In Vivo Bio-Distribution Study of 64Cu (II)-Labelled Copper (II) Complexes of Peptides Mimics in Balb/C Mice-Development of Copper Based Anti-Inflammatory Agents

Abstract

Bio-distribution of 64Cu-labelled copper(II) complexes of N,N'-di(aminoethylene)-2,6-pyridinedicarbonylamine, Bis-(N,N-dimethylethyl)-2,6-pyridinedicarboxamide and N,N'-bis[2(2-pyridyl)-methyl]pyridine-2,6-pyridinedicarboxamide was determined using Balb/c mice. Radio labelled copper (II) complexes of peptides mimics were injected in animals intravenously via tail vein and by applying on anterior dorsal side. After 1, 6 and 24 hour post-injection animals were sacrificed and organs or samples removed for measuring activity using gamma counter. Compounds accumulated in various parts of the body 1, 6 and 24 hour post administration. Intravenous and dermal absorption studies showed that these compounds have 50% retention in the body 24 hours after administration.

Aqueous Solution Equilibria and Spectral Features of Copper Complexes with Tripeptides Containing Glycine or Sarcosine and Leucine or Phenylalanine

“…The copper(II) binds to the amine, the amide and the imidazole of Asp-Ala-His in the C-terminus of the protein [19,20]. Using this sequence as a design template, Zvimba [5,18] and Odisitse [1,6,21,22] synthesized and tested a series of amide ligands. Zvimba [18] found that replacing an amine with an amide significantly reduced the in vivo copper(II) mobilizing ability of the ligand, but increased the lipophilicity of the complex.…”

“…Zvimba [18] found that replacing an amine with an amide significantly reduced the in vivo copper(II) mobilizing ability of the ligand, but increased the lipophilicity of the complex. On the other hand, in murine biodistribution studies, Odisitse [22] found significant trans-dermal absorption and retention of copper(II) using amide ligands with a terminal pyridine.…”