Some remarks on the biological application of gold(III) complexes

Gold(III) complexes are widely studied as antitumor agents and show good results. The interaction with biologically active thiols (thiomalate, cysteine, glutathione (GSH) and human serum albumin) of a number of gold(III) complexes with N-containing polydentate ligands in aqueous solution with pH 7.4 and 0.2 M NaCl was studied. Complexes with 1,10-phenanthroline and 2,2'-bipyridyl, Au(phen)(OH)₂⁺ and Au(bipy)(OH)₂⁺, react fast with an excess of any of these thiols and in less than a few seconds transform into gold(I) bis-thiolate complexes. For complexes with deprotonated ethylenediamine and diethylenetriamine, Au(en)(en-H)²⁺ and Au(dien-H)(Cl,OH)⁺, at a significant excess of GSH, a relatively long-lived gold(III) complex Au^III(GSH)_iL_j is formed. At t = 37 °C, it transforms into the gold(I) bis-thiolate complex Au(GSH)₂ by 90% in 4 h. However, for other thiols, the rate of decomposition of similar complexes is about 10 times higher. Some other complexes were also considered. In all cases, a fairly fast reduction of gold(III) to gold(I) occurs with the formation of the gold(I) bis-thiolates.