Abstract

Studies using cell-free systems have shown that chelation of ferrous iron by rutin and formation of the complex (Rt – Fe) resulted in the appearance of site-specific pseudo-peroxidase activity against hydrogen peroxide, but does not affect the ligand’s ability to interact with peroxynitrite. Anti-inflammatory properties of rutin (Rt) and its complex with ferrous iron were studied in vitro under conditions of bacterial lipopolysaccharide (LPS)-induced inflammation in endothelial cells of the human umbilical vein (HUVEC). The Rt – Fe complex at a dose of 50 µmol/L was found to significantly reduce the level of LPS-induced mRNA expression of inflammatory mediators IL-6, IL-1B, IL-8, MCP1 and COX-2 and the level of secretion of IL-6 and IL-8 in the culture medium, while Rt under the same concentration was ineffective. Experiments performed in vivo indicate that prior administration of the Rt – Fe complex in a dose of 12.5 µmol/kg dramatically eliminated LPS-induced pyrogenic reaction of in Wistar rats. From the above data, it can be concluded that complexation with bivalent iron enhances of antioxidant properties of Rt, leads to appearance of anti-inflammatory activity and expands the area of its possible pharmacological use.

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