In vitro and in vivo assessment of the antioxidant potential of isoxazole derivatives

Abstract

AbstractPreviously developed fluorophenyl-isoxazole-carboxamides derivatives were re-synthesized and their scavenging activity against DPPH free radical and inhibitory activity against lipase and α-amylase enzymes were evaluated. The inhibition of the tested enzymes was weak while the most potent activities were observed in the DPPH assay. In particular, compounds2aand2cdemonstrated high antioxidant potency with IC50values of 0.45 ± 0.21 and 0.47 ± 0.33 µg/ml, respectively, when compared to Trolox, the positive control compound, which has an IC50value of 3.10 ± 0.92 µg/ml. Based on the in vitro results, the most potent compound2awas chosen for in vivo evaluation of antioxidant properties using 20 male mice injected intra-peritoneally and divided into four groups. The in vivo results revealed that total antioxidant capacity (TAC) obtained for mice treated with2awas two folds greater than that of mice treated with the positive control Quercetin. Although further biological and preclinical investigations need to be performed to assess the therapeutic potential of2a, the results of this study show promising antioxidant activities both in vitro and in vivo.