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Inorganics
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Evaluation of the Potential Biological Activity of Metallo-Drugs
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Evaluation of the Potential Biological Activity of Metallo-Drugs

A special issue of Inorganics (ISSN 2304-6740). This special issue belongs to the section "Bioinorganic Chemistry".

Deadline for manuscript submissions: 30 June 2025 | Viewed by 5912

Special Issue Editors

Dr. Snežana Jovanović-Stević

E-Mail Website
Guest Editor
University of Kragujevac, Faculty of Medical Sciences, Department of Pharmacy, Svetozara Markovića 69, 34000 Kragujevac, Serbia
Interests: transition metal complexes; kinetics; biomolecules; interactions
Special Issues, Collections and Topics in MDPI journals
Dr. Jovana V. Bogojeski

E-Mail Website
Guest Editor
Faculty of Science, University of Kragujevac, Radoja Domanovića 12, 34000 Kragujevac, Serbia
Interests: coordination chemistry; kinetics and mechanism; biomolecules; interactions

Special Issue Information

Dear Colleagues,

Cancer is the second leading cause of death after cardiovascular diseases. The use of transition metal complexes as chemotherapeutics has been well established. Until now, cisplatin, a platinum(II) complex which is an indispensable part in the therapy of various types of tumors, has demonstrated most success. However, serious side effects and drug resistance during its application limit the clinical use of cisplatin, leading many scientists to design new platinum complexes that are structurally similar to cisplatin. Some of them have shown significant potential anticancer activity, even better than cisplatin. Today, research is directed toward complexes of ions of other transition metals such as palladium(II), gold(III), ruthenium(II), osmium(II), rhodium(III), copper(II), etc. It is well known that metal-based compounds exert anticancer activity via interaction with DNA molecules. On the other hand, interaction of these compounds with some sulfur-containing bio-molecules can cause side effects. In order to evaluate potential antitumor activity, selectivity of action and toxicity of metallo-drugs, it is necessary to examine the kinetics and mechanism of their reactions with DNA segments, as well as with DNA molecules themselves. Further, the binding of anticancer agents to proteins is an important factor in the pharmacological response of drugs. Serum albumins (SAs) are the most abundant proteins in plasma and have a crucial role in the transport of many drugs to the target sites. Thus, the study of interaction between transition metal complexes and serum albumin proteins can provide useful information about the therapeutic efficiency of the drug. In this Special Issue, we wish to publish the latest developments in the design of transition metal-based compounds and their potential clinical applications through original research articles and short critical reviews.

Dr. Snežana Jovanović-Stević
Dr. Jovana V. Bogojeski
Guest Editors

Manuscript Submission Information

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Keywords

  • synthesis
  • metal-based drugs
  • DNA/serum albumin proteins
  • small molecules
  • interactions

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Published Papers (5 papers)

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Research

15 pages, 6979 KiB  
Article
Analysis of Biomolecular Changes in HeLa Cervical Cancer Cell Line Induced by Interaction with [Pd(dach)Cl2]
by Vanja Ralić, Maja D. Nešić, Tanja Dučić, Milutin Stepić, Lela Korićanac, Katarina Davalieva and Marijana Petković
Inorganics 2025, 13(1), 20; https://doi.org/10.3390/inorganics13010020 - 14 Jan 2025
Viewed by 587
Abstract
Transition metal complexes have been used in medicine for several decades, but their intracellular effects are not yet fully elucidated. Therefore, in this study, we investigate biomolecular changes induced by a palladium(II) complex in cervical carcinoma (HeLa) cells as a model to study [...] Read more.
Transition metal complexes have been used in medicine for several decades, but their intracellular effects are not yet fully elucidated. Therefore, in this study, we investigate biomolecular changes induced by a palladium(II) complex in cervical carcinoma (HeLa) cells as a model to study the subtle changes caused by transition metal ions ingested by the cells. The impact of dichloro(1,2-diaminocyclohexane)palladium(II), [Pd(dach)Cl2], was studied by synchrotron radiation-based Fourier transform infrared (SR FTIR) spectroscopy, a powerful tool for studying alterations in cellular components’ biochemical composition and biomolecular secondary structure on a single-cell level. A spectral analysis, complemented by statistics, revealed that the Pd(II) complex considerably affected all major types of macromolecules in HeLa cells and induced structural changes in proteins through an increased formation of cross-β-sheets and causes structural rearrangement in deoxyribonucleic acid (DNA) through potential chromosome fragmentation. Although a certain level of lipid peroxidation was detectable by SR FTIR spectroscopy and confirmed by an analysis of cellular lipids by matrix-assisted laser desorption and ionisation time-of-flight mass spectrometry, the oxidative stress is not a significant mechanism by which Pd(II) expresses the effect on the HeLa cells. Full article
(This article belongs to the Special Issue Evaluation of the Potential Biological Activity of Metallo-Drugs)
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12 pages, 2879 KiB  
Article
Interaction of Phenanthroline-Containing Copper Complexes with Model Phospholipid Membranes
by Priscilla Freddi, Natalia Alvarez, Gianella Facchin and Antonio J. Costa-Filho
Inorganics 2024, 12(12), 307; https://doi.org/10.3390/inorganics12120307 - 26 Nov 2024
Viewed by 868
Abstract
Medicinal Inorganic Chemistry has provided oncology with metallodrugs for cancer treatment, including several promising candidate drugs. In particular, copper(II) coordination compounds with phenanthroline stand out as potential anticancer agents. In this work, we used Differential Scanning Calorimetry and Electron Spin Resonance to investigate [...] Read more.
Medicinal Inorganic Chemistry has provided oncology with metallodrugs for cancer treatment, including several promising candidate drugs. In particular, copper(II) coordination compounds with phenanthroline stand out as potential anticancer agents. In this work, we used Differential Scanning Calorimetry and Electron Spin Resonance to investigate the interaction of the copper phenanthroline complexes [Cu(phen)]2+ and [Cu(L-dipeptide)(phenanthroline) (L-dipeptide: L-Ala-Gly and L-Ala-Phe)) with model lipid membranes (1,2-dipalmitoyl-sn-glycero-3-phosphocholine, DPPC, and 1,2-dipalmitoyl-sn-glycero-3-phospho-(1′-rac-glycerol) sodium salt, DPPG). Our results showed that the complexes interact with the membrane models, fluidizing them. The [Cu(phen)]2+ presented a different localization than the free ligand phen. The dipeptide modulated the localization of the complex in the membrane and the modifications induced in the physicochemical properties of the lipid vesicles. A stronger interaction with DPPG anionic membranes was observed, which mimic membranes with negatively charged surfaces, as found on several tumor cells. Full article
(This article belongs to the Special Issue Evaluation of the Potential Biological Activity of Metallo-Drugs)
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14 pages, 3523 KiB  
Article
Comparative Study of Docking Tools for Evaluation of Potential Copper Metallodrugs and Their Interaction with TMPRSS2
by Sergio Vázquez-Rodríguez, Diego Ramírez-Contreras, Lisset Noriega, Amalia García-García, Brenda L. Sánchez-Gaytán, Francisco J. Meléndez, Walter Filgueira de Azevedo, Jr., María Eugenia Castro and Enrique González-Vergara
Inorganics 2024, 12(11), 282; https://doi.org/10.3390/inorganics12110282 - 30 Oct 2024
Viewed by 826
Abstract
COVID-19 has caused over seven million deaths globally due to its high transmission rate. The virus responsible for the disease requires a transmembrane protease serine type II (TMPRSS2-7MEQ) to infiltrate host cells and has been linked to several cancers, particularly prostate cancer. To [...] Read more.
COVID-19 has caused over seven million deaths globally due to its high transmission rate. The virus responsible for the disease requires a transmembrane protease serine type II (TMPRSS2-7MEQ) to infiltrate host cells and has been linked to several cancers, particularly prostate cancer. To investigate COVID-19 potential therapies, a series of Casiopeina-like copper complexes containing 1,10-Phenanthroline and amino acids were investigated as TMPRSS2 inhibitors. The molecular structures of twelve Phenanthroline copper complexes were calculated, and their global reactivity indices were analyzed using DFT and conceptual DFT methods. Three molecular docking algorithms were employed to identify the most effective inhibitors by examining their interactions with amino acid residues in the target protein’s catalytic activity triad (Asp345, His296, and Ser441). All complexes are docked above the catalytic site, blocking the interaction with substrates. The Phenanthroline complexes showed better interactions than the Bipyridine complexes, likely due to increased hydrophobic contacts. Analogs’ cationic nature and amino acids’ basic side chains bring them near the active site by interacting with Asp435. The top complexes in this study contain Ornithine, Lysine, and Arginine, making them promising alternatives for researching new drugs for COVID-19 and cancers like prostate cancer. Full article
(This article belongs to the Special Issue Evaluation of the Potential Biological Activity of Metallo-Drugs)
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23 pages, 6782 KiB  
Article
Synthesis of Cobalt(III) Complexes Derived from Pyridoxal: Structural Cleavage Evaluations and In Silico Calculations for Biological Targets
by Liniquer André Fontana, Francisco Mainardi Martins, Josiéli Demetrio Siqueira, Carlos Serpa, Otávio Augusto Chaves and Davi Fernando Back
Inorganics 2024, 12(6), 171; https://doi.org/10.3390/inorganics12060171 - 18 Jun 2024
Cited by 2 | Viewed by 1318
Abstract
This study sought to investigate the synthesis of eight complexes constituted by a cobalt(III) (CoIII) metallic center coordinated to two units of iminic ligands LnC (n = 1–4, L1C–L4C), which are derivatives of pyridoxal hydrochloride and anilines with [...] Read more.
This study sought to investigate the synthesis of eight complexes constituted by a cobalt(III) (CoIII) metallic center coordinated to two units of iminic ligands LnC (n = 1–4, L1C–L4C), which are derivatives of pyridoxal hydrochloride and anilines with thioether function containing one to four carbons. Depending on the source of the cobalt ion and the addition (or not) of a non-coordinating counterion, complexes with distinct structures may form, being categorized into two series: [CoIII(LnC)(L0C)] (n = 1–4, C1’–C4’) with a LnC ligand and a ligand that has a thiolate function which cleaves the C-S(thioether) bond (L0C) and [CoIII(LnC)2]PF6 (n = 1–4, C1–C4) with two similar units of the same LnC ligand. The occurrence (or not) of cleavage in the eight complexes was observed by elucidating the solid-state structures by single crystal X-ray diffraction. This exciting method allows the synthesis of CoIII complexes without cleaving the C-S bonds from the ligands, thereby not requiring an inert atmosphere in the reaction systems. The synthesized complexes were evaluated by in silico calculations on viable biological targets such as deoxyribonucleic acid, superoxide dismutase enzyme, human serum albumin, and the structural spike glycoprotein of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) with the receptor binding domain (RBD) in both up and down conformations without and in complex with the cellular receptor angiotensin-converting enzyme 2 (ACE2). Overall, in silico results suggested that all the inorganic complexes under study are potential anticancer/antiviral agents; however, C4 and C4’ are the best candidates for future in vitro assays. Full article
(This article belongs to the Special Issue Evaluation of the Potential Biological Activity of Metallo-Drugs)
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12 pages, 2507 KiB  
Article
Investigating the Anticancer Properties of Novel Functionalized Platinum(II)–Terpyridine Complexes
by Roberta Panebianco, Maurizio Viale, Valentina Giglio and Graziella Vecchio
Inorganics 2024, 12(6), 167; https://doi.org/10.3390/inorganics12060167 - 15 Jun 2024
Viewed by 1560
Abstract
Novel platinum(II) complexes of 4′-substituted terpyridine ligands were synthesized and characterized. Each complex had a different biomolecule (amine, glucose, biotin and hyaluronic acid) as a targeting motif, potentially improving therapeutic outcomes. We demonstrated that complexes can self-assemble in water into about 150 nm [...] Read more.
Novel platinum(II) complexes of 4′-substituted terpyridine ligands were synthesized and characterized. Each complex had a different biomolecule (amine, glucose, biotin and hyaluronic acid) as a targeting motif, potentially improving therapeutic outcomes. We demonstrated that complexes can self-assemble in water into about 150 nm nanoparticles. Moreover, the complexes were assayed in vitro toward a panel of human cancer cell lines (ovarian adenocarcinoma A2780, lung cancer A549, breast adenocarcinoma MDA-MB-231, neuroblastoma SHSY5Y) to explore the impact of the pendant moiety on the terpyridine toxicity. The platinum complex of terpyridine amine derivative, [Pt(TpyNH2)Cl]Cl, showed the best antiproliferative effect, which was higher than cisplatin and [Pt(Tpy)Cl]Cl. Selective in vitro antiproliferative activity was achieved in A549 cancer cells with the Pt–HAtpy complex. These findings underline the potential of these novel platinum(II) complexes in cancer therapy and highlight the importance of tailored molecular design for achieving enhanced therapeutic effects. Full article
(This article belongs to the Special Issue Evaluation of the Potential Biological Activity of Metallo-Drugs)
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