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Pharmaceutics
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Natural Products for Anticancer Application
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Natural Products for Anticancer Application

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: 20 March 2025 | Viewed by 15947

Special Issue Editors

Dr. Alessandro Maugeri

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Guest Editor
Department of Health Sciences, University "Magna Græcia" of Catanzaro, 88100 Catanzaro, Italy
Interests: natural products; molecular pharmacology; cancer; inflammation; neuroprotection
Special Issues, Collections and Topics in MDPI journals
Dr. Santa Cirmi

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Guest Editor
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98166 Messina, Italy
Interests: natural products; molecular pharmacology; cancer; inflammation; neuroprotection
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Michele Navarra

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Guest Editor
Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, viale Annunziata, I-98168 Messina, Italy
Interests: natural products; molecular pharmacology; cancer; inflammation; neuroprotection
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Thomas Efferth

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Guest Editor
Department of Pharmaceutical Biology, Institute of Pharmaceutical and Biomedical Sciences, Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany
Interests: natural products; molecular pharmacology; cancer; drug resistance; genome-wide profiling
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

We are pleased to invite you to contribute an article to a Special Issue of Pharmaceutics called “Natural Products for Anticancer Application”.

Cancer still represents one of the most alarming burdens of our society, despite the unceasing advances achieved by the scientific community. Therefore, novel strategies able to prevent and/or manage neoplasms are constantly sought after to hamper their onset and development.

The plant kingdom has long been a remarkable source of countless chemical substances with noteworthy pharmacological properties, including anticancer ones. Natural remedies are now being consumed as part of a method for strengthening our defenses against cellular degeneration, eventually potentially leading to the initiation of cells into cancerous ones. Moreover, the possible synergism of components constituting them can be exploited to achieve stronger effects.

This Special Issue aims to assemble recent scientific evidence on the anticancer properties of natural products, both as single phytochemicals and phytocomplexes, after their complete qualiquantitative chemical characterization, studied in both preclinical and clinical settings.

In this Special Issue, original research articles, reviews systematic reviews, and meta-analyses are all welcome.

We look forward to receiving your contributions.

Dr. Alessandro Maugeri
Dr. Santa Cirmi
Prof. Dr. Michele Navarra
Prof. Dr. Thomas Efferth
Guest Editors

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.

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. Pharmaceutics 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 2900 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

  • natural products
  • cancer
  • plant extracts
  • phytochemicals
  • preclinical
  • clinical

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Published Papers (8 papers)

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Research

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20 pages, 7024 KiB  
Article
Auraptene Boosts the Efficacy of the Tamoxifen Metabolites Endoxifen and 4-OH-Tamoxifen in a Chemoresistant ER+ Breast Cancer Model
by Angel Pulido-Capiz, Brenda Chimal-Vega, Luis Pablo Avila-Barrientos, Alondra Campos-Valenzuela, Raúl Díaz-Molina, Raquel Muñiz-Salazar, Octavio Galindo-Hernández and Victor García-González
Pharmaceutics 2024, 16(9), 1179; https://doi.org/10.3390/pharmaceutics16091179 - 6 Sep 2024
Viewed by 1418
Abstract
Approximately 80% of breast cancer (BC) cases are estrogen receptor positive (ER+) and sensitive to hormone treatment; Tamoxifen is a prodrug, and its main plasmatic active metabolites are 4-hydroxytamoxifen (4-OH Tam) and endoxifen. Despite the effectiveness of tamoxifen therapy, resistance can be developed. [...] Read more.
Approximately 80% of breast cancer (BC) cases are estrogen receptor positive (ER+) and sensitive to hormone treatment; Tamoxifen is a prodrug, and its main plasmatic active metabolites are 4-hydroxytamoxifen (4-OH Tam) and endoxifen. Despite the effectiveness of tamoxifen therapy, resistance can be developed. An increment in eukaryotic initiation factor-4A complex (eIF4A) activity can result in tamoxifen-resistant tumor cells. For this work, we developed a cell variant resistant to 4-OH Tam and endoxifen, denominated MCF-7Var E; then, the aim of this research was to reverse the acquired resistance of this variant to tamoxifen metabolites by incorporating the natural compound auraptene. Combination treatments of tamoxifen derivatives and auraptene successfully sensitized the chemoresistant MCF-7Var E. Our data suggest a dual regulation of eIF4A and ER by auraptene. Joint treatments of 4-OH Tam and endoxifen with auraptene identified a novel focus for chemoresistance disruption. Synergy was observed using the auraptene molecule and tamoxifen-derived metabolites, which induced a sensitization in MCF-7Var E cells and ERα parental cells that was not observed in triple-negative breast cancer cells (TNBC). Our results suggest a synergistic effect between auraptene and tamoxifen metabolites in a resistant ER+ breast cancer model, which could represent the first step to achieving a pharmacologic strategy. Full article
(This article belongs to the Special Issue Natural Products for Anticancer Application)
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20 pages, 9271 KiB  
Article
Oxyresveratrol in Breast Cancer Cells: Synergistic Effect with Chemotherapeutics Doxorubicin or Melphalan on Proliferation, Cell Cycle Arrest, and Cell Death
by Carlos Luan Alves Passos, Christian Ferreira, Aline Gabrielle Alves de Carvalho, Jerson Lima Silva, Rafael Garrett and Eliane Fialho
Pharmaceutics 2024, 16(7), 873; https://doi.org/10.3390/pharmaceutics16070873 - 29 Jun 2024
Cited by 4 | Viewed by 1368
Abstract
Breast cancer is the second most common type of cancer in the world. Polyphenols can act at all stages of carcinogenesis and oxyresveratrol (OXY) promising anticancer properties, mainly associated with chemotherapy drugs. The aim of this study was to investigate the effect of [...] Read more.
Breast cancer is the second most common type of cancer in the world. Polyphenols can act at all stages of carcinogenesis and oxyresveratrol (OXY) promising anticancer properties, mainly associated with chemotherapy drugs. The aim of this study was to investigate the effect of OXY with doxorubicin (DOX) or melphalan (MEL), either isolated or associated, in MCF-7 and MDA-MB-231 breast cancer cells. Our results showed that OXY, DOX, and MEL presented cytotoxicity, in addition to altering cell morphology. The synergistic association of OXY + DOX and OXY + MEL reduced the cell viability in a dose-dependent manner. The OXY, DOX, or MEL and associations were able to alter the ROS production, ∆Ψm, and cell cycle; DOX and OXY + DOX led the cells to necrosis. Furthermore, OXY and OXY + MEL were able to lead the cells to apoptosis and upregulate caspases-3, -7, -8, and -9 in both cells. LC-HRMS showed that 7-deoxidoxorubicinone and doxorubicinol, responsible for the cardiotoxic effect, were not identified in cells treated with the OXY + DOX association. In summary, our results demonstrate for the first time the synergistic effect of OXY with chemotherapeutic agents in breast cancer cells, offering a new strategy for future animal studies. Full article
(This article belongs to the Special Issue Natural Products for Anticancer Application)
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16 pages, 3357 KiB  
Article
Antimutagenicity and Antioxidant Activity of Castanea sativa Mill. Bark Extract
by Sofia Gasperini, Giulia Greco, Sabrina Angelini, Patrizia Hrelia, Carmela Fimognari and Monia Lenzi
Pharmaceutics 2023, 15(10), 2465; https://doi.org/10.3390/pharmaceutics15102465 - 14 Oct 2023
Viewed by 1410
Abstract
Castanea sativa Mill. (Cs), a plant traditionally employed in nutrition and to treat various respiratory and gastrointestinal infections, possesses cancer chemopreventive characteristics. In particular, Cs bark extract previously demonstrated antiproliferative and pro-apoptotic activities against a leukemic lymphoblastic cell line. Starting from this evidence, [...] Read more.
Castanea sativa Mill. (Cs), a plant traditionally employed in nutrition and to treat various respiratory and gastrointestinal infections, possesses cancer chemopreventive characteristics. In particular, Cs bark extract previously demonstrated antiproliferative and pro-apoptotic activities against a leukemic lymphoblastic cell line. Starting from this evidence, the aim of this paper was to investigate the possibility to affect also the earlier phases of the carcinogenic process by evaluating Cs bark extract’s antimutagenic properties, in particular using the “In Vitro Mammalian Cell Micronucleus Test” on TK6 cells performed by flow cytometry. For this purpose, since an ideal chemopreventive agent should be virtually nontoxic, the first step was to exclude the extract’s genotoxicity. Afterwards, the antimutagenic effect of the extract was evaluated against two known mutagens, the clastogen mitomycin C (MMC) and the aneugen vinblastine (VINB). Our results indicate that Cs bark extract protected cells from MMC-induced damage (micronuclei frequency fold increase reduction from 2.9 to 1.8) but not from VINB. Moreover, we demonstrated that Cs bark extract was a strong antioxidant and significantly reduced MMC-induced ROS levels by over 2 fold. Overall, our research supports the assumption that Cs bark extract can counteract MMC mutagenicity by possibly scavenging ROS production. Full article
(This article belongs to the Special Issue Natural Products for Anticancer Application)
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20 pages, 6731 KiB  
Article
The Novel Artemisinin Dimer Isoniazide ELI-XXIII-98-2 Induces c-MYC Inhibition, DNA Damage, and Autophagy in Leukemia Cells
by Mohamed Elbadawi, Joelle C. Boulos, Mona Dawood, Min Zhou, Waseem Gul, Mahmoud A. ElSohly, Sabine M. Klauck and Thomas Efferth
Pharmaceutics 2023, 15(4), 1107; https://doi.org/10.3390/pharmaceutics15041107 - 30 Mar 2023
Cited by 4 | Viewed by 2577
Abstract
The proto-oncogenic transcription factor c-MYC plays a pivotal role in the development of tumorigenesis, cellular proliferation, and the control of cell death. Its expression is frequently altered in many cancer types, including hematological malignancies such as leukemia. The dimer isoniazide ELI-XXIII-98-2 is a [...] Read more.
The proto-oncogenic transcription factor c-MYC plays a pivotal role in the development of tumorigenesis, cellular proliferation, and the control of cell death. Its expression is frequently altered in many cancer types, including hematological malignancies such as leukemia. The dimer isoniazide ELI-XXIII-98-2 is a derivative of the natural product artemisinin, with two artemisinin molecules and an isoniazide moiety as a linker in between them. In this study, we aimed to study the anticancer activity and the molecular mechanisms of this dimer molecule in drug-sensitive CCRF-CEM leukemia cells and their corresponding multidrug-resistant CEM/ADR5000 sub-line. The growth inhibitory activity was studied using the resazurin assay. To reveal the molecular mechanisms underlying the growth inhibitory activity, we performed in silico molecular docking, followed by several in vitro approaches such as the MYC reporter assay, microscale thermophoresis, microarray analyses, immunoblotting, qPCR, and comet assay. The artemisinin dimer isoniazide showed a potent growth inhibitory activity in CCRF-CEM but a 12-fold cross-resistance in multidrug-resistant CEM/ADR5000 cells. The molecular docking of artemisinin dimer isoniazide with c-MYC revealed a good binding (lowest binding energy of −9.84 ± 0.3 kcal/mol) and a predicted inhibition constant (pKi) of 66.46 ± 29.5 nM, which was confirmed by microscale thermophoresis and MYC reporter cell assays. Furthermore, c-MYC expression was downregulated by this compound in microarray hybridization and Western blotting analyses. Finally, the artemisinin dimer isoniazide modulated the expression of autophagy markers (LC3B and p62) and the DNA damage marker pH2AX, indicating the stimulation of both autophagy and DNA damage, respectively. Additionally, DNA double-strand breaks were observed in the alkaline comet assay. DNA damage, apoptosis, and autophagy induction could be attributed to the inhibition of c-MYC by ELI-XXIII-98-2. Full article
(This article belongs to the Special Issue Natural Products for Anticancer Application)
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Review

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21 pages, 3014 KiB  
Review
The Role of Pentacyclic Triterpenoids in Non-Small Cell Lung Cancer: The Mechanisms of Action and Therapeutic Potential
by Young-Shin Lee, Ryuk Jun Kwon, Hye Sun Lee, Jae Heun Chung, Yun Seong Kim, Han-Sol Jeong, Su-Jung Park, Seung Yeon Lee, Taehwa Kim and Seong Hoon Yoon
Pharmaceutics 2025, 17(1), 22; https://doi.org/10.3390/pharmaceutics17010022 - 26 Dec 2024
Viewed by 746
Abstract
Lung cancer remains a major global health problem because of its high cancer-related mortality rate despite advances in therapeutic approaches. Non-small cell lung cancer (NSCLC), a major subtype of lung cancer, is more amenable to surgical intervention in its early stages. However, the [...] Read more.
Lung cancer remains a major global health problem because of its high cancer-related mortality rate despite advances in therapeutic approaches. Non-small cell lung cancer (NSCLC), a major subtype of lung cancer, is more amenable to surgical intervention in its early stages. However, the prognosis for advanced NSCLC remains poor, owing to limited treatment options. This underscores the growing need for novel therapeutic strategies to complement existing treatments and improve patient outcomes. In recent years, pentacyclic triterpenoids, a group of natural compounds, have emerged as promising candidates for cancer therapy due to their anticancer properties. Pentacyclic triterpenoids, such as lupeol, betulinic acid, betulin, oleanolic acid, ursolic acid, glycyrrhetinic acid, glycyrrhizin, and asiatic acid, have demonstrated the ability to inhibit cell proliferation and angiogenesis, induce apoptosis, suppress metastasis, and modulate inflammatory and immune pathways in NSCLC cell line models. These compounds exert their effects by modulating important signaling pathways such as NF-κB, PI3K/Akt, and MAPK. Furthermore, advances in drug delivery technologies such as nanocarriers and targeted delivery systems have improved the bioavailability and therapeutic efficacy of triterpenoids. However, despite promising preclinical data, rigorous clinical trials are needed to verify their safety and efficacy. This review explores the role of triterpenoids in NSCLC and therapeutic potential in preclinical models, focusing on their molecular mechanisms of action. Full article
(This article belongs to the Special Issue Natural Products for Anticancer Application)
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15 pages, 1369 KiB  
Review
Exploring the Potential Use of Natural Products Together with Alkalization in Cancer Therapy
by Masahide Isowa, Reo Hamaguchi, Ryoko Narui, Hiromasa Morikawa, Toshihiro Okamoto and Hiromi Wada
Pharmaceutics 2024, 16(6), 787; https://doi.org/10.3390/pharmaceutics16060787 - 10 Jun 2024
Viewed by 1422
Abstract
Cancer treatment is a significant focus in medicine, owing to the increasing global incidence of cancers. Patients with advanced cancers that do not respond to conventional therapies have limited options and an unfavorable prognosis. Consequently, researchers are investigating complementary approaches to conventional treatments. [...] Read more.
Cancer treatment is a significant focus in medicine, owing to the increasing global incidence of cancers. Patients with advanced cancers that do not respond to conventional therapies have limited options and an unfavorable prognosis. Consequently, researchers are investigating complementary approaches to conventional treatments. One such approach is alkalization therapy, which aims to neutralize the acidic tumor microenvironment (TME) by increasing its pH level. The acidic TME promotes inflammation, tumor progression, and drug resistance. Alkalization therapy has been demonstrated to be effective for various cancers. In addition, natural products, such as triterpenoids, parthenolides, fulvic acid, Taxus yunnanensis, and apple pectin have the potential to alleviate symptoms, maintain physical fitness, and improve treatment outcomes of cancer patients through their anti-inflammatory, antioxidant, and anticancer properties. In this review, we focus on the effects of alkalization therapy and natural products on cancer. Furthermore, we present a case series of advanced cancer patients who received alkalization therapy and natural products alongside standard treatments, resulting in long-term survival. We posit that alkalization therapy together with supplementation with natural products may confer benefits to cancer patients, by mitigating the side effects of chemotherapy and complementing standard treatments. However, further research is warranted to validate these clinical findings. Full article
(This article belongs to the Special Issue Natural Products for Anticancer Application)
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15 pages, 290 KiB  
Review
Mechanisms of Action of Phytoestrogens and Their Role in Familial Adenomatous Polyposis
by Irene Falsetti, Gaia Palmini, Teresa Iantomasi, Maria Luisa Brandi and Francesco Tonelli
Pharmaceutics 2024, 16(5), 640; https://doi.org/10.3390/pharmaceutics16050640 - 10 May 2024
Cited by 1 | Viewed by 1944
Abstract
Familial adenomatous polyposis (FAP) is a rare disease characterized by the development of adenomatous polyps in the colon and rectum already in adolescence. If left untreated, patients develop colorectal cancer (CRC) with a 100% probability. To date, the gold standard of FAP management [...] Read more.
Familial adenomatous polyposis (FAP) is a rare disease characterized by the development of adenomatous polyps in the colon and rectum already in adolescence. If left untreated, patients develop colorectal cancer (CRC) with a 100% probability. To date, the gold standard of FAP management is surgery, which is associated with morbidity and mortality. A chemopreventive agent capable of delaying, preventing and reversing the development of CRC has been sought. Several classes of drugs have been used but to date no chemopreventive drug has been found for the management of this disease. In recent years, the importance of estrogen receptors in FAP and CRC, particularly the β subtype, has emerged. Indeed, the expression of the latter is strongly reduced in adenomatous polyps and CRC and is inversely correlated with the aggressiveness of the disease. Since phytoestrogens have a high affinity for this receptor, they have been suggested for use as chemopreventive agents in FAP and CRC. A combination of phytoestrogens and insoluble fibres has proved particularly effective. In this review, the various mechanisms of action of phytoestrogens were analyzed and the effectiveness of using phytoestrogens as an effective chemopreventive strategy was discussed. Full article
(This article belongs to the Special Issue Natural Products for Anticancer Application)
24 pages, 1063 KiB  
Review
Therapeutic Effects of Essential Oils and Their Bioactive Compounds on Prostate Cancer Treatment
by Leticia Santos Pimentel, Luciana Machado Bastos, Luiz Ricardo Goulart and Lígia Nunes de Morais Ribeiro
Pharmaceutics 2024, 16(5), 583; https://doi.org/10.3390/pharmaceutics16050583 - 24 Apr 2024
Cited by 2 | Viewed by 3066
Abstract
Since prostate cancer (PCa) relies on limited therapies, more effective alternatives are required. Essential oils (EOs) and their bioactive compounds are natural products that have many properties including anticancer activity. This review covers studies published between 2000 and 2023 and discusses the anti-prostate [...] Read more.
Since prostate cancer (PCa) relies on limited therapies, more effective alternatives are required. Essential oils (EOs) and their bioactive compounds are natural products that have many properties including anticancer activity. This review covers studies published between 2000 and 2023 and discusses the anti-prostate cancer mechanisms of the EOs from several plant species and their main bioactive compounds. It also provides a critical perspective regarding the challenges to be overcome until they reach the market. EOs from chamomile, cinnamon, Citrus species, turmeric, Cymbopogon species, ginger, lavender, Mentha species, rosemary, Salvia species, thyme and other species have been tested in different PCa cell lines and have shown excellent results, including the inhibition of cell growth and migration, the induction of apoptosis, modulation in the expression of apoptotic and anti-apoptotic genes and the suppression of angiogenesis. The most challenging aspects of EOs, which limit their clinical uses, are their highly lipophilic nature, physicochemical instability, photosensitivity, high volatility and composition variability. The processing of EO-based products in the pharmaceutical field may be an interesting alternative to circumvent EOs’ limitations, resulting in several benefits in their further clinical use. Identifying their bioactive compounds, therapeutic effects and chemical structures could open new perspectives for innovative developments in the field. Moreover, this could be helpful in obtaining versatile chemical synthesis routes and/or biotechnological drug production strategies, providing an accurate, safe and sustainable source of these bioactive compounds, while looking at their use as gold-standard therapy in the close future. Full article
(This article belongs to the Special Issue Natural Products for Anticancer Application)
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