Platicur is a cis-diamine-platinum(II) complex linked to curcumin. Previous studies have shown that the photoactivation of Platicur, with visible light, is responsible for the production of active species of platinum(II) and a photoactive curcumin. The active species formed act synergistically causing an interesting anticancer activity. In this work, we tried to improve the antitumor activity of photoactivated Platicur by using a nano delivery system. With this aim, Platicur's aqueous chitosan nanocolloids were synthesized, Figure 1. The preliminary in vitro biological assays on HeLa tumor cell line have demonstrated a significantly higher cytotoxicity (a significantly lower IC50 dose) of the photoactivated nanocolloids with Platicur, compared to the photoactivated Platicur not encapsulated in the nanocolloids. The use of a metabolomic approach based on NMR spectroscopy in the research of the mechanism of action or for the evaluation of the tumor response to the anticancer metal drugs is a new tool of recent growth. The side effects induced by metal based drugs, the prediction of the response to treatment and the key information on the mechanism of action (for known and new compounds) could be easily obtained using NMR-based metabolomics. [2, 3] For this reason, the 1H NMR spectroscopy coupled with multivariate statistical analysis was used to characterize the metabolic variations of intracellular metabolites and the compositional changes of the corresponding culture media of HeLa cells treated with photoactivated Platicur nanocolloids. The metabolomic analysis allowed to highlight specific metabolic differences between the cells treated with photoactivated Platicur nanocoloids compared to non-photoactivated ones. The NMR has once again proved to be a valid tool for the study of the mechanism of action of metal-based drugs.

Photoactivated aqueous nanocolloids of Platicur: NMR metabolomic study of treated HeLa cancer cells

Federica De Castro;Michele Benedetti;Francesca Baldassarre;Laura Del Coco;Giuseppe Ciccarella;Francesco P. Fanizzi.
2020-01-01

Abstract

Platicur is a cis-diamine-platinum(II) complex linked to curcumin. Previous studies have shown that the photoactivation of Platicur, with visible light, is responsible for the production of active species of platinum(II) and a photoactive curcumin. The active species formed act synergistically causing an interesting anticancer activity. In this work, we tried to improve the antitumor activity of photoactivated Platicur by using a nano delivery system. With this aim, Platicur's aqueous chitosan nanocolloids were synthesized, Figure 1. The preliminary in vitro biological assays on HeLa tumor cell line have demonstrated a significantly higher cytotoxicity (a significantly lower IC50 dose) of the photoactivated nanocolloids with Platicur, compared to the photoactivated Platicur not encapsulated in the nanocolloids. The use of a metabolomic approach based on NMR spectroscopy in the research of the mechanism of action or for the evaluation of the tumor response to the anticancer metal drugs is a new tool of recent growth. The side effects induced by metal based drugs, the prediction of the response to treatment and the key information on the mechanism of action (for known and new compounds) could be easily obtained using NMR-based metabolomics. [2, 3] For this reason, the 1H NMR spectroscopy coupled with multivariate statistical analysis was used to characterize the metabolic variations of intracellular metabolites and the compositional changes of the corresponding culture media of HeLa cells treated with photoactivated Platicur nanocolloids. The metabolomic analysis allowed to highlight specific metabolic differences between the cells treated with photoactivated Platicur nanocoloids compared to non-photoactivated ones. The NMR has once again proved to be a valid tool for the study of the mechanism of action of metal-based drugs.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11587/441780
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