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Antiproliferative and Anti-inflammatory Activities of Plant-Derived Compounds

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

Deadline for manuscript submissions: closed (31 October 2021) | Viewed by 17902

Special Issue Editors


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Guest Editor
Department of Oncology and Molecular Medicine, Istituto Superiore di Sanità, Viale Regina Elena 299, 00161 Rome, Italy
Interests: biochemistry; melanoma cell biology; cancer immunomodulation; phytochemicals
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department Biochemistry & Molecular Biology, The Medical College of Georgia at Augusta University, Augusta, GA 30912, USA
Interests: gut microbiome; liver diseases; aging; energy metabolism; natural compounds
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

In recent years, plant-derived compounds have been extensively studied for their several beneficial effects on human health. Historically, phytochemicals have played a pivotal role in traditional medicine, and they have often represented excellent precursors or prototypes of several drugs. A wide number of studies sustain that natural compounds, contained in common foods and beverages, improve human health by counteracting inflammation, oxidative stress, and metabolic dysfunctions. In fact, herbal preparations are able to reduce risk factors for several pathologies, including metabolic syndrome, obesity, diabetes, cardiovascular diseases, neurodegenerative diseases, and cancer.

This Special Issue aims to highlight recent advances in the antiproliferative and anti-inflammatory activities of plant-derived compounds. Covered aspects include but are not limited to in vitro and in vivo biological activity, anticancer potential, antioxidant properties of natural molecules, and their derivatives. 

We invite researchers to contribute reviews or original articles on the health-promoting effects of phytochemicals. 

Potential topics include but are not limited to the following:

  • Plant-derived compounds as anticancer and anti-inflammatory agents;
  • Effects of phytochemicals or nutraceuticals against human oxidative stress-related diseases;
  • Characterization of phytochemicals with immunomodulatory activities;
  • Phytochemicals as an epigenetic modulator;
  • Herbal therapeutants in ameliorating experimental chronic diseases;
  • Clinical applications of phytochemicals in treating oxidative stress and inflammation.

Dr. Claudio Tabolacci
Dr. Ravirajsinh N. Jadeja
Guest Editors

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Keywords

  • Phytochemicals
  • Herbal extract
  • Phytotherapy
  • Cancer
  • Oxidative stress
  • Inflammation
  • Immunomodulators

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Published Papers (4 papers)

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Research

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12 pages, 5757 KiB  
Article
Turmeric Extract (Curcuma longa) Mediates Anti-Oxidative Effects by Reduction of Nitric Oxide, iNOS Protein-, and mRNA-Synthesis in BV2 Microglial Cells
by Jana Streyczek, Matthias Apweiler, Lu Sun and Bernd L. Fiebich
Molecules 2022, 27(3), 784; https://doi.org/10.3390/molecules27030784 - 25 Jan 2022
Cited by 9 | Viewed by 4362
Abstract
Plant-derived products have been used since the beginnings of human history to treat various pathological conditions. Practical experience as well as a growing body of research suggests the benefits of the use of turmeric (Curcuma longa) and some of its active [...] Read more.
Plant-derived products have been used since the beginnings of human history to treat various pathological conditions. Practical experience as well as a growing body of research suggests the benefits of the use of turmeric (Curcuma longa) and some of its active components in the reduction of oxidative stress, a mechanism leading to neurodegeneration. In this current study, we investigated the effects of a preparation of Curcuma longa, and its constituents curcumin, tetrahydrocurcumin, and curcumenol, in one of the molecular pathways leading to oxidative stress, which is the release of NO, a free radical involved in stress conditions, using the BV2 microglial cell line. The concentration-dependent reduction of NO is linked to reduced amounts of iNOS protein- and mRNA-synthesis and is possibly mediated by the phosphorylation of mitogen-activated protein kinases (MAPK) such as p42/44 or p38 MAPK. Therefore, the use of turmeric extract is a promising therapeutic option for diseases linked to the dysregulation of oxidative stress, with fewer side-effects in comparison to the currently used pharmacotherapeutics. Full article
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13 pages, 2066 KiB  
Article
Cytotoxicity of Frutalin on Distinct Cancer Cells Is Independent of Its Glycosylation
by Carla Oliveira, Ana Isabel Freitas, Nair Campos, Lucília Saraiva and Lucília Domingues
Molecules 2021, 26(16), 4712; https://doi.org/10.3390/molecules26164712 - 4 Aug 2021
Cited by 2 | Viewed by 2279
Abstract
Frutalin is a plant lectin with beneficial immunobiological action, although the access to its active form is still restricted. Moreover, there is a knowledge gap on isoform activity and glycosylation impact on its bioactivity, and recombinant production protocols were seen as ineffective. Here, [...] Read more.
Frutalin is a plant lectin with beneficial immunobiological action, although the access to its active form is still restricted. Moreover, there is a knowledge gap on isoform activity and glycosylation impact on its bioactivity, and recombinant production protocols were seen as ineffective. Here, a simpler and faster production and purification protocol was developed, attaining a yield of purified frutalin 3.3-fold higher than that obtained previously. Hemagglutination assays confirmed that this frutalin isoform could not agglutinate rabbit erythrocytes, while maintaining the native tetrameric structure, as indicated by DLS analysis, and strong interaction with methyl-alpha-galactose, in fluorescence spectroscopy studies. The cytotoxicity of the recombinant frutalin isoform was shown in a broad panel of human cancer cells: colon (HCT116), melanoma (A375), triple-negative breast cancer (MDA-MB-231), and ovarian (IGROV-1). Treatment with 8.5–11.8 μM TrxFTL reduced proliferation of all cancer cells to half in 48 h. This anti-proliferative effect encompasses the p53 pathway since it was significantly reduced in p53-null colon cancer cells (HCT116 p53−/−; GI50 of 25.0 ± 3.0 μM), when compared to the isogenic p53-positive cells (HCT116 p53+/+; GI50 of 8.7 ± 1.8 μM; p < 0.002). This recombinantly produced frutalin isoform has relevant cytotoxic effect and its biological activity is not dependent on glycosylation. The developed E. coli production and purification protocol generates high yield of non-glycosylated frutalin isoform with potent cytotoxic activity, enabling the development of novel anticancer p53-targeting therapies. Full article
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15 pages, 7146 KiB  
Article
Targeting Melanoma-Initiating Cells by Caffeine: In Silico and In Vitro Approaches
by Claudio Tabolacci, Martina Cordella, Stefania Rossi, Marialaura Bonaccio, Adriana Eramo, Carlo Mischiati, Simone Beninati, Licia Iacoviello, Antonio Facchiano and Francesco Facchiano
Molecules 2021, 26(12), 3619; https://doi.org/10.3390/molecules26123619 - 13 Jun 2021
Cited by 8 | Viewed by 5433
Abstract
The beneficial effects of coffee on human diseases are well documented, but the molecular mechanisms of its bioactive compounds on cancer are not completely elucidated. This is likely due to the large heterogeneity of coffee preparations and different coffee-based beverages, but also to [...] Read more.
The beneficial effects of coffee on human diseases are well documented, but the molecular mechanisms of its bioactive compounds on cancer are not completely elucidated. This is likely due to the large heterogeneity of coffee preparations and different coffee-based beverages, but also to the choice of experimental models where proliferation, differentiation and immune responses are differently affected. The aim of the present study was to investigate the effects of one of the most interesting bioactive compounds in coffee, i.e., caffeine, using a cellular model of melanoma at a defined differentiation level. A preliminary in silico analysis carried out on public gene-expression databases identified genes potentially involved in caffeine’s effects and suggested some specific molecular targets, including tyrosinase. Proliferation was investigated in vitro on human melanoma initiating cells (MICs) and cytokine expression was measured in conditioned media. Tyrosinase was revealed as a key player in caffeine’s mechanisms of action, suggesting a crucial role in immunomodulation through the reduction in IL-1β, IP-10, MIP-1α, MIP-1β and RANTES secretion onto MICs conditioned media. The potent antiproliferative effects of caffeine on MICs are likely to occur by promoting melanin production and reducing inflammatory signals’ secretion. These data suggest tyrosinase as a key player mediating the effects of caffeine on melanoma. Full article
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Review

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16 pages, 2122 KiB  
Review
Flavonoids: A Myth or a Reality for Cancer Therapy?
by Cinzia Forni, Massimiliano Rossi, Ilaria Borromeo, Giordana Feriotto, Giovambattista Platamone, Claudio Tabolacci, Carlo Mischiati and Simone Beninati
Molecules 2021, 26(12), 3583; https://doi.org/10.3390/molecules26123583 - 11 Jun 2021
Cited by 52 | Viewed by 4821
Abstract
Nutraceuticals are biologically active molecules present in foods; they can have beneficial effects on health, but they are not available in large enough quantities to perform this function. Plant metabolites, such as polyphenols, are widely diffused in the plant kingdom, where they play [...] Read more.
Nutraceuticals are biologically active molecules present in foods; they can have beneficial effects on health, but they are not available in large enough quantities to perform this function. Plant metabolites, such as polyphenols, are widely diffused in the plant kingdom, where they play fundamental roles in plant development and interactions with the environment. Among these, flavonoids are of particular interest as they have significant effects on human health. In vitro and/or in vivo studies described flavonoids as essential nutrients for preventing several diseases. They display broad and promising bioactivities to fight cancer, inflammation, bacterial infections, as well as to reduce the severity of neurodegenerative and cardiovascular diseases or diabetes. Therefore, it is not surprising that interest in flavonoids has sharply increased in recent years. More than 23,000 scientific publications on flavonoids have described the potential anticancer activity of these natural molecules in the last decade. Studies, in vitro and in vivo, show that flavonoids exhibit anticancer properties, and many epidemiological studies confirm that dietary intake of flavonoids leads to a reduced risk of cancer. This review provides a glimpse of the mechanisms of action of flavonoids on cancer cells. Full article
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