In this study, we developed a novel method of PPAR gamma ligand screening by measuring the increase in fluorescent polarization accompanied by the interaction of a fluorescent co-activator and PPAR gamma. Sterol receptor co-activator-1 (SRC-1), a major PPAR gamma co-activator, was probed

by fluorescent TAMRA by the Amber codon fluorescence. probe method. Polarization was increased by adding PPAR gamma ligands to a solution containing labeled SRC-1 (designated TAMRA-SRC-S) and PPAR gamma. The disassociation constants (Kd) of the PPAR gamma synthesized ligands, pioglitazone (221 nm), troglitazone (83.0 nm), and 15-deoxy-Delta 12,14-prostaglandin J(2) (15d-Delta PGJ(2)) (156 nm), were determined by this method. Farnesol (2.89 mu m) and bixin (21.1 mu m), which we have reported to be PPAR gamma ligands, increased the fluorescent HDAC inhibition polarization. Their Kd values were in agreement with the ED(50) values obtained in the luciferase assay. The results

indicate that the method is valuable for screening natural PPAR gamma ligands.”
“Human cysticercosis by Taenia crassiceps is rare although it is considered of zoonotic risk, especially to immunocompromised individuals. Albendazole and praziquantel are widely used and effective in its treatment. Their active forms inhibit the glucose uptake by the parasite and induce muscle contractions that alter its glycogen levels interfering in the energetic metabolism of the parasite and leading to its death. The aim of this study

was to evaluate 4EGI-1 alterations in glycolysis, the tricarboxylic acid cycle and glucose concentrations caused by low dosage treatments of the hosts with albendazole and praziquantel. Therefore, T. crassiceps intraperitoneally infected mice were treated by gavage feeding with 5.75 or 11.5 mg/kg of albendazole Selleckchem SCH727965 and 3.83 or 7.67 mg/kg of praziquantel. The treated mice were euthanized after 24 h and the cysticerci collected were morphologically classified into initial, larval or final phases. Concentrations of the organic acid produced and glucose were evaluated to detect alterations into the glycolysis and the tricarboxylic acid cycle pathways through chromatography and spectrophotometry. The low dosage treatment caused a partial blockage of the glucose uptake by the cysticerci in spite of the non significant difference between its concentrations. An activation of the tricarboxylic acid cycle was noted in the cysticerci that received the treatment due to an increase in the production of citrate, malate and alpha-ketoglutarate and the consumption of oxaloacetate, succinate and fumarate. The detection of alpha-ketoglutarate indicates that the cysticerci which were exposed to the drugs after host treatment present different metabolic pathways than the ones previously described after in vitro treatment. (C) 2011 Elsevier Inc. All rights reserved.