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Keywords = dark and photoinduced toxicity

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16 pages, 5747 KB  
Article
Method for Isolating Hypericin from Hypericum perforatum and Preparing Its Micelles for Biomedical Applications
by Dmitry Medvedev, Vasilisa Dalinina, Polina Golik, Polina Lavrinova, Ekaterina Plotnikova, Maksim Usachev, Veronika Usatova, Mikhail Grin, Tatiana Abakumova and Petr Ostroverkhov
Molecules 2026, 31(12), 2048; https://doi.org/10.3390/molecules31122048 - 11 Jun 2026
Viewed by 499
Abstract
Hypericin (Hyp) is a naturally occurring photosensitizer (PS) exhibiting a broad spectrum of biological activities. However, its high hydrophobicity significantly limits its medical applicability. This study aimed to develop an efficient method for extracting Hyp from Hypericum perforatum L. biomass and to obtain [...] Read more.
Hypericin (Hyp) is a naturally occurring photosensitizer (PS) exhibiting a broad spectrum of biological activities. However, its high hydrophobicity significantly limits its medical applicability. This study aimed to develop an efficient method for extracting Hyp from Hypericum perforatum L. biomass and to obtain its water-soluble micellar formulation. A protocol for Hyp isolation from the aerial parts of the plant was established, involving a preliminary defatting step using a Soxhlet apparatus, followed by ultrasonic-assisted extraction with acetone. The water-soluble formulation was prepared via the thin-film hydration method using the nonionic block copolymer Pluronic F-127. The resulting micelles demonstrated colloidal stability, with a mean hydrodynamic diameter of approximately 30 nm. A high Hyp loading efficiency was achieved, with an encapsulation efficiency (EE) of 95.4 ± 2.7%, yielding a concentration of 600.6 ± 16.6 µM within the micellar formulation. In vitro biological studies were performed using the murine GL261 glioblastoma cell line. The micellar Hyp formulation exhibited efficient time-dependent cellular accumulation and photoinduced cytotoxicity, with no observable dark toxicity. The proposed method enables the production of a stable Hyp formulation that retains its photosensitizing properties, thereby opening promising avenues for its application in photodynamic and sonodynamic therapies. Full article
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16 pages, 10397 KB  
Article
A Nonanuclear Pd-Based Coordination Cage Featuring Ni-Chelated Porphyrin Ligand for Cancer Therapy via Combination of Chemodynamic and Photodynamic Modalities
by Meng-Lin Dong, Ye Ning, Yuan-Hui Jia, Wen-Hua Zhang, Wenqiang Lu and Yiming Mao
Molecules 2026, 31(11), 1874; https://doi.org/10.3390/molecules31111874 - 29 May 2026
Viewed by 556
Abstract
Reactive oxygen species (ROS)-mediated cancer therapy has attracted extensive attention due to its high spatiotemporal selectivity and minimal side effects. Herein, we report a nonanuclear Pd-based coordination cage of Pd6-TMPP(Ni), constructed from Ni-chelated TMPP(Ni) as the metalloligand and Pd2+ [...] Read more.
Reactive oxygen species (ROS)-mediated cancer therapy has attracted extensive attention due to its high spatiotemporal selectivity and minimal side effects. Herein, we report a nonanuclear Pd-based coordination cage of Pd6-TMPP(Ni), constructed from Ni-chelated TMPP(Ni) as the metalloligand and Pd2+ ions (H2TMPP = meso-tetrakis (6-methylpyridin-3-yl) porphyrin). Pd6-TMPP(Ni) integrates dual ROS-generation for cancer therapy, viz., hydroxyl radical (•OH) production and photoinduced singlet oxygen (1O2) generation. In vitro cytotoxicity assays against cancer cell lines NCI-H82 (lung cancer), A549 (lung cancer), KYSE-510 (esophageal cancer), and Te-1 (esophageal cancer) reveal its potent dark toxicity (IC50: 1.9–2.1 μmol L−1) and phototoxicity (IC50: 0.8–1.5 μmol L−1), which is attributed to enhanced intracellular ROS accumulation. This work develops a versatile therapeutic platform that harnesses Ni-induced •OH for chemodynamic therapy (CDT) and porphyrin-generated 1O2 for photodynamic therapy (PDT), thereby mitigating the oxygen dependence of conventional PDT. Full article
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17 pages, 6220 KB  
Article
Erbium Orthoniobate-Tantalates: Structural, Luminescent and Mechanical Properties of ErNbxTa1−xO4 Ceramics and Bactericidal Properties of ErNbO4 Powder
by Mikhail Palatnikov, Olga Shcherbina, Nadezhda Fokina, Maxim Smirnov, Elena Zelenina, Sofja Masloboeva and Diana Manukovskaya
Ceramics 2025, 8(4), 130; https://doi.org/10.3390/ceramics8040130 - 22 Oct 2025
Viewed by 1468
Abstract
Fine powders of erbium niobate-tantalates ErNbxTa1−xO4 (x = 0; 0.1; 0.3; 0.5; 0.7; 0.9; 1) have been synthesized by the liquid-phase method in this study. Ceramic samples have been prepared using conventional sintering from these powders. Rietveld refinement [...] Read more.
Fine powders of erbium niobate-tantalates ErNbxTa1−xO4 (x = 0; 0.1; 0.3; 0.5; 0.7; 0.9; 1) have been synthesized by the liquid-phase method in this study. Ceramic samples have been prepared using conventional sintering from these powders. Rietveld refinement of XRD patterns of polycrystals determined the phase composition and clarified the parameters of the phase structure of ErNbxTa1−xO4 solid solutions depending on the Nb/Ta ratio. The morphological features of the microstructure of erbium niobate-tantalate ceramics have been studied. Their mechanical properties, strength characteristics (Young’s modulus, microhardness) and critical stress intensity factor of the first kind KIC have been estimated. The photoluminescent properties of ceramic solid solutions of erbium niobate-tantalates depending on the composition have been studied. Dark and photoinduced toxicity of finely dispersed ErNbO4 powders have been studied in relation to Gram-positive, Gram-negative and spore-forming microorganisms. The best indicators of antibacterial activity of ErNbO4 have been demonstrated in relation to Gram-positive cells of Micrococcus sp. The discovered properties open up the possibility of not only traditional use as functional materials, but also the use of these materials for disinfection of surfaces, water and biological tissues. Full article
(This article belongs to the Topic High Performance Ceramic Functional Materials)
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17 pages, 2621 KB  
Article
Synthesis and Biological Properties of EGFR-Targeted Photosensitizer Based on Cationic Porphyrin
by Yulia S. Bortnevskaya, Nikita A. Shiryaev, Nikita S. Zakharov, Oleg O. Kitoroage, Margarita A. Gradova, Natalia Yu. Karpechenko, Alexander S. Novikov, Elena D. Nikolskaya, Mariia R. Mollaeva, Nikita G. Yabbarov, Natal’ya A. Bragina and Kseniya A. Zhdanova
Pharmaceutics 2023, 15(4), 1284; https://doi.org/10.3390/pharmaceutics15041284 - 19 Apr 2023
Cited by 19 | Viewed by 3412
Abstract
Photodynamic therapy (PDT) in oncology is characterized by low invasiveness, minimal side effects, and little tissue scarring. Increasing the selectivity of PDT agents toward a cellular target is a new approach intended to improve this method. This study is devoted to the design [...] Read more.
Photodynamic therapy (PDT) in oncology is characterized by low invasiveness, minimal side effects, and little tissue scarring. Increasing the selectivity of PDT agents toward a cellular target is a new approach intended to improve this method. This study is devoted to the design and synthesis of a new conjugate based on meso-arylporphyrin with a low-molecular-weight tyrosine kinase inhibitor, Erlotinib. A nano-formulation based on Pluronic F127 micelles was obtained and characterized. The photophysical and photochemical properties and biological activity of the studied compounds and their nano-formulation were studied. A significant, 20–40-fold difference between the dark and photoinduced activity was achieved for the conjugate nanomicelles. After irradiation, the studied conjugate nanomicelles were 1.8 times more toxic toward the EGFR-overexpressing cell line MDA-MB-231 compared to the conditionally normal NKE cells. The IC50 was 0.073 ± 0.014 μM for the MDA-MB-231 cell line and 0.13 ± 0.018 μM for NKE cells after irradiation for the target conjugate nanomicelles. Full article
(This article belongs to the Special Issue Cancer Therapy Resistance: Choosing Kinase Inhibitors)
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40 pages, 12372 KB  
Review
Lights and Dots toward Therapy—Carbon-Based Quantum Dots as New Agents for Photodynamic Therapy
by Svetlana Jovanović, Zoran Marković, Milica Budimir, Jovana Prekodravac, Danica Zmejkoski, Dejan Kepić, Aurelio Bonasera and Biljana Todorović Marković
Pharmaceutics 2023, 15(4), 1170; https://doi.org/10.3390/pharmaceutics15041170 - 6 Apr 2023
Cited by 59 | Viewed by 7317
Abstract
The large number of deaths induced by carcinoma and infections indicates that the need for new, better, targeted therapy is higher than ever. Apart from classical treatments and medication, photodynamic therapy (PDT) is one of the possible approaches to cure these clinical conditions. [...] Read more.
The large number of deaths induced by carcinoma and infections indicates that the need for new, better, targeted therapy is higher than ever. Apart from classical treatments and medication, photodynamic therapy (PDT) is one of the possible approaches to cure these clinical conditions. This strategy offers several advantages, such as lower toxicity, selective treatment, faster recovery time, avoidance of systemic toxic effects, and others. Unfortunately, there is a small number of agents that are approved for usage in clinical PDT. Novel, efficient, biocompatible PDT agents are, thus, highly desired. One of the most promising candidates is represented by the broad family of carbon-based quantum dots, such as graphene quantum dots (GQDs), carbon quantum dots (CQDs), carbon nanodots (CNDs), and carbonized polymer dots (CPDs). In this review paper, these new smart nanomaterials are discussed as potential PDT agents, detailing their toxicity in the dark, and when they are exposed to light, as well as their effects on carcinoma and bacterial cells. The photoinduced effects of carbon-based quantum dots on bacteria and viruses are particularly interesting, since dots usually generate several highly toxic reactive oxygen species under blue light. These species are acting as bombs on pathogen cells, causing various devastating and toxic effects on those targets. Full article
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13 pages, 3413 KB  
Article
Preliminary Toxicity Evaluation of a Porphyrin Photosensitizer in an Alternative Preclinical Model
by Miryam Chiara Malacarne, Maristella Mastore, Marzia Bruna Gariboldi, Maurizio Francesco Brivio and Enrico Caruso
Int. J. Mol. Sci. 2023, 24(4), 3131; https://doi.org/10.3390/ijms24043131 - 5 Feb 2023
Cited by 6 | Viewed by 2983
Abstract
In photodynamic therapy (PDT), a photosensitizer (PS) excited with a specific wavelength, and in the presence of oxygen, gives rise to photochemical reactions that lead to cell damage. Over the past few years, larval stages of the G. mellonella moth have proven to [...] Read more.
In photodynamic therapy (PDT), a photosensitizer (PS) excited with a specific wavelength, and in the presence of oxygen, gives rise to photochemical reactions that lead to cell damage. Over the past few years, larval stages of the G. mellonella moth have proven to be an excellent alternative animal model for in vivo toxicity testing of novel compounds and virulence testing. In this article, we report a series of preliminary studies on G. mellonella larvae to evaluate the photoinduced stress response by a porphyrin (PS) (TPPOH). The tests performed evaluated PS toxicity on larvae and cytotoxicity on hemocytes, both in dark conditions and following PDT. Cellular uptake was also evaluated by fluorescence and flow cytometry. The results obtained demonstrate how the administration of PS and subsequent irradiation of larvae affects not only larvae survival rate, but also immune system cells. It was also possible to verify PS’s uptake and uptake kinetics in hemocytes, observing a maximum peak at 8 h. Given the results obtained in these preliminary tests, G. mellonella appears to be a promising model for preclinical PS tests. Full article
(This article belongs to the Special Issue Materials for Photobiology 2.0)
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15 pages, 4105 KB  
Article
Efficient Removal of Cr(VI) by TiO2 Based Micro-Nano Reactor via the Synergy of Adsorption and Photocatalysis
by Yu Song, Xi Lu, Zhibao Liu, Wenfei Liu, Ligang Gai, Xiang Gao and Hongfang Ma
Nanomaterials 2022, 12(2), 291; https://doi.org/10.3390/nano12020291 - 17 Jan 2022
Cited by 37 | Viewed by 4827
Abstract
The low-toxicity treatment of chromium-containing wastewater represents an important way of addressing key environmental problems. In this study, a core-shell structural ZIF-8@TiO2 photocatalyst was synthesized by a simple one-step hydrothermal method. The obtained composite photocatalyst possessed improved photocatalytic activity compared with TiO [...] Read more.
The low-toxicity treatment of chromium-containing wastewater represents an important way of addressing key environmental problems. In this study, a core-shell structural ZIF-8@TiO2 photocatalyst was synthesized by a simple one-step hydrothermal method. The obtained composite photocatalyst possessed improved photocatalytic activity compared with TiO2. The results indicated that the optimized ZIF-8@TiO2 composite exhibited the highest removal efficiency with 93.1% of Cr(VI) after 120 min under UV-vis irradiation. The removal curves and XPS results indicated that the adsorbed Cr(VI) on the ZIF-8 during the dark process was preferentially reduced. The superior removal efficiency of ZIF-8@TiO2 is attributed to the combination of both high adsorption of ZIF-8, which attracted Cr(VI) on the composite surface, and the high separation efficiency of photo-induced electron-hole pairs. For the mixture of wastewater that contained methyl orange and Cr(VI), 97.1% of MO and 99.7% of Cr(VI) were removed after 5 min and 60 min light irradiation, respectively. The high removal efficiency of multiple pollutants provides promising applications in the field of Cr(VI) contaminated industrial wastewater treatment. Full article
(This article belongs to the Special Issue State-of-the-Art Environmental Nanoscience and Nanotechnology)
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15 pages, 1903 KB  
Article
Influence of Polymer Charge on the Localization and Dark- and Photo-Induced Toxicity of a Potential Type I Photosensitizer in Cancer Cell Models
by Mikael Lindgren, Odrun A. Gederaas, Monica Siksjø, Tom A. Hansen, Lena Chen, Bastien Mettra, Chantal Andraud and Cyrille Monnereau
Molecules 2020, 25(5), 1127; https://doi.org/10.3390/molecules25051127 - 3 Mar 2020
Cited by 4 | Viewed by 4501
Abstract
A current trend within photo-dynamic therapy (PDT) is the development of molecular systems targeting hypoxic tumors. Thus, type I PDT sensitizers could here overcome traditional type II molecular systems that rely on the photo-initiated production of toxic singlet oxygen. Here, we investigate the [...] Read more.
A current trend within photo-dynamic therapy (PDT) is the development of molecular systems targeting hypoxic tumors. Thus, type I PDT sensitizers could here overcome traditional type II molecular systems that rely on the photo-initiated production of toxic singlet oxygen. Here, we investigate the cell localization properties and toxicity of two polymeric anthracene-based fluorescent probes (neutral Ant-PHEA and cationic Ant-PIm). The cell death and DNA damage of Chinese hamster ovary cancer cells (CHO-K1) were characterized as combining PDT, cell survival studies (MTT-assay), and comet assay. Confocal microscopy was utilized on samples incubated together with either DRAQ5, Lyso Tracker Red, or Mito Tracker Deep Red in order to map the localization of the sensitizer into the nucleus and other cell compartments. While Ant-PHEA did not cause significant damage to the cell, Ant-PIm showed increased cell death upon illumination, at the cost of a significant dark toxicity. Both anthracene chromophores localized in cell compartments of the cytosol. Ant-PIm showed a markedly improved selectivity toward lysosomes and mitochondria, two important biological compartments for the cell’s survival. None of the two anthracene chromophores showed singlet oxygen formation upon excitation in solvents such as deuterium oxide or methanol. Conclusively, the significant photo-induced cell death that could be observed with Ant-PIm suggests a possible type I PDT mechanism rather than the usual type II mechanism. Full article
(This article belongs to the Special Issue Photodynamic Therapy in Cancer Treatment)
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