Antileishmanial action of organometallic complexes of Pt(II) and Rh(I)

The three organometallic complexes [(Cis-PtII (DDH) (2,5-Dihidroxibenzensulfonic)2, RhI (CO)2 Cl(2-Aminobenzothiazole) and RhI (CO)2 Cl(5-Cl-2-Methilbenzothiazole) used in this study had been previously found to have a high in vitro activity against promastigote and amastigote like forms of Leishmania donovani. Here, the cytotoxic effect of these new organometallic complexes on the J-774 macrophages were studied. Only the RhI(CO)2 Cl(2-Aminobenzothiazole) complex induced substantial toxicity in the cells. Also, we assayed the effect of this complex on the parasite's biosynthesis of macromolecules. The RhI(CO)2 Cl (5-Cl-2-Methylbenzothiazole) complex inhibitied DNA, RNA, and protein synthesis. On the other hand, the two other compounds tested did not inhibit the incorporation of radioactive precursors. Finally important ultrastructural alterations in the parasites treated with the two non-cytotoxic complexes were observed.

Superoxide dismutase from Trichuris ovis, inhibiton by benzimidazoles and pyrimidine derivatives

Three superoxide dismutase isoenzymes of different cellular location were detected in an homogenate of Thrichuris ovis. Each of these molecular forms was purified by differential centrifugation and precipitation with ammonium sulphate, followed by chromatography on DEAE-cellulose and Sephadex G-75 columns. The activity levels of the two molecular forms detected in the mitochondrial (one cyanide sensitive Cu-Zn-SOD and the other cyanide intensitive Mn-Sod were higher than that of the superoxide dismutase detected in the cytoplasmic fraction (cyanid sensitive Cu-Zn-SOD). All the mollecular forms present evident differences to the SODs contained in the host liver. Molecular mass and some of the physical and chemical aproperties of the enzyme was determined for all three molecular forms. An inhibitory effect on the SOD of the parasite an the host was detected with a series of compounds, some of wich markedly inhibited parasite ensyme but not host enzyme

Estudio ultraestructural de la accion de dos derivados benzo (de) isoquinolil-1,3-diona sobre Trypanosoma cruzi "in vitro". / Ultrastructural study of the effect of 2 derivatives benzo (de) isoquinoline-1,3-dione on Trypanosoma cruzi in vitro

Fueron analizadas las alteraciones a nivel ultraestructural, producidas por dos derivados benzo (de) isoquinolil-1,3-dioma, en formas de cultivo de Trypanosoma cruzi.Estos compuestos, M-12210 y FA-142, son drogas intercalantes del DNA que tienen una gran afinidad por este. El DNA del kinetoplasto pierde su estructura regular de doble hilera, produciendose arqueamientos la cromatina aparece irregularmente condensada en los nucleos, en el citoplasma se observa gran cantidad de inclusiones lipidicas y vacuolas

In vitro action of three benzo (de) isoquinoline-1,3-dione derivatives against Trypanosoma cruzi

Investigou-se a acao "in vitro" contra Trypanosoma cruzi, forma epimastigota, de tres derivados benzo (de) isoquinolina 1,3 dionas, (5 nitro-2-(2 dimetilaminoetil); 5-nitro 2-(2-(1 pirrolidina) etil) e 5 amino-2-(2-dimetilaminoetil)). Os resultados obtidos neste trabalho, mostram que os tres compostos inibem o crescimento normal da forma de cultura de Trypanosoma cruzi