The Role of Natural Extracts and Phytochemicals in Cancer Therapy

A special issue of Cells (ISSN 2073-4409).

Deadline for manuscript submissions: closed (15 September 2023) | Viewed by 6391

Special Issue Editors


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Guest Editor
Department of Biomedicine, Neurosciences and Advanced Diagnostics (BIND), Institute of Biochemistry, University of Palermo, Via del Vespro, 131, 90127 Palermo, Italy
Interests: breast cancer; chemotherapy resistance; cancer stem cells; NAFLD; natural drugs
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Guest Editor
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), Laboratory of Biochemistry, University of Palermo, Viale delle Scienze, ed. 16, 90128 Palermo, Italy
Interests: TNBC; miRNA; cell death; cancer stem cells
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The plant world is one of the main sources of active molecules used by researchers to find new anti-cancer therapies. Phytochemicals are generally organic compounds of low molecular weight produced by the primary and secondary metabolism of plants. They frequently possess antitumor and antimutagenic properties thanks to their antioxidant and anti-inflammatory action. For instance, many anti-tumor drugs of natural origin, such as vinca alkaloids (vincristine and vinblastine), are used, thanks their antiblastic properties.

The purpose of this Special Issue is to collect original articles or reviews concerning the effect of natural extracts, such as essential oils and phytochemicals, in relation to the following topics:

  • Antitumor and/or protective effects in in vitro and in vivo models, with the identification of the biochemical pathways involved;
  • Potential efficacy deriving from their integration in standard oncological therapies;
  • Preventive and anti-mutagenic action;
  • Action on cancer stem cells and resistance to chemotherapy.

Dr. Daniela Carlisi
Dr. Anna De Blasio
Guest Editors

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Published Papers (4 papers)

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Research

22 pages, 14441 KiB  
Article
Cytotoxic Effect Induced by Sicilian Oregano Essential Oil in Human Breast Cancer Cells
by Diana Di Liberto, Nicolò Iacuzzi, Giovanni Pratelli, Antonella Porrello, Antonella Maggio, Salvatore La Bella, Anna De Blasio, Antonietta Notaro, Antonella D’Anneo, Sonia Emanuele, Federica Affranchi, Michela Giuliano, Marianna Lauricella and Daniela Carlisi
Cells 2023, 12(23), 2733; https://doi.org/10.3390/cells12232733 - 29 Nov 2023
Cited by 1 | Viewed by 1636
Abstract
Origanum vulgare L. is an aromatic plant that exerts antibacterial, antioxidant, anti-inflammatory, and antitumor activities, mainly due to its essential oil (EO) content. In this study, we investigated the possible mechanism underlying the in vitro antitumor activity of EO extracted by hydrodistillation of [...] Read more.
Origanum vulgare L. is an aromatic plant that exerts antibacterial, antioxidant, anti-inflammatory, and antitumor activities, mainly due to its essential oil (EO) content. In this study, we investigated the possible mechanism underlying the in vitro antitumor activity of EO extracted by hydrodistillation of dried flowers and leaves of Origanum vulgare L. grown in Sicily (Italy) in MDA-MB-231 and MCF-7 breast cancer cell lines. Gas chromatography–mass spectrometry analysis of Oregano essential oil (OEO) composition highlighted the presence of twenty-six major phytocompounds, such as p-cymene, γ-terpinene, and thymoquinone p-acetanisole. OEO possesses strong antioxidant capacity, as demonstrated by the DPPH test. Our studies provided evidence that OEO reduces the viability of both MCF-7 and MDA-MB-231 cells. The cytotoxic effect of OEO on breast cancer cells was partially counteracted by the addition of z-VAD-fmk, a general caspase inhibitor. Caspases and mitochondrial dysfunction appeared to be involved in the OEO-induced death mechanism. Western blotting analysis showed that OEO-induced activation of pro-caspases-9 and -3 and fragmentation of PARP decreased the levels of Bcl-2 and Bcl-xL while increasing those of Bax and VDAC. In addition, fluorescence microscopy and cytofluorimetric analysis showed that OEO induces a loss of mitochondrial membrane potential in both cell lines. Furthermore, we tested the effects of p-cymene, γ-terpinene, thymoquinone, and p-acetanisole, which are the main components of OEO. Our findings highlighted that the effect of OEO on MDA-MB-231 and MCF-7 cells appears to be mainly due to the combination of different constituents of OEO, providing evidence of the potential use of OEO for breast cancer treatment. Full article
(This article belongs to the Special Issue The Role of Natural Extracts and Phytochemicals in Cancer Therapy)
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18 pages, 3597 KiB  
Article
Attenuating Colorectal Cancer Using Nine Cultivars of Australian Lupin Seeds: Apoptosis Induction Triggered by Mitochondrial Reactive Oxygen Species Generation and Caspases-3/7 Activation
by Kishor Mazumder, Asma Aktar, Sujatha Ramasamy, Biswajit Biswas, Philip G. Kerr and Christopher Blanchard
Cells 2023, 12(21), 2557; https://doi.org/10.3390/cells12212557 - 31 Oct 2023
Viewed by 1584
Abstract
As Australian lupin cultivars are rich sources of polyphenols, dietary fibers, high-quality proteins, and abundant bioactive compounds with significant antioxidant, antidiabetic, and anticancer activities, this research work is aimed at investigating the colon cancer alleviation activity of nine cultivars of lupin seeds on [...] Read more.
As Australian lupin cultivars are rich sources of polyphenols, dietary fibers, high-quality proteins, and abundant bioactive compounds with significant antioxidant, antidiabetic, and anticancer activities, this research work is aimed at investigating the colon cancer alleviation activity of nine cultivars of lupin seeds on HCT116 and HT29 colon carcinoma cell lines through anti-proliferation assay, measurement of apoptosis, and identification of the mechanism of apoptosis. Nine cultivars were pre-screened for anti-proliferation of HCT116 and HT29 cells along with consideration of the impact of heat processing on cancer cell viability. Mandelup and Jurien showed significant inhibition of HCT116 cells, whereas the highest inhibition of HT29 cell proliferation was attained by Jurien and Mandelup. Processing decreased the anti-proliferation activity drastically. Lupin cultivars Mandelup, Barlock, and Jurien (dose: 300 μg/mL) induced early and late apoptosis of colon cancer cells in Annexin V-FITC assay. The mechanism of apoptosis was explored, which involves boosting of caspases-3/7 activation and intracellular reactive oxygen species (ROS) generation in HCT116 cells (Mandelup and Barlock) and HT29 cells (Jurien and Mandelup). Thus, the findings showed that lupin cultivars arrest cell cycles by inducing apoptosis of colorectal carcinoma cells triggered by elevated ROS generation and caspases-3/7 activation. Full article
(This article belongs to the Special Issue The Role of Natural Extracts and Phytochemicals in Cancer Therapy)
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20 pages, 6593 KiB  
Article
New Propargyloxy Derivatives of Galangin, Kaempferol and Fisetin—Synthesis, Spectroscopic Analysis and In Vitro Anticancer Activity on Head and Neck Cancer Cells
by Robert Kubina, Kamil Krzykawski, Arkadiusz Sokal, Marcel Madej, Arkadiusz Dziedzic and Monika Kadela-Tomanek
Cells 2023, 12(18), 2288; https://doi.org/10.3390/cells12182288 - 15 Sep 2023
Cited by 1 | Viewed by 918
Abstract
Head and neck cancer (HNC) therapy is limited; therefore, new solutions are increasingly being sought among flavonoids, which exhibit numerous biological properties, including potential anticancer activity. However, because they are mostly insoluble in water, are unstable and have low bioavailability, they are subjected [...] Read more.
Head and neck cancer (HNC) therapy is limited; therefore, new solutions are increasingly being sought among flavonoids, which exhibit numerous biological properties, including potential anticancer activity. However, because they are mostly insoluble in water, are unstable and have low bioavailability, they are subjected to chemical modification to obtain new derivatives with better properties. This study aimed to synthesize and analyze new propargyloxy derivatives of galangin, kaempferol and fisetin, and to evaluate their anticancer activity against selected HNC cell lines. The obtained derivatives were assessed by spectroscopic analysis; next, their anticancer activity was evaluated using a flow cytometer and real-time cell analysis. The results showed that only the fisetin derivative was suitable for further analysis, due to the lack of crystal formation of the compound. The fisetin derivative statistically significantly increases the number of cells in the G2/M phase (p < 0.05) and increases cyclin B1 levels. A statistically significant increase in the number of apoptotic cells after being exposed to the tested compound was also observed (p < 0.05). The data indicate that the obtained fisetin derivative exhibits anticancer activity by affecting the cell cycle and increasing apoptosis in selected HNC lines, which suggests its potential use as a new medicinal agent in the future. Full article
(This article belongs to the Special Issue The Role of Natural Extracts and Phytochemicals in Cancer Therapy)
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20 pages, 11523 KiB  
Article
Kaempferol and Fisetin-Related Signaling Pathways Induce Apoptosis in Head and Neck Cancer Cells
by Robert Kubina, Kamil Krzykawski, Arkadiusz Dziedzic and Agata Kabała-Dzik
Cells 2023, 12(12), 1568; https://doi.org/10.3390/cells12121568 - 06 Jun 2023
Cited by 5 | Viewed by 1639
Abstract
Despite the relative effectiveness of standard cancer treatment strategies, head and neck cancer (HNC) is still considered one of the leading causes of mortality and morbidity. While selected bioactive compounds of plant origin reveal a pro-apoptotic effect, kaempferol and fisetin flavonols have been [...] Read more.
Despite the relative effectiveness of standard cancer treatment strategies, head and neck cancer (HNC) is still considered one of the leading causes of mortality and morbidity. While selected bioactive compounds of plant origin reveal a pro-apoptotic effect, kaempferol and fisetin flavonols have been reported as potential anti-cancer agents against malignant neoplasms. To date, their exact role in signaling pathways of head and neck cancer cells is largely unknown. Based on the various methods of cytotoxicity testing, we elucidated that kaempferol and fisetin inhibit proliferation, reduce the capacity of cell migration, and induce apoptosis in SCC-9, SCC-25, and A-253 HNC cells in a dose-dependent manner in vitro (p < 0.05, fisetin IC50 values of 38.85 µM, 62.34 µM, and 49.21 µM, and 45.03 µM, 49.90 µM, and 47.49 µM for kaempferol–SCC-9, SCC-25, and A-253, respectively). The obtained results showed that exposure to kaempferol and fisetin reduces Bcl-2 protein expression, simultaneously leading to the arrest in the G2/M and S phases of the cell cycle. Kaempferol and fisetin inhibit cell proliferation by interfering with the cell cycle, which is strongly associated with the induction of G2/M arrest, and induce apoptosis by activating caspase-3 and releasing cytochrome c in human HNC cells. In addition, investigating flavonols, by inhibiting anti-apoptotic proteins from the Bcl-2 family and damaging the mitochondrial transmembrane potential, increased the level of cytochrome c. While flavonols selectively induce apoptosis of head and neck cancer cells, they may support oncological therapy as promising agents. The discovery of new derivatives may be a breakthrough in the search for effective chemotherapeutic agents with less toxicity and thus fewer side effects. Full article
(This article belongs to the Special Issue The Role of Natural Extracts and Phytochemicals in Cancer Therapy)
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