REACTIVE OXYGEN GENERATION BY AZOMETHINE-H - A NEW ANTIMALARIAL DRUG

Superoxide radical (O-2(-)) is a free radical that may be involved in various toxic processes. Cu-Zn superoxide dismutase catalyzes the dismutation of the superoxide free radical and protects cells from oxidative damage. A rat bioassay validated for the identification of the toxic effects of azomethine H revealed increased serum activities of amylase, alanine transaminase, and alkaline phosphatase. The lipoperoxide and bilirubin concentrations were also increased in animals that received azomethine H (1 g/kg) from ascorbic or hydrochloric acid solutions. Azomethine H increased Cu-Zn superoxide dismutase activity. This elevation of Cu-Zn superoxide dismutase activity was highest on the 7th day and was at levels comparable with those of control rats from day 60 onwards. Superoxide is an important intermediate in the action and toxicity of azomethine H.

Turbinatine, a potential key intermediate in the biosynthesis of corynanthean-type indole alkaloids

Extraction of the leaves of Chimarrhis turbinata has led to the isolation of turbinatine (1), a new corynanthean-type indole alkaloid, besides four known indole alkaloids, strictosidine, 5alpha-carboxystrictosidine, vallesiachotamine, and isovallesiachotamine. The structural determination of 1 was based on 1D and 2D spectroscopic data. An evaluation of the DNA-damaging activities of the isolates was performed by means of a bioassay using mutant strains of Saccharomyces cerevisiae, which indicated these compounds were weakly active.

Época de sobressemeadura de gramíneas anuais de inverno e de verão no capim-Tifton 85: produção e composição botânica

The experiment was conducted at UNESP-Jaboticabal during the 2001-2002 winter-spring-summer periods to evaluate the herbage mass, botanical composition, dry matter production of mix pastures, and leaf: sheat-stem ration of Tifton 85 or overseeding with annual winter or summer species. The treatments were: pearl millet (Pennisetum americanum (L.) Leeke) plus bristeal oat (Avena strigosa Schreb); sorghum sudan grass (Sorghum bicolor (L.) Moench x Sorghum sudanense (Piper) Stapf) (SS AG2501 C) plus bristeal oat, overseeded on Tifton 85 area on 06/19/02/04, or 07/02/02, and Tifton 85, conducted in a randomized block design. The AG2501 contributed with a small participation in the botanical composition and the presence of millet in the experiment was not observed. Highest herbage mass at first and second evaluations related to first seeding time was 63% higher compared to the second seeding time. The herbage mass were similar he production in the other evaluations were similar. on the second seeding time, it was observed highest oat species in relation to the first seeding time. The leaf: sheat-stem ration decreased during the experiment due to the pasture botanical composition changes.

Nitrogen management in maize cover crop rotations

Winter cover crops can affect N nutrition of the following maize crop. Although legumes have been recommend for maize rotations, in tropical areas grasses may be more interesting because they provide a longer protection of soil surface. Legumes can add N to the system and grasses can compete with maize for the available nutrient. An experiment was conducted in Botucatu, São Paulo State, Brazil, to study N dynamics in the soil surface straw-maize system as affected by N fertilization management and species included in the no-till rotation. Treatments were fallow, black oat (Avena strigosa), pearl millet (Pennisetum glaucum), white lupins (Lupinus albus), black oat fertilized with N. and pearl millet fertilized with N. Maize was grown afterwards in the same plots, receiving 0.0, 60.0 and 120.0 kg ha(-1) of N sidedressed 30 days after plant emergence. Soil, straw and maize samples were taken periodically. The highest corn yields were observed when it was cropped after pearl millet fertilized with N. Nitrogen side dressed application up to 120 kg ha(-1) was not able to avoid corn yield decrease caused by black oat. Grasses can be recommended in maize rotations in tropical areas, provided they receive nitrogen fertilizer and show no allelopathy. Due to its higher ON ratio and dry matter yield they are better than legumes, protecting the soil surface for a longer period. Pearl millet is particularly interesting because it enhances N use efficiency by the following maize crop. For a better N availability/demand synchronism, the cover crops should be desiccated right before maize planting.

Isolation and sequence determination of peptides in the venom of the spider wasp (Cyphononyx dorsalis) guided by matrix-assisted laser desorption/ionization time of flight (MALDI-TOF) mass spectrometry

Micro-scale (sub-pmol) isolation and sequence determination of three peptides from the venom of the solitary spider wasp Cyphononyx dorsalis is described. We isolated two novel peptides Cd-125 and Cd-146 and a known peptide Thr(6)-bradykinin from only two venom sacs of solitary spider wasp Cyphononyx dorsalis without bioassay-guided fractionation. but instead guided by MALDI-TOF MS. The MALDI-TOF MS analysis of each fraction showed the purity and molecular weight of the components, which led to the isolation of the peptides virtually without loss of sample amount. The sequences of the novel peptides Cd-125 (Asp-Thr-Ala-Arg-Leu-Lys-Trp-His) and Cd-146 (Ser-Glu-Thr-Gly-Asn-Thr-Val-Thr-Val-Lys-Gly-Phe-Ser-Pro-Leu-Arg) were determined by Edman degradation together with mass spectrometry. and finally corroborated by solid-phase synthesis. The known peptide Thr(6)-bradykinin (Arg-Pro-Pro-Gly-Phe-Thr-Pro-Phe-Arg) was identified by comparison with the synthetic authentic specimen. This is the first example for any kinins to be found in Pompilidae wasp venoms. The procedure reported here can be applicable to studies on many other components of solitary wasp venoms with limited sample availability. (C) 2001 Elsevier B.V. Ltd. All rights reserved.

Insecticidal activity of chemical constituents from Aristolochia pubescens against Anticarsia gemmatalis larvae

Acetone and ethanol extracts of the tubercula and several compounds isolated from Aristolochia pubescens (Willd) were bioassayed on velvebean caterpillars, Anticarsia gemmatalis (Hubner), for evaluation of the insecticidal activities. of the extracts subjected to bioassay, the acetone extract showed the highest activity. (-)-Cubebin did not show activity against soybean caterpillars, whereas aristolochic acid and ent-kaur-15-en-17-ol increased the larval period. These compounds, and (+)-eudesmin and (+)-sesamin, reduced the viability of this period, giving rise to malformed adults. These extracts and compounds are therefore potential botanical insecticide agents for the control of velvetbean caterpillars in soybean crops. (C) 2003 Society of Chemical Industry.

Leaching of nitrate and ammonium from cover crop straws as affected by rainfall

Nitrogen (N) mineralization dynamics in no-till systems is affected, among other factors, by N amount and quality in the mulch and by climatic conditions. Leaching of NO3-N and NH4-N from six plant species used as soil cover crops in tropical environments were evaluated when the straw was submitted to rainfall after chemical desiccation. Millet (Pennisetum glaucum), guinea sorghum (Sorghum vulgare), black oat (Avena strigosa), triticale (Triticum secale), Indian hemp (Crotalaria juncea), and brachiaria (Brachiaria decumbens) were grown in a greenhouse, in Botucatu-SP, Brazil. Forty-five days after emergence, the plants were cut at the root collar, oven-dried, and submitted to simulated rainfalls of 4.4, 8.7, 17.04, 34.9, and 69.8 mm, considering an amount of straw equivalent to 8 t ha(-1) of dry matter. The amounts of N-NO3- extracted from the straw by rainwater were very small. However, accumulated rainfall around 70 mm caused ammonium leaching ranging from 2.5 to 9.5kg ha(-1), depending on the species. Plant residues of triticale and black oat (grasses) and Indian hemp (legume) showed high N leaching intensity with the first rains after chemical desiccation. The amount of N leached from straw was highly correlated with N tissue content.

TOXIC EFFECTS OF WATER EUTROPHICATION ON PANCREATIC, HEPATIC AND OSTEOGENIC TISSUES OF RATS

Pollution, industrial solvents, concentrations of metals and other environmental agents are widely related to biochemicals values which are used in disease diagnosis of environmental toxicity. A rat bioassay validated for the identification of toxic effects of eutrophication revealed increased serum activities of amylase, alanine transaminase (BLT) and alkaline phosphatase (ALP) in rats that received algae, filtered water and nickel or cadmium from drinking water. Serum Cu-Zn superoxide dismutase activity decreased from its basal level of 40.8 +/- 2.3 to 26.4 U/mg protein, at 7 days of algae and at 48 hr of nickel and cadmium water ingestion. The observation that lipoperoxide concentration was not altered in rats treated with filtered water, while amylase, ALT and ALP were increased in these rats and in those treated with nickel or cadmium, indicated that pancreatic, hepatic and osteogenic lesions by eutrophication were not related to superoxide radicals, and might be due to a novel toxic environmental agent found in filtered and non-filtered algae water.

Persistence and effectiveness of pyrethroids in plastic strips against Varroa jacobsoni (Acari : Varroidae) and mite resistance in a mediterranean area

An apiary trial was conducted in 1997 in Sardinia, Italy, to verify the effectiveness of fluvalinate in polyvinyl chloride strips and flumethrin in polyethylene strips against Varroa jacobsoni Oudemans. Two indices to evaluate the efficacy of the treatments were adopted: percentage change in mite infestation of worker-sealed brood cells considering only treated hives and percentage change in mite mortality, and the natural variation in mite populations recorded in control hives during the trial. All acaricide treatments reduced the level of mite infestation of both sealed brood and adult bees. However, their effectiveness was slightly reduced in comparison to previous studies because of mite resistance phenomena. Portions of polyethylene strips of flumethrin from treated hives were sampled weekly to determine acaricide persistence using gas chromatography. After 4 wk, a slight reduction (approximate to9%) of the active ingredient content was observed, A laboratory bioassay also was performed to establish the resistance of adult female mites to fluvalinate, Mites were sampled from the experimental apiary and from various Sardinian apiaries which had primarily been subjected to fluvalinate applications in plastic strips or wood inserts for years. Mite resistance varied from 0 to 96%, depending on the acaricide management adopted, the lowest resistance level occurred in an apiary where pyrethroids had never been used, whereas the highest level occurred in an apiary with intensive use of fluvalinate in wood inserts.

BIOACTIVE AND OTHER PIPERIDINE ALKALOIDS FROM CASSIA-LEPTOPHYLLA

Four new piperidine alkaloids, leptophyllin A (4), 3-acetylleptophyllin A (5), leptophyllin B (8), and (-)-spectaline (1), and 3 known piperidine alkaloids, (-)-spectalinine (2), canavaline (3), and iso-6-canavaline (7), were isolated by a bioassay-guided fractionation of a leaf extract of Cassia leptophylla. The alkaloids 1 - 3 were active in a mechanism-based DNA-modifying yeast assay and 2 was moderately active in Vero monkey and Chinese hamster ovary cell cytotoxicity assays.

A DNA-damaging sesquiterpene and other constituents from Frullania nisquallensis

Bioassay-guided fractionation of an MeCOEt extract of Frullania nisquallensis Sull. has furnished a DNA-damaging sesquiterpene, costunolide (1), and two inactive compounds, a sesquiterpene (-)-frullanolide (2) and a tridepside tenuiorin (3). C-13-NMR data of 3 are reported.

Utilization of Spirillum volutans for monitoring the toxicity of effluents of a cellulose and paper industry

The motility of Spirillum volutans was used for monitoring the toxicity of effluents of a cellulose and paper industry. Results indicated that there was no correlation between organic content and the toxic effects of the residues in the effluents. The effluents from the chlorination step and from the sludge ponds presented the highest toxicity. on the other hand, the final effluent from the biological treatment basin had no toxic agent. This bioassay showed to be a simple and reliable technique that can be used for adequately monitoring the toxicity of effluents.

Experimental toxoplasmosis in broiler chicks

To evaluate chicken toxoplasmosis both as an economic and a public health subject, 84 broiler chicks of a commercial strain, 30 days old, were distributed into seven groups of 12 birds (three replications of four chicks) experimentally infected with three developing T. gondii stages of the P strain as follows: tachyzoites. intravenous (two groups: 5.0 x 10(5) and 5.0 x 10(6)), cysts, per os (two groups: 1.0 x 10(2) and 1.0 x 10(3)) and oocysts, per os (three groups: 5.0 x 10(2), 5.0 x 10(3) and 5.0 x 10(4)). Twelve chicks received only a placebo (control group). During the next 30 days the following parameters were estimated: productivity (weight gain and feed conversion), clinical signs, including rectal temperature and parasitemia (bioassay). No clinical signs suggesting toxoplasmosis were seen and no statistical differences on productivity standards were found in comparison between inoculated and control chicks. However, fowls inoculated with tachyzoites and oocysts occasionally showed hyperthermia. Some haematological changes were detected in fowls inoculated with T. gondii. Anatomo-histopathological changes were not observed. From 14 parasitemias detected, 35.7% appeared on the 5th day after inoculation and 57.1% of them resulted from oocysts inoculation. After 30-35 days all birds were slaughtered: fragments from 12 organs or tissues from each of them were subjected to artificial peptic digestion and after that injected into T. gondii antibody-free mice (IIFR). T. gondii was detected in brain (12), pancreas (five), spleen (five), retina (five), kidney (two), heart (four), proventriculus (three), liver (two), intestine (two), lung (one), and skeletal muscle (one). Similar to observations with parasitemia, from 42 T. gondii isolations, 59.5% came from chicks which had received oocysts. It can thus be inferred that the developing form, expelled by cats, is the most important for T. gondii chicken infection and that brain is the most infected organ in birds. Attention must be paid to the potential importance of chicken meat in public health, since T. gondii was isolated from skeletal and heart muscles. (C) 1997 Elsevier B.V. B.V.

Tumor necrosis factor-alpha in gestation and puerperium of women with gestational hypertension and pre-eclampsia

Problem High plasma levels of tumor necrosis factor-alpha (TNF-alpha) in pregnant women have been associated with the pathogenesis of pre-eclampsia (PE). This study evaluated TNF-alpha plasma levels and monocyte production in gestational hypertension (GH) and PE during gestation and at puerperium.Method of study This study included 128 women, of whom 20 were non-pregnant (NP) normotensive (NT), and 108 were pregnant: 36 NT, 27 with GH, and 45 with PE. Peripheral blood plasma was used for TNF-alpha and uric acid determination. TNF-alpha was determined in plasma and lipopolysaccharide (LPS)-stimulated and non-stimulated monocyte supernatants by L929 bioassay.Results Tumor necrosis factor-alpha and uric acid plasma levels were higher in PE than in GH pregnancies. In both hypertensive groups, these parameters positively correlated and were significantly more elevated than in NT and NP women. TNF-alpha plasma levels and monocyte production were higher in hypertensive than in NT women during gestation, and significantly decreased at puerperium. Although decreased, TNF-alpha release in LPS-stimulated PE monocytes, was still significantly higher than in the other pregnant groups.Conclusion In vivo monocyte activation in GH and PE pregnant women was characterized by in vitro TNF-alpha production. The fact that higher circulating concentrations of TNF-alpha and uric acid were observed in PE than in GH suggests an association with disease severity.

Potencial alelopático e levantamento do banco natural de sementes sob a copa de Copaifera langsdorffii Desf

the aim of this study was to evaluate the allelopathic effect of soil samples collected under the canopies of three specimens of Copaifera langsdorffii the germination of Lactuca sativa and survey the natural seed bank according to seasonality. To test the allelopathic effect was carried experiments of pre and post-emergence with seeds of L. sativa and to quantify the stock of seeds, soil samples were collected from three specimens at three distances from the stem (1, 2 and 3 m) and at three depths (0-5, 5-10 and 10-15cm) in the region of savanna in the dry and wet seasons. The samples tested in bioassay of pre-emergence no significant influence on germinability, mean germination time and mean germination speed, but showed a difference in the synchronism of germination, these data were independent of sampling station. In test for post-emergence was observed statistical difference in the parameters evaluate (length of primary roots and hypocotyls) in both seasons. To quantify the natural seed bank were macroscopic analysis of each soil sample with the help of stereoscopic microscope. The analysis of the natural seed bank showed a larger number of seeds in the 0-5cm and in distance of 2m for both seasons. The results suggest the presence of allelochemical substances in soil samples collected under the canopy of Copaifera langsdorffii.