Eficácia e perda do herbicida 2,4-d amina aplicado com diferentes volumes de calda e pontas de pulverização

O presente trabalho teve como objetivo avaliar a eficácia do herbicida 2,4-D amina na dessecação de plantas daninhas, bem como quantificar as suas perdas durante o processo de aplicação, com a utilização de diferentes volumes de calda e pontas de pulverização. O experimento foi conduzido em delineamento de blocos casualizados, com seis tratamentos e quatro repetições, dispostos em esquema fatorial 3 x 2: três pontas de pulverização (ponta de jato plano duplo de pré-orifício, jato plano defletor e jato plano defletor com indução de ar) e dois volumes de aplicação (80 e 130 L ha-1) com a presença do ingrediente ativo 2,4-D amina (806 g ha-1 de i.a.). Foi realizada a avaliação de deposição de calda nas plantas daninhas, perdas para o solo e perdas por exoderiva, pela quantificação do herbicida nos diferentes alvos por cromatografia líquida de alta eficiência (HPLC). Também foi avaliado o controle de plantas daninhas na área experimental. Concluiu-se que o volume de aplicação de 80 L ha-1 e gotas grossas podem ser utilizados na dessecação com o herbicida 2,4-D amina, sem comprometer a cobertura do alvo; pontas de jato plano defletor com indução de ar promoveram maior perda de herbicida para o solo; e as diferentes pontas de pulverização empregadas, com gotas médias, grossas e muito grossas, bem como os volumes de aplicação de 80 e 130 L ha-1, não influenciaram o controle das plantas daninhas. Não se detectou exoderiva com a metodologia empregada.

Sulfated bromophenols from Osmundaria obtusiloba (C. Agardh) R. E. Norris (Rhodophyta, Ceramiales)

Two new sulfated oligobromophenols from the marine red algae Osmundaria obtusiloba, 4-(1'-potassium sulfate, 2,3-dibromo, 1',4,5-trihydroxybenzyl) - 4''-(1'''-potassium sulfate, 2'',3''-dibromo, 1''',4'',5''-trihydroxybenzyl) sulfate and 1'-(2, 3-dibromo, 4-potassium sulfate, 1', 4, 5-trihydroxybenzyl) - 4''-(1''' potassium sulfate, 2'', 3''-dibromo, 1''', 4'', 5'' trihydroxybenzyl) sulfate, are herein reported. Besides them it was obtained 2, 2', 3, 3'-tetrabromo-4, 4', 5, 5'-tetrahydroxydiphenylmethane, 2, 3-dibromo-p-hydroxybenzyl methyl ether (methyl lanosol), dipotassium 2,3-dibromo-5-hydroxybenzyl 1',4-disulfate, 24-methylenecolest-5-en-3-beta-ol and alpha-D-mannopyranosyl-(1->2')-glycerate (digeneaside). The structures were determined by analysis of the spectroscopic data (IR, NMR and MS) and comparison with the literature. The 13CNMR data for dipotassium 2,3-dibromo-5hydroxybenzyl-1',4-disulfate are described here for the first time. The present study also suggests a mild method to isolate and to purify sulfated compounds.

Anxiolytic-like effects of 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate in mice

The pharmacological effects of 4-phenyl-2-trichloromethyl-3H-1,5-benzodiazepine hydrogen sulfate (PTMB), a novel synthetic benzodiazepine, were examined in mice. In the elevated plus-maze test of anxiety, 0.3-1 mg/kg diazepam ip (F(3,53) = 3.78; P<0.05) and 1-10 mg/kg PTMB ip increased (F(5,98) = 3.26; P<0.01), whereas 2 mg/kg picrotoxin ip decreased (F(3,59) = 8.32; P<0.001) the proportion of time spent in the open arms, consistent with an anxiolytic action of both benzodiazepines, and an anxiogenic role for picrotoxin. In the holeboard, 1.0 mg/kg diazepam ip increased (F(3,54) = 2.78; P<0.05) and 2 mg/kg picrotoxin ip decreased (F(3,59) = 4.69; P<0.01) locomotor activity. Rotarod assessment revealed that 1 mg/kg diazepam ip and 3, 10 and 30 mg/kg PTMB ip produced significant motor incoordination compared to vehicle control (F(4,70) = 7.6; P<0.001). These data suggest that the recently synthesized PTMB compound possesses anxiolytic activity and produces motor incoordination similar to those observed with diazepam.

Gliclazide and bedtime insulin are more efficient than insulin alone for type 2 diabetic patients with sulfonylurea secondary failure

To determine the effects of combined therapy of gliclazide and bedtime insulin on glycemic control and C-peptide secretion, we studied 25 patients with type 2 diabetes and sulfonylurea secondary failure, aged 56.8 ± 8.3 years, with a duration of diabetes of 10.6 ± 6.6 years, fasting plasma glucose of 277.3 ± 64.6 mg/dl and a body mass index of 27.4 ± 4.8 kg/m². Patients were submitted to three therapeutic regimens lasting 2 months each: 320 mg gliclazide (phase 1), 320 mg gliclazide and bedtime NPH insulin (phase 2), and insulin (phase 3). At the end of each period, glycemic and C-peptide curves in response to a mixed meal were determined. During combined therapy, there was a decrease in all glycemic curve values (P<0.01). Twelve patients (48%) reached fasting plasma glucose <140 mg/dl with a significant weight gain of 64.8 kg (43.1-98.8) vs 66.7 kg (42.8-101.4) (P<0.05), with no increase in C-peptide secretion or decrease in HbA1. C-Peptide glucose score (C-peptide/glucose x 100) increased from 0.9 (0.2-2.1) to 1.3 (0.2-4.7) during combined therapy (P<0.01). Despite a 50% increase in insulin doses in phase 3 (12 U (9-30) vs 18 U (11-60); P<0.01) only 3 patients who responded to combined therapy maintained fasting plasma glucose <140 mg/dl (P<0.02). A tendency to a higher absolute increase in C-peptide (0.99 (0.15-2.5) vs 0.6 (0-2.15); P = 0.08) and C-peptide incremental area (2.47 (0.22-6.2) vs 1.2 (0-3.35); P = 0.07) was observed among responders. We conclude that combined therapy resulted in a better glucose response to a mixed meal than insulin alone and should be tried in type 2 diabetic patients before starting insulin monotherapy, despite difficulties in predicting the response.

Glutamatergic neurotransmission modulates hypoxia-induced hyperventilation but not anapyrexia

The interaction between pulmonary ventilation (V E) and body temperature (Tb) is essential for O2 delivery to match metabolic rate under varying states of metabolic demand. Hypoxia causes hyperventilation and anapyrexia (a regulated drop in Tb), but the neurotransmitters responsible for this interaction are not well known. Since L-glutamate is released centrally in response to peripheral chemoreceptor stimulation and glutamatergic receptors are spread in the central nervous system we tested the hypothesis that central L-glutamate mediates the ventilatory and thermal responses to hypoxia. We measured V E and Tb in 40 adult male Wistar rats (270 to 300 g) before and after intracerebroventricular injection of kynurenic acid (KYN, an ionotropic glutamatergic receptor antagonist), alpha-methyl-4-carboxyphenylglycine (MCPG, a metabotropic glutamatergic receptor antagonist) or vehicle (saline), followed by a 1-h period of hypoxia (7% inspired O2) or normoxia (humidified room air). Under normoxia, KYN (N = 5) or MCPG (N = 8) treatment did not affect V E or Tb compared to saline (N = 6). KYN and MCPG injection caused a decrease in hypoxia-induced hyperventilation (595 ± 49 for KYN, N = 7 and 525 ± 84 ml kg-1 min-1 for MCPG, N = 6; P < 0.05) but did not affect anapyrexia (35.3 ± 0.2 for KYN and 34.7 ± 0.4ºC for MCPG) compared to saline (912 ± 110 ml kg-1 min-1 and 34.8 ± 0.2ºC, N = 8). We conclude that glutamatergic receptors are involved in hypoxic hyperventilation but do not affect anapyrexia, indicating that L-glutamate is not a common mediator of this interaction.

Partial characterization and anticoagulant activity of a heterofucan from the brown seaweed Padina gymnospora

The brown algae Padina gymnospora contain different fucans. Powdered algae were submitted to proteolysis with the proteolytic enzyme maxataze. The first extract of the algae was constituted of polysaccharides contaminated with lipids, phenols, etc. Fractionation of the fucans with increasing concentrations of acetone produced fractions with different proportions of fucose, xylose, uronic acid, galactose, and sulfate. One of the fractions, precipitated with 50% acetone (v/v), contained an 18-kDa heterofucan (PF1), which was further purified by gel-permeation chromatography on Sephadex G-75 using 0.2 M acetic acid as eluent and characterized by agarose gel electrophoresis in 0.05 M 1,3 diaminopropane/acetate buffer at pH 9.0, methylation and nuclear magnetic resonance spectroscopy. Structural analysis indicates that this fucan has a central core consisting mainly of 3-ß-D-glucuronic acid 1-> or 4-ß-D-glucuronic acid 1 ->, substituted at C-2 with alpha-L-fucose or ß-D-xylose. Sulfate groups were only detected at C-3 of 4-alpha-L-fucose 1-> units. The anticoagulant activity of the PF1 (only 2.5-fold lesser than low molecular weight heparin) estimated by activated partial thromboplastin time was completely abolished upon desulfation by solvolysis in dimethyl sulfoxide, indicating that 3-O-sulfation at C-3 of 4-alpha-L-fucose 1-> units is responsible for the anticoagulant activity of the polymer.

Impact of a 2-year intervention program on cardiometabolic profile according to the number of goals achieved

We investigated the impact of lifestyle goal achievement on cardiovascular risk factors after a 2-year behavioral intervention program applied to 394 adults (113 with diabetes, mean age 60.2 ± 11.4 years, 56% women) and targeting four goals: ≥5% weight loss; ≥150 min/week physical activities; <10% saturated fat intake/day; ≥400 g fruit and vegetable intake/day. Baseline characteristics and changes in variables after intervention among the four categories of number of goals achieved (none, 1, 2, and ≥3) were compared by independent ANOVA or the Kruskal-Wallis test. Individuals without diabetes achieving a higher number of goals were more likely to be older (3 or 4 goals: 61.8 ± 12.6 years vs none: 53.3 ± 10.3 years, P < 0.05) and to have a lower mean BMI (3 or 4 goals: 21.7 ± 2.6 kg/m² vs none: 29.0 ± 4.8 kg/m², P < 0.05), diastolic blood pressure (3 or 4 goals: 77.3 ± 2.1 mmHg vs none: 85.4 ± 9.6 mmHg, P < 0.05), triglyceride (3 or 4 goals: 116.1 ± 95.1 mg/dL vs none: 144.8 ± 65.5 mg/dL, P < 0.05) and insulin levels (3 or 4 goals: 3.6 ± 2.4 μU/L vs none: 5.7 ± 4.0 μU/L, P < 0.05) than those achieving fewer goals. The absolute changes in cardiovascular risk factors tended to be more pronounced with increasing number of goals achieved in individuals without diabetes. The intervention had a beneficial impact on the cardiometabolic profile of individuals with normal or altered glucose metabolism. The number of goals achieved in this lifestyle intervention was associated with the magnitude of improvement of cardiovascular risk factors in individuals without diabetes. Participants with a better cardiometabolic profile seemed to be more likely to have a healthy lifestyle.

Estimate of dietary intake of chloropropanols (3-MCPD and 1,3-DCP) and health risk assessment

Chloropropanols, including 3-monochloropropane-1,2-diol (3-MCPD) and 1,3-dichloropropan-2-ol (1,3-DCP), comprise a group of chemical contaminants with carcinogenic and genotoxic properties. They have been found in a variety of processed foods and food ingredients, such as hydrolyzed vegetable protein, soy sauce, cereal-based products, malt-derived ingredients, and smoked foods. This study aimed to assess the dietary exposure to 3-MCPD and 1,3-DCP in Brazil and verify whether the presence of these substances in foods could represent health risks. The intake was calculated by combining data on food consumption, provided by the Consumer Expenditure Survey 2008-2009, with the levels of contaminant occurrence determined by gas chromatography-mass spectrometry. The exposure to 3-MCPD ranged from 0.06 to 0.51 µg.kg bw-1.day-1 considering average and high consumers, while the intake of 1,3-DCP was estimated to be 0.0036 µg.kg bw-1.day-1 in the worst case scenario evaluated. Based on these results, it was verified that the Brazilians' exposure to chloropropanols does not present a significant health risk. However, the consumption of specific foods containing high levels of 3-MCPD could exceed the provisional maximum tolerable daily intake of 2 µg.kg bw-1 established for this compound and, therefore, represent a potential concern.