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Article

The Ca2+-ATPase Inhibition Potential of Gold(I, III) Compounds

1
CCMar, FCT, Universidade do Algarve, 8005-139 Faro, Portugal
2
CCMar, ISE, Universidade do Algarve, 8005-139 Faro, Portugal
3
LAQV-REQUIMTE, Department of Chemistry, NOVA School of Science and Technology, Universidade NOVA de Lisboa, 2829-516 Caparica, Portugal
*
Author to whom correspondence should be addressed.
Inorganics 2020, 8(9), 49; https://doi.org/10.3390/inorganics8090049
Received: 22 July 2020 / Revised: 19 August 2020 / Accepted: 26 August 2020 / Published: 30 August 2020
(This article belongs to the Special Issue Gold Complexes)
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. View Full-Text
Keywords: Gold(I, III) compounds; Ca2+-ATPase; P-type ATPases inhibitors; anticancer Gold(I, III) compounds; Ca2+-ATPase; P-type ATPases inhibitors; anticancer
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MDPI and ACS Style

Fonseca, C.; Fraqueza, G.; Carabineiro, S.A.C.; Aureliano, M. The Ca2+-ATPase Inhibition Potential of Gold(I, III) Compounds. Inorganics 2020, 8, 49. https://doi.org/10.3390/inorganics8090049

AMA Style

Fonseca C, Fraqueza G, Carabineiro SAC, Aureliano M. The Ca2+-ATPase Inhibition Potential of Gold(I, III) Compounds. Inorganics. 2020; 8(9):49. https://doi.org/10.3390/inorganics8090049

Chicago/Turabian Style

Fonseca, Custódia; Fraqueza, Gil; Carabineiro, Sónia A.C.; Aureliano, Manuel. 2020. "The Ca2+-ATPase Inhibition Potential of Gold(I, III) Compounds" Inorganics 8, no. 9: 49. https://doi.org/10.3390/inorganics8090049

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