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Medicinal Mechanisms of Biologically Active Compounds in Cancer
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Medicinal Mechanisms of Biologically Active Compounds in Cancer

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 October 2025 | Viewed by 1138

Special Issue Editor

Dr. Karthik Gourishetti

E-Mail Website
Guest Editor
Biotherapeutics Laboratory, School of Medicine, University of South Carolina, Columbia, SC 29209, USA
Interests: immuno oncology; natural products; drug discovery; drug delivery; glioblastoma; pancreatic ductal adeno carcinoma

Special Issue Information

Dear Colleagues,

The Special Issue “Medicinal Mechanisms of Biologically Active Compounds in Cancer” delves into the significant role of natural compounds in cancer therapy. It emphasizes the mechanisms through which these biologically active substances, sourced from plants, fungi, and marine life, exert their anti-cancer effects. The Issue highlights their ability to induce apoptosis, inhibit tumor growth, and enhance the efficacy of conventional treatments. Key pathways involved in modulating cell proliferation and improving therapeutic outcomes are discussed in detail. Additionally, the antioxidant properties of these compounds are crucial in alleviating the oxidative stress associated with cancer progression. This collection of research aims to provide valuable insights for scientists looking to incorporate natural compounds into cancer treatment strategies, ultimately enhancing patient care and outcomes.

Dr. Karthik Gourishetti
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

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Keywords

  • biologically active compounds
  • cancer treatment
  • apoptosis
  • tumor growth
  • natural products
  • oxidative stress

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Published Papers (2 papers)

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19 pages, 4958 KiB  
Article
Xanthohumol Sensitizes Melanoma Cells to Vemurafenib by Lowering Membrane Cholesterol and Increasing Membrane Fluidity
by Marine Devinat, Jessica Thevenard-Devy, Fatiha Ghilane, Jerome Devy, Lise Chazee, Christine Terryn, Laurent Duca, Emmanuelle Devarenne-Charpentier and Hassan El Btaouri
Int. J. Mol. Sci. 2025, 26(5), 2290; https://doi.org/10.3390/ijms26052290 - 4 Mar 2025
Viewed by 634
Abstract
Chemoresistance remains one of the major obstacles to cancer treatment. The search for specific molecules that could improve cancer treatment has become one of the objectives of biomedical research. Identifying new natural molecules to enhance chemotherapy treatment or improve sensitization to conventional therapies [...] Read more.
Chemoresistance remains one of the major obstacles to cancer treatment. The search for specific molecules that could improve cancer treatment has become one of the objectives of biomedical research. Identifying new natural molecules to enhance chemotherapy treatment or improve sensitization to conventional therapies has become a key objective. Here, we evaluated the effect of Xanthohumol (XN) extracted from hop on SKMEL-28 melanoma cells and their sensitization to vemurafenib (VEM) treatment. We measured the XN effect on cell viability and apoptosis. We also assessed the effect of XN on membrane fluidity and membrane cholesterol levels. Finally, we studied the impact of XN on cell sensitization to VEM. Here, we showed that XN reduced SKMEL-28 cell viability through an apoptotic mechanism. Our results demonstrated the potential role of XN in sensitizing cancer cells to VEM with a less toxic effect on non-tumor cells. A study of XN’s molecular mechanism showed that XN was able to induce cholesterol depletion and increased fluidity in SKMEL-28 cancer cells. This leads to an increase in VEM incorporation. Here, we describe the importance of the strategy to modulate membrane fluidity by XN in order to significantly improve anticancer therapy. Full article
(This article belongs to the Special Issue Medicinal Mechanisms of Biologically Active Compounds in Cancer)
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21 pages, 11551 KiB  
Article
Buxus natalensis (Oliv.) Hutch (Buxaceae) Exhibits Its Anticancer Potential by Stimulating ROS Production and Caspase-p53-BCL-2-Dependent Apoptosis in Hepatocellular Carcinoma and Prostate Cancer Cell Lines
by Emmanuel Mfotie Njoya, Gaetan T. Tabakam, Chika I. Chukwuma and Tshepiso J. Makhafola
Int. J. Mol. Sci. 2025, 26(9), 4173; https://doi.org/10.3390/ijms26094173 - 28 Apr 2025
Viewed by 129
Abstract
Buxus natalensis is recognized as a rich source of triterpenoidal alkaloids that are known to be effective in fighting different cancer types. Nevertheless, to date, no anticancer potential of B. natalensis extract has been yet described. Here, we investigated the antiproliferative activity of [...] Read more.
Buxus natalensis is recognized as a rich source of triterpenoidal alkaloids that are known to be effective in fighting different cancer types. Nevertheless, to date, no anticancer potential of B. natalensis extract has been yet described. Here, we investigated the antiproliferative activity of different B. natalensis leaf extracts on eight cancer cell lines (MCF-7, 4T1, Caco-2, HeLa, A549, HepG2, DU145, and LNCaP). Chang liver cell line derived from normal liver tissue, was used as control. B. natalensis hydroethanolic leaf extract (BNHLE) was found to exert significant cytotoxic effect against cancerous cell lines, with the highest efficacy being observed on LNCaP and HepG2 with IC50 values of 47.39 and 78.01 µg/mL, respectively. Interestingly, BNHLE was less cytotoxic towards Chang liver cells with an IC50 value of 334.10 µg/mL, yielding selectivity index (SI) values of 6.96 and 4.22 against LNCaP and HepG2 cells, respectively. The study of mechanism of action revealed that BNHLE exerted its antiproliferative effect by inducing ROS production and caspase -3/-7, and -9 activities in LNCaP and HepG2 cells. Moreover, it was found that BNHLE activated apoptosis in both cancerous cell lines by enhancing the expression levels of p53, while suppressing the expression of NF-κB-p65 and BCL-2 protein levels in a dose-dependent manner. The phytochemical analysis of BNHLE showed the presence of flavonoids (24.45 mgQE/g extract) and phenolics (84.64 mgGAE/g extract), and its LC-MS profiling identified several compounds including robinin and rutin, which are known for their cytotoxic effect against different cancer cell lines, such as hepatocellular carcinoma and prostate cancer cell lines. Several compounds are still unknown from B. natalensis, but the data obtained so far justify the use of B. natalensis as a potential source of bioactive compounds against hepatocellular and prostate cancers. Full article
(This article belongs to the Special Issue Medicinal Mechanisms of Biologically Active Compounds in Cancer)
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