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Cytotoxicity, Antioxidant and Anticancer Activity of Natural Products, 2nd Edition

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: 20 May 2025 | Viewed by 2544

Special Issue Editor


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Guest Editor
Faculty of Biology, Plovdiv University “Paisii Hilendarski”, 24 Tsar Assen Str., 4000 Plovdiv, Bulgaria
Interests: cell biology; immunology; immunomodulation; biomarkers; autoimmune diseases; allergy; cytotoxicity; anticancer activity; natural products; probiotics; prebiotics; nanoparticles
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Special Issue Information

Dear Colleagues,

The main reason for the high economic and social burden of cancer is the lack of effective drug agents and therapies. Therefore, the efforts of a large part of the scientific community are directed at identifying new anticancer compounds from natural sources (plants, algae or other organisms) as well as developing new formulations in order to increase the healing potential and minimize the side effects of currently used therapeutic agents. Thus, the search for new biologically active compounds is important for the discovery of new drugs relative to the treatment of cancer.

Evaluation of the anticancer activity is performing by detection of specific cytotoxicity of the test agent, affecting fundamental cellular functions of cancer cells causing their death. Changes in metabolic processes (e.g., mitochondrial activity) and the level of ATP or free radicals are early indicators of cell damage. Disruption of the plasma membrane integrity increases the concentration of enzymes in the extracellular environment, which together with the DNA fragmentation are key parameters for assessing the cell damage. Therefore, anticancer activity is assessed on the basis of specific cytotoxicity observed by examining the basic parameters of cell damage.

This Special Issue aims to publish original research studies related to the isolation and characterization of natural products with anticancer activity as well as their molecular mechanisms of action or effects on a particular metabolic or signalling pathway. Authors are invited to submit their high-quality articles, reviews or short communications concerning this topic. Multidisciplinary studies involving in vitro and/or in vivo experiments that address specific delivery of anticancer drugs by using different novel technologies based on natural products are also welcome.

Importantly, the exact active ingredient of plant extract must be reported in the submitted research manuscript, since papers describing effects of mixed extraction from plants will not be accepted. More published papers could be found in the closed Special Issue: Cytotoxicity, Antioxidant and Anticancer Activity of Natural Products.

Prof. Dr. Balik Dzhambazov
Guest Editor

Manuscript Submission Information

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Keywords

  • natural products
  • anticancer activity
  • apoptosis
  • immunomodulation
  • free radicals
  • proliferation
  • phytomolecules
  • nanoparticles
  • drug delivery

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Published Papers (2 papers)

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Research

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19 pages, 7566 KiB  
Article
Cytotoxicity, Proapoptotic Activity and Drug-like Potential of Quercetin and Kaempferol in Glioblastoma Cells: Preclinical Insights
by Magdalena Kusaczuk, Elena Tovar-Ambel, Paola Martín-Cabrera, Mar Lorente, Nélida Salvador-Tormo, Agnieszka Mikłosz, Adrian Chabowski, Guillermo Velasco and Monika Naumowicz
Int. J. Mol. Sci. 2024, 25(19), 10740; https://doi.org/10.3390/ijms251910740 - 5 Oct 2024
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Abstract
Despite the increasing understanding of the pathogenesis of glioblastoma (GBM), treatment options for this tumor remain limited. Recently, the therapeutic potential of natural compounds has attracted great interest. Thus, dietary flavonoids quercetin (QCT) and kaempferol (KMF) were investigated as potential cytostatic agents in [...] Read more.
Despite the increasing understanding of the pathogenesis of glioblastoma (GBM), treatment options for this tumor remain limited. Recently, the therapeutic potential of natural compounds has attracted great interest. Thus, dietary flavonoids quercetin (QCT) and kaempferol (KMF) were investigated as potential cytostatic agents in GBM. Moreover, the physicochemical properties of QCT and KMF, determining their bioavailability and therapeutic efficiency, were evaluated. We proved that both polyphenols significantly reduced the viability of GBM cells. We also demonstrated that both QCT and KMF evoked the cytotoxic effect in T98G cells via induction of apoptotic cell death as shown by increased activity of caspase 3/7 and caspase 9 together with an overexpression of the cleaved form of PARP. Apoptosis was additionally accompanied by the activation of stress responses in QCT- and KMF-treated cells. Both polyphenols caused oxidative stress and endoplasmic reticulum (ER) stress, as demonstrated by the increased generation of reactive oxygen species (ROS), deregulated expressions of superoxide dismutases (SOD2 and Sod1 on protein and transcriptomic levels, respectively), as well as an overexpression of ERO1α, GRP78, p-JNK, and an up-regulation of Chop, Atf4 and Atf6α genes. The antitumor effect of QCT and KMF was also confirmed in vivo, showing reduced growth of tumor xenografts in the chick chorioallantoic membrane (CAM) experiment. Moreover, electrophoretic light scattering (ELS) was used to measure the zeta potential of cell membranes upon exposition to QCT and KMF. Additionally, on the basis of existing physicochemical data, the drug-likeness score of QCT and KMF was evaluated. Analyses showed that both compounds accomplish Lipinski’s Rule of 5, and they both fit into the criteria of good central nervous system (CNS) drugs. Altogether, our data support the idea that QCT and KMF might be plausible candidates for evaluation as therapeutic agents in preclinical models of glioblastoma. Full article
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Review

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14 pages, 1598 KiB  
Review
Research on the Action and Mechanism of Pharmacological Components of Omphalia lapidescens
by Keyang Xu, Li Wang and Dan He
Int. J. Mol. Sci. 2024, 25(20), 11016; https://doi.org/10.3390/ijms252011016 - 13 Oct 2024
Viewed by 860
Abstract
Omphalia lapidescens is a macrofungus that is used in traditional Chinese medicine for its insecticidal and stagnation-relieving properties. The active ingredients of this fungus including proteins, polysaccharides and sterols have been demonstrated to exhibit antiparasitic, anti-inflammatory, and antitumor effects. Omphalia has been used [...] Read more.
Omphalia lapidescens is a macrofungus that is used in traditional Chinese medicine for its insecticidal and stagnation-relieving properties. The active ingredients of this fungus including proteins, polysaccharides and sterols have been demonstrated to exhibit antiparasitic, anti-inflammatory, and antitumor effects. Omphalia has been used in clinical cancer treatment. Many studies on Omphalia have concentrated on its cytotoxicity and anticancer effects. However, the investigation of its natural metabolites remains a significant area for further research. This review presents a comprehensive analysis of the research progress concerning the pharmacological components of Omphalia. The aim of this discussion is to provide a reference for further in-depth study of Omphalia, with the objective of exploring its potential value. Therefore, the focus of this review was on the classification of metabolites in Omphalia and their mechanisms of action. Full article
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