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Natural Products in Drug Discovery for Anticancer Treatment

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 March 2025 | Viewed by 8521

Special Issue Editors


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Guest Editor
Department of Pharmacognosy with Medicinal Plants Garden, Medical University of Lublin, Chodźki 1 St., 20-093 Lublin, Poland
Interests: natural products; secondary metabolites; anticancer activity; bioactivity-guided isolation; chromatography; LC-MS/MS; NMR; natural drugs; semisynthetic derivatives of natural drugs
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Co-Guest Editor
Department of Cell Biology, Maria Curie-Sklodowska University, Akademicka 19, 20-033 Lublin, Poland
Interests: cell culture; cell signaling; cell cycle; carcinogenesis; metastasis; oxidative stress

Special Issue Information

Dear Colleagues,

For centuries, natural medicines have been used to improve human health. Currently, there is a renaissance in the exploration of natural sources in search of structures for the design of new drugs, especially for anticancer treatment, including semi-synthetic bioactive molecules. New sophisticated techniques such as LC-MS/MS and NMR allow for the detailed study of the chemical structure of compounds to better understand their potential and make natural medicine even safer. To this end, various new bioactivity testing protocols were also discovered and developed to better understand the mechanisms of action of the discovered bioactive molecules.

In this proposed Special Issue, we encourage researchers to share their research results with the wider community to create opportunities to better understand and advance this important field of research and to bring it closer to readers. The presentation of the results may bring inspiration and new perspectives useful for the development of new drugs that have the potential to improve human life.

Dr. Magdalena Bartnik
Dr. Adrianna Sławińska-Brych
Guest Editors

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Published Papers (3 papers)

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Research

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22 pages, 4413 KiB  
Article
Evaluation of the Biological Effect of Non-UV-Activated Bergapten on Selected Human Tumor Cells and the Insight into the Molecular Mechanism of Its Action
by Magdalena Bartnik, Adrianna Sławińska-Brych, Magdalena Mizerska-Kowalska and Barbara Zdzisińska
Int. J. Mol. Sci. 2023, 24(21), 15555; https://doi.org/10.3390/ijms242115555 - 25 Oct 2023
Cited by 2 | Viewed by 1425
Abstract
There is some evidence that non-photoactivated psoralens may be active against breast and colon tumor cells. Therefore, we evaluated the antiproliferative, proapoptotic, and anti-migrative effect of 5-methoxypsoralen (5-MOP) isolated from Peucedanum tauricum MB fruits in human colorectal adenocarcinoma (HT-29 and SW620), osteosarcoma (Saos-2 [...] Read more.
There is some evidence that non-photoactivated psoralens may be active against breast and colon tumor cells. Therefore, we evaluated the antiproliferative, proapoptotic, and anti-migrative effect of 5-methoxypsoralen (5-MOP) isolated from Peucedanum tauricum MB fruits in human colorectal adenocarcinoma (HT-29 and SW620), osteosarcoma (Saos-2 and HOS), and multiple myeloma (RPMI8226 and U266). Dose- and cell-line-dependent effects of 5-MOP on viability and proliferation were observed, with the strongest inhibitory effect against Saos-2 and a moderate effect against the HOS, HT-29, and SW620 cells. Multiple myeloma showed low sensitivity. The high viability of human normal cell cultures (HSF and hFOB) in a wide range of 5-MOP concentrations tested (6.25–100 µM) was confirmed. Moreover, the migration of treated Saos-2, SW620, and HT-29 cell lines was impaired, as indicated via a wound healing assay. Flow cytometry analysis conducted on Saos-2 cells revealed the ability of 5-MOP to block the cell cycle in the G2 phase and trigger apoptosis, which was accompanied by a loss of mitochondrial membrane potential, caspases (-9 and -3) activation, the altered expression of the Bax and Bcl-2 proteins, and decreased AKT phosphorylation. This is the first report evaluating the antiproliferative and antimigratory impact of non-UV-activated bergapten on the abovementioned (except for HT-29) tumor cells, which provides new data on the potential role of 5-MOP in inhibiting the growth of various types of therapeutic-resistant cancers. Full article
(This article belongs to the Special Issue Natural Products in Drug Discovery for Anticancer Treatment)
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Review

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18 pages, 1768 KiB  
Review
Buds and Bugs: A Fascinating Tale of Gut Microbiota and Cannabis in the Fight against Cancer
by Ahmad K. Al-Khazaleh, Kayla Jaye, Dennis Chang, Gerald W. Münch and Deep Jyoti Bhuyan
Int. J. Mol. Sci. 2024, 25(2), 872; https://doi.org/10.3390/ijms25020872 - 10 Jan 2024
Viewed by 3586
Abstract
Emerging research has revealed a complex bidirectional interaction between the gut microbiome and cannabis. Preclinical studies have demonstrated that the gut microbiota can significantly influence the pharmacological effects of cannabinoids. One notable finding is the ability of the gut microbiota to metabolise cannabinoids, [...] Read more.
Emerging research has revealed a complex bidirectional interaction between the gut microbiome and cannabis. Preclinical studies have demonstrated that the gut microbiota can significantly influence the pharmacological effects of cannabinoids. One notable finding is the ability of the gut microbiota to metabolise cannabinoids, including Δ9-tetrahydrocannabinol (THC). This metabolic transformation can alter the potency and duration of cannabinoid effects, potentially impacting their efficacy in cancer treatment. Additionally, the capacity of gut microbiota to activate cannabinoid receptors through the production of secondary bile acids underscores its role in directly influencing the pharmacological activity of cannabinoids. While the literature reveals promising avenues for leveraging the gut microbiome–cannabis axis in cancer therapy, several critical considerations must be accounted for. Firstly, the variability in gut microbiota composition among individuals presents a challenge in developing universal treatment strategies. The diversity in gut microbiota may lead to variations in cannabinoid metabolism and treatment responses, emphasising the need for personalised medicine approaches. The growing interest in understanding how the gut microbiome and cannabis may impact cancer has created a demand for up-to-date, comprehensive reviews to inform researchers and healthcare practitioners. This review provides a timely and invaluable resource by synthesizing the most recent research findings and spotlighting emerging trends. A thorough examination of the literature on the interplay between the gut microbiome and cannabis, specifically focusing on their potential implications for cancer, is presented in this review to devise innovative and effective therapeutic strategies for managing cancer. Full article
(This article belongs to the Special Issue Natural Products in Drug Discovery for Anticancer Treatment)
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29 pages, 7425 KiB  
Review
Pyrrolizidine Alkaloids—Pros and Cons for Pharmaceutical and Medical Applications
by Kavindi Jayawickreme, Dawid Świstak, Ewa Ozimek, Emilia Reszczyńska, Anna Rysiak, Anna Makuch-Kocka and Agnieszka Hanaka
Int. J. Mol. Sci. 2023, 24(23), 16972; https://doi.org/10.3390/ijms242316972 - 30 Nov 2023
Cited by 4 | Viewed by 2401
Abstract
Heterocyclic organic compounds named pyrrolizidine alkaloids (PAs) belong to a group of alkaloids and are synthesized by either plants or microorganisms. Therefore, they are naturally occurring secondary metabolites. They are found in species applied in the pharmaceutical and food industries, thus a thorough [...] Read more.
Heterocyclic organic compounds named pyrrolizidine alkaloids (PAs) belong to a group of alkaloids and are synthesized by either plants or microorganisms. Therefore, they are naturally occurring secondary metabolites. They are found in species applied in the pharmaceutical and food industries, thus a thorough knowledge of their pharmacological properties and toxicology to humans is of great importance for their further safe employment. This review is original because it synthesizes knowledge of plant and microbial PAs, which is unusual in the scientific literature. We have focused on the Boraginaceae family, which is unique due to the exceptional richness and diversity of its PAs in plant species. We have also presented the microbial sources of PAs, both from fungi and bacteria. The structure and metabolism of PAs have been discussed. Our main aim was to summarize the effects of PAs on humans, including both negative, toxic ones, mainly concerning hepatotoxicity and carcinogenicity, as well as potentially positive ones for pharmacological and medical applications. We have collected the results of studies on the anticancer activity of PAs from plant and microbial sources (mainly Streptomyces strains) and on the antimicrobial activity of PAs on different strains of microorganisms (bacteria and fungi). Finally, we have suggested potential applications and future perspectives. Full article
(This article belongs to the Special Issue Natural Products in Drug Discovery for Anticancer Treatment)
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