BZ) is widely documented in Chagas disease and has been primarily associated with variations in the drug susceptibility of Trypanosoma cruzi strains. In humans, therapeutic success has been assessed by the negativation of anti-T. cruzi antibodies, a process that may take up to 10 years. A protocol for early screening of the drug resistance of infective strains would be valuable for orienting physicians towards alternative therapies, with a combination of existing drugs or new anti-T. cruzi agents. We developed a procedure that couples the isolation of parasites by haemoculture with quantification of BZ susceptibility in the resultant epimastigote forms. BZ activity was standardized with reference strains, which showed IC50 to BZ between 7.6-32 µM. The assay was then applied to isolates from seven chronic patients prior to administration of BZ therapy. The IC50 of the strains varied from 15.6 ± 3-51.4 ± 1 µM. Comparison of BZ susceptibility of the pre-treatment isolates of patients considered cured by several criteria and of non-cured patients indicates that the assay does not predict therapeutic outcome. A two-fold increase in BZ resistance in the post-treatment isolates of two patients was verified. Based on the profile of nine microsatellite loci, sub-population selection in non-cured patients was ruled out.

Phlebotomines (Diptera, Psychodidae) in the Ribeira Valley Speleological Province - 1. Parque Estadual Intervales, state of São Paulo, Brazil

The identification of the sandfly fauna and investigation of some ecological aspects of its populations in areas frequented by tourists of the PEI, an Atlantic forest reserve with many caves, were the objective of this study. Captures were undertaken monthly from January 2001 to December 2002, with automatic light traps installed in 13 ecotopes, including caves, forests, domiciliary and peridomiciliary environments, and by aspiration in armadillo burrows. Additionally, although not at regular intervals, Shannon traps were installed in forests and anthropic environments, aspirations were made on cave walls, among roots and fallen leaves, and some insects were captured while biting researchers. A total of 891 sandflies belonging to 21 species were captured. Six hundred specimens representing 19 species were captured with light traps, 215 in anthropic (2.24 insects/trap) and 385 in extra-domiciliary (1.46 insects/trap) environments. Brumptomyia troglodytes was the most abundant species (the Standardised Index of Species Abundance = 0.705). Pintomyia monticola predominated in the Shannon traps and showed anthropophilic and diurnal activity. Psathyromyia pascalei predominated in the aspirations; the largest number being in armadillo burrows. Eleven species were captured in caves; although some might be troglophiles, the majority used these ecotopes as resting places. Nyssomyia intermedia, Nyssomyia neivai and Migonemyia migonei, implicated in the transmission of cutaneous leishmaniasis in the Southeastern Brazilian region, were all found, though in such low densities as to suggest minimal risk of the disease in the PEI.

Effects of flooding of the River Paraná on the temporal activity of Anopheles (Nyssorhynchus) darlingi Root (Diptera: Culicidae), at the border state of Mato Grosso do Sul and São Paulo, Brazil

INTRODUCTION: Study of the temporal activity of malaria vectors during the implantation of a hydroelectric power station on the River Paraná, intended to generate electrical energy. The river separates the States of São Paulo and Mato Grosso do Sul, in Brazil. The objective was to verify whether alterations occurred in the wealth and diversity indices of Anopheles, following two successive floods, extended to the temporal activity and nycthemeral rhythm followed over a five year period. METHODS: Mosquito capture was performed monthly using the Human Attraction Technique and Shannon Traps. The first, executed for 24h, provided the nycthemeral rhythm and the second, lasting 15h, permitted the tracking of Anopheles during the two floods. RESULTS: The bimodal pattern of Anopheles darlingi defined before these floods was modified throughout the environment interventions. The same effect had repercussions on the populations of An albitarsis s.l., An triannulatus and An galvaoi. Activity prior to twilight was less affected by the environment alterations. CONCLUSIONS: The dam construction provoked changes in Anopheles temporal activity patterns, permitting classification of the area as an ecologically steady and unstable situation. Differences observed in Anopheles behavior due to the capture methods revealed the influence of solo and multiple attractiveness inside the populations studied.

Effects of an intervention in eating habits and physical activity in Japanese-Brazilian women with a high prevalence of metabolic syndrome in Bauru, São Paulo State, Brazil

We evaluated the impact of a lifestyle intervention on the cardiometabolic risk profile of women participating in the Study on Diabetes and Associated Diseases in the Japanese-Brazilian Population in Bauru. This was a non-controlled experimental study including clinical and laboratory values at baseline and after a 1-year intervention period. 401 Japanese-Brazilian women were examined (age 60.8±11.7 years), and 365 classified for metabolic syndrome (prevalence = 50.6%). Subjects with metabolic syndrome were older than those without (63.0±10.0 vs. 56.7±11.6 years, p < 0.01). After intervention, improvements in variables were found, except for C-reactive protein. Body mass index and waist circumference decreased, but adiposity reduction was more pronounced in the abdominal region (87.0±9.7 to 84.5±11.2cm, p < 0.001). Intervention-induced differences in total cholesterol, LDL, and post-challenge glucose were significant; women who lost more than 5% body weight showed a better profile than those who did not. The lifestyle intervention in Japanese-Brazilian women at high cardiometabolic risk improved anthropometric and laboratory parameters, but it is not known whether such benefits will persist and result in long-term reduction in cardiovascular events.

Prevalência de diagnóstico auto-referido de osteoporose, Brasil, 2006

OBJETIVO: Estimar a prevalência de osteoporose auto-referida (com diagnóstico médico prévio) e de fatores de risco e proteção associados. MÉTODOS: Estudo transversal baseado em dados do sistema de Vigilância de Fatores de Risco e Proteção para Doenças Crônicas por Inquérito Telefônico (VIGITEL). Foram entrevistados 54.369 indivíduos com idade >18 anos residentes em domicílios servidos por pelo menos uma linha telefônica fixa nas capitais brasileiras e Distrito Federal em 2006. Estimativas de osteoporose segundo fatores socioeconômicos, comportamentais e índice de massa corporal foram estratificadas por sexo. Foram calculados riscos de ocorrência de osteoporose para cada variável individualmente, e em modelo multivariado, considerando-se odds ratio como proxy da razão de prevalência. RESULTADOS: A prevalência de osteoporose referida foi de 4,4%, predominantemente entre mulheres (7,0%), com idade >45 anos, estado civil não solteiro e ex-fumante. Entre homens, ter mais de 65 anos, ser casado ou viúvo e sedentário associaram-se positivamente ao desfecho. CONCLUSÕES: Dentre os fatores associados à osteoporose, destacam-se aspectos modificáveis relacionados com a prevenção da doença, como a atividade física e tabagismo.

Hipertensão arterial referida e indicadores antropométricos de gordura em idosos

OBJETIVO: Investigar a associação entre hipertensão arterial referida (HAr) e indicadores antropométricos de gordura, corporal e abdominal em idosos do município de São Paulo. MÉTODOS: Os dados de 1894 idosos foram baseados na pesquisa Saúde, Bem-Estar e Envelhecimento - SABE, 2000. Os indicadores antropométricos utilizados foram: Índice de Massa Corporal (IMC), perímetro da cintura (PC), razão cintura/quadril (RCQ) e razão cintura/estatura (RCE). Utilizou-se regressão logística binária, estratificada por sexo. RESULTADOS: A hipertensão arterial associou-se aos indicadores antropométricos. No modelo final (ajustado para idade, escolaridade, tabagismo, atividade física e diabetes), em ambos os sexos, o IMC apresentou maior força estatística, apesar de, nas mulheres, apresentar-se similar aos outros indicadores. À exceção da RCE, em homens, a HAr associou-se, positiva e independentemente, aos outros indicadores. CONCLUSÃO: Os resultados sugerem a relevância desses indicadores, para, precocemente, detectar os riscos para o desenvolvimento dessa doença e intervir na sua prevenção e controle.

Avaliação nutricional e risco cardiovascular em executivos submetidos a check-up

OBJETIVO: Avaliar estado nutricional e risco cardiovascular de executivos. MÉTODOS: Estudo transversal. Foram avaliados 329 executivos de ambos os gêneros, com idade entre 31 e 70 anos, submetidos a check-up de saúde em hospital privado do município de São Paulo. Foram mensuradas as variáveis referentes a peso, estatura e circunferência da cintura (CC) e determinado o Índice de Massa Corporal (IMC). Foram analisados pressão arterial, níveis séricos de colesterol total e frações, triacilglicerol, glicose e ácido úrico. Prática habitual de atividade física foi avaliada por meio do Questionário Internacional de Atividade Física (IPAQ) e o risco cardiovascular pelo Escore de Framingham. A análise de variância e o método de Bonferroni foram utilizados para o tratamento estatístico. RESULTADOS: Média de idade foi 44,6 anos (DP=6,8), predominando o gênero masculino (89,7%). Quanto ao estilo de vida, 17% eram tabagistas e 7,3% sedentários. Os resultados médios encontrados para os exames clínicos e bioquímicos foram: pressão arterial 117,8 x 78,6 mmHg (DP=12 x 8,3), colesterol total 200,5 mg/dL (DP=35,9), LDL-c 121,8 mg/dL (DP=29,9), HDL-c 52,2 mg/dL (DP=10,9), triacilglicerol 133,7 mg/dL (DP=76,8), glicose 96,3 mg/dL (DP=20,5) e ácido úrico 6,0 e 4,2 mg/dL (DP=1,0 e 0,9) para homens e mulheres, respectivamente. O IMC médio foi de excesso de peso (26,1kg/m²; DP=6,8). A CC média estava normal entre as mulheres (79,6cm; DP=7,3) e indicou risco elevado para doenças crônicas entre os homens (96,1cm; DP=8,9). O Risco de Framingham médio foi de 5,7%. CONCLUSÃO: Os executivos estavam com excesso de peso e apresentaram baixo risco cardiovascular.

Randomized, controlled trial promotes physical activity and reduces consumption of sweets and sodium among overweight and obese adults

The present study sought to assess the impact of an intervention to reduce weight and control risk factors of noncommunicable chronic diseases in overweight or obese adults who are users of primary and secondary healthcare units of the public health system of Pelotas, Brazil. We hypothesized that individuals who received an educational intervention regarding how to lose weight and prevent other noncommunicable chronic disease risk factors through nutrition would lose weight and acquire active habits during leisure time more frequently than individuals under regular care. Two hundred forty-one participants from the Nutrition Outpatient Clinic of the Medical Teaching Hospital of the Federal University of Pelotas, Brazil, aged 20 years or older and classified as overweight or obese were randomly allocated to either the intervention group (IG; n = 120) or control group (CG; n = 121). The IG received individualized nutritional care for 6 months, and the CG received individualized usual care of the health services. Intention-to-treat analyses showed that at 6 months, mean fasting glycemia and daily consumption of sweet foods and sodium were reduced, and the time spent on physical leisure activity was increased in IG. Analysis of adherence to the protocol of the study revealed that individuals from IG had lost more in body weight, waist circumference, and fasting glucose compared to the CG. Leisure time physical activity increased in IG. Individuals adhered equally to the dietetic recommendations, irrespective of the nutrition approach that was used

Fat and fiber consumption are associated with peripheral arterial disease in a cross-sectional study of a japanese-brazilian population

Background The Western diet plays a role for the epidemics of obesity and related diseases. This study examined a possible association between peripheral arterial disease (PAD) and the dietary components of Japanese immigrants living in Brazil. Methods and Results In this cross-sectional study, 1,267 subjects (aged =30 years) with complete dietary, clinical and laboratory data were studied according to a standardized protocol. Ankle-to-brachial index was used to identify subjects with PAD. The overall prevalence of PAD was 14.6%. Subjects with PAD were older, had lower education and higher mean values of blood pressure, triglycerides, and fasting and 2-h plasma glucose levels compared with those without the disease. Among the subjects with PAD, the consumption of fiber from whole grains (3.0 vs 3.4 g, p=0.001) and linoleic acids (11.0 vs 11.7 g, p=0.017) were lower and intake of total (72.8 vs 69.1 g, p=0.016) and saturated fatty acids (17.4 vs 16.3 g, p=0.012) were higher than those without PAD. Results of multiple logistic regression analysis showed a significant association between PAD with high total fat intake, low intake of fiber from fruit and oleic acid, independently of other variables. Conclusions Despite limitations in examining the cause - effect relationship, the data support the notion that diet could be important in reducing the occurrence of PAD

Fatores associados à obesidade global e à obesidade abdominal em mulheres na pós-menopausa

OBJETIVOS: avaliar a prevalência de obesidade global e obesidade abdominal, em mulheres pós-menopausa, segundo o grau de instrução, nível de atividade física, uso de terapia hormonal na menopausa (THM) e paridade. MÉTODOS: foram entrevistadas 157 mulheres na pós-menopausa, atendidas em dois ambulatórios públicos da cidade de São Paulo, São Paulo, Brasil. A obesidade foi determinada segundo o índice de massa corporal (IMC > 30,0) e segundo o percentual de gordura corporal (%GC > 37%). A obesidade abdominal foi determinada pela relação cintura-quadril (RCQ > 0,85). RESULTADOS: a prevalência de obesidade global foi 34,4% (segundo o IMC) e de 40,1% (segundo o %GC). A prevalência de obesidade abdominal foi de 73,8%. Grande parte das entrevistadas referiu até sete anos de instrução formal (47,8%), foi considerada sedentária ou insuficientemente ativa (52,3%) e nunca tinha utilizado THM oral ou tinha utilizado por menos de 12 meses (72,0%). Foi constatada maior prevalência de obesidade global no grupo de mulheres sedentárias ou insuficientemente ativas e no grupo de não usuárias de THM (p<0,05). Quanto à obesidade abdominal, fator de risco para doenças cardiovasculares (DCV), apenas o grau de instrução mostrou-se associado à RCQ (p<0,05). CONCLUSÕES: mulheres após a menopausa, fisicamente ativas e usuárias de THM exibiram menor prevalência de obesidade global, porém a prevalência de obesidade abdominal foi alta e ainda maior nas mulheres com menor grau de instrução

The burden of physical activity on type 2 diabetes public healthcare expenditures among adults: a retrospective study

Background: Determinants of public healthcare expenditures in type 2 diabetics are not well investigated in developing nations and, therefore, it is not clear if higher physical activity decreases healthcare costs. The purpose of this study was to analyze the relationship between physical activity and the expenditures in public healthcare on type 2 diabetes mellitus treatment. Methods: Cross-sectional study carried out in Brazil. A total of 121 type 2 diabetics attended to in two Basic Healthcare Units were evaluated. Public healthcare expenditures in the last year were estimated using a specific standard table. Also evaluated were: socio-demographic variables; chronological age; exogenous insulin use; smoking habits; fasting glucose test; diabetic neuropathy and anthropometric measures. Habitual physical activity was assessed by questionnaire. Results: Age (r = 0.20; p = 0.023), body mass index (r = 0.33; p = 0.001) and waist-to-hip ratio (r = 0.20; p = 0.025) were positively related to expenditures on medication for the treatment of diseases other than diabetes. Insulin use was associated with increased expenditures. Higher physical activity was associated with lower expenditure, provided medication for treatment of diseases other than diabetes (OR = 0.19; p = 0.007) and medical consultations (OR = 0.26; p = 0.029). Conclusions: Type 2 diabetics with higher enrollment in physical activity presented consistently lower healthcare expenditures for the public healthcare system.

Metabolic syndrome and dietary components are associated with coronary artery disease risk score in free-living adults: a cross-sectional study

Background: Coronary artery disease (CAD) is among the main causes of death in developed countries, and diet and lifestyle can influence CAD incidence. Objective: To evaluate the association of coronary artery disease risk score with dietary, anthropometric and biochemical components in adults clinically selected for a lifestyle modification program. Methods: 362 adults (96 men, 266 women, 53.9 +/- 9.4 years) fulfilled the inclusion criteria by presenting all the required data. The Framingham score was calculated and the IV Brazilian Guideline on Dyslipidemia and Prevention of Atherosclerosis was adopted for classification of the CAD risks. Anthropometric assessments included waist circumference (WC), body fat and calculated BMI (kg/m(2)) and muscle-mass index (MMI kg/m(2)). Dietary intake was estimated through 24 h dietary recall. Fasting blood was used for biochemical analysis. Metabolic Syndrome (MS) was diagnosed using NCEP-ATPIII (2001) criteria. Logistic regression was used to determine the odds of CAD risks according to the altered components of MS, dietary, anthropometric, and biochemical components. Results: For a sample with a BMI 28.5 +/- 5.0 kg/m(2) the association with lower risk (<10% CAD) were lower age (<60 years old), and plasma values of uric acid. The presence of MS within low, intermediary, and high CAD risk categories was 30.8%, 55.5%, and 69.8%, respectively. The independent risk factors associated with CAD risk score was MS and uric acid, and the protective factors were recommended intake of saturated fat and fiber and muscle mass index. Conclusion: Recommended intake of saturated fat and dietary fiber, together with proper muscle mass, are inversely associated with CAD risk score. On the other hand, the presence of MS and high plasma uric acid are associated with CAD risk score.

Ticks produce highly selective chemokine binding proteins with antiinflammatory activity

Bloodsucking parasites such as ticks have evolved a wide variety of immunomodulatory proteins that are secreted in their saliva, allowing them to feed for long periods of time without being detected by the host immune system. One possible strategy used by ticks to evade the host immune response is to produce proteins that selectively bind and neutralize the chemokines that normally recruit cells of the innate immune system that protect the host from parasites. We have identified distinct cDNAs encoding novel chemokine binding proteins (CHPBs), which we have termed Evasins, using an expression cloning approach. These CHBPs have unusually stringent chemokine selectivity, differentiating them from broader spectrum viral CHBPs. Evasin-1 binds to CCL3, CCL4, and CCL18; Evasin-3 binds to CXCL8 and CXCL1; and Evasin-4 binds to CCL5 and CCL11. We report the characterization of Evasin-1 and -3, which are unrelated in primary sequence and tertiary structure, and reveal novel folds. Administration of recombinant Evasin-1 and - 3 in animal models of disease demonstrates that they have potent antiinflammatory properties. These novel CHBPs designed by nature are even smaller than the recently described single-domain antibodies (Hollinger, P., and P. J. Hudson. 2005. Nat. Biotechnol. 23: 1126-1136), and may be therapeutically useful as novel antiinflammatory agents in the future.

Antioxidant activity and phenolic composition of herbal infusions consumed in Brazil

Processed tea and herbal infusions were Studied for their phenol content, antioxidant activity and main flavonoids. Total phenolics were determined by Folin-Ciocalteu method and ranged from N.D. to 46.46 +/- 0.44 mg/g GAE. Flavonoids were investigated by HPLC, and myricetin, quercetin, kaempferol were identified in black, green, and chamomile tea. Antioxidant activity was evaluated using two methods: DPPH and beta-carotene bleaching test (BCB). Using the BCB, the highest activities were found for infusions of black tea, mate, lemongrass, chamomile, and fennel; whereas fresh herbal infusions presented the lowest activities. Using the DPPH method, fresh herbal infusions presented the highest activities. Processed leaves with the lowest IC50 values were green and black tea (147.63 and 288.60 mu g/mL, respectively). The results of this research show that the infusions studied are good Source of compounds presenting antioxidant activity in vitro.