Polyoxometalates as antitumor agents: Bioactivity of a new polyoxometalate with copper on a human osteosarcoma model

León, Ignacio E.; Porro, V.; Astrada, Soledad; Egusquiza, María G.; Cabello, Carmen I.; Bollati-Fogolín, Mariela; Etcheverry, Susana B.

doi:10.1016/j.cbi.2014.10.012

Cited by 42 publications

(21 citation statements)

References 47 publications

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“…with mean values of 16 and 41 % for complex II and III, respectively (p<0.01) at lower concentrations, the complexes did not show a differential behavior at higher concentrations (p>0.05). As we previously reported 45 These findings are in agreement with our results 46,47 .…”

Section: Cytotoxic Effectsupporting

confidence: 94%

Crystal structure, Hirshfeld surface analysis, spectroscopic and biological studies on sulfamethazine and sulfaquinoxaline ternary complexes with 2,2′-biquinoline

et al. 2018

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Section: Cytotoxic Effectsupporting

confidence: 94%

Crystal structure, Hirshfeld surface analysis, spectroscopic and biological studies on sulfamethazine and sulfaquinoxaline ternary complexes with 2,2′-biquinoline

et al. 2018

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“…This study describes, for the first time, that POTs can affect aquaporin function and lead to the inhibition of cancer cell migration. POMs are potential candidates for anticancer drugs in the future since several types of POMs showed anticancer activities at various concentrations ranging from nM to µM [3,9,13,[37][38][39][40][41][42][43][44]. In fact, in most cases, when compared with already approved anticancer drugs, POMs were more efficient.…”

Section: Discussionmentioning

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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“…Importantly, arrest in G0/G1 or G2/M phases have been extensively described with antitumoural drugs, 30 different types of NPs 31 and even polyoxometalates. 32 …”

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confidence: 99%

In vitro cell cytotoxicity profile and morphological response to polyoxometalate-stabilised gold nanoparticles

et al. 2016

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The size and redox properties of molecular polyoxometalates (POMs) make them extremely relevant for bioapplications: from disrupting tumour growth and enzyme inhibition, to DNA-intercalating agents and antimicrobial applications. Their unique ability to reversibly dominate and receive electrons, coupled with their high anionic charge, also makes them suitable for the preparation of zero-valent state metal nanoparticles (NPs) from molecular precursors. Polyoxometalate-stabilised nanoparticles (NPs@POM) are therefore an ideal delivery vehicle for bioactive POMs. Here we show how POM-stabilised gold NPs (AuNPs@POM) are massively internalised into Vero (kidney epithelial) and B16 (skin melanoma) cell lines with variable cytotoxic effects. Cell viability assays and quantification of cytoplasmic membrane composition revealed that the Vero cell line was unaltered by the internalisation of these hybrid particles; while their internalisation in B16 tumour cells produced mild cytotoxic effects and an antiproliferative cell cycle arrest in the G0/G1 and G2/M phases. The observed perturbation of the tumour cell line combined with the high degree of internalisation means that these (or similar) NPs@POM could serve as candidates for a range of bioapplications in diagnostics or therapy.

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Polyoxometalates as antitumor agents: Bioactivity of a new polyoxometalate with copper on a human osteosarcoma model

Cited by 42 publications

References 47 publications

Crystal structure, Hirshfeld surface analysis, spectroscopic and biological studies on sulfamethazine and sulfaquinoxaline ternary complexes with 2,2′-biquinoline

Crystal structure, Hirshfeld surface analysis, spectroscopic and biological studies on sulfamethazine and sulfaquinoxaline ternary complexes with 2,2′-biquinoline

The Aquaporin-3-Inhibiting Potential of Polyoxotungstates

In vitro cell cytotoxicity profile and morphological response to polyoxometalate-stabilised gold nanoparticles

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