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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: 30 December 2023 | Viewed by 5079

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Prof. Dr. Barbara Valtancoli

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Department of Chemistry “Ugo Schiff”, University of Florence, via della Lastruccia 3-13, 50019 Sesto Fiorentino, Italy
Interests: supramolecular chemistry; inorganic compounds; ruthenium polypyridyl complexes; anion coordination; in solution studies

Dr. Luca Conti

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Department of Chemistry “Ugo Schiff”, Università degli Studi di Firenze, via della Lastruccia 3-13, 50019 Sesto Fiorentino, Italy
Interests: supramolecular chemistry; ruthenium polypyridyl complexes; inorganic synthesis; photodynamic therapy (PDT); photoactivated chemotherapy (PACT); fluorescent compounds
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Dear Colleagues,

Since the unexpected discovery by Rosenberg and his co-workers, cisplatin and its analogs have been largely employed in the clinical treatment of several cancers. However, despite their potential, some crucial issues such as poor tumor selectivity and the occurrence of severe side effects, made it urgent to explore suitable alternatives.

This has opened the way to the study of other transition metal complexes over the last few decades, that have been shown to possess encouraging antitumoral activities, by virtue of many different mechanisms of action. At the same time, the antibacterial properties of many of them have been highlighted too. Indeed, a series of peculiar features, such as the extremely versatile chemical physical repertoire, the capacity to interact with key biological targets (such as DNA and proteins) and the multimodal mechanisms of action (just to name a few), make this class of compounds a challenging choice to develop therapeutic alternatives with improved outcomes.

This Special Issue of the International Journal of Molecular Sciences focuses on the design of metal complexes for application in the biomedical field, with a special interest in their antitumoral and antibacterial potential. Original research articles and review papers that deal with the different mechanisms of action pursued by these compounds are welcomed by this issue.

Prof. Dr. Barbara Valtancoli
Dr. Luca Conti
Guest Editors

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

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Keywords

metal-based drugs
drug discovery
anticancer activity
antibacterial activity
transition metal complexes

Published Papers (4 papers)

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Research

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Open AccessArticle

Mechanochemical Preparation, Solid-State Characterization, and Antimicrobial Performance of Copper and Silver Nitrate Coordination Polymers with L- and DL-Arginine and Histidine

and

Int. J. Mol. Sci. 2023, 24(6), 5180; https://doi.org/10.3390/ijms24065180 - 08 Mar 2023

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Abstract

The antimicrobial activity of the novel coordination polymers obtained by co-crystallizing the amino acids arginine or histidine, as both enantiopure L and racemic DL forms, with the salts Cu(NO₃)₂ and AgNO₃ has been investigated to explore the effect of chirality in the cases of enantiopure and racemic forms. The compounds [Cu·AA·(NO₃)₂]_CPs and [Ag·AA·NO₃]_CPs (AA = L-Arg, DL-Arg, L-His, DL-His) were prepared by mechanochemical, slurry, and solution methods and characterized by X-ray single-crystal and powder diffraction in the cases of the copper coordination polymers, and by powder diffraction and by solid-state NMR spectroscopy in the cases of the silver compounds. The two pairs of coordination polymers, [Cu·L-Arg·(NO₃)₂·H₂O]_CP and [Cu·DL-Arg·(NO₃)₂·H₂O]_CP, and [Cu·L-Hys·(NO₃)₂·H₂O]_CP and [Cu·DL-His·(NO₃)₂·H₂O]_CP, have been shown to be isostructural in spite of the different chirality of the amino acid ligands. A similar structural analogy could be established for the silver complexes on the basis of SSNMR. The activity against the bacterial pathogens Pseudomonas aeruginosa, Escherichia coli, and Staphylococcus aureus was assessed by carrying out disk diffusion assays on lysogeny agar media showing that, while there is no significant effect arising from the use of enantiopure or chiral amino acids, the coordination polymers exert an appreciable antimicrobial activity comparable, when not superior, to that of the metal salts alone. Full article

(This article belongs to the Special Issue Current Advances in Metal Complexes with Biological Activity)

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Open AccessArticle

MAPLE Processed Nanostructures for Antimicrobial Coatings

Ariana Hudiță

Valentina Grumezescu

Oana Gherasim

Alexandru Mihai Grumezescu

Gabriela Dorcioman

Irina Negut

Ovidiu-Cristian Oprea

and

Int. J. Mol. Sci. 2022, 23(23), 15355; https://doi.org/10.3390/ijms232315355 - 05 Dec 2022

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Abstract

Despite their great benefits for debilitated patients, indwelling devices are prone to become easily colonized by resident and opportunistic microorganisms, which have the ability to attach to their surfaces and form highly specialized communities called biofilms. These are extremely resistant to host defense mechanisms and antibiotics, leading to treatment failure and device replacement, but also to life-threatening complications. In this study, we aimed to optimize a silica (SiO₂)-coated magnetite (Fe₃O₄)-based nanosystem containing the natural antimicrobial agent, eugenol (E), suitable for MAPLE (matrix-assisted pulsed laser evaporation) deposition as a bioactive coating for biomedical applications. X-ray diffraction, thermogravimetric analysis, Fourier-transform infrared spectroscopy, and transmission electron microscopy investigations were employed to characterize the obtained nanosystems. The in vitro tests evidenced the superior biocompatibility of such nanostructured coatings, as revealed by their non-cytotoxic activity and ability to promote cellular proliferation and sustain normal cellular development of dermal fibroblasts. Moreover, the obtained nanocoatings did not induce proinflammatory events in human blood samples. Our studies demonstrated that Fe₃O₄ NPs can improve the antimicrobial activity of E, while the use of a SiO₂ matrix may increase its efficiency over prolonged periods of time. The Fe₃O₄@SiO₂ nanosystems showed excellent biocompatibility, sustaining human dermal fibroblasts’ viability, proliferation, and typical architecture. More, the novel coatings lack proinflammatory potential as revealed by the absence of proinflammatory cytokine expression in response to human blood sample interactions. Full article

(This article belongs to the Special Issue Current Advances in Metal Complexes with Biological Activity)

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Open AccessArticle

Highly Charged Ru(II) Polypyridyl Complexes as Photosensitizer Agents in Photodynamic Therapy of Epithelial Ovarian Cancer Cells

Luca Conti

Gina Elena Giacomazzo

Patrick Severin Sfragano

and

Int. J. Mol. Sci. 2022, 23(21), 13302; https://doi.org/10.3390/ijms232113302 - 01 Nov 2022

Cited by 2 | Viewed by 1311

Abstract

Ovarian cancer recurrence is frequent and associated with chemoresistance, leading to extremely poor prognosis. Herein, we explored the potential anti-cancer effect of a series of highly charged Ru(II)-polypyridyl complexes as photosensitizers in photodynamic therapy (PDT), which were able to efficiently sensitize the formation of singlet oxygen upon irradiation (Ru1²⁺ and Ru2²⁺) and to produce reactive oxygen species (ROS) in their corresponding dinuclear metal complexes with the Fenton active Cu(II) ion/s ([CuRu1]⁴⁺ and [Cu₂Ru2]⁶⁺). Their cytotoxic and anti-tumor effects were evaluated on human ovarian cancer A2780 cells both in the absence or presence of photoirradiation, respectively. All the compounds tested were well tolerated under dark conditions, whereas they switched to exert anti-tumor activity following photoirradiation. The specific effect was mediated by the onset of programed cell death, but only in the case of Ru1²⁺ and Ru2²⁺ was preceded by the loss of mitochondrial membrane potential soon after photoactivation and ROS production, thus supporting the occurrence of apoptosis via type II photochemical reactions. Thus, Ru(II)-polypyridyl-based photosensitizers represent challenging tools to be further investigated in the identification of new therapeutic approaches to overcome the innate chemoresistance to platinum derivatives of some ovarian epithelial cancers and to find innovative drugs for recurrent ovarian cancer. Full article

(This article belongs to the Special Issue Current Advances in Metal Complexes with Biological Activity)

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Review

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Open AccessReview

Metal Complexes as Promising Matrix Metalloproteinases Regulators

Yen Thi Nguyen

Namdoo Kim

and

Hyuck Jin Lee

Int. J. Mol. Sci. 2023, 24(2), 1258; https://doi.org/10.3390/ijms24021258 - 09 Jan 2023

Cited by 1 | Viewed by 1185

Abstract

Nowadays, cancers and dementia, such as Alzheimer’s disease, are the most fatal causes of death. Many studies tried to understand the pathogenesis of those diseases clearly and develop a promising way to treat the diseases. Matrix metalloproteinases (MMPs) have been reported to be involved in the pathology of cancers and AD through tumor cell movement and amyloid degradation. Therefore, control of the levels and actions of MMPs, especially MMP-2 and MMP-9, is necessary to care for and/or cure cancer and AD. Various molecules have been examined for their potential application as regulators of MMPs expression and activity. Among the molecules, multiple metal complexes have shown advantages, including simple synthesis, less toxicity and specificity toward MMPs in cancer cells or in the brain. In this review, we summarize the recent studies and knowledge of metal complexes (e.g., Pt-, Ru-, Au-, Fe-, Cu-, Ni-, Zn-, and Sn-complexes) targeting MMPs and their potentials for treating and/or caring the most fatal human diseases, cancers and AD. Full article

(This article belongs to the Special Issue Current Advances in Metal Complexes with Biological Activity)

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