Quinoline-based compounds as modulators of HIV transcription through NF-kappaB and Sp1 inhibition.

18 quinoline-based compounds were tested for antiviral properties against human immunodeficiency syndrome (HIV). The compounds tested here contain quinoline or tetrahydroquinoline rings and can be divided into two main groups: group 1 includes 4-(2-oxopyrrolidinyl-1)-1,2,3,4-tetrahydroquinolines with 2-(3-nitrophenyl) substituent (N-series) or 2-(3-aminophenyl) moiety (H-series), and group 2 includes 2-(3-nitrophenyl)- or 2-(3-aminophenyl)-substituted quinolines (S-series). Two different antiviral assays were performed in order to test the anti-HIV activity of compounds: 3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) and recombinant virus assay (RVA). Results showed that the most active compounds were 2-aryl quinolines, particularly those containing methoxy substituents or no substituents in the quinoline skeleton. HIV transcription inhibition appears to be their target in both resting and phorbol myristate acetate (PMA) activated primary lymphocytes, and nuclear factor-kappaB (NF-kappaB) and specificity protein-1 (SP1) seems to be the most important transcription factors involved in their action.

Efecto antioxidante de frutas y hortalizas de la zona central de Chile / Antioxidant effect of fruits and vegetables of central region of Chile

Las especies reactivas del oxígeno (ERO) causan daño celular que se puede expresar como patología, tales como las enfermedades cardiovasculares (ECV) y otras enfermedades crónicas no transmisibles. El organismo humano cuenta con sistemas antioxidantes; algunos provienen de la dieta, especialmente de frutas y hortalizas, otros los genera el mismo organismo de manera endógena. El objetivo de este estudio fue conocer la capacidad antioxidante in vitro de algunas frutas y hortalizas que se consumen en la Región del Maule de Chile. Las once especies de frutas y 16 de hortalizas empleadas en el estudio fueron adquiridas en el Centro Regional de Abastecimiento de Talca, en época de cosecha; a partir de ellas se obtuvo extractos acuosos y metanólicos. La actividad antioxidante se determinó mediante decoloración del radical violeta 2,2-difenil-I-picril hidrazilo hidratado (DPPH). En general la actividad antioxidante, en extractos metanólicos, fue mayor en frutas (70,3 por ciento; 87,7-54,3 por ciento de decoloración) que en hortalizas (54,7 por ciento; 44,3-79,7 por ciento) (p < 0.003) y dependiente de la concentración del extracto evaluado. En los ensayos a 1000 f < g/m, la mayoría de las frutas mostraron un porcentaje de decoloración superior al 60 por ciento y las que presentaron mayor actividad antioxidante fueron frambuesa, frutilla y kiwi. Entre las hortalizas, las que presentaron mayor actividad antioxidante, fueron los tomates seguidos por pepino dulce, betarraga, melón tuna, pimentón y sandía. La actividad antioxidante observada en la mayoría de las frutas y hortalizas evaluadas podría ser un argumento científico a dar a conocer en las campañas de promoción del consumo interno y en la exportación de productos hortofrutícolas.

The reactive oxygen species (ERO) cause cell damage that can be expressed as a disease, including cardiovascular disease (CVD) and other non transmissible chronic diseases. The human body has antioxidant systems, some come from the diet, especially fruits and vegetables, and others are generated by the same organism as an endogenous way. The aim of this study was to determine the in vitro antioxidant capacity of some fruits and vegetables that are consumed in the Maule Region, Chile. Eleven species of fruits and 16 of vegetables used in the study were obtained at the Regional Center of Fruits and Vegetables of Talca during the harvest season, and different aqueous and methanol extract were obtained. The antioxidant activity was determined by purple discoloration of the radical 2,2-diphenyl-1-picryl hidrazilo hydrated (DPPH). In general the antioxidant activity was slightly higher in fruits (70,3 percent; 87,7-54,3 percent) than in vegetables (54,7 percent; 44,3-79,7 percent) (p < 0.003) and it was dependent on the concentration of the extract. In the tests at 1000 ug/m, most fruits showed a higher percentage of discoloration over to 60 percent; those that showed higher antioxidant activity were raspberry, strawberry and kiwi. Among vegetables, those showing higher antioxidant activity were tomato, followed by melon pear, red beet, melon (type tuna), sweet pepper and watermelon. The antioxidant activity observed in most fruits and vegetables could be assessed as a scientific argument to make known in promotional campaigns in national consumption and the horticultural products exports.