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Nature-Inspired Antitumor Agents, 2nd Edition

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

Deadline for manuscript submissions: 31 May 2025 | Viewed by 2489

Special Issue Editor

Special Issue Information

Dear Colleagues,

Medicinal chemistry in the twenty-first century has undergone innovative developments due to revolutions in biotechnology and informatics. These advances are mainly within the lead optimization process, but a very significant portion of these leads will continue to contain molecules which originate from natural products (NPs). The diversity of species from terrestrial plants, animals, microorganisms, and marine organisms results in a multitude of secondary metabolites with novel chemical structures and innovative mechanisms of action.

This renaissance of NPs is most allied with total synthesis, semi-synthesis, and analogue-based design. Nevertheless, other biotechnology and cheminformatics approaches are being used to investigate leads from nature. Among the activities of NPs, antitumor activity stands out. NPs like doxorubicin and taxol have their place in chemotherapy alongside new immunotherapies.

This Special Issue focuses on recent breakthroughs, which will help develop new antitumor agents inspired by the variety of NPs emerging as chemotherapeutics, and which intends to collect the state of the art with original research and review articles that consider NP analogues as potential antitumor drug candidates. Unique topics are welcomed.

Dr. Honorina Cidade
Guest Editor

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Keywords

  • natural products
  • antitumor activity
  • NPs analogues-based design

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Related Special Issue

Published Papers (3 papers)

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Research

29 pages, 11365 KiB  
Article
Modulation of Tumor Metabolism in Acute Leukemia by Plant-Derived Polymolecular Drugs and Their Effects on Mitochondrial Function
by Cindy Arévalo, Carolina Carlosama, Laura Rojas, Mónica P. Cala, Marie-Paule Hamon, Bertrand Friguet, Alfonso Barreto and Susana Fiorentino
Molecules 2025, 30(8), 1783; https://doi.org/10.3390/molecules30081783 - 16 Apr 2025
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Abstract
The analysis of tumor metabolism offers promising opportunities for developing new therapeutic strategies. Plant-derived polymolecular drugs can regulate cellular metabolism, making them potential candidates for treatment. This study examined the metabolic effects of plant-derived polymolecular drugs—P2Et, Anamu-SC, and Esperanza—on leukemic cell lines (lymphoid [...] Read more.
The analysis of tumor metabolism offers promising opportunities for developing new therapeutic strategies. Plant-derived polymolecular drugs can regulate cellular metabolism, making them potential candidates for treatment. This study examined the metabolic effects of plant-derived polymolecular drugs—P2Et, Anamu-SC, and Esperanza—on leukemic cell lines (lymphoid and myeloid types) and primary leukemic blasts. The metabolic analysis included oxidative status, glucose consumption, extracellular acidification, oxygen consumption, mitochondrial dynamics, and untargeted metabolomics. Additionally, the effect of co-treatment with conventional chemotherapeutic drugs was investigated. Results showed that P2Et and Anamu-SC reduced the viability and proliferation of all tumor cell lines, exhibiting antioxidant effects. Anamu-SC decreased reactive oxygen species levels in lymphoid tumor cells. Mitochondrial activity was selectively affected by the plant-derived polymolecular drugs, with Anamu-SC and Esperanza causing more significant, potentially reversible damage compared to P2Et. Anamu-SC and Esperanza increased levels of phosphatidylcholines and carnitines. The co-administration of plant-derived polymolecular drugs with chemotherapeutics improved the cytostatic efficacy of cytarabine. In conclusion, this research highlights the promising pharmacological activity of Anamu-SC and Esperanza as mitocans for the treatment of acute leukemia. The study emphasizes the practical significance of combining plant-derived polymolecular drugs with conventional chemotherapeutics to enhance their cytostatic efficacy. Full article
(This article belongs to the Special Issue Nature-Inspired Antitumor Agents, 2nd Edition)
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19 pages, 9082 KiB  
Article
New Difunctional Derivatives of Betulin: Preparation, Characterization and Antiproliferative Potential
by Elwira Chrobak, Marta Świtalska, Joanna Wietrzyk and Ewa Bębenek
Molecules 2025, 30(3), 611; https://doi.org/10.3390/molecules30030611 - 30 Jan 2025
Viewed by 698
Abstract
Biologically active compounds of natural origin, such as betulin, are a source of obtaining new medicinal substances. The presence of chemically active hydroxyl groups in the betulin structure at C-3 and C-28 positions enables esterification with dicarboxylic acid anhydrides or carboxylic acids. As [...] Read more.
Biologically active compounds of natural origin, such as betulin, are a source of obtaining new medicinal substances. The presence of chemically active hydroxyl groups in the betulin structure at C-3 and C-28 positions enables esterification with dicarboxylic acid anhydrides or carboxylic acids. As a result of a four-step synthesis, difunctional betulin derivatives were obtained, which were evaluated for their antiproliferative activity against the following human cell lines: leukemia (MV4-11), (A549), breast cancer (MCF-7), prostate adenocarcinoma (PC-3), colon cancer (HCT116), pancreatic cancer (MiaPaca-2), and melanoma (Hs294T). The target 3-carboxyacyl-28-alkynyloyl betulin derivatives showed significant antiproliferative activity against MV4-11 cells. For 3-carboxyacylbetulins and their selected alkynyl derivatives, studies to investigate the effect on the cell cycle and apoptosis process, as well as drug similarity analysis, were performed. Full article
(This article belongs to the Special Issue Nature-Inspired Antitumor Agents, 2nd Edition)
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29 pages, 2776 KiB  
Article
Insights into the Mode of Action of Novel Morpholinated Curcumin Derivatives Exhibiting Potent Antitumor Activity in Bladder Cancer Cells In Vitro
by Paulina Kobylka, Pawel Bakun, Joanna Kuzminska, Tomasz Goslinski, Marek Murias and Malgorzata Kucinska
Molecules 2025, 30(2), 295; https://doi.org/10.3390/molecules30020295 - 13 Jan 2025
Viewed by 887
Abstract
Although curcumin is a well-known natural polyphenol with many biological activities, its clinical application has been limited by low aqueous solubility and stability. Therefore, curcumin derivatives have been proposed to overcome these limitations and increase anticancer activity. This study tested curcumin derivatives with [...] Read more.
Although curcumin is a well-known natural polyphenol with many biological activities, its clinical application has been limited by low aqueous solubility and stability. Therefore, curcumin derivatives have been proposed to overcome these limitations and increase anticancer activity. This study tested curcumin derivatives with modified feruloyl moieties (2a and 2a-B) and the β-diketo moiety (2a-B) to better understand their anticancer mechanism against human bladder cancer cells. The anticancer activity of 2a and 2a-B was determined using MTT (hypoxic conditions) and LDH (normoxic conditions) assays. An ELISA-based protein panel was used to find the potential molecular targets, while flow cytometric, colorimetric, fluorescent, and luminescent assays were used to investigate the cell death mechanism. It was shown that compound 2a exerted a more potent cytotoxic effect under hypoxic conditions, while compound 2a-B demonstrated a comparable effect in normoxic and hypoxic conditions. The potential molecular targets modified by 2a and 2a-B depending on oxygen concentration were also proposed. Both compounds alter cell cycle progression by blocking the cell cycle in the G2/M phase and decreasing the percentage of cells in the G0/G1 phase. Compound 2a-B led to phosphatidylserine translocation, increased caspase 3/7 activity, and decreased mitochondrial membrane potential, suggesting a mitochondrial apoptosis pathway. We found that the Akt signaling pathway may modulate the activity of compound 2a-B, as evidenced by enhanced cytotoxic activity in combination with MK-2206, an Akt 1/2/3 inhibitor. Thus, our results provide new insights into the anticancer activity of compounds 2a and 2a-B; however, further studies are needed to better understand their therapeutic potential. Full article
(This article belongs to the Special Issue Nature-Inspired Antitumor Agents, 2nd Edition)
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