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Pharmaceutics
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Natural Products in Photodynamic Therapy
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Natural Products in Photodynamic Therapy

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 20 March 2025 | Viewed by 4152

Special Issue Editors

Prof. Dr. Renato Sonchini Gonçalves

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Guest Editor
Department of Chemistry, Laboratory of Chemistry of Natural Products, Federal University of Maranhão, São Luís 65080-805, Brazil
Interests: combination therapy; nanotechnology; nanomedicine; photodynamic therapy; natural products
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Gustavo Braga

E-Mail Website
Guest Editor
Department of Chemistry, Federal University of Maranhão, São Luís 65080-805, Brazil
Interests: nanoformulation; nanotechnology; nanomedicine; physical-chemistry; photodynamic therapy
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

More than a century ago, scientists discovered that when light is combined with specific chemicals, it can cause the death of cells. Acridine, eosin, and haematoporphyrin were the first natural products of the timeline employed as photosensitizers (PS) in photodynamic therapy (PDT). PS, light, and oxygen are the three main elements of PDT, and are required to selectively generate reactive oxygen species in therapeutic targets, leading the cell to die with less invasiveness, low toxicity, and side effects. From 1999 onwards, first- and second-generation PS, like porphyrin, chlorin, and cyanine, and other dyes, such as methylene blue, toluidine blue, rose bengal, and hypericin, were used in the design of drugs for use in PDT, with some of these being approved by the FDA. Despite increasing amounts of research in the last decade focusing on PDT, its effects and applications, to date, less attention has been paid to plant extracts or molecules of natural origin and the study of their phototoxic activity. In this Special Issue, we aim to receive original research articles and review articles regarding the use of natural products as PS and/or as bioactive compounds in association with photodynamic therapy for application as combination therapy.

Prof. Dr. Renato Sonchini Gonçalves
Prof. Dr. Gustavo Braga
Guest Editors

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Keywords

  • photodynamic therapy
  • photosensitizer
  • natural product
  • bioactive compounds
  • combination therapy

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Published Papers (3 papers)

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Research

17 pages, 13618 KiB  
Article
Cytotoxic and Immunomodulatory Effects of Hypericin as a Photosensitizer in Photodynamic Therapy Used on Skin Cell Cultures
by Magdalena Krupka-Olek, Andrzej Bożek, Zenon P. Czuba, Małgorzata Kłósek, Grzegorz Cieślar and Aleksandra Kawczyk-Krupka
Pharmaceutics 2024, 16(6), 696; https://doi.org/10.3390/pharmaceutics16060696 - 23 May 2024
Viewed by 1138
Abstract
Determination of the hypericin–photodynamic (HY–PDT) effect on the secretion of cytokines secreted by the skin cells, may be the basis for using the immunomodulatory effect of photodynamic action in the treatment of inflammatory skin diseases. The study aimed to evaluate the cytotoxic and [...] Read more.
Determination of the hypericin–photodynamic (HY–PDT) effect on the secretion of cytokines secreted by the skin cells, may be the basis for using the immunomodulatory effect of photodynamic action in the treatment of inflammatory skin diseases. The study aimed to evaluate the cytotoxic and immunomodulatory effects of hypericin (HY) in photodynamic therapy (PDT) performed in vitro on cultures of selected skin cell lines. The study used two human cell lines, primary dermal fibroblast (HDFa) and primary epidermal keratinocytes (HEKa). The MTT test was used to define the metabolic activity of treated cells. Cell supernatants subjected to sublethal PDT were assessed to determine the interleukins: IL-2, IL-8, IL-10, IL-11, IL-19, IL-22, and metalloproteinase 1 (MMP-1). The results confirm the destructive effect of HY–PDT and the immunomodulatory effects of sublethal doses on the selected skin cells, depending on the concentration of HY and the light doses. No statistically significant differences were noted in IL-2 and IL-10 concentration after HY–PDT for HEKa and HDFa lines. After using HY–PDT, the concentration of IL-8, MMP-1, IL-22, and IL-11 significantly decreased in the HEKa line. Moreover, the concentration of IL-19 and MMP-1 significantly decreased in the HDFa line. The concentration of IL-11 in the HDFa line after using only the HY, without the light, increased but decreased after HY–PDT. Our experiment confirmed that HY–PDT has not only a cytotoxic effect but, used in sublethal doses, also presents immunomodulatory properties. These may be an advantage of HY–PDT when used in the treatment of persistent skin inflammation, connected with the release of pro-inflammatory cytokines resistant to conventional treatment methods. Full article
(This article belongs to the Special Issue Natural Products in Photodynamic Therapy)
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12 pages, 2649 KiB  
Article
Natural Phytochemical and Visible Light at Different Wavelengths Show Synergistic Antibacterial Activity against Staphylococcus aureus
by Jae-Young Jeong and You-Jin Hwang
Pharmaceutics 2024, 16(5), 612; https://doi.org/10.3390/pharmaceutics16050612 - 1 May 2024
Viewed by 1156 | Correction
Abstract
As the risk of antibiotic-resistant bacteria increases, interest in non-antibiotic treatment is also increasing. Among the methods used in non-antibiotic therapy, natural antibiotics such as essential oils have disadvantages such as low efficiency. In the case of phototherapy, the light used for antibacterial [...] Read more.
As the risk of antibiotic-resistant bacteria increases, interest in non-antibiotic treatment is also increasing. Among the methods used in non-antibiotic therapy, natural antibiotics such as essential oils have disadvantages such as low efficiency. In the case of phototherapy, the light used for antibacterial activities has low penetration into the human body because of its short wavelength, making it of low medical utility. To solve this problem, this study aimed to determine conditions for enhancing the antibacterial activity of natural phytochemicals and visible light. Four natural phytochemical extracts that showed high antibacterial properties in previous studies were analyzed. Synergistic effects on antibacterial activity and cytotoxicity were determined when natural phytochemical extracts and visible light were simultaneously used. As a result, it was confirmed that the antibacterial activity increased by four times when Sanguisorba officinalis L. was irradiated with 465 nm for 10 min and 520 nm for 40 min, and Uncaria gambir Roxb. was irradiated with 465 nm for 10 min and 520 nm for 60 min compared to when Sanguisorba officinalis L. and Uncaria gambir Roxb. were used alone. The synergistic effect on antibacterial activity was independent of the absorption peak of the natural phytochemical extracts. In addition, in the case of natural phytochemical extracts with improved antibacterial activity, it was confirmed that the improvement of antibacterial activity was increased in inverse proportion to the light irradiation wavelength and in proportion to the light irradiation time. The antibacterial activity was enhanced regardless of antibiotic resistance. In the case of cytotoxicity, it was confirmed that there was no toxicity to A549 cells when treated with 465 nm, the shortest wavelength among the natural phytochemical extracts. These results show how to replace blue light, which has been underutilized due to its low transmittance and cytotoxicity. They also demonstrate the high medical potential of using natural phytochemical and visible light as a combination therapy. Full article
(This article belongs to the Special Issue Natural Products in Photodynamic Therapy)
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18 pages, 5480 KiB  
Article
Immunomodulatory Effect of Hypericin-Mediated Photodynamic Therapy on Oral Cancer Cells
by Marcin Olek, Agnieszka Machorowska-Pieniążek, Zenon P. Czuba, Grzegorz Cieślar and Aleksandra Kawczyk-Krupka
Pharmaceutics 2024, 16(1), 42; https://doi.org/10.3390/pharmaceutics16010042 - 27 Dec 2023
Cited by 2 | Viewed by 1345
Abstract
In 2020, there were 377,713 new oral and lip cancer diagnoses and 177,757 deaths. Oral cancer is a malignancy of the head and neck region, and 90% of cases are squamous cell carcinomas (OSCCs). One of the alternative methods of treating pre-cancerous lesions [...] Read more.
In 2020, there were 377,713 new oral and lip cancer diagnoses and 177,757 deaths. Oral cancer is a malignancy of the head and neck region, and 90% of cases are squamous cell carcinomas (OSCCs). One of the alternative methods of treating pre-cancerous lesions and oral cancer is photodynamic therapy (PDT). In addition to the cytotoxic effect, an important mechanism of PDT action is the immunomodulatory effect. This study used the OSCC (SCC-25) cell line and the healthy gingival fibroblast (HGF-1) line. A compound of natural origin—hypericin (HY)—was used as the photosensitizer (PS). The HY concentrations of 0–1 µM were used. After two hours of incubation with PS, the cells were irradiated with light doses of 0–20 J/cm2. The MTT test determined sublethal doses of PDT. Cell supernatants subjected to sublethal PDT were assessed for interleukin 6 (IL-6), soluble IL-6 receptor alpha (sIL-6Ralfa), sIL-6Rbeta, IL-8, IL-10, IL-11 IL-20, IL-32, and Pentraxin-3 using the Bio-Plex ProTM Assay. The phototoxic effect was observed starting with a light dose of 5 J/cm2 and amplified with increasing HY concentration and a light dose. HY-PDT affected the SCC-25 cell secretion of sIL-6Rbeta, IL-20, and Pentraxin-3. HY alone increased IL-8 secretion. In the case of HGF-1, the effect of HY-PDT on the secretion of IL-8 and IL-32 was found. Full article
(This article belongs to the Special Issue Natural Products in Photodynamic Therapy)
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