Inhibition of Na+/K+- and Ca2+-ATPase activities by phosphotetradecavanadate

Fraqueza, Gil; Fuentes, Juan; Krivosudský, Lukáš; Dutta, Saikat; Mal, Sib Sankar; Roller, Alexander; Giester, Gerald; Rompel, Annette; Aureliano, Manuel

doi:10.1016/j.jinorgbio.2019.110700

Cited by 34 publications

(38 citation statements)

References 54 publications

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“…Gold(I) compounds 2 and 4 strongly inhibit Ca 2+ -ATPase, showing IC50 values of 0.8 and 0.9 µM. Using exactly the same experimental conditions as those of the present study, similar Ca 2+ -ATPase IC50 values of inhibition were previously determined for polyoxotungstates (POTs), such as P2W18 (0.6 µM) and for Se2W29 (IC50 = 0.3 µM), as well as for polyoxovanadates (POVs), such as PV14 (IC50 = 1 µM) [31,32]. However, a lower capacity was observed for some POTs, such as TeW6 (IC50 = 200 µM) [31].…”

Section: Discussionsupporting

confidence: 86%

“…Inhibitory power (IC50) ranging from 1 to 35 µM was reported for decaniobate [Nb10O28] 6− (IC50 = 35 µM) and for Keggin-based polyoxotungstates (POTs), such as mono-substituted CoW11 (IC50 = 4 µM), tri-lacunary SiW9 (IC50 =16 µM) and AsW9 (20 µM), lacunary Dawson type P2W12 (11 µM), and also for As2W19 (28 µM) [31]. Note that the P-type ATPases have long been known to be inhibited by metal complexes although the structural details of its inhibitory mechanism remain unresolved [27,29,[31][32][33][34][35]. Regarding the Ca 2+ -ATPase, it was previously determined that polyoxovanadates, such as decavanadate (V10) (IC50 = 15 µM), are more powerful Ca 2+ -ATPase inhibitors than monomeric vanadate (V1) (IC50 = 80 µM).…”

Section: Discussionmentioning

confidence: 99%

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

et al. 2020

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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.

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Section: Discussionsupporting

confidence: 86%

Section: Discussionmentioning

confidence: 99%

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

et al. 2020

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“…Thus, POMs exhibit outstanding physical, chemical, and biochemical properties that remain to be completely understood and applied. Due to these properties, POMs are studied in environmental, chemical, and industrial fields, particularly in the areas of catalysis, corrosion prevention, smart glasses, and macromolecular crystallography, as well as in biology, such as for cancer treatment, bacterial infection, and diabetes, among others [1][2][3][4][5][6]. Although the number of POM studies with anticancer effects is increasing, their mechanisms of action in each type of cancer cell are still far from being understood [3].…”

Section: Introductionmentioning

confidence: 99%

“…Although the number of POM studies with anticancer effects is increasing, their mechanisms of action in each type of cancer cell are still far from being understood [3]. The antitumor activity of these inorganic compounds seems to be caused, at least in part, by the inhibition of certain enzymes such as alkaline phosphatases, kinases, ecto-nucleotidases, glucosidases, and P-type ATPases [5][6][7][8]. Moreover, some POMs are also understood to interfere with mitochondria function and DNA, while others can exert an immunomodulatory activity [9,10].…”

Section: Introductionmentioning

confidence: 99%

The Aquaporin-3-Inhibiting Potential of Polyoxotungstates

Pimpão

Silva

Mósca

et al. 2020

IJMS

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Polyoxometalates (POMs) are of increasing interest due to their proven anticancer activities. Aquaporins (AQPs) were found to be overexpressed in tumors bringing particular attention to their inhibitors as anticancer drugs. Herein, we report for the first time the ability of polyoxotungstates (POTs), such as of Wells–Dawson P2W18, P2W12, and P2W15, and Preyssler P5W30 structures, to affect aquaporin-3 (AQP3) activity and impair melanoma cell migration. The tested POTs were revealed to inhibit AQP3 function with different effects, with P2W18, P2W12, and P5W30 being the most potent (50% inhibitory concentration (IC50) = 0.8, 2.8, and 3.2 µM), and P2W15 being the weakest (IC50 > 100 µM). The selectivity of P2W18 toward AQP3 was confirmed in yeast cells transformed with human aquaglyceroporins. The effect of P2W12 and P2W18 on melanoma cells that highly express AQP3 revealed an impairment of cell migration between 55% and 65% after 24 h, indicating that the anticancer properties of these compounds may in part be due to the blockage of AQP3-mediated permeability. Altogether, our data revealed that P2W18 strongly affects AQP3 activity and cancer cell growth, unveiling its potential as an anticancer drug against tumors where AQP3 is highly expressed.

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“…The significant interest in coordination chemistry of oxo vanadium species is owing to their relevance to organic catalysis [4,5] and bioactivity [6][7][8][9][10]. It is very meaningful to synthesize complexes based on vanadium.…”

Section: Commentmentioning

confidence: 99%