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Anticancer Drug Discovery and Development II

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 July 2024 | Viewed by 11726

Special Issue Editors

Department of Biochemistry and General Chemistry, University of Rzeszów, 35-310 Rzeszów, Poland
Interests: cancer; drug delivery; magnetic resonance imaging; diagnostics; treatment
Special Issues, Collections and Topics in MDPI journals
Department of Photomedicine and Physical Chemistry, University of Rzeszów, 35-310 Rzeszow, Poland
Interests: photodynamic therapy; diagnostics; photosensitizers; treatment; drug delivery, fiber optics, singlet oxygen
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Photodynamic therapy, which uses a photosensitizer, light and oxygen to kill cancer cells, is an adjuvant therapy that can be applied following the removal of a tumor to kill residual cancer cells on the resection border. Despite the use of traditional treatment, which may include adjuvant photodynamic therapy, there is still a poor prognosis for cancer patients, since cancer cells have been detected at a distance up to 4 cm beyond the identifiable borders of the tumor and recurrent cancer usually develops adjacent to the resection borders. As there is evidence to suggest that is necessary to develop third-generation photosensitizers for precision photodynamic therapy, which can bind to targeted areas of difficult-to-reach microinvasion for cancer eradication, while preserving sensitive healthy tissues and improving patient outcomes. This Special Issue will be devoted to various aspects of photodynamic therapy; however, each of these aspects will oscillate around anticancer drug discovery and development. We welcome papers pertaining to the synthesis and applications of photosensitizers for photodynamic therapy, clinical trials with the use of photosensitizers, papers regarding the interactions of photosensitizers with drugs and vitamins, reviews and metanalyses, and original research. Precision photodynamic therapy, with the use of novel photosensitizers, represents a type of point source targeting. Ensuring precision in this therapy is important for killing cancer cells, and may help provide insights into treatment and diagnostics.

Prof. Dr. Dorota Bartusik-Aebisher
Prof. Dr. David Aebisher
Guest Editors

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 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

  • cancer
  • drug delivery
  • magnetic resonance imaging
  • diagnostics
  • treatment
  • photodynamic therapy
  • diagnostics
  • photosensitizers
  • photomedicine

Published Papers (5 papers)

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Research

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13 pages, 3201 KiB  
Article
Carbon Dots Derived from Tea Polyphenols as Photosensitizers for Photodynamic Therapy
by Yuxiang Yang, Haizhen Ding, Zijian Li, Antonio Claudio Tedesco and Hong Bi
Molecules 2022, 27(23), 8627; https://doi.org/10.3390/molecules27238627 - 06 Dec 2022
Cited by 12 | Viewed by 1954
Abstract
Photodynamic therapy (PDT) has become an emerging cancer treatment method. Choosing the photosensitizer (PS) compounds is one of the essential factors that can influence the PDT effect and action. Carbon dots (CDs) have shown great potential as photosensitizers in PDT of cancers due [...] Read more.
Photodynamic therapy (PDT) has become an emerging cancer treatment method. Choosing the photosensitizer (PS) compounds is one of the essential factors that can influence the PDT effect and action. Carbon dots (CDs) have shown great potential as photosensitizers in PDT of cancers due to their excellent biocompatibility and high generation of reactive oxygen species (ROS). Here, we used tea polyphenol as raw material for synthesized tea polyphenol carbon dots (T−CDs) that show dual emission bands of red and blue fluorescence and can efficiently generate hydroxyl radicals (OH) under mildly visible irradiation with a LED light (400–500 nm, 15 mW cm−2). The extremely low cytotoxicity and excellent biocompatibility of T−CDs without light irradiation were tested using MTT and hemolytic assay. Further, T−CDs have been shown by in vivo experiments, using a mouse breast cancer cell line (4T1) subcutaneously injected in the back of the mouse buttock as a model, to effectively inhibit the tumor cell proliferation in solid tumors and show an excellent PDT effect. In addition, pathological sections of the mice tissues after further treatment showed that the T−CDs had no apparent impact on the major organs of the mice and did not produce any side effect lesions. This work demonstrates that the as−synthesized T−CDs has the potential to be used as a PS in cancer treatment. Full article
(This article belongs to the Special Issue Anticancer Drug Discovery and Development II)
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18 pages, 3366 KiB  
Article
The Lebanese Red Algae Jania rubens: Promising Biomolecules against Colon Cancer Cells
by Mariam Rifi, Zeina Radwan, Reem AlMonla, Ziad Fajloun, Jean Marc Sabatier, Achraf Kouzayha, Marwan El-Sabban, Hiba Mawlawi and Zeina Dassouki
Molecules 2022, 27(19), 6617; https://doi.org/10.3390/molecules27196617 - 05 Oct 2022
Cited by 2 | Viewed by 2290
Abstract
Colorectal cancer (CRC) is ranked the second most lethal type of tumor globally. Thus, developing novel anti-cancer therapeutics that are less aggressive and more potent is needed. Recently, natural bioactive molecules are gaining interest as complementary and supportive antineoplastic treatments due to their [...] Read more.
Colorectal cancer (CRC) is ranked the second most lethal type of tumor globally. Thus, developing novel anti-cancer therapeutics that are less aggressive and more potent is needed. Recently, natural bioactive molecules are gaining interest as complementary and supportive antineoplastic treatments due to their safety, effectiveness, and low cost. Jania rubens (J. rubens) is a red coral seaweed abundant in the Mediterranean and bears a significant pharmacological essence. Despite its therapeutic potential, the natural biomolecules extracted from this alga are poorly identified. In this study, the proximal analysis revealed high levels of total ash content (66%), 11.3% proteins, 14.5% carbohydrates, and only 4.5% lipids. The elemental identification showed magnesium and calcium were high among its macro minerals, (24 ± 0.5 mg/g) and (33 ± 0.5 mg/g), respectively. The Chlorophyll of J. rubens was dominated by other pigments with (0.82 ± 0.02 mg/g). A 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay identified effective antioxidant activity in various J. rubens extracts. More importantly, a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) tetrazolium reduction and wound healing assays indicate that organic extracts from J. rubens significantly counteract the proliferation of colon cancer cell lines (HCT-116 and HT-29) and inhibit their migratory and metastatic properties in a dose and time-dependent manner. Overall, this study provides insight into the physicochemical properties of red seaweed, J. rubens, and identifies its significant antioxidant, cytotoxic, and anti-migratory potential on two colorectal cell lines, HCT-116 and HT-29. Full article
(This article belongs to the Special Issue Anticancer Drug Discovery and Development II)
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20 pages, 3786 KiB  
Article
Photon Upconversion in Small Molecules
by Dorota Bartusik-Aebisher, Mateusz Mielnik, Grzegorz Cieślar, Ewa Chodurek, Aleksandra Kawczyk-Krupka and David Aebisher
Molecules 2022, 27(18), 5874; https://doi.org/10.3390/molecules27185874 - 10 Sep 2022
Cited by 2 | Viewed by 2233
Abstract
Upconversion (UC) is a process that describes the emission of shorter-wavelength light compared to that of the excitation source. Thus, UC is also referred to as anti-Stokes emission because the excitation wavelength is longer than the emission wavelength. UC materials are used in [...] Read more.
Upconversion (UC) is a process that describes the emission of shorter-wavelength light compared to that of the excitation source. Thus, UC is also referred to as anti-Stokes emission because the excitation wavelength is longer than the emission wavelength. UC materials are used in many fields, from electronics to medicine. The objective of using UC in medical research is to synthesize upconversion nanoparticles (UCNPs) composed of a lanthanide core with a coating of adsorbed dye that will generate fluorescence after excitation with near-infrared light to illuminate deep tissue. Emission occurs in the visible and UV range, and excitation mainly in the near-infrared spectrum. UC is observed for lanthanide ions due to the arrangement of their energy levels resulting from f-f electronic transitions. Organic compounds and transition metal ions are also able to form the UC process. Biocompatible UCNPs are designed to absorb infrared light and emit visible light in the UC process. Fluorescent dyes are adsorbed to UCNPs and employed in PDT to achieve deeper tissue effects upon irradiation with infrared light. Fluorescent UCNPs afford selectivity as they may be activated only by illumination of an area of diseased tissue, such as a tumor, with infrared light and are by themselves atoxic in the absence of infrared light. UCNP constructs can be monitored as to their location in the body and uptake by cancer cells, aiding in evaluation of exact doses required to treat the targeted cancer. In this paper, we review current research in UC studies and UCNP development. Full article
(This article belongs to the Special Issue Anticancer Drug Discovery and Development II)
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Review

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16 pages, 1341 KiB  
Review
The Use of Photodynamic Therapy in the Treatment of Brain Tumors—A Review of the Literature
by Dorota Bartusik-Aebisher, Aleksandra Żołyniak, Edyta Barnaś, Agnieszka Machorowska-Pieniążek, Piotr Oleś, Aleksandra Kawczyk-Krupka and David Aebisher
Molecules 2022, 27(20), 6847; https://doi.org/10.3390/molecules27206847 - 13 Oct 2022
Cited by 18 | Viewed by 2762
Abstract
The treatment of neoplastic disease of the brain is still a challenge for modern medicine. Therefore, advanced methodologies are needed that can rationally and successfully contribute to the early diagnosis of primary and metastatic tumors growing within the brain. Photodynamic therapy (PDT) seems [...] Read more.
The treatment of neoplastic disease of the brain is still a challenge for modern medicine. Therefore, advanced methodologies are needed that can rationally and successfully contribute to the early diagnosis of primary and metastatic tumors growing within the brain. Photodynamic therapy (PDT) seems to be a valuable method of treatment for precancerous and cancerous lesions including brain tumors. The main advantage of PDT is its high efficiency, minimal invasiveness and no serious side effects, compared with chemotherapy and radiotherapy. This review was conducted through a comprehensive search of articles, scientific information databases and the websites of organizations dealing with cancer treatment. Key points from clinical trials conducted by other researchers are also discussed. The common databases such as PubMed, Google Scholar, EBSCO, Scopus, and Elsevier were used. Articles in the English language of reliable credibility were mainly analyzed. The type of publications considered included clinical and preclinical studies, systematic reviews, and case reports. Based on these collected materials, we see that scientists have already demonstrated the potential of PDT application in the field of brain tumors. Therefore, in this review, the treatment of neoplasm of the Central Nervous System (CNS) and the most common tumor, glioblastoma multiforme (GBM), have been explored. In addition, an overview of the general principles of PDT, as well as the mechanism of action of the therapy as a therapeutic platform for brain tumors, is described. The research was carried out in June 2022. Full article
(This article belongs to the Special Issue Anticancer Drug Discovery and Development II)
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25 pages, 2165 KiB  
Review
Multinuclear MRI in Drug Discovery
by Dorota Bartusik-Aebisher, Zuzanna Bober, Jolanta Zalejska-Fiolka, Aleksandra Kawczyk-Krupka and David Aebisher
Molecules 2022, 27(19), 6493; https://doi.org/10.3390/molecules27196493 - 01 Oct 2022
Cited by 4 | Viewed by 1833
Abstract
The continuous development of magnetic resonance imaging broadens the range of applications to newer areas. Using MRI, we can not only visualize, but also track pharmaceutical substances and labeled cells in both in vivo and in vitro tests. 1H is widely used [...] Read more.
The continuous development of magnetic resonance imaging broadens the range of applications to newer areas. Using MRI, we can not only visualize, but also track pharmaceutical substances and labeled cells in both in vivo and in vitro tests. 1H is widely used in the MRI method, which is determined by its high content in the human body. The potential of the MRI method makes it an excellent tool for imaging the morphology of the examined objects, and also enables registration of changes at the level of metabolism. There are several reports in the scientific publications on the use of clinical MRI for in vitro tracking. The use of multinuclear MRI has great potential for scientific research and clinical studies. Tuning MRI scanners to the Larmor frequency of a given nucleus, allows imaging without tissue background. Heavy nuclei are components of both drugs and contrast agents and molecular complexes. The implementation of hyperpolarization techniques allows for better MRI sensitivity. The aim of this review is to present the use of multinuclear MRI for investigations in drug delivery. Full article
(This article belongs to the Special Issue Anticancer Drug Discovery and Development II)
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