Special Issue "Applications of Medicinal Bioinorganic Chemistry"

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (31 January 2021).

Special Issue Editors

Prof. Dr. Guido Crisponi
Website
Guest Editor
Faculty of Biology and Pharmacy, University of Cagliari, Cagliari, Italy
Interests: analytical chemistry; bioinorganic chemistry; chelation therapy
Dr. Alicia Dominguez-Martin
Website
Guest Editor
Department of Inorganic Chemistry, Faculty of Pharmacy, University of Granada, 18071 Granada, Spain
Interests: bioinorganic chemistry; nucleic acids; molecular recognition; multicomponent pharmaceutical materials; co-drugs
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Special Issue Information

Dear Colleagues,

In this Special Issue of Pharmaceuticals entitled “Applications of Medicinal Bioinorganic Chemistry”, we aim to explore the potential of bioinorganic chemistry applied to medicinal chemistry. The growing field of bioinorganic chemistry has expanded the knowledge of the functions of metal ions in the human organism, their homeostatic control, and the influence of disequilibrium on the onset and progression of different pathologies.

The therapeutic use of metal-based drugs dates back to the starting of civilization. A number of metal-based drugs can be found in the pharmacopoeia at the start of the last century, such as mercuric ions in the treatment of syphilis; silver as one of the few drugs capable of healing infections, burns, and wounds, and preventing contagious diseases; gold in the treatment of rheumatoid arthritis;  or  lithium as an antidepressant.

Nowadays, the use of metal ions in the diagnosis and treatment of diseases is continuously increasing, finding applications as contrast agents for CT and MRI, in developing essential diagnosis techniques in modern medicine, and as drugs for clinical use in anticancer therapy. The knowledge of the molecular base of neurodegenerative diseases (Parkinson’s, Alzheimer’s, etc.) has opened the way to new drugs for the treatment of these burdensome diseases. In medicinal chemistry, chelating agents have been used for the scavenging of toxic metal ions, in particular iron chelators for thalassemia patients, which extended both life expectance and quality of life.

In this Special Issue, Pharmaceuticals welcomes original research articles and reviews devoted to life science, pharmaceutical science, and clinical science research within the field of applications of medicinal bioinorganic chemistry.

Prof. Dr. Guido Crisponi
Dr. Alicia Dominguez-Martin
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All papers will be peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 1800 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • Metal-based drugs
  • Contrast agents
  • Anticancer drugs
  • Neurodegenerative diseases
  • Chelating agents
  • Ionophores

Published Papers (6 papers)

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Research

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Open AccessArticle
Hyaluronic Acid-Modified and Doxorubicin-Loaded Gold Nanoparticles and Evaluation of Their Bioactivity
Pharmaceuticals 2021, 14(2), 101; https://doi.org/10.3390/ph14020101 - 28 Jan 2021
Abstract
Functionalized gold nanoparticles (AuNPs) have been successfully used in many fields as a result of having low cytotoxicity, good biocompatibility, excellent optical properties, and their ability to target cancer cells. Here, we synthesized AuNP carriers that were modified by hyaluronic acid (HA), polyethylene [...] Read more.
Functionalized gold nanoparticles (AuNPs) have been successfully used in many fields as a result of having low cytotoxicity, good biocompatibility, excellent optical properties, and their ability to target cancer cells. Here, we synthesized AuNP carriers that were modified by hyaluronic acid (HA), polyethylene glycol (PEG), and adipic dihydrazide (ADH). The antitumor drug doxorubicin (Dox) was loaded into AuNP carriers and attached chemically. The Au nanocomposite [email protected] was able to disperse uniformly in aqueous solution, with a diameter of 15 nm. The results of a 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide (MTT) assay indicated that AuNP carriers displayed very little toxicity toward cells in high doses, although the antitumor properties of Au nanocomposites were significantly enhanced. Cellular uptake experiments demonstrated that AuNPs modified with hyaluronic acid were more readily ingested by HepG2 and HCT-116 cells, as they have a large number of CD44 receptors. A series of experiments measuring apoptosis such as Rh123 and annexin V-FITC staining, and analysis of mitochondrial membrane potential (MMP) analysis, indicated that apoptosis played a role in the inhibition of cell proliferation by [email protected] Excessive production of reactive oxygen species (ROS) was the principal mechanism by which the Au nanocomposites inhibited cell proliferation, leading to apoptosis. Thus, the Au nanocomposites, which allowed cell imaging in real-time and induced apoptosis in specific cell types, represent theragnostic agents with potential for future clinical applications in bowel cancer. Full article
(This article belongs to the Special Issue Applications of Medicinal Bioinorganic Chemistry)
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Open AccessArticle
Combined Effect of Caspase-Dependent and Caspase-Independent Apoptosis in the Anticancer Activity of Gold Complexes with Phosphine and Benzimidazole Derivatives
Pharmaceuticals 2021, 14(1), 10; https://doi.org/10.3390/ph14010010 - 24 Dec 2020
Abstract
Since the potential anticancer activity of auranofin was discovered, gold compounds have attracted interest with a view to developing anticancer agents that follow cytotoxic mechanisms other than cisplatin. Two benzimidazole gold(I) derivatives containing triphenylphosphine (Au(pben)(PPh3)) (1) or triethylphosphine (Au(pben)(PEt [...] Read more.
Since the potential anticancer activity of auranofin was discovered, gold compounds have attracted interest with a view to developing anticancer agents that follow cytotoxic mechanisms other than cisplatin. Two benzimidazole gold(I) derivatives containing triphenylphosphine (Au(pben)(PPh3)) (1) or triethylphosphine (Au(pben)(PEt3)) (2) were prepared and characterized by standard techniques. X-ray crystal structures for 1 and 2 were solved. The cytotoxicity of 1 and 2 was tested in human neuroblastoma SH-SY5Y cells. Cells were incubated with compounds for 24 h with concentrations ranging from 10 µM to 1 nM, and the half-maximal inhibitory concentration (IC50) was determined. 1 and 2 showed an IC50 of 2.7 and 1.6 µM, respectively. In order to better understand the type of cell death induced by compounds, neuroblastoma cells were stained with Annexin-FITC and propidium iodide. The fluorescence analysis revealed that compounds were inducing apoptosis; however, pre-treatment with the caspase inhibitor Z-VAD did not reduce cell death. Analysis of compound effects on caspase-3 activity and reactive oxygen species (ROS) production in SH-SY5Y cells revealed an antiproliferative ability mediated through oxidative stress and both caspase-dependent and caspase-independent mechanisms. Full article
(This article belongs to the Special Issue Applications of Medicinal Bioinorganic Chemistry)
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Review

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Open AccessReview
Monofunctional Platinum(II) Anticancer Agents
Pharmaceuticals 2021, 14(2), 133; https://doi.org/10.3390/ph14020133 - 07 Feb 2021
Abstract
Platinum-based anticancer drugs represented by cisplatin play important roles in the treatment of various solid tumors. However, their applications are largely compromised by drug resistance and side effects. Much effort has been made to circumvent the drug resistance and general toxicity of these [...] Read more.
Platinum-based anticancer drugs represented by cisplatin play important roles in the treatment of various solid tumors. However, their applications are largely compromised by drug resistance and side effects. Much effort has been made to circumvent the drug resistance and general toxicity of these drugs. Among multifarious designs, monofunctional platinum(II) complexes with a general formula of [Pt(3A)Cl]+ (A: Ammonia or amine) stand out as a class of “non-traditional” anticancer agents hopeful to overcome the defects of current platinum drugs. This review aims to summarize the development of monofunctional platinum(II) complexes in recent years. They are classified into four categories: fluorescent complexes, photoactive complexes, targeted complexes, and miscellaneous complexes. The intention behind the designs is either to visualize the cellular distribution, or to reduce the side effects, or to improve the tumor selectivity, or inhibit the cancer cells through non-DNA targets. The information provided by this review may inspire researchers to conceive more innovative complexes with potent efficacy to shake off the drawbacks of platinum anticancer drugs. Full article
(This article belongs to the Special Issue Applications of Medicinal Bioinorganic Chemistry)
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Open AccessReview
Mercury Toxicity and Detection Using Chromo-Fluorogenic Chemosensors
Pharmaceuticals 2021, 14(2), 123; https://doi.org/10.3390/ph14020123 - 05 Feb 2021
Cited by 1
Abstract
Mercury (Hg), this non-essential heavy metal released from both industrial and natural sources entered into living bodies, and cause grievous detrimental effects to the human health and ecosystem. The monitoring of Hg2+ excessive accumulation can be beneficial to fight against the risk [...] Read more.
Mercury (Hg), this non-essential heavy metal released from both industrial and natural sources entered into living bodies, and cause grievous detrimental effects to the human health and ecosystem. The monitoring of Hg2+ excessive accumulation can be beneficial to fight against the risk associated with mercury toxicity to living systems. Therefore, there is an emergent need of novel and facile analytical approaches for the monitoring of mercury levels in various environmental, industrial, and biological samples. The chromo-fluorogenic chemosensors possess the attractive analytical parameters of low-cost, enhanced detection ability with high sensitivity, simplicity, rapid on-site monitoring ability, etc. This review was narrated to summarize the mercuric ion selective chromo-fluorogenic chemosensors reported in the year 2020. The design of sensors, mechanisms, fluorophores used, analytical performance, etc. are summarized and discussed. Full article
(This article belongs to the Special Issue Applications of Medicinal Bioinorganic Chemistry)
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Open AccessReview
Zinc(II)—The Overlooked Éminence Grise of Chloroquine’s Fight against COVID-19?
Pharmaceuticals 2020, 13(9), 228; https://doi.org/10.3390/ph13090228 - 01 Sep 2020
Cited by 2
Abstract
Zn(II) is an inhibitor of SARS-CoV-2′s RNA-dependent RNA polymerase, and chloroquine and hydroxychloroquine are Zn(II) ionophores–this statement gives a curious mind a lot to think about. We show results of the first clinical trials on chloroquine (CQ) and hydroxychloroquine (HCQ) in the [...] Read more.
Zn(II) is an inhibitor of SARS-CoV-2′s RNA-dependent RNA polymerase, and chloroquine and hydroxychloroquine are Zn(II) ionophores–this statement gives a curious mind a lot to think about. We show results of the first clinical trials on chloroquine (CQ) and hydroxychloroquine (HCQ) in the treatment of COVID-19, as well as earlier reports on the anticoronaviral properties of these two compounds and of Zn(II) itself. Other FDA-approved Zn(II) ionophores are given a decent amount of attention and are thought of as possible COVID-19 therapeutics. Full article
(This article belongs to the Special Issue Applications of Medicinal Bioinorganic Chemistry)
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Open AccessReview
Gold Nanoparticles: A New Golden Era in Oncology?
Pharmaceuticals 2020, 13(8), 192; https://doi.org/10.3390/ph13080192 - 12 Aug 2020
Cited by 3
Abstract
In recent years, the spectrum of possible applications of gold in diagnostics and therapeutic approaches in clinical practice has changed significantly, becoming surprisingly broad. Nowadays, gold-based therapeutic agents are used in the therapy of multiple human diseases, ranging from degenerative to infectious diseases [...] Read more.
In recent years, the spectrum of possible applications of gold in diagnostics and therapeutic approaches in clinical practice has changed significantly, becoming surprisingly broad. Nowadays, gold-based therapeutic agents are used in the therapy of multiple human diseases, ranging from degenerative to infectious diseases and, in particular, to cancer. At the basis of these performances of gold, there is the development of new gold-based nanoparticles, characterized by a promising risk/benefit ratio that favors their introduction in clinical trials. Gold nanoparticles appear as attractive elements in nanomedicine, a branch of modern clinical medicine, which combines high selectivity in targeting tumor cells and low toxicity. Thanks to these peculiar characteristics, gold nanoparticles appear as the starting point for the development of new gold-based therapeutic strategies in oncology. Here, the new gold-based therapeutic agents developed in recent years are described, with particular emphasis on the possible applications in clinical practice as anticancer agents, with the aim that their application will give rise to a new golden age in oncology and a breakthrough in the fight against cancer. Full article
(This article belongs to the Special Issue Applications of Medicinal Bioinorganic Chemistry)
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