Cytotoxic sub-nanometer aqueous platinum clusters as potential antitumoral agents. Issue 24 (31st October 2022)

• Record Type: Journal Article
• Authors: Greco, Rossella; García-Lainez, Guillermo; Oliver-Meseguer, Judit; Marini, Carlo; Domínguez, Irene; López-Haro, Miguel; Hernández-Garrido, Juan Carlos; Cerón-Carrasco, José Pedro; Andreu, Inmaculada; Leyva-Pérez, Antonio
• Is Part Of: Nanoscale advances. Volume 4:Issue 24(2022)
• Page Start: 5281
• Page End: 5289
• Publication Date: 2022-10-31
• Subjects: 620.5
• DOI: 10.1039/d2na00550f
• Languages: English
• ISSNs: 2516-0230

Abstract

Abstract : Ligand-free sub-nanometer metal clusters (MCs) in neat water show extremely high antitumoral activity, including for cisplatin-resistant cells. Abstract : Ligand-free sub-nanometer metal clusters (MCs) of Pt, Ir, Rh, Au and Cu, are prepared here in neat water and used as extremely active (nM) antitumoral agents for HeLa and A2870 cells. The preparation just consists of adding the biocompatible polymer ethylene-vinyl alcohol (EVOH) to an aqueous solution of the corresponding metal salt, to give liters of a MC solution after filtration of the polymer. Since the MC solution is composed of just neat metal atoms and water, the intrinsic antitumoral activity of the different sub-nanometer metal clusters can now fairly be evaluated. Pt clusters show an IC50 of 0.48 μM for HeLa and A2870 cancer cells, 23 times higher than that of cisplatin and 1000 times higher than that of Pt NPs, and this extremely high cytotoxicity also occurs for cisplatin-resistant (A2870 cis) cells, with a resistance factor of 1.4 (IC50 = 0.68 μM). Rh and Ir clusters showed an IC50 ∼ 1 μM. Combined experimental and computational studies support an enhanced internalization and cytotoxic activation.