Biological Activity of Metal Complexes

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

Deadline for manuscript submissions: 15 July 2025 | Viewed by 4099

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Guest Editor
Department of Biological Engineering, Massachusetts Institute of Technology, Cambridge, MA, USA
Interests: inorganic; bioinorganic; medicinal chemistry; cancer research; MRI; neurochemistry
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Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute to this Special Issue on the "Biological Activity of Metal Complexes". Metal complexes play a crucial role in various biological processes and have significant potential in therapeutic applications. This issue aims to explore recent advances in the field, focusing on the synthesis, characterization, and biological evaluation of metal complexes. The intersection of inorganic chemistry and biology offers exciting opportunities for developing novel diagnostic and therapeutic agents.

We seek high-quality research articles and reviews that address the biological activity of metal complexes. Topics of interest include, but are not limited to, the design and synthesis of metal complexes, their interactions with biological targets, and their applications in medicine and biotechnology. The goal is to highlight cutting-edge research that advances our understanding of how metal complexes can be used to develop new treatments for diseases.

Research areas may include (but are not limited to) the following:

  • Synthesis and characterization of biologically active metal complexes;
  • Mechanisms of action of metal-based drugs;
  • Metal complexes in cancer therapy;
  • Metal complexes as antimicrobial agents;
  • Bioinorganic chemistry of metal complexes;
  • Metal complexes in diagnostic imaging;
  • Toxicological studies of metal complexes.

We look forward to receiving your contributions.

Dr. Vinay K. Sharma
Guest Editor

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Keywords

  • porphyrins
  • corroles
  • theranostic agents
  • photo/sonodynamic therapy
  • stimuli-responsive materials
  • magnetic resonance imaging (MRI)
  • contrast agents
  • calcium imaging
  • neurotransmitter sensors
  • liposomes

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Published Papers (4 papers)

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Research

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12 pages, 4429 KiB  
Article
Optimized NaYF4: Er3+/Yb3+ Upconversion Nanocomplexes via Oleic Acid for Biomedical Applications
by Ha Thi Phuong, Le Thi Vinh, Tong Quang Cong, Tran Quoc Tien, Nguyen Duc Van, Vu Thi Hong Ha, Vu Ngoc Phan, Le Thi Hoi, Pham Duc Thang, Do Thi Thao and Tran Thu Huong
Inorganics 2025, 13(5), 140; https://doi.org/10.3390/inorganics13050140 - 29 Apr 2025
Viewed by 93
Abstract
This study presents the synthesis of NaYF4: Er3+/Yb3+ upconversion luminescent nanomaterials using a wet chemistry method. The role of oleic acid in influencing the size, shape, and luminescent properties of the materials was also investigated. The results showed [...] Read more.
This study presents the synthesis of NaYF4: Er3+/Yb3+ upconversion luminescent nanomaterials using a wet chemistry method. The role of oleic acid in influencing the size, shape, and luminescent properties of the materials was also investigated. The results showed that, at a suitable oleic acid concentration of 10−3 M, the obtained nanoparticles exhibited a nearly spherical morphology with diameters ranging from 150 to 250 nm and predominantly display a hexagonal (β-NaYF4) crystalline phase. Photoluminescence measurements under 980 nm laser excitation reveal that these nanoparticles emit strong, stable luminescence with narrow emission bands characteristic of Er3+ transitions. Subsequently, the nanoparticles were coated with a silica shell, functionalized with amine groups, and conjugated with IgG antibodies via glutaraldehyde (GA) to form the bio-nano complex β-NaYF4: Er3+/Yb3+@SNGA-IgG. In vitro experiments using fluorescence microscopy demonstrated that the complex effectively labels HeLa cervical cancer cells. With its robust upconversion luminescence and excellent biocompatibility, the developed nanocomplex shows promising potential for rapid pathogen detection and other biomedical applications. Full article
(This article belongs to the Special Issue Biological Activity of Metal Complexes)
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22 pages, 2686 KiB  
Article
Novel Tricarbonylrhenium-Anthrapyrazole Complexes with DNA-Binding and Antitumor Properties: In Vitro and In Vivo Pharmacokinetic Studies with 99mTc-Analogue
by Georgios Paparidis, Melpomeni Akrivou, George Psomas, Ioannis S. Vizirianakis, Antonios Hatzidimitriou, Catherine Gabriel, Dimosthenis Sarigiannis and Dionysia Papagiannopoulou
Inorganics 2024, 12(9), 254; https://doi.org/10.3390/inorganics12090254 - 21 Sep 2024
Cited by 1 | Viewed by 1360
Abstract
Organometallic complexes of fac-tricarbonylrhenium have been shown to exhibit anticancer properties. Anthrapyrazole anticancer agents act as DNA intercalators and topoisomerase IIα inhibitors, leading to double-strand breaks (DBS) and cell cycle arrest. This work involves the synthesis and biological evaluation of novel fac [...] Read more.
Organometallic complexes of fac-tricarbonylrhenium have been shown to exhibit anticancer properties. Anthrapyrazole anticancer agents act as DNA intercalators and topoisomerase IIα inhibitors, leading to double-strand breaks (DBS) and cell cycle arrest. This work involves the synthesis and biological evaluation of novel fac-tricarbonyl-rhenium complexes with anthrapyrazole derivatives. The anthrapyrazole moiety was synthesized from 1,8-dihydroxyanthraquinone, and three ligands L1, L2 and L3 were prepared. Ligand L1 coordinates via the phenolic O and pyrazole N as bidentate chelator forming the fac-[Re(CO)3(κ2-N,O)(MeOH)]-type complex, ReL1. Ligand L2 contains a pendant picolylamine N,N′-chelating system, forming the bidentate fac-[Re(CO)3(κ2-N,N′)Br]-type complex, ReL2. Ligand L3 contains a pendant picolylaminomonoacetic acid chelating system, forming a tridentate fac-[Re(CO)3(κ3-N,N′,O)]-type complex, ReL3. Complex ReL4 contains a picolylamine chelator, forming a complex with structure fac-[Re(CO)3(κ2-N,N′)Br], which was synthesized as a model for ReL2, and its coordination mode was resolved by X-ray crystallography. The complexes were characterized spectroscopically, and their biological properties were evaluated in vitro, in terms of DNA binding as well as for the cytotoxicity against CT-26 tumor cell line. Tumor cell cytotoxicity was high for ligand L2 and complex ReL2, exhibiting IC50 values of 0.36 and 0.64 μΜ, respectively. The most promising complex ReL2 was evaluated further by the preparation of its congener γ-emitting technetium-99m radio-complex, 99mTcL2. The in vitro uptake in CT26 tumor cells and the in vivo uptake in CT26 tumor-bearing mice of 99mTcL2 was determined, and its pharmacokinetic profile was established. These data indicate that the 99mTc complex has suitable properties to enter tumor cells in vitro and in vivo, and therefore ReL2 is promising for further evaluation. Full article
(This article belongs to the Special Issue Biological Activity of Metal Complexes)
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15 pages, 8725 KiB  
Article
Accomplishment of α-Chymotrypsin on Photodynamic Effect of Octa-Substituted Zn(II)- and Ga(III)-Phthalocyanines against Melanoma Cells
by Vanya Mantareva, Diana Braikova, Neli Vilhelmova-Ilieva, Ivan Angelov and Ivan Iliev
Inorganics 2024, 12(8), 204; https://doi.org/10.3390/inorganics12080204 - 29 Jul 2024
Cited by 2 | Viewed by 1304
Abstract
Octa-methylpyridiloxy-substituted Zn(II)- and Ga(III)-phthalocyanines (ZnPc1 and GaPc1) were studied on human pigmented melanoma (SH4) and keratinocyte (HaCaT) cell lines. The efficacy of ZnPc1 and GaPc1 against melanoma cells was compared to the results in the presence of a proteaseα-chymotrypsin (ChT). The [...] Read more.
Octa-methylpyridiloxy-substituted Zn(II)- and Ga(III)-phthalocyanines (ZnPc1 and GaPc1) were studied on human pigmented melanoma (SH4) and keratinocyte (HaCaT) cell lines. The efficacy of ZnPc1 and GaPc1 against melanoma cells was compared to the results in the presence of a proteaseα-chymotrypsin (ChT). The synthesis and characterization of compounds were carried out using well-known approaches. The formation of physical conjugates due to the addition of ChT was studied via absorption and fluorescence. The proteolytic activity of ChT was verified with casein as a substrate. The photosafety of compounds was proven on embryonal cells (BALB 3T3) under solar exposure (LED 360–1100 nm). The photodynamic activity of GaPc1 and ZnPc1 was studied for a concentration range of irradiation (LED 660 nm). The reduction of the proteolytic activity of ChT was observed only for the irradiation of ZnPc1 or GaPc1. GaPc1 and ChT and their conjugates, except ZnPc1 (PIF ~6), were evaluated as photo-safe to solar light (PIF < 2). The efficiency of GaPc1 was shown to be much higher than that of ZnPc1 in their individual applications. The phototherapeutic index of GaPc1 (PI = 1.71) on SH4 cells was higher for the conjugate. α-Chymotrypsin and phthalocyanine have the advantages of reducing high toxicity and increasing the phototherapeutic index. Full article
(This article belongs to the Special Issue Biological Activity of Metal Complexes)
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Review

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18 pages, 2189 KiB  
Review
Noble Metal Complexes in Cancer Therapy: Unlocking Redox Potential for Next-Gen Treatments
by Alina Stefanache, Alina Monica Miftode, Marcu Constantin, Roxana Elena Bogdan Goroftei, Iulia Olaru, Cristian Gutu, Alexandra Vornicu and Ionut Iulian Lungu
Inorganics 2025, 13(2), 64; https://doi.org/10.3390/inorganics13020064 - 19 Feb 2025
Viewed by 623
Abstract
(1) Context: Cancer is still a major problem worldwide, and traditional therapies like radiation and chemotherapy often fail to alleviate symptoms because of side effects, systemic toxicity, and mechanisms of resistance. Beneficial anticancer effects that spare healthy tissues are made possible by [...] Read more.
(1) Context: Cancer is still a major problem worldwide, and traditional therapies like radiation and chemotherapy often fail to alleviate symptoms because of side effects, systemic toxicity, and mechanisms of resistance. Beneficial anticancer effects that spare healthy tissues are made possible by the distinctive redox characteristics of noble metal complexes, especially those containing palladium, gold, silver, and platinum. (2) Methods: The redox processes, molecular targets, and therapeutic uses of noble metal complexes in cancer have been the subject of much study over the last 20 years; novel approaches to ligand design, functionalization of nanoparticles, and tumor-specific drug delivery systems are highlighted. (3) Results: Recent developments include Pt(IV) prodrugs and terpyridine-modified Pt complexes for enhanced selectivity and decreased toxicity; platinum complexes, like cisplatin, trigger reactive oxygen species (ROS) production and DNA damage. Functionalized gold nanoparticles (AuNPs) improve targeted delivery and theranostic capabilities, while gold complexes, particularly Au(I) and Au(III), inhibit redox-sensitive processes such as thioredoxin reductase (TrxR). (4) Conclusions: Ag(I)-based compounds and nanoparticles (AgNPs) induce DNA damage and mitochondrial dysfunction by taking advantage of oxidative stress. As redox-based anticancer medicines, noble metal complexes have the ability to transform by taking advantage of certain biochemical features to treat cancer more effectively and selectively. Full article
(This article belongs to the Special Issue Biological Activity of Metal Complexes)
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