Registro Completo |
Biblioteca(s): |
Embrapa Pantanal. |
Data corrente: |
11/09/1997 |
Data da última atualização: |
10/09/2010 |
Autoria: |
LEON, L. L; CANTO-CAVALHEIRO, M.M.; TRAJANO-MENEZES, V.; SILVA, R. A. M. S.; D'AVILA, A. M. R.; ECHEVARRIA, A.; SANTOS, L. H. S.; GOMES CARDOSO, L.; JANSEN, A. M. |
Afiliação: |
FIOCRUZ. Departamento de Imunologia e Parasitologia (Rio de Janeiro, RJ); EMBRAPA. Centro de Pesquisa Agropecuaria do Pantanal (Corumba, MS); UFRRJ. Departamento de Quimica (Rio de Janeiro, RJ). |
Título: |
Synthetic amidines: a possible new therapeutic choice for the treatment of "Mal de cadeiras". |
Ano de publicação: |
1996 |
Fonte/Imprenta: |
Memorias do Instituto Oswaldo Cruz, Rio de Janeiro, v.91, p.107, 1996. Suplemento. |
Idioma: |
Inglês |
Conteúdo: |
Among all species of trypanosome, Trypanosoma evansi has the widest distribution and the greatest range of mammalian host. This parasite has been reported in Africa, Asia, the MiddleEast, South and Central America and parts of Europe. T. evansi is responsible for a devastating horse disease known as "Mal de cadeiras" in the Pantanal region, in the Mato Grosso state (the disease is known as surra in the Old World). It seems that the disease was introduced in South America during the XVIth century by Spanish settlers and in the Pantanal region in 1850 (Hoare, 1965; Santos & Sereno, 1992). However, no effective drug treatment was available until 1930 and since then, Berenyl have been used, although some resistant strain hab been noticed. "Mal de cadeiras" represent a very important economical problem and we decided to assay some new compounds which had shown to be active against other trypanosomatids (Leon et al., 1995; Canto-Cavalheiro et al., 1995). These new compounds belongs to the class of amidines: N, N'-diphenyl-4-R-benzamidine, where R=H, Br,Cl, CN, NO2, CH3 and OCH3 and the drug screening was performed in serial dilution triplicates from 160ug to 5ug solubilized in DMSO. T. evansi trypomastigotes were raised in immunosupressed (cyclophosphamide, 200mg/kg) rats injected with parasite stabilates. When rat developed infection they were bled and the parasites were separated from the blood cells by anion-exchange chromatography (DE-52). To assay the amidines, trypomastigotes (4X10 6/ml) were resuspended in phosphate saline glucose (PSG) and Schneider's medium (1:1) and incubated at 25oC. The drug activity was evaluated after 24h incubation by countings in Neubauer's chamber and the remaining parasites were inoculated in immunosupressed rats, in order to determine if there was a lost of the infective capacity. Our preliminary data showed that the most active compound were the metoxy and the methyl-derivate with LDs of 16 and 14uM, respectively. MenosAmong all species of trypanosome, Trypanosoma evansi has the widest distribution and the greatest range of mammalian host. This parasite has been reported in Africa, Asia, the MiddleEast, South and Central America and parts of Europe. T. evansi is responsible for a devastating horse disease known as "Mal de cadeiras" in the Pantanal region, in the Mato Grosso state (the disease is known as surra in the Old World). It seems that the disease was introduced in South America during the XVIth century by Spanish settlers and in the Pantanal region in 1850 (Hoare, 1965; Santos & Sereno, 1992). However, no effective drug treatment was available until 1930 and since then, Berenyl have been used, although some resistant strain hab been noticed. "Mal de cadeiras" represent a very important economical problem and we decided to assay some new compounds which had shown to be active against other trypanosomatids (Leon et al., 1995; Canto-Cavalheiro et al., 1995). These new compounds belongs to the class of amidines: N, N'-diphenyl-4-R-benzamidine, where R=H, Br,Cl, CN, NO2, CH3 and OCH3 and the drug screening was performed in serial dilution triplicates from 160ug to 5ug solubilized in DMSO. T. evansi trypomastigotes were raised in immunosupressed (cyclophosphamide, 200mg/kg) rats injected with parasite stabilates. When rat developed infection they were bled and the parasites were separated from the blood cells by anion-exchange chromatography (DE-52). To assay the amidines, trypomastigote... Mostrar Tudo |
Palavras-Chave: |
Mal de cadeiras. |
Thesaurus Nal: |
Brazil; Pantanal; Trypanosoma evansi. |
Categoria do assunto: |
-- |
Marc: |
LEADER 02761naa a2200265 a 4500 001 1791634 005 2010-09-10 008 1996 bl uuuu u00u1 u #d 100 1 $aLEON, L. L 245 $aSynthetic amidines$ba possible new therapeutic choice for the treatment of "Mal de cadeiras". 260 $c1996 520 $aAmong all species of trypanosome, Trypanosoma evansi has the widest distribution and the greatest range of mammalian host. This parasite has been reported in Africa, Asia, the MiddleEast, South and Central America and parts of Europe. T. evansi is responsible for a devastating horse disease known as "Mal de cadeiras" in the Pantanal region, in the Mato Grosso state (the disease is known as surra in the Old World). It seems that the disease was introduced in South America during the XVIth century by Spanish settlers and in the Pantanal region in 1850 (Hoare, 1965; Santos & Sereno, 1992). However, no effective drug treatment was available until 1930 and since then, Berenyl have been used, although some resistant strain hab been noticed. "Mal de cadeiras" represent a very important economical problem and we decided to assay some new compounds which had shown to be active against other trypanosomatids (Leon et al., 1995; Canto-Cavalheiro et al., 1995). These new compounds belongs to the class of amidines: N, N'-diphenyl-4-R-benzamidine, where R=H, Br,Cl, CN, NO2, CH3 and OCH3 and the drug screening was performed in serial dilution triplicates from 160ug to 5ug solubilized in DMSO. T. evansi trypomastigotes were raised in immunosupressed (cyclophosphamide, 200mg/kg) rats injected with parasite stabilates. When rat developed infection they were bled and the parasites were separated from the blood cells by anion-exchange chromatography (DE-52). To assay the amidines, trypomastigotes (4X10 6/ml) were resuspended in phosphate saline glucose (PSG) and Schneider's medium (1:1) and incubated at 25oC. The drug activity was evaluated after 24h incubation by countings in Neubauer's chamber and the remaining parasites were inoculated in immunosupressed rats, in order to determine if there was a lost of the infective capacity. Our preliminary data showed that the most active compound were the metoxy and the methyl-derivate with LDs of 16 and 14uM, respectively. 650 $aBrazil 650 $aPantanal 650 $aTrypanosoma evansi 653 $aMal de cadeiras 700 1 $aCANTO-CAVALHEIRO, M.M. 700 1 $aTRAJANO-MENEZES, V. 700 1 $aSILVA, R. A. M. S. 700 1 $aD'AVILA, A. M. R. 700 1 $aECHEVARRIA, A. 700 1 $aSANTOS, L. H. S. 700 1 $aGOMES CARDOSO, L. 700 1 $aJANSEN, A. M. 773 $tMemorias do Instituto Oswaldo Cruz, Rio de Janeiro$gv.91, p.107, 1996. Suplemento.
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Registro original: |
Embrapa Pantanal (CPAP) |
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