Natural products from Brazilian biodiversity as a source of new models for medicinal chemistry

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Antigenic typing of brazilian rabies virus samples isolated from animals and humans, 1989-2000

Amostras de vírus rábico isoladas de animais e humanos no período de 1989 a 2000 foram tipificadas antigenicamente com a utilização de um painel de anticorpos monoclonais contra a nucleoproteína viral, pré-estabelecido para o estudo da epidemiologia molecular do vírus rábico isolado nas Américas. As amostras testadas foram isoladas no laboratório de diagnóstico do Instituto Pasteur e outros centros de diagnóstico de raiva no Brasil. Além das cepas de vírus rábico fixo CVS-31/96-IP, mantida em cérebro de camundongos e a PV-BHK/97, mantida em cultura de células, cepas de vírus rábico isoladas de cães, gatos, bovinos, eqüinos, morcegos, ovinos, caprino, suínos, raposa, sagüí, coatí, guaxinim e humanos, totalizaram 330 amostras. Seis variantes antigênicas foram definidas, compatíveis com perfís observados no painel de anticorpos monoclonais pré-estabelecido utilizado, as de número 2 (cão), 3 (Desmodus rotundus), 4 (Tadarida brasiliensis), 5 (Vampiro da Venezuela), 6 (Lasiurus cinereus) e Lab (reagente a todos os anticorpos utilizados), além de outros seis perfís desconhecidos, não compatíveis com aqueles observados no painel utilizado. A maior variabilidade foi observada entre as amostras isoladas de morcegos insetívoros e a variante mais comum isolada entre as espécies foi a variante 3 (Desmodus rotundus). Estes fatos podem representar a existência de múltiplos ciclos de transmissão independentes, envolvendo diferentes espécies de morcegos.

A comparison of global estimates of marine primary production from ocean color

The third primary production algorithm round robin (PPARR3) compares output from 24 models that estimate depth-integrated primary production from satellite measurements of ocean color, as well as seven general circulation models (GCMs) coupled with ecosystem or biogeochemical models. Here we compare the global primary production fields corresponding to eight months of 1998 and 1999 as estimated from common input fields of photosynthetically-available radiation (PAR), sea-surface temperature (SST), mixed-layer depth, and chlorophyll concentration. We also quantify the sensitivity of the ocean-color-based models to perturbations in their input variables. The pair-wise correlation between ocean-color models was used to cluster them into groups or related output, which reflect the regions and environmental conditions under which they respond differently. The groups do not follow model complexity with regards to wavelength or depth dependence, though they are related to the manner in which temperature is used to parameterize photosynthesis. Global average PP varies by a factor of two between models. The models diverged the most for the Southern Ocean, SST under 10 degrees C, and chlorophyll concentration exceeding 1 mg Chlm(-3). Based on the conditions under which the model results diverge most, we conclude that current ocean-color-based models are challenged by high-nutrient low-chlorophyll conditions, and extreme temperatures or chlorophyll concentrations. The GCM-based models predict comparable primary production to those based on ocean color: they estimate higher values in the Southern Ocean, at low SST, and in the equatorial band, while they estimate lower values in eutrophic regions (probably because the area of high chlorophyll concentrations is smaller in the GCMs). Further progress in primary production modeling requires improved understanding of the effect of temperature on photosynthesis and better parameterization of the maximum photosynthetic rate. (c) 2006 Elsevier Ltd. All rights reserved.

Characteristics of Yersinia pseudotuberculosis isolated from animals in Brazil

Strains (105) of Yersinia pseudotuberculosis isolated in Brazil between 1982 and 1990 mere bio-serotyped. They were also studied for plasmid profile, autoagglutination and calcium dependence at 37 degrees C, Congo red uptake, pyrazinamidase activity, esculin hydrolysis, salicin fermentation and drug sensitivity: 95.24% were biotype 2, serogroup O:3; 2.86% were biotype 1, serogroup O:1; and 1.90% were biotype 2, non-agglutinable. Plasmids were found in 77.14% of the strains (one in each strain). There was total correlation between the presence of the virulence plasmid and autoagglutination, calcium dependence at 37 degrees C and Congo red uptake. The esculin, salicin and pyrazinamidase tests were not efficient in differentiating pathogenic from non-pathogenic Y, pseudotuberculosis isolates. All strains were highly sensitive to the drugs used. These results indicate that Y. pseudotuberculosis is a potential pathogen for humans in Brazil, especially because the bio-serogroups detected among animals are those most frequently associated with human diseases.

Natural Products from Garcinia brasiliensis as Leishmania Protease Inhibitors

The infections by protozoans of the genus Leishmania are a major worldwide health problem, with high endemicity in developing countries. The drugs of choice for the treatment of leishmaniasis are the pentavalent antimonials, which cause renal and cardiac toxicity. As part of a search for new drugs against leishmaniasis, we evaluated the in vitro Leishmania protease inhibition activity of extracts (hexanic, ethyl-acetate, and ethanolic) and fukugetin, a bioflavonoid purified from the ethyl-acetate extract of the pericarp of the fruit of Garcinia brasiliensis, a tree native to Brazilian forests. The isolated compound was characterized by using spectral analyses with nuclear magnetic resonance, mass spectroscopy, ultraviolet, and infrared techniques. The ethyl-acetate extract and the compound fukugetin showed significant activity as inhibitors of Leishmania's proteases, with mean (+/- SD) IC(50) (50% inhibition concentration of protease activity) values of 15.0 +/- 1.3 mu g/mL and 3.2 +/- 0.5 mu M/mL, respectively, characterizing a bioguided assay. In addition, this isolated compound showed no activity against promastigote and amastigote forms of L. (L.) amazonensis and mammalian cells. These results suggest that fukugetin is a potent protease inhibitor of L. (L.) amazonensis and does not cause toxicity in mammalian or Leishmania cells in vitro. This study provides new perspectives on the development of novel drugs that have leishmanicidal activity obtained from natural products and that target the parasite's proteases.

Exports of non-fuel primary products

Includes bibliography

Carcass and meat traits of lambs fed by-products from the processing of oil seeds

We evaluated the effect of adding by-products from the processing of oil seeds in the diet of lambs on the carcass and meat traits. Twenty-four non-castrated weaned male Santa Inês lambs with approximately 70 days of age and initial average weight of 19.11 ± 2.12 kg were distributed into a completely randomized design. Treatments consisted of diets containing by-products with 70% of concentrate and 30% of tifton hay (Cynodon spp.) and were termed SM: control with soybean meal; SC: formulated with soybean cake; SUC: formulated with sunflower cake and PC: formulated with peanut cake. Diets had no effects on the carcass traits evaluated. There was no significant effect on the mean values of perirenal, omental and mesenteric fats (0.267, 0.552 and 0.470 kg, respectively) and there was no influence on the percentages of moisture, ether extract, crude protein or ash in the loin between experimental diets. Diets containing by-products from the processing of oil seeds did not change fatty acids found in lamb meat. The use of by-products from oil seeds provided similar carcass and meat traits, thus their use can be recommended as eventual protein and energy sources for feedlot lambs.

Natural Products from Cyanobacteria with Antimicrobial and Antitumor Activity

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Nitric Oxide and Nitroxyl Products from the Reaction of L-Cysteine with trans-[RuNO(NH3)(4)P(OEt)(3)](PF6)(3)

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Characteristics of Yersinia pseudotuberculosis isolated from animals in Brazil

Strains (105) of Yersinia pseudotuberculosis isolated in Brazil between 1982 and 1990 were bio-serotyped. They were also studied for plasmid profile, autoagglutination and calcium dependence at 37 degrees C, Congo red uptake, pyrazinamidase activity, esculin hydrolysis, salicin fermentation and drug sensitivity: 95.24% were biotype 2, serogroup O:3; 2.86% were biotype 1, serogroup O:1; and 1.90% were biotype 2, non-agglutinable. Plasmids were found in 77.14% of the strains (one in each strain). There was total correlation between the presence of the virulence plasmid and autoagglutination, calcium dependence at 37 degrees C and Congo red uptake. The esculin, salicin and pyrazinamidase tests were not efficient in differentiating pathogenic from non-pathogenic Y. pseudotuberculosis isolates. All strains were highly sensitive to the drugs used. These results indicate that Y. pseudotuberculosis is a potential pathogen for humans in Brazil, especially because the bio-serogroups detected among animals are those most frequently associated with human diseases.

Restructured products from tilapia industry by products: the effects of tapioca starch and washing cycles

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Determination of flagellar types by PCR-RFLP analysis of enteropathogenic Escherichia coli (EPEC) and Shiga toxin-producing E. coli (STEC) strains isolated from animals in Sao Paulo, Brazil

This study evaluated the polymerase chain reaction- restriction fragment length polymorphism (PCR-RFLP) analysis of fliC for typing flagella antigen (H) of Shiga toxin-producing Escherichia coil (STEC) and enteropathogenic E. coli (EPEC) strains isolated from different animals. The molecular typing of the H type was efficient in the determination of 93 (85%) strains. Two nonmotile (H-) E. coil strains showed a PCR-RFLP electrophoretic profile that did not match known H type patterns. The fliC nucleotide sequence of strains B2N and 4a revealed a nucleotide substitution at the restriction site and a nucleotide insertion that generated a stop codon, respectively. The results of this study showed that PCR-RFLP analysis of fliC is faster, less laborious and as efficient for the determination of H type E. coli isolated from animals, compared to serotyping and that it is useful in determining H type in nonmotile strains and strains expressing non-reactive H antigens. Moreover, the fliC sequence of strain B2N suggests that we could have found a new flagellin antigen type. (C) 2010 Elsevier Ltd. All rights reserved.

Aniline-1,4-benzoquinone as a model system for the characterization of products from aniline oligomerization in low acidic media

Increase in the pH medium of aniline polymerization is used for giving products of different morphologies, which are often wrongly attributed to PANI chains. Infrared and Raman spectroscopic data, supported by quantum chemical calculations, show that aniline-1,4-benzoquinone (AnBzq) is a model system for the characterization of the products of aniline oligomerization in low acidic media. The Raman spectra excited at different laser lines reveal the bichromophoric nature of AnBzq, whose absorption bands at 550 nm and 440 nm can be attributed to pi-pi* transitions of the delocalized benzoquinone and amino-phenyl moieties, respectively. (C) 2012 Elsevier B.V. All rights reserved.