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Biodistribution (as determined by the radiolabelled equivalent) of a gold(III) bis(pyrrolide‐imine) Schiff base complex: a potential chemotherapeutic
Author(s) -
Akerman Matthew P.,
Munro Orde Q.,
Mongane Modisenyane,
Staden Johan A.,
Rae William I. D.,
Bester Cornelius J.,
MarjanovicPainter Biljana,
Szucs Zoltan,
Zeevaart Jan Rijn
Publication year - 2013
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3068
Subject(s) - biodistribution , chemistry , imine , schiff base , ligand (biochemistry) , radiosynthesis , chelation , stereochemistry , excretion , radiochemistry , in vivo , nuclear chemistry , in vitro , biochemistry , organic chemistry , receptor , microbiology and biotechnology , biology , catalysis
The biodistribution of an N 2 N 2 ′ tetradentate gold(III) chelate, which is known to be cytotoxic towards a range of human cancer cell lines, was determined by a radiolabelled equivalent of the compound. The 198 Au‐labelled gold(III) chelate of a bis(pyrrolide‐imine) Schiff base ligand with a three‐carbon di(azomethine) linkage was successfully synthesised with a high radiochemical yield of 73% and radiochemical purity of >95%. The high energy γ‐ray emitted by the 198 Au nucleus was used to follow the biodistribution of the compound in vivo in six male Sprague Dawley rats on a gamma camera. The log P o/w value of the nat Au analogue, −1.92(2), showed that the compound is hydrophilic and therefore likely to largely remain in the blood pool. This was confirmed by the biodistribution study, which showed 21% of the injected dose (ID) remained in the blood pool 4.5 h after injection. This decreased to 10.8% over a 24‐h period. The activity measured in the lungs, 1.48%ID/g, remained relatively constant over a 24‐h period suggesting that the complex had accumulated in the lungs in the form of particulates, and could not be cleared by the test subjects. The t ½ for the heart and lungs was greater than 24 h. Excretion of the test compound is seemingly via the kidneys, but is slow with approximately 30% of the ID excreted within 24 h.