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Title: In vitro effects of some gold complexes on Na<sup>+</sup>/K<sup>+</sup> ATPase activity and cell proliferation
Authors: Petrović, Voin
Colovic, Mirjana
Krstić, Danijela
Vujačić, Ana
Petrovic, Sandra
Joksic, Gordana
Bugarčić, Živadin
Vasic, Vesna
Issue Date: 2013
Abstract: The in vitro influence of gold(III) complexes, H[AuCl4], [Au(DMSO)2Cl2]Cl and [Au(bipy)Cl2]Cl (bipy = 2,2′-bipyridine), upon commercially available Na+/K+ ATPase activity, purified from porcine brain cortex, was investigated. Additionally, the complexes were tested on human lymphocytes, and incidence of micronuclei and cell proliferation index was determined. Concentration-dependent inhibition of the enzyme for all three compounds was obtained, but with differing potencies. Calculated IC50 from Hill analysis were (in M): 5.75 × 10- 7, 5.50 × 10- 6 and 3.98 × 10- 5, for H[AuCl4], [Au(DMSO)2Cl 2]Cl and [Au(bipy)Cl2]Cl, respectively, while Hill coefficient values, n, were above 1 in all cases. This inhibition can be prevented using -SH donating ligands such as L-Cys and glutathione, and these ligands can also cause a recovery of the enzyme activity after the induced inhibition. Kinetic analysis demonstrated that each of the studied gold(III) complexes affects Na+/K+ ATPase reducing maximum enzymatic velocity, Vmax, but not significantly changing the affinity for the substrate (KM value), implying a noncompetitive mode of the interaction. Furthermore, among investigated gold(III) complexes, the [Au(bipy)Cl2]Cl complex exhibits a strong cytotoxic effect on human lymphocytes, which suggests its potential for use in antitumor therapy. © 2013 Elsevier Inc.
Type: article
DOI: 10.1016/j.jinorgbio.2013.03.013
ISSN: 0162-0134
SCOPUS: 2-s2.0-84875992731
Appears in Collections:Faculty of Science, Kragujevac

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