Investigation of the antinociceptive efficacy and relative potency of extended duration injectable 3-acylmorphine-6-sulfate prodrugs in rats

This investigation was designed to examine the antinociceptive activity in rats of 3-O-acyl prodrugs of M6S relative to the parent drug, after intravenous and intramuscular injection, using the tail flick latency test of antinociception. M6S, 3-acetylmorphine-6-sulfate (3AcM6S), 3-propionylmorphine-6-sulfate (3PrM6S), 3-butanoylmorphine-6-sulfate (3BuM6S) and 3-heptanoylmorphine-6-sulfate (3HpM6S) were administered by the IV route in a dose of 4.10 mu mol/kg. Relatively high levels of antinociception (>40% Maximum Possible Effect) were achieved following administration of M6S, 3AcM6S and 3PrM6S, whereas insignificant antinociception (<20%MPE) was achieved following administration of 3BuM6S or 3HpM6S. Although the mean duration of action for 3AcM6S (6 h) was longer than for M6S or 3PrM6S (4 h), the mean area (+/- S.E.M.) under the degree of antinociception versus time curve (AUG) for 3AcM6S (151.6 +/- 6.9%MPE h) was not significantly different (p <0.05) from that for M6S (120.8 +/- 32.7%MPE h) or for 3PrM6S (106.0 +/- 21.3%MPE h). The mean ED50 (range) doses for M6S, 3AcM6S and 3PrM6S were calculated to be 4.16 (3.61-4.48), 4.32 (3.55-5.09) and 4.54 (4.21-4.79) mu mol/kg, respectively. Preliminary studies were conducted on potential long-acting formulations containing 8 x ED50 doses of M6S and the 3-acetyl and 3-propionyl esters suspended in soybean oil. These showed that 3PrM6S gave a greater AUC (mean + S.E.M.) (1087.4 +/- 97.4%MPE h) and longer duration of action (20 h) than did M6S (613.1 +/- 155.9%MPE h; 10 h duration) or 3AcM6S (379.3 + 114.2%MPE h: 8 h duration). Further studies are needed to more fully investigate these findings. (C) 1998 Elsevier Science B.V. All rights reserved.

Changes in the racial composition of Phytophthora sojae in Australia between 1979 and 1996

Surveys of commercial soybean fields, disease nurseries, and trial plots of soybean were conducted throughout eastern Australia between 1979 and 1996, and 694 isolates of Phytophthora sojae were collected and classified into races. Fourteen races, 1, 2, 4, 10, 15, and 25, and eight new races, 46 to 53, were identified, but only races 1, 4, 15, 25, 46, and 53 were found in commercial fields. Races 1 and 15 were the only races found in commercial fields in the soybean-growing areas of Australia up until 1989, with race 1 being the dominant race. Race 4 was found in central New South Wales in 1989 on cultivars with the Rps1a gene, and it is now the dominant race in central and southern New South Wales. Races 46 and 53 have only been found once, in southern New South Wales, and race 25 was identified in the same region in 1994 on a cultivar with the Rps1k gene. Only races 1 and 15 have been found in the northern soybean-growing regions, with the latter dominating, which coincides with the widespread use of cultivars with the Rps2 gene. Changes in the race structure of the P. sojae population from commercial fields in Australia follow the deployment of specific resistance genes.

Oxidation of oxa and thia fatty acids and related compounds catalysed by 5-and 15-lipoxygenase

The modified fatty acids, (Z,Z,Z)-(octadeca-6,9,12-trienyloxy)acetic acid, (Z,Z,Z)-(octadeca-9,12,15-trienyloxy)acetic acid, (all-Z)-(eicosa-5,8,11,14-tetraenyloxy)acetic acid, (all-Z)-(eicosa-5,8,11,14-tetraenylthio)acetic acid, 3-[(all-Z)-(eicosa-5,8,11,14-tetraenylthio)]propionic acid, (all-Z)-(eicosa-5,8,11,14-tetraenylthio)succinic acid, N-[(all-Z)-(eicosa-5,8,11,14-tetraenoyl)]glycine and N-[(all-Z)-(eicosa-5,8,11,14-tetraenoyl)]aspartic acid, all react with soybean 15-lipoxygenase. The products were treated with triphenylphosphine to give alcohols, which were isolated using HPLC. Analysis of the alcohols using negative ion tandem electrospray mass spectrometry, and by comparison with compounds obtained by autoxidation of arachidonic acid, shows that each enzyme catalysed oxidation occurs at the omega -6 position of the substrate. In a similar fashion, it has been found that (Z,Z,Z)-(octadeca-6,9,12-trienyloxy)acetic acid, (Z,Z,Z)-(octadeca-9,12,15-trienyloxy)acetic acid, (all-Z)-(eicosa-5,8,11,14-tetraenylthio)acetic acid and N-[(all-Z)-(eicosa-5,8, 11.14-tetraenylthio)]propionic acid each undergoes regioselective oxidation at the carboxyl end of the polyene moiety on treatment with potato 5-lipoxygenase. Neither (all-Z)-(eicosa-5,8,11,14-tetraenylthio)succinic acid nor N-[(all-Z)-(eicosa-5,8,11,14-tetraenoyl)]aspartic acid reacts in the presence of this enzyme, while N-[(all-Z)-(eicosa-5,8,11,14-tetraenoyl)]glycine affords the C11' oxidation product. The alcohol derived from (Z,Z,Z)-(octadeca-6,9, 12-trienyloxy)acetic acid using the 15-lipoxygenase reacts at the C6' position with the 5-lipoxygenase. (C) 2001 Elsevier Science Ltd. All rights reserved.

Soybean: unrealized income losses avoided during harvest.

The wastes occurred during the harvest cause a hard impact in the agricultural business. About the soy fields, recent researches indicate that half of this waste could be avoided, reducing the cost of production and resultant earning of the companies. The purpose of this article is to analyze the estimative of soy harvest field area of 2006/07 to 2007/08 and respective production, subsidy estimate the waste that could be avoided during the harvest, considerating tolerable levels of 60 Kg by hectare, accordant is the model adopted on USA e Brazil. This research was based in a bibliographic study to explain and analyze all sides, practical and theoretical around the investigate problem. It was checked that is possible expect and avoid these wastes during the harvest. Such wastes overcome the mark of 20,000 ton/year, that in money talks represent over R$ 1.000.000 mil/year. Conclude however that wastes when treated provide a production cost reduction, indicating execution and a positive impact on agricultural companies` earnings.

Effect of fish oil containing parenteral lipid emulsions on neutrophil chemotaxis and resident-macrophages` phagocytosis in rats

Background & aims: There is scarce information about immune function and parenteral. fish oil (FO). The influence of a new parenteral. lipid emulsion (LE) containing fish oil (SMOF) was experimentally evaluated on neutrophils` chemotaxis and macrophages` phagocytosis. Methods: Adult mate Lewis rats (n = 40) were randomized into five groups; one non-surgical. control and four to receive parenteral LE or saline infusion through jugular vein catheterization: SMOF (mixture of 30% medium-chain triglycerides, 30% soybean, 25% olive and 15% fish oils); MCT/LCT (physical mixture of 50% medium-chain triglycerides and 50% soybean oil); MCT/LCT/FO (80% MCT/LCT supplemented with 20% FO) and SS (saline). In the 5th experimental day and after intravenous colloidal carbon injection, blood and tissue (liver, lung and spleen) samples were collected and immunological analyses were performed. Results: LE didn`t influence neutrophil chemotaxis. SMOF didn`t influence phagocytosis (p > 0.05) while MCT/LCT and MCT/LCT/FO LE increased the number of liver and lung resident macrophages that had engaged in phagocytosis compared with CO-NS and SS (p < 0.05). Only MCT/LCT/FO increased the number of spleen resident macrophages that had engaged in phagocytosis (p < 0.05). Conclusions: LE, independently of composition, had no influence on neutrophils` chemotaxis, but showed different effect on phagocytosis by macrophages. SMOF LE had neutral effect while fish oil LE enriched with MCT/LCT LE increased resident-macrophages` phagocytosis. (c) 2007 Elsevier Ltd and European Society for Clinical Nutrition and Metabolism. All rights reserved.

The soybean concentrated extract proliferates the vagina of adult rats

Objective: The aim of this study was to evaluate changes induced on the vagina of ovariectomized rats after treatment with soybean concentrated extract or conjugated equine estrogens and the association of both drugs. Methods: We conducted an experimental study with 50 ovariectomized rats that were randomly divided into five equal groups of 10 animals: GI received vehicle, GII received soybean concentrated extract 46 mg/kg per day, GIII received soybean concentrated extract 120 mg/kg per day, GIV received conjugated equine estrogens 50 mu g/kg per day, and GV received conjugated equine estrogens 50 mu g/kg and soybean concentrated extract 46 mg/kg per day. The substances were administered by gavage during 21 consecutive days. After that, the animals were killed under anesthesia and the vagina was removed for histological and immunohistochemical analysis. Data were initially submitted to analysis of variance. Whenever a significant difference was detected, the study was complemented with the Tukey-Kramer test for multiple comparisons. Results: GII did not show any differences on the vaginal epithelium or collagen compared with GI. GIII presented an increase in vaginal epithelium and collagen amount. GIV had the highest amount of collagen and the signals of vaginal proliferation. GV did not show any additional effect compared with GIV. Conclusions: Our data suggest that a high dose of isoflavone-rich soy extract may have positive effects on the vaginal structures of ovariectomized rats, but this action is less than that of estrogen treatment on vaginal thickness. In addition, soy extract may not block the estrogen effect on vaginal tissue.

Eosinophilic pneumonitis induced by aerosol-administered diesel oil and pyrethrum to mice

Objective. To confirm the episode of eosinophilic pneumonitis that occurred in March 2001 in Manaus, Amazon, northern Brazil, as secondary to home aerosolization with 2% cypermethrin diluted in diesel compared with the more conventional 1% cypermethrin and soybean solution used in prophylaxis of dengue. Methods. Four groups of Swiss mice were kept in polycarbonate cages aerosolized with one of the following solutions: diesel, diesel and cypermethrin, soy oil and cypermethrin, and saline. Three and 6 days after exposure, resistance and compliance of the respiratory system and white cell kinetics in peripheral blood and lung tissue were analyzed. Results. The group exposed to diesel and cypermethrin showed higher respiratory system resistance (p < 0.001), lower compliance (p = 0.03), and increased eosinophils in blood (p = 0.03) and lung tissue (p = 0.005) compared with the other groups. There was an increase of neutrophils in the blood of all experimental groups on the third day after exposure (p < 0.001). Conclusions. We concluded that diesel associated with cypermethrin induced lung hyperresponsiveness in this experimental model and was associated with increased polymorphonuclear cells (eosinophils and neutrophils) in blood and lungs. This effect is strongest on the third day after exposure. These results are similar to the episode that occurred in Manaus in 2001 and suggest that diesel plus cypermethrin home aerosolization for arbovirosis prophylaxis should be revised.