Publication in PLoS ONE

In this paper, we reported in vitro and in vivo anti-inflammatory activities of a series of copper(II)-lawsone complexes of the general composition [Cu(Law)2(LN)x(H2O)(2-x)yH2O; = 1-2, HLaw = 2-hydroxy-1,4-naphthoquinone, and LN = heterocyclic N-donor ligand. Some of the complexes showed the ability to suppress significantly the activation of nuclear factor κB (NF-κB) both by lipopolysaccharide and TNF-alpha at 100 nM level in the similar manner as the reference drug prednisone (at 1 µM level) and were also able to suppress the inflammatory response in vivo in hind-paw edema model on rats. The most active complexes 13 diminished the formation of edema similarly as the reference drug indomethacine. In addition, a strong intracellular pro-oxidative effect of all the complexes has been found in vitro. The overall effect of the complexes, dominantly 13, shows similarity to anti-inflammatory drug benoxaprofen, known to induce intracellular pro-oxidative effects.



Date: 25. jul 2017 | Author: agch

Department of Inorganic Chemistry

Faculty of Science
Palacký University in Olomouc

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