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        Natural Products from Garcinia brasiliensis as Leishmania Protease Inhibitors

        Ivan O. Pereira,Diego M. Assis,Maria A. Juliano,Rodrigo L.O.R. Cunha,Clara L. Barbieri,Luis V.S. do Sacramento,Marcos J. Marques,Marcelo H. dos Santos 한국식품영양과학회 2011 Journal of medicinal food Vol.14 No.6

        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) IC50 (50% inhibition concentration of protease activity) values of 15.0±1.3 μg/mL and 3.2±0.5 μM/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.

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        A laminated composite plate finite element a-priori corrected for locking

        João Elias Abdalla Filho,Ivan Moura Belo,Michele Schunemann Pereira 국제구조공학회 2008 Structural Engineering and Mechanics, An Int'l Jou Vol.28 No.5

        A four-node plate finite element for the analysis of laminated composites which is developed using strain gradient notation is presented. The element is based on a first-order shear deformation theory and on the equivalent lamina assumption. Strains and stresses can be calculated at different points through the thickness of the plate. They are averaged values due to the equivalent lamina assumption. A shear correction factor is used as the transverse shear strain is taken to be constant over the plate thickness while its actual variation is parabolic. Strain gradient notation, which is physically interpretable, allows for the detailed a-priori analysis of the finite element model. The polynomial expansions are inspected and spurious terms responsible for modeling errors are identified in the shear strains polynomial expansions. The element is corrected by simply removing the spurious terms from the shear strains expansions. The element is implemented into a FORTRAN finite element code in two versions; namely, with and without spurious terms. Results are compared to show the effects of the spurious terms on the solutions. It is also shown that a refined mesh composed of corrected elements provides solutions which approximate very well the analytical solutions, validating the procedure.

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