Noble Metals in Medicinal Inorganic Chemistry

Dear Colleagues,

The study and development of noble metal-based drugs is a promising approach to designing new drugs for treating several diseases. Cisplatin and other platinum-based compounds are powerful chemotherapeutic agents used currently in the clinical treatment of cancer. The chemical and biological properties of coordination and organometallic compounds have allowed the design of new metallodrugs that include different metal ions. Ruthenium-based compounds have seen advanced clinical trials as potential novel anticancer drugs. Gold-based drugs are currently used in the clinic for the treatment of rheumatoid arthritis. These metal ions and rhodium, iridium, palladium, osmium, and other denominated noble elements have been the subject of study of several investigations due to their interesting pharmacological properties; therefore, it is relevant to the development of novel metal compounds with highlighted pharmacological properties, such as anticancer, antirheumatic, antimalarial, antibacterial, antiparasitic, antifungal, and antiviral drugs.

In this Special Issue, we wish to cover the most recent advances in the development of noble metals in medicinal inorganic chemistry by hosting a mix of original research articles and reviews.

Dr. Esteban Rodríguez-Arce
Prof. Dr. Dinorah Gambino
Guest Editors

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• metallodrugs
• bioactive noble metals
• medicinal inorganic chemistry
• coordination and organometallic compounds
• biological studies
• mechanism of action
• pharmacological properties

Title: synthesis, characterization, and biological evaluation of a new metal compound as a potential antiparasitic agent
Authors: Dinorah Gambino; Esteban Rodríguez-Arce
Affiliation: Área Química Inorgánica, Facultad de Química, Universidad de la República, Montevideo 11800, Uruguay; Departamento de Química Inorgánica y Analítica, Universidad de Chile, Casilla 233, Santiago, Chile
Abstract: The topic would be focused on developing a new Noble Metal compound with activity against Trypanosomatid parasites which cause Neglected Tropical diseases.

Title: Mechanism of anti-Trypanosoma cruzi action of Gold(I) compounds: a theoretical and experimental approach
Authors: Javiera Órdenes-Rojas; Paola Risco; José Ortega-Campos; Germán Barriga-González; Ana Liempi; Ulrike Kemmerling; Dinorah Gambino; Lucía Otero; Claudio Olea-Azar; Esteban Rodríguez-Arce
Affiliation: Departamento de Química Inorgánica y Analítica, Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, Dr. Carlos Lorca Tobar 964, Casilla 223, Santiago, Chile
Abstract: In the search for a more effective chemotherapy for the treatment of Chagas’ disease, caused by Trypanosoma cruzi parasite, the use of gold compounds may be a promising approach. In this work, four gold(I) compounds [AuCl(HL)], (HL= bioactive 5-nitrofuryl containing thiosemicarbazones) were studied. Compounds were theoretically characterized showing identical chemical structures with the metal ion located in a linear coordination environment and the thiosemicarbazones acting as monodentate ligands. Cyclic voltammetry and Electron Spin Resonance (ESR) studies demonstrated that the complexes could generate the nitro anion radical (NO2·-) by reduction of the nitro moiety. The compounds were evaluated in vitro on the trypomastigote form of T. cruzi and human cells of endothelial morphology. Gold compounds showed activity in the micromolar range against T. cruzi. The most active compounds (IC50 of around 10 μM) showed an enhancement of the antiparasitic activity compared with their respective bioactive ligands and moderate selectivity. To get insight into the anti-chagasic mechanism of action, the intracellular free radical production capacity of the gold compounds was assessed by ESR and fluorescence measurements. DMPO (5,5-dimethyl-1-pirroline-N-oxide) spin adducts related to the bioreduction of the complexes and redox cycling processes were characterized. The potential oxidative stress mechanism against T. cruzi was confirmed.