In vitro and in vivo studies of N,N '-bis[2(2-pyridyl)-methyl]pyridine-2, 6-dicarboxamide-copper(II) and rheumatoid arthritis

Journal article

Authors / Editors

Odisitse, Sebusi

Research Areas

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Publication Details

Author list: Odisitse S, Jackson GE

Publisher: Elsevier

Place: OXFORD

Publication year: 2008

Journal: Polyhedron (0277-5387)

Journal acronym: POLYHEDRON

Volume number: 27

Issue number: 1

Start page: 453

End page: 464

Number of pages: 12

ISSN: 0277-5387

Languages: English-Great Britain (EN-GB)

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Abstract

The thermodynamic equilibria of copper(II), zinc(II) and calcium(II) with N,N '-bis[2(2-pyridyl)-methyl]pyridine-2,6-dicarboxamide (L1) have been studied at 25 degrees C and anionic strength of 0.15 mol dm(-3). Spectroscopic studies suggest metal ion complexation promotes deprotonation and coordination of the amide nitrogens resulting in overall tetragonal coordination of Cu2+. Blood-plasma modelling predicts that Cu(II) competes effectively against Zn(II) and Ca(II) for L1 in vivo. Octanol-water partition coefficient studies show that Cu(II)-L1 complexes are reasonably lipophilic. However, the CuL1H(-2) species which predominates at the physiological pH of 7.4 has poor superoxide dismutase activity. Bio-distribution experiments showed activity accumulation and retention in the body of about 50% of the injected dose for the [Cu-64]Cu(II)-L1 complex after 24 h. (C) 2007 Elsevier Ltd. All rights reserved.

Keywords

bio-distribution, potentiometry, spectroscopic, Thermodynamic

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