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Natural and Synthetic Molecules with Anticancer Activity: Pharmacological Basis and...
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Natural and Synthetic Molecules with Anticancer Activity: Pharmacological Basis and Mechanistic Insight

A special issue of Biomedicines (ISSN 2227-9059). This special issue belongs to the section "Drug Discovery, Development and Delivery".

Deadline for manuscript submissions: 30 June 2025 | Viewed by 5273

Special Issue Editors

Dr. Hassan Ebrahim

E-Mail Website
Guest Editor
Department of Biomedical Sciences, Edward Via College of Osteopathic Medicine, Louisiana Campus, Monroe, LA 71203, USA
Interests: drug discovery; cancer pharmacology; novel molecular targets; herbal medicine
Special Issues, Collections and Topics in MDPI journals
Dr. Ángela Patricia Hernandez

E-Mail Website
Guest Editor
1. Department of Pharmaceutical Sciences, Organic Chemistry Area, University of Salamanca, Salamanca, Spain
2. Department of Medicine and Cytometry General Service-Nucleus, CIBERONC, Cancer Research Centre (IBMCC/CSIC/USAL/IBSAL), Salamanca, Spain
Interests: drug discovery; natural products; immunotherapy; nanomedicine; medicinal chemistry; organic chemistry; cancer
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Cancer is one of the most challenging health problems encountered humanity and ranks among the top leading causes of death worldwide according to statistics from the World Health Organization (WHO). While substantial advancements have been achieved towards the early detection of the disease along with the creation of targeted/selective therapies, cancer is still claiming more victims. The deleterious side-effects and development of resistance to the current clinically used chemotherapeutics necessitate continuing research to better understand the pathology of the disease and design more effective therapeutics. Natural products with defined molecular compounds or their semisynthetic derivatives have been well-documented for their potent antitumor activity, as exemplified in multiple FDA-approved drugs such as paclitaxel, vincristine, doxorubicin, and bleomycin. They are defined as having novel chemical scaffolds, 3D pharmacophores, and unique mechanistic modes of action. In some cases, total synthesis of natural products with defined molecular compounds or inspired scaffolds has provided biomolecules for drug development. On the other hand, another approach is ligand-based anticancer drug discovery, which relies on the screening of mega libraries of chemically diverse synthetic molecules against relevant targets, while the structure-based approach involves the rational design and synthesis of biomolecules to optimize their binding to a validated macromolecular target of a known 3D molecular architecture. In this context, this Special Issue is aimed at encouraging scientists in the field of anticancer drug development to publish their recent finding on the mechanistic mode of action of defined natural, semisynthetic, and synthetic biomolecules with emphasis on their anticancer molecular pharmacology.

Dr. Hassan Ebrahim
Dr. Angela Patricia Hernandez
Guest Editors

Manuscript Submission Information

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Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Biomedicines is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2600 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • anticancer
  • molecular pharmacology
  • mechanistic mode of action
  • signal transduction
  • in vitro
  • preclinical
  • natural products
  • synthesis

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Published Papers (4 papers)

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Research

19 pages, 4020 KiB  
Article
Angiotensin 1–7 and the Non-Peptide MAS-R Agonist AVE0991 Inhibit Breast Cancer Cell Migration and Invasion
by Mariam M. Alfoudiry and Maitham A. Khajah
Biomedicines 2025, 13(3), 567; https://doi.org/10.3390/biomedicines13030567 - 24 Feb 2025
Viewed by 504
Abstract
Background: Endocrine resistance in breast cancer is associated with the epithelial-to-mesenchymal transition (EMT), resulting in enhanced cell proliferation, motility, and invasion and leading to a poor prognosis. There are few studies regarding the role of Angiotensin II (Ang II) and Angiotensin 1–7 (Ang [...] Read more.
Background: Endocrine resistance in breast cancer is associated with the epithelial-to-mesenchymal transition (EMT), resulting in enhanced cell proliferation, motility, and invasion and leading to a poor prognosis. There are few studies regarding the role of Angiotensin II (Ang II) and Angiotensin 1–7 (Ang 1–7) in relation to breast cancer, with contradictory outcomes. This study aims to investigate the expression of Ang 1–7 and MAS-R and evaluate the effects of Ang II, Ang 1–7, and the MAS-R agonist AVE0991 on EMT induction and reversal. Methods: The effects of Ang II and Ang 1–7 on normal and breast cancer cell lines were determined using various techniques for cell proliferation (MTT), motility (scratch assay), and invasion (Cultrex assay). Also, the expression/localization profiles of Ang 1–7 and its receptor (MAS-R), as well as various EMT markers, were determined using immunofluorescence, western blot, and ELISA. Results: Ang II significantly decreased the motility of the tested cell lines; however, it did not have a significant effect on their proliferation or invasion. The expression profiles of the tested EMT markers were not affected by Ang II treatment. The expression levels of Ang 1–7 and MAS-R were significantly higher in the normal breast epithelial cells and estrogen receptor ER compared to the ER+ breast cancer cells. Treatment with Ang 1–7 or the non-peptide MAS-R agonist AVE0991 significantly reduced the migration and invasion of the tested cell lines without modulating the tested EMT markers. Compared to Ang 1–7, AVE0991 exhibited a more prominent dose-dependent inhibitory effect on the proliferation, motility, and invasion of the ER− breast cancer cells. Conclusions: Ang 1–7 and AVE0991 play a promising therapeutic role in breast cancer, in part by reducing cell motility and invasion. Full article
(This article belongs to the Special Issue Natural and Synthetic Molecules with Anticancer Activity: Pharmacological Basis and Mechanistic Insight)
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17 pages, 5268 KiB  
Article
Anti-Proliferative Activity of Ethylenediurea Derivatives with Alkyl and Oxygen-Containing Groups as Substituents
by Maxim Oshchepkov, Leonid Kovalenko, Antonida Kalistratova, Galina Sherstyanykh, Evgenia Gorbacheva, Alexey Antonov, Nisreen Khadour and Mikhail Akimov
Biomedicines 2025, 13(2), 316; https://doi.org/10.3390/biomedicines13020316 - 29 Jan 2025
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Abstract
Background/Objectives: Natural cytokinins are a promising group of anti-tumor agents. In this work, we hypothesized that modification of the ethylenediurea moiety with alkyl and oxygen-containing groups could be a way to enhance the anti-proliferative properties of the molecule. Methods: Ten new [...] Read more.
Background/Objectives: Natural cytokinins are a promising group of anti-tumor agents. In this work, we hypothesized that modification of the ethylenediurea moiety with alkyl and oxygen-containing groups could be a way to enhance the anti-proliferative properties of the molecule. Methods: Ten new analogs of ethylenediurea with these substitutions were tested for anti-proliferative activity in the human cancer cell lines MDA-MB-231 (breast cancer), A-375 (melanoma), and U-87 MG (glioblastoma) during 72 h of incubation using resazurin test and evaluated the substances receptor using molecular docking. Results: The compound with the carbamate link and ethylene substituent on the phenyl ring inhibited proliferation in these models by 70–90% without cytotoxic effects. The compound did not affect the viability of the immortalized fibroblast cell line Bj-5ta. The compound was also able to enhance the action of doxorubicin and temozolomide by about 20%. According to the molecular modeling data, the probable receptor target for the synthesized compound was the A2AR adenosine receptor. Conclusions: The results obtained on the ethylenediurea analogs with ethyl substituent in the aromatic ring are promising for the development of novel anticancer therapeutics. Full article
(This article belongs to the Special Issue Natural and Synthetic Molecules with Anticancer Activity: Pharmacological Basis and Mechanistic Insight)
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14 pages, 2885 KiB  
Article
Triple Combinations of Histone Lysine Demethylase Inhibitors with PARP1 Inhibitor–Olaparib and Cisplatin Lead to Enhanced Cytotoxic Effects in Head and Neck Cancer Cells
by Dawid Dorna, Robert Kleszcz and Jarosław Paluszczak
Biomedicines 2024, 12(6), 1359; https://doi.org/10.3390/biomedicines12061359 - 19 Jun 2024
Cited by 2 | Viewed by 1622
Abstract
PARP inhibitors are used to treat cancers with a deficient homologous recombination (HR) DNA repair pathway. Interestingly, recent studies revealed that HR repair could be pharmacologically impaired by the inhibition of histone lysine demethylases (KDM). Thus, we investigated whether KDM inhibitors could sensitize [...] Read more.
PARP inhibitors are used to treat cancers with a deficient homologous recombination (HR) DNA repair pathway. Interestingly, recent studies revealed that HR repair could be pharmacologically impaired by the inhibition of histone lysine demethylases (KDM). Thus, we investigated whether KDM inhibitors could sensitize head and neck cancer cells, which are usually HR proficient, to PARP inhibition or cisplatin. Therefore, we explored the effects of double combinations of KDM4–6 inhibitors (ML324, CPI-455, GSK-J4, and JIB-04) with olaparib or cisplatin, or their triple combinations with both drugs, on the level of DNA damage and apoptosis. FaDu and SCC-040 cells were treated with individual compounds and their combinations, and cell viability, apoptosis, DNA damage, and gene expression were assessed using the resazurin assay, Annexin V staining, H2A.X activation, and qPCR, respectively. Combinations of KDM inhibitors with cisplatin enhanced cytotoxic effects, unlike combinations with olaparib. Triple combinations of KDM inhibitors with cisplatin and olaparib exhibited the best cytotoxic activity, which was associated with DNA damage accumulation and altered expression of genes associated with apoptosis induction and cell cycle arrest. In conclusion, triple combinations of KDM inhibitors (especially GSK-J4 and JIB-04) with cisplatin and olaparib represent a promising strategy for head and neck cancer treatment. Full article
(This article belongs to the Special Issue Natural and Synthetic Molecules with Anticancer Activity: Pharmacological Basis and Mechanistic Insight)
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11 pages, 1690 KiB  
Article
Antiproliferative Effects in Colorectal Cancer and Stabilisation in Cyclodextrins of the Phytoalexin Isorhapontigenin
by Silvia Navarro-Orcajada, Francisco José Vidal-Sánchez, Irene Conesa, Francisco Escribano-Naharro, Adrián Matencio and José Manuel López-Nicolás
Biomedicines 2023, 11(11), 3023; https://doi.org/10.3390/biomedicines11113023 - 10 Nov 2023
Cited by 3 | Viewed by 1365
Abstract
Isorhapontigenin has been proposed as a better alternative for oral administration than the famous resveratrol, as it shares many biological activities, but with a structure that could make its delivery easier. Although this hydrophobic structure could enhance bioavailability, it could also be a [...] Read more.
Isorhapontigenin has been proposed as a better alternative for oral administration than the famous resveratrol, as it shares many biological activities, but with a structure that could make its delivery easier. Although this hydrophobic structure could enhance bioavailability, it could also be a disadvantage in the development of products. In this research, we study the antiproliferative activity of this stilbene against colorectal cancer and overcome its limitations through molecular encapsulation in cyclodextrins. The cytotoxic activity against human colorectal cancer cells of isorhapontigenin was similar to that of resveratrol or piceatannol, supporting its use as a bioactive alternative. The study of the encapsulation through fluorescence spectroscopy and molecular docking revealed that the complexation satisfies a 1:1 stoichiometry and that HP-β-CD is the most suitable CD to encapsulate this stilbene. Through a spectrophotometric assay, it was observed that this CD could double the basal water solubility, exceeding the solubility of other hydroxylated stilbenes. The stability of these inclusion complexes was higher at a pH below 9 and refrigeration temperatures. Moreover, the use of CDs retained more than 78% of isorhapontigenin after storage for 12 weeks, compared to 15% in free form. Overall, these findings could help design novel formulations to better deliver isorhapontigenin. Full article
(This article belongs to the Special Issue Natural and Synthetic Molecules with Anticancer Activity: Pharmacological Basis and Mechanistic Insight)
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