Gold Compounds Inhibit the Ca2+-ATPase Activity of Brain PMCA and Human Neuroblastoma SH-SY5Y Cells and Decrease Cell Viability

Plasma membrane calcium ATPases (PMCA) are key proteins in the maintenance of (Ca2+) homeostasis. Dysregulation PMCA function is associated with several human pathologies, including neurodegenerative diseases, and, therefore, these potential drug targets to counteract those diseases. Gold compounds, namely Au(I), well-known for their therapeutic use rheumatoid arthritis and other diseases centuries. Herein, we report ability dichloro(2-pyridinecarboxylate)gold(III) (1), chlorotrimethylphosphinegold(I) (2), 1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidenegold(I) chloride (3), chlorotriphenylphosphinegold(I) (4) compounds interfere Ca2+-ATPase activity pig brain purified membranes from SH-SY5Y neuroblastoma cell cultures. The Au(III) compound (1) inhibits IC50 value 4.9 µM, while Au(I) (2, 3, 4) inhibit protein values 2.8, 21, 0.9 respectively. Regarding native substrate MgATP, gold 1 4 showed a non-competitive type inhibition, whereas 2 3 mixed inhibition. All complexes cytotoxic effects on cells, although were more than 4. In summary, this work shows that both Au (I III) high-affinity inhibitors fractions cells. Additionally, they exert strong effects.