ABSTRACT
Nitro-fatty acids are formed and detected in human plasma, cell membranes, and tissue, modulating metabolic as well as inflammatory signaling pathways. Here we discuss the mechanisms of nitro-fatty acid formation as well as their key chemical and biochemical properties. The electrophilic properties of nitro-fatty acids to activate anti-inflammatory signaling pathways are discussed in detail. A critical issue is the influence of nitroarachidonic acid on prostaglandin endoperoxide H synthases, redirecting arachidonic acid metabolism and signaling. We also analyze in vivo data supporting nitro-fatty acids as promising pharmacological tools to prevent inflammatory diseases.
Subject(s)
Humans , Anti-Inflammatory Agents/metabolism , Arachidonic Acid/metabolism , Fatty Acids/biosynthesis , Nitric Oxide/metabolism , Nitro Compounds/metabolism , Signal Transduction/physiology , Anti-Inflammatory Agents/chemistry , Fatty Acids/chemistry , Heme Oxygenase-1/metabolism , NADPH Oxidases/metabolism , /metabolism , NF-kappa B/metabolism , Nitro Compounds/chemistry , Peroxisome Proliferator-Activated Receptors/metabolism , Prostaglandin-Endoperoxide Synthases/metabolismABSTRACT
O bicho-mineiro Leucoptera coffeella (Guérin-Mèneville), uma das pragas mais importantes da cafeicultura brasileira, é controlado principalmente com inseticidas. O objetivo deste trabalho foi estudar os resíduos e a translocação do inseticida tiametoxam em folhas de cafeeiros, bem como avaliar seu efeito no controle do bicho-mineiro, comparando-o com o aldicarbe, utilizado como padrão. Para isto, foi instalado um experimento no município de Garça, SP, no período de dezembro/2001 a agosto/2002. Os tratamentos utilizados foram: aldicarbe 150 G, nas doses de 2,25 e 4,50 g i.a./cova, tiametoxam 10 GR, nas doses de 0,15 e 0,30 g i.a./cova e testemunha (sem aplicação). Amostras de ramos foram colhidas em pré-contagem e aos 30, 60, 90, 120, 150, 180, 210 e 240 dias após a aplicação, em três alturas dos cafeeiros (terços inferior, médio e superior), avaliando-se a porcentagem de folhas minadas. As determinações de aldicarbe e seus metabólitos ativos, aldicarbe sulfoxido e sulfona, e os de tiametoxam foram feitas por cromatografia em fase gasosa usando-se detector de nitrogênio-fósforo e de espectrometria de massas, respectivamente. Os resultados indicaram translocação uniforme de ambos inseticidas nos três terços das plantas de café, quando aplicados no solo. Foi constatada também, a maior persistência do tiametoxam, cujos resíduos foram encontrados até oito meses após a aplicação, enquanto os metabólitos sulfóxido e sulfona foram encontrados entre quatro e seis meses após a aplicação. Foi observado controle do bicho-mineiro pela aplicação de ambos inseticidas.
Subject(s)
Animals , Aldicarb/metabolism , Coffea/drug effects , Insecticides/metabolism , Lepidoptera/drug effects , Nitro Compounds/metabolism , Oxazines/metabolism , Pest Control, Biological/methods , Plant Leaves/metabolism , Thiazoles/metabolism , Nitro Compounds/pharmacology , Oxazines/pharmacology , Thiazoles/pharmacologyABSTRACT
Nitrobenzylthioinosine [NBRT] an equilibrative nucleoside transporter inhibitor, was anabolized to its nucleotides following incubation with human erythrocytes, fresh and cultured leukemic cells. Concentration of NBMPR and its nucleotides in acute myelogenus leukemic [AML] cells were significantly higher than those in chronic lymphocytic [CLL] and chronic myelogenous [CML] leukemic cells. However, no significant correlation was found between concentration of cellular NBMPR and its nucleotides. In contrast to lymphocytes, human erythrocytes anabolized NBMPR only to NBMPR-monophosphate but no di- or triphosphate NBMPR was found following incubation of NBMPR with human erythrocytes. Phosphorylation of NBMPR in lymphocytes was almost completely inhibited in the presence of 10 micro M of adenosine kinase inhibitor, 5-iodotubercidin, indicating that anabolism of NBMPR was cayalyzed by adenosine kinase. NBMPR was stable up to 86% in plasma following in vitro incubation with whole blood obtained from leukemic patients. 6-thioinosine was the only significant metabolite of NBMPR in plasma [8% of total radioactive dose]. NBMPR was stable following overnight incubation with human purine nucleoside phosphorylase. No incorporation of NBMPR and/or its metabolites in nucleic acids was observed following overnight incubation of [3H]- NBMPR with fresh leukemic lymphocytes