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New iron(III) anti-cancer aminobisphenolate/phenanthroline complexes: Enhancing their therapeutic potential using
Cristina P Matos1, Melissa Albino2, Joana Lopes2
1Centro de Química Estrutural, Institute of Molecular Sciences and Departamento de Química, Instituto Superior Técnico, Universidade de Lisboa, 1049-001 Lisboa, Portugal; Centro de Ciências e Tecnologias Nucleares, Instituto Superior Técnico, Universidade de Lisboa, 2695-066 Bobadela LRS, Portugal.
Abstract:
Malignant melanoma is an aggressive and deadly form of skin cancer and novel and improved therapeutic options are needed. A promising strategy involves the use of metallodrugs combined with liposomes for targeted delivery to cancer cells. In this work, a family of iron(III) complexes was synthesized bearing a trianionic aminobisphenolate ligand (L) and phenanthroline-type co-ligands (NN). Four ternary iron complexes of general formula [Fe(L)(NN)] were obtained: [Fe(L)(amphen)] (1), [Fe(L)(phen)] (2), [Fe(L)(Clphen)] (3), and [Fe(L)(Mephen)] (4), as well as a fifth complex [Fe(L)(NEt3)(H2O)] (5) without the bidentate co-ligand. All complexes were characterized by analytic and spectroscopic techniques and demonstrated to be stable in aqueous environment. Complexes 1 and 2 were able to bind DNA and presented high cytotoxic activity towards human cancer cells. Complex 1 (IronC) was selected for incorporation into different liposomal formulations, which were fully characterized and screened against murine melanoma cells. The IronC liposomal formulation with the highest incorporation efficiency (∼95%) and a low IC50 value (7.1 ± 0.7 μM) was selected for in vivo evaluation. In a syngeneic murine melanoma model the liposomal formulation of IronC yielded the highest impairment on tumour progression when compared with the control, temozolomide, and with the iron complex in free form.
Insights
New iron complexes show promise for treating melanoma. Liposomal delivery of a specific iron complex (IronC) effectively inhibited tumor progression in mice, outperforming existing treatments.
Area of Science:
- Inorganic Chemistry
- Cancer Therapeutics
- Nanomedicine
Background:
- Malignant melanoma is an aggressive skin cancer requiring novel treatments.
- Metallodrugs and liposomes offer potential for targeted cancer therapy.
- Iron complexes are being explored for their cytotoxic properties.
Purpose of the Study:
- To synthesize and characterize novel iron(III) complexes for potential melanoma treatment.
- To evaluate the efficacy of these complexes, particularly when encapsulated in liposomes.
- To assess the in vivo therapeutic potential of the most promising formulation.
Main Methods:
- Synthesis and characterization of five iron(III) complexes with aminobisphenolate and phenanthroline ligands.
- Assessment of DNA binding and cytotoxicity of the iron complexes against human cancer cells.
- Development and in vitro/in vivo evaluation of liposomal formulations of a selected iron complex (IronC) in a murine melanoma model.
Main Results:
- Four ternary iron complexes and one related complex were successfully synthesized and found stable in aqueous media.
- Complexes 1 and 2 exhibited DNA binding and significant cytotoxicity against human cancer cells.
- Liposomal IronC demonstrated high incorporation efficiency (~95%) and potent in vivo anti-tumor activity in a murine melanoma model, surpassing controls and free IronC.
Conclusions:
- Novel iron(III) complexes show promise as cytotoxic agents against melanoma.
- Liposomal encapsulation enhances the delivery and efficacy of IronC for melanoma treatment.
- The developed IronC liposomal formulation represents a promising therapeutic strategy for malignant melanoma.
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