Abstract
The therapeutic applications of gold are well-known for many centuries. The most used gold compounds contain Au(I). Herein, we report, for the first time, the ability of four Au(I) and Au(III) complexes, namely dichloro (2-pyridinecarboxylate) Au(III) (abbreviated as 1), chlorotrimethylphosphine Au(I) (2), 1,3-bis(2,6-diisopropylphenyl) imidazole-2-ylidene Au(I) chloride (3), and chlorotriphenylphosphine Au(I) (4), to affect the sarcoplasmic reticulum (SR) Ca2+-ATPase activity. The tested gold compounds strongly inhibit the Ca2+-ATPase activity with different effects, being Au(I) compounds 2 and 4 the strongest, with half maximal inhibitory concentration (IC50) values of 0.8 and 0.9 µM, respectively. For Au(III) compound 1 and Au(I) compound 3, higher IC50 values are found (4.5 µM and 16.3 µM, respectively). The type of enzymatic inhibition is also different, with gold compounds 1 and 2 showing a non-competitive inhibition regarding the native substrate MgATP, whereas for Au compounds 3 and 4, a mixed type of inhibition is observed. Our data reveal, for the first time, Au(I) compounds with powerful inhibitory capacity towards SR Ca2+ATPase function. These results also show, unprecedently, that Au (III) and Au(I) compounds can act as P-type ATPase inhibitors, unveiling a potential application of these complexes.
Highlights
Gold compounds were used in medicine in ancient Egypt, Arabia, India, and China [1]
In 1927, colloidal gold started to be used in rheumatoid arthritis (RA), and in 2013, Au(III) compounds were reported for the first time as Na+ /K+ -ATPase inhibitors [2,3]
Discussion effects of the ATPase were the same as without any incubation, suggesting that the Au compounds are theobserved effects ofcan thebefour gold compounds mentioned above
Summary
Gold compounds were used in medicine in ancient Egypt, Arabia, India, and China [1]. Later on, in Europe, Paracelsus (1493–1541) described the preparation of red colloidal gold by reduction of gold trichloride with an alcoholic extract of plants, followed by the addition of sugar or syrup.This preparation was named aurum potable, quinta essential auri, or oleum auri, being used in the treatment of several diseases (such as syphilis), for improving strength, prolonging life and rejuvenating.In 1618, Francisco Antonii published the first book on colloidal gold, which was preserved until nowadays. In Europe, Paracelsus (1493–1541) described the preparation of red colloidal gold by reduction of gold trichloride with an alcoholic extract of plants, followed by the addition of sugar or syrup. This preparation was named aurum potable, quinta essential auri, or oleum auri, being used in the treatment of several diseases (such as syphilis), for improving strength, prolonging life and rejuvenating. In 1618, Francisco Antonii published the first book on colloidal gold, which was preserved until nowadays. It contains information on the preparation of gold colloids and on its medical applications, including practical suggestions. In 1927, colloidal gold started to be used in rheumatoid arthritis (RA), and in 2013, Au(III) compounds were reported for the first time as Na+ /K+ -ATPase inhibitors [2,3]
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