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New Advances on Photosensitiser or Inhibitors Molecules for Cancer Treatment
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New Advances on Photosensitiser or Inhibitors Molecules for Cancer Treatment

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: 20 March 2025 | Viewed by 10252

Special Issue Editor

Prof. Dr. Maria Raposo

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Guest Editor
LIBPhys, Departmento de Física, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, Campus da Caparica, 2829-516 Caparica, Portugal
Interests: sensors; organic devices; layer-by-layer films; solid state physics; optical devices; drug delivery systems; liposomes; Langmuir films; adsorption; effect of radiation on biological matter
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues, 

The photodynamic therapy concept in which low energy radiation is used on cancer cells with added DNA targeted photosensitizing molecules. The irradiation reaching these molecules enhances the generation of reactive oxygen species (ROS) which possesses cytotoxic effect on DNA. The use of photosensitizing molecules, which can intercalate with DNA helix through physical interactions instead of covalent bonds, prevents damage to normal cells and create radicals in cancer cells when submitted to radiation. But the action of photosensitizing molecules can be maximized if the DNA repair machinery is constrained by affecting the DNA repair proteins using inhibitor molecules that can reduce the effect of the repair and thus sensitize the cells for radiation therapy. This Special Issue of IJMS focuses on the latest developments on new photosensitiser or inhibitors molecules and on the effect of photosensitiser or inhibitors molecules encapsulated or not on biological molecules as DNA and/or DNA repair proteins and on cells in presence of radiation. This Special Issue, “New Advances on Photosensitiser or Inhibitors Molecules for Cancer Treatment”, invites review articles and full-length papers that explore the development or/and the role of photosensitiser or inhibitors molecules near of biological molecules or of cells in presence of radiation. Moreover, papers providing new insights into the development of new systems of encapsulation of these photosensitiser or inhibitors molecules for easier delivery to tumour area are also encouraged.

Dr. Maria Raposo
Guest Editor

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Keywords

  • photosensitiser molecules
  • inhibitors molecules
  • biomolecules damage
  • DNA-intercalators
  • oxidative stress
  • cell/tissue specificity
  • drug delivery systems
  • photodynamic therapy

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Published Papers (5 papers)

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Research

17 pages, 3275 KiB  
Article
Hijacking 5-Fluorouracil Chemoresistance in Triple Negative Breast Cancer via microRNAs-Loaded Chitosan Nanoparticles
by Sherif Ashraf Fahmy, Noha Khalil Mahdy, Adham H. Mohamed, Fatma A. Mokhtar and Rana A. Youness
Int. J. Mol. Sci. 2024, 25(4), 2070; https://doi.org/10.3390/ijms25042070 - 8 Feb 2024
Viewed by 2094
Abstract
Chemotherapy is still the mainstay of treatment for triple-negative breast cancer (TNBC) patients. Yet only 20% of TNBC patients show a pathologic complete response (pCR) after neoadjuvant chemotherapy. 5-Fluorouracil (5-FU) is a stable cornerstone in all recommended chemotherapeutic protocols for TNBC patients. However, [...] Read more.
Chemotherapy is still the mainstay of treatment for triple-negative breast cancer (TNBC) patients. Yet only 20% of TNBC patients show a pathologic complete response (pCR) after neoadjuvant chemotherapy. 5-Fluorouracil (5-FU) is a stable cornerstone in all recommended chemotherapeutic protocols for TNBC patients. However, TNBC patients’ innate or acquired chemoresistance rate for 5-FU is steeply escalating. This study aims to unravel the mechanism behind the chemoresistance of 5-FU in the aggressive TNBC cell line, MDA-MB-231 cells, to explore further the role of the tumor suppressor microRNAs (miRNAs), miR-1275, miR-615-5p, and Let-7i, in relieving the 5-FU chemoresistance in TNBC, and to finally provide a translational therapeutic approach to co-deliver 5-FU and the respective miRNA oligonucleotides using chitosan-based nanoparticles (CsNPs). In this regard, cellular viability and proliferation were investigated using MTT and BrdU assays, respectively. 5-FU was found to induce JAK/STAT and PI3K/Akt/mTOR pathways in MDA-MB-231 cells with contaminant repression of their upstream regulators miR-1275, miR-615-5p, and Let-7i. Moreover, CsNPs prepared using the ionic gelation method were chosen and studied as nanovectors of 5-FU and a combination of miRNA oligonucleotides targeting TNBC. The average particle sizes, surface charges, and morphologies of the different CsNPs were characterized using dynamic light scattering (DLS) and transmission electron microscopy (TEM), respectively. In addition, the encapsulation efficiency (EE%), drug loading capacity (DLC%), and release manner at two different pH values were assessed. In conclusion, the novel CsNPs co-loaded with 5-FU and the combination of the three miRNA oligonucleotides demonstrated synergistic activity and remarkable repression in cellular viability and proliferation of TNBC cells through alleviating the chemoresistance to 5-FU. Full article
(This article belongs to the Special Issue New Advances on Photosensitiser or Inhibitors Molecules for Cancer Treatment)
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14 pages, 9741 KiB  
Article
HSA-ZW800-PEG for Enhanced Optophysical Stability and Tumor Targeting
by Paul Jang, Jinhui Ser, Kevin Cardenas, Hajin Joanne Kim, Morgan Hickey, Jiseon Jang, Jason Gladstone, Aisha Bailey, Jason Dinh, Vy Nguyen, Emma DeMarco, Surbhi Srinivas, Homan Kang, Satoshi Kashiwagi, Kai Bao, Atsushi Yamashita and Hak Soo Choi
Int. J. Mol. Sci. 2024, 25(1), 559; https://doi.org/10.3390/ijms25010559 - 31 Dec 2023
Cited by 3 | Viewed by 1636
Abstract
Small molecule fluorophores often face challenges such as short blood half-life, limited physicochemical and optical stability, and poor pharmacokinetics. To overcome these limitations, we conjugated the zwitterionic near-infrared fluorophore ZW800-PEG to human serum albumin (HSA), creating HSA-ZW800-PEG. This conjugation notably improves chemical, physical, [...] Read more.
Small molecule fluorophores often face challenges such as short blood half-life, limited physicochemical and optical stability, and poor pharmacokinetics. To overcome these limitations, we conjugated the zwitterionic near-infrared fluorophore ZW800-PEG to human serum albumin (HSA), creating HSA-ZW800-PEG. This conjugation notably improves chemical, physical, and optical stability under physiological conditions, addressing issues commonly encountered with small molecules in biological applications. Additionally, the high molecular weight and extinction coefficient of HSA-ZW800-PEG enhances biodistribution and tumor targeting through the enhanced permeability and retention effect. The unique distribution and elimination dynamics, along with the significantly extended blood half-life of HSA-ZW800-PEG, contribute to improved tumor targetability in both subcutaneous and orthotopic xenograft tumor-bearing animal models. This modification not only influences the pharmacokinetic profile, affecting retention time and clearance patterns, but also enhances bioavailability for targeting tissues. Our study guides further development and optimization of targeted imaging agents and drug-delivery systems. Full article
(This article belongs to the Special Issue New Advances on Photosensitiser or Inhibitors Molecules for Cancer Treatment)
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36 pages, 9847 KiB  
Article
Imidazo-Pyrazole-Loaded Palmitic Acid and Polystyrene-Based Nanoparticles: Synthesis, Characterization and Antiproliferative Activity on Chemo-Resistant Human Neuroblastoma Cells
by Giulia Elda Valenti, Barbara Marengo, Marco Milanese, Guendalina Zuccari, Chiara Brullo, Cinzia Domenicotti and Silvana Alfei
Int. J. Mol. Sci. 2023, 24(19), 15027; https://doi.org/10.3390/ijms241915027 - 9 Oct 2023
Cited by 2 | Viewed by 1671
Abstract
Neuroblastoma (NB) is a childhood cancer, commonly treated with drugs, such as etoposide (ETO), whose efficacy is limited by the onset of resistance. Here, aiming at identifying new treatments for chemo-resistant NB, the effects of two synthesized imidazo-pyrazoles (IMPs) (4G and 4I [...] Read more.
Neuroblastoma (NB) is a childhood cancer, commonly treated with drugs, such as etoposide (ETO), whose efficacy is limited by the onset of resistance. Here, aiming at identifying new treatments for chemo-resistant NB, the effects of two synthesized imidazo-pyrazoles (IMPs) (4G and 4I) were investigated on ETO-sensitive (HTLA-230) and ETO-resistant (HTLA-ER) NB cells, detecting 4I as the more promising compound, that demonstrated IC50 values lower than those of ETO on HTLA ER. Therefore, to further improve the activity of 4I, we developed 4I-loaded palmitic acid (PA) and polystyrene-based (P5) cationic nanoparticles (P5PA-4I NPs) with high drug loading (21%) and encapsulation efficiency (97%), by a single oil-in-water emulsification technique. Biocompatible PA was adopted as an emulsion stabilizer, while synthesized P5 acted as an encapsulating agent, solubilizer and hydrophilic–lipophilic balance (HLB) improver. Optic microscopy and cytofluorimetric analyses were performed to investigate the micromorphology, size and complexity distributions of P5PA-4I NPs, which were also structurally characterized by chemometric-assisted Fourier transform infrared spectroscopy (FTIR). Potentiometric titrations allowed us to estimate the milliequivalents of PA and basic nitrogen atoms present in NPs. P5PA-4I NPs afforded dispersions in water with excellent buffer capacity, essential to escape lysosomal degradation and promote long residence time inside cells. They were chemically stable in an aqueous medium for at least 40 days, while in dynamic light scattering (DLS) analyses, P5PA-4I showed a mean hydrodynamic diameter of 541 nm, small polydispersity (0.194), and low positive zeta potentials (+8.39 mV), assuring low haemolytic toxicity. Biological experiments on NB cells, demonstrated that P5PA-4I NPs induced ROS-dependent cytotoxic effects significantly higher than those of pristine 4I, showing a major efficacy compared to ETO in reducing cell viability in HTLA-ER cells. Collectively, this 4I-based nano-formulation could represent a new promising macromolecular platform to develop a new delivery system able to increase the cytotoxicity of the anticancer drugs. Full article
(This article belongs to the Special Issue New Advances on Photosensitiser or Inhibitors Molecules for Cancer Treatment)
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12 pages, 6415 KiB  
Article
Design, Synthesis and Antitumor Activity of 1H-indazole-3-amine Derivatives
by Congyu Wang, Mei Zhu, Xuesha Long, Qin Wang, Zhenchao Wang and Guiping Ouyang
Int. J. Mol. Sci. 2023, 24(10), 8686; https://doi.org/10.3390/ijms24108686 - 12 May 2023
Cited by 4 | Viewed by 2225
Abstract
A series of indazole derivatives were designed and synthesized by molecular hybridization strategy, and these compounds were evaluated the inhibitory activities against human cancer cell lines of lung (A549), chronic myeloid leukemia (K562), prostate (PC-3), and hepatoma (Hep-G2) by methyl thiazolyl tetrazolium (MTT) [...] Read more.
A series of indazole derivatives were designed and synthesized by molecular hybridization strategy, and these compounds were evaluated the inhibitory activities against human cancer cell lines of lung (A549), chronic myeloid leukemia (K562), prostate (PC-3), and hepatoma (Hep-G2) by methyl thiazolyl tetrazolium (MTT) colorimetric assay. Among these, compound 6o exhibited a promising inhibitory effect against the K562 cell line with the IC50 (50% inhibition concentration) value of 5.15 µM, and this compound showed great selectivity for normal cell (HEK-293, IC50 = 33.2 µM). Moreover, compound 6o was confirmed to affect apoptosis and cell cycle possibly by inhibiting Bcl2 family members and the p53/MDM2 pathway in a concentration-dependent manner. Overall, this study indicates that compound 6o could be a promising scaffold to develop an effective and low-toxic anticancer agent. Full article
(This article belongs to the Special Issue New Advances on Photosensitiser or Inhibitors Molecules for Cancer Treatment)
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16 pages, 3712 KiB  
Article
Phototoxic Potential of Different DNA Intercalators for Skin Cancer Therapy: In Vitro Screening
by Thais P. Pivetta, Tânia Vieira, Jorge C. Silva, Paulo A. Ribeiro and Maria Raposo
Int. J. Mol. Sci. 2023, 24(6), 5602; https://doi.org/10.3390/ijms24065602 - 15 Mar 2023
Cited by 3 | Viewed by 2069
Abstract
Photodynamic therapy is a minimally invasive procedure used in the treatment of several diseases, including some types of cancer. It is based on photosensitizer molecules, which, in the presence of oxygen and light, lead to the formation of reactive oxygen species (ROS) and [...] Read more.
Photodynamic therapy is a minimally invasive procedure used in the treatment of several diseases, including some types of cancer. It is based on photosensitizer molecules, which, in the presence of oxygen and light, lead to the formation of reactive oxygen species (ROS) and consequent cell death. The selection of the photosensitizer molecule is important for the therapy efficiency; therefore, many molecules such as dyes, natural products and metallic complexes have been investigated regarding their photosensitizing potential. In this work, the phototoxic potential of the DNA-intercalating molecules—the dyes methylene blue (MB), acridine orange (AO) and gentian violet (GV); the natural products curcumin (CUR), quercetin (QT) and epigallocatechin gallate (EGCG); and the chelating compounds neocuproine (NEO), 1,10-phenanthroline (PHE) and 2,2′-bipyridyl (BIPY)—were analyzed. The cytotoxicity of these chemicals was tested in vitro in non-cancer keratinocytes (HaCaT) and squamous cell carcinoma (MET1) cell lines. A phototoxicity assay and the detection of intracellular ROS were performed in MET1 cells. Results revealed that the IC50 values of the dyes and curcumin in MET1 cells were lower than 30 µM, while the values for the natural products QT and EGCG and the chelating agents BIPY and PHE were higher than 100 µM. The IC50 of MB and AO was greatly affected by irradiation when submitted to 640 nm and 457 nm light sources, respectively. ROS detection was more evident for cells treated with AO at low concentrations. In studies with the melanoma cell line WM983b, cells were more resistant to MB and AO and presented slightly higher IC50 values, in line with the results of the phototoxicity assays. This study reveals that many molecules can act as photosensitizers, but the effect depends on the cell line and the concentration of the chemical. Finally, significant photosensitizing activity of acridine orange at low concentrations and moderate light doses was demonstrated. Full article
(This article belongs to the Special Issue New Advances on Photosensitiser or Inhibitors Molecules for Cancer Treatment)
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