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Reis D.C.,Federal University of Minas Gerais | Pinto M.C.X.,Federal University of Minas Gerais | Souza-Fagundes E.M.,Federal University of Minas Gerais | Wardell S.M.S.V.,Institute Tecnologia em Farmacos | And 2 more authors.
European Journal of Medicinal Chemistry | Year: 2010

The antimony(III) complexes [Sb(2Bz4DH)Cl 2] (1), [Sb(H2Bz4M)Cl 3]·2H 2O (2) and [Sb(2Bz4Ph)Cl 2] (3) were obtained with 2-benzoylpyridine thiosemicarbazone (H2Bz4DH) and its N(4)-methyl (H2Bz4M) and N(4)-phenyl (H2Bz4Ph) derivatives. H2Bz4DH, H2Bz4Ph and complexes (1-3) exhibited high cytotoxic activity against HL-60 and Jurkat human leukemia cell lines. When these compounds were tested against HL-60 cells with ectopic expression of BcrAbl, Bcl-2 or Bcl-X L, which confer resistance to apoptosis against a variety of death-inducing agents, the cytotoxicity was much lower, indicating apoptosis to be part of their mechanism of action. The cytotoxic activity of complexes 2 and 3 against HL-60 and Jurkat cells was significantly higher than that of the corresponding thiosemicarbazones, suggesting coordination to be an interesting strategy of cytotoxic dose reduction. [Sb(2Bz4DH)Cl 2] (1), [Sb(H2Bz4M)Cl 3] (2) and [Sb(2Bz4Ph)Cl 2] (3) were obtained with 2-benzoylpyridine thiosemicarbazone (H2Bz4DH) and its N(4)-methyl (H2Bz4M) and N(4)-phenyl (H2Bz4Ph) derivatives. H2Bz4DH, H2Bz4Ph and 1-3 were highly cytotoxic to leukemia cells. © 2010 Elsevier Masson SAS. All rights reserved. Source


Soares D.C.,Federal University of Rio de Janeiro | Portella N.A.,Federal University of Rio de Janeiro | Ramos M.F.D.S.,Federal University of Rio de Janeiro | Siani A.C.,Institute Tecnologia em Farmacos | Saraiva E.M.,Federal University of Rio de Janeiro
Evidence-based Complementary and Alternative Medicine | Year: 2013

This study investigated the leishmanicidal activity against Leishmania amazonensis of four commercial oils from Copaifera spp. named as C1, C2, C3, and C4, the sesquiterpene and diterpene pools obtained from distilling C4, and isolated β-caryophyllene (CAR). Copaiba oils chemical compositions were analyzed by gas chromatography and correlated with biological activities. Diterpenes-rich oils C2 and C3 showed antipromastigote activity. Sesquiterpenes-rich C1 and C4, and isolated CAR presented a dose-dependent activity against intracellular amastigotes, with ICof 2.9 μg/mL, 2.3 μg/mL, and 1.3 μg/mL (6.4 μM), respectively. Based on the highest antiamastigote activity and the low toxicity to the host cells, C4 was steamdistillated to separate pools of sesquiterpenes and diterpenes. Both pools were less active against L. amazonensis and more toxic for the macrophages than the whole C4 oil. The leishmanicidal activity of C3 and C4 oils, as well as C4 fractions and CAR, appears to be independent of nitric oxide production by macrophages. This study pointed out β-caryophyllene as an effective antileishmanial compound and also to its role as potential chemical marker in copaiba oils or fractions derived thereof, aiming further development of this rainforest raw material for leishmaniasis therapy. © 2013 Deivid C. Soares et al. Source


Cipriani F.A.,Federal University of Rio de Janeiro | Figueiredo M.R.,Institute Tecnologia em Farmacos | Soares G.L.G.,Federal University of Rio Grande do Sul | Kaplan M.A.C.,Federal University of Rio de Janeiro
Quimica Nova | Year: 2012

Our solemn homage to the great Master Otto R. Gottlieb who knew how to teach the mystery of evolutionary relationships between chemistry and its natural sources. The micromolecular chemical study of the family Bignoniaceae shows a profile predominantly characterized by the occurrence of metabolites derived from acetic acid biosynthetic pathways such as terpenoids, quinones, flavonoids and special aromatic derivatives. Analysis of different chemosystematic parameters for the metabolite data collected, provided valuable information for the systematic characterization of the Bignoniaceae family within the Angiosperm derived taxa. Source


Figueiredo T.A.,Institute Tecnologia em Farmacos | De Andrade Schramm J.M.,Escola Nacional de Saude Publica Sergio Arouca | Pepe V.L.E.,Escola Nacional de Saude Publica Sergio Arouca
Cadernos de Saude Publica | Year: 2014

The World Health Organization (WHO) defines essential medicines as those that meet the population’s priority healthcare needs. Their selection aims to reflect collective needs, thus recommending the use of studies on global burden of disease. An exploratory study was performed to link the medicines from the RENAME lists to Global Burden of Disease in Brazil (1998 and 2008) and the scientific evidence. The study thus sought to verify whether the RENAME (2002 to 2012) met WHO guidelines for drug selection. Although RENAME 2010 and 2012 both adhere to Global Burden of Disease in Brazil 2008, the 2012 version includes a longer list of medicines and appears to be pressured by the growing market for new technologies. Thus, RENAME is no longer a list of essential medicines, but has become a list of financing for pharmaceutical care. Source


Moulton T.P.,State University of Rio de Janeiro | Magalhaes-Fraga S.A.P.,Institute Tecnologia em Farmacos | Brito E.F.,State University of Rio de Janeiro | Barbosa F.A.,Federal University of Minas Gerais
Hydrobiologia | Year: 2010

Coarse particulate organic matter is often broken down by specialist shredder invertebrates in temperate streams. In some tropical streams, larger, non-specialist, omnivorous fauna, (macroconsumers), particularly decapod shrimps and crabs, have been found to process coarse particulate matter. Larger shrimps and fish may also prey on or inhibit smaller invertebrates. Depending on the relative importance of larger and smaller fauna in leaf processing and in predatory interactions, we could expect that exclusion of larger fauna could either result in a decrease in leaf processing (if they were important in shredding or bioturbation) or increase in leaf processing if they negatively affected smaller shredders. We tested this by excluding fauna of different sizes from leaf peaks using bags with different sizes of mesh -0.2 mm (exclusion of most fauna), 2 mm (exclusion of larger fauna), and 10 mm (access to most fauna). Bag effect on leaf processing was minimized by constructing the bags of the same, fine, material, and sewing a relatively small window of the required mesh size. The experiment was conducted on two occasions in three streams of the urban forest of Parque Estadual da Pedra Branca, city of Rio de Janeiro. The three streams differed in larger fauna of shrimps (Macrobrachium potiuna), crabs, tadpoles, and fish. Packs were incubated for six time intervals and the rate of leaf processing calculated as the exponential rate of loss of leaf material. Rate of leaf processing was faster in bags with the largest mesh size; the rates in the other two mesh sizes were not statistically different. Rates varied between experiments and among streams. We could not attribute the faster leaf processing to any particular component of the larger fauna; the patterns of differences among streams and between experiments were not associated with particular taxa. There was no general trend of fewer smaller fauna in the presence of macroconsumers; the few smaller taxa that were different between mesh sizes were variously less and more abundant in the 10-mm mesh bags compared to the 2-mm. Known shredders were rare in the smaller fauna; the mining chironomid Stenochironomus was common, but was apparently not affected by larger fauna and apparently did not increase leaf processing. We conclude that macroconsumers and not smaller fauna had a positive effect on leaf processing, and this confirms a pattern observed in some other coastal Neotropical streams. © Springer Science+Business Media B.V. 2009. Source

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