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Resveratrol and other Stilbenes: Effects on Dysregulated Gene Expression in Cancers and Novel Delivery Systems.
Poltronieri, P, Xu, B, Giovinazzo, G
Anti-cancer agents in medicinal chemistry. 2021;(5):567-574
Abstract
Trans-resveratrol (RESV), pterostilbene, trans-piceid and trans-viniferins are bioactive stilbenes present in grapes and other plants. Several groups applied biotechnology to introduce their synthesis in plant crops. Biochemical interaction with enzymes, regulation of non-coding RNAs, and activation of signaling pathways and transcription factors are among the main effects described in literature. However, solubility in ethanol, short half-life, metabolism by gut bacteria, make the concentration responsible for the effects observed in cultured cells difficult to achieve. Derivatives obtained by synthesis, trans-resveratrol analogs and methoxylated stilbenes show to be more stable and allow the synthesis of bioactive compounds with higher bioavailability. However, changes in chemical structure may require testing for toxicity. Thus, the delivery of RESV and its natural analogs incorporated into liposomes or nanoparticles, is the best choice to ensure stability during administration and appropriate absorption. The application of RESV and its derivatives with anti-inflammatory and anticancer activity is presented with description of novel clinical trials.
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Strategies to Modulate Specialized Metabolism in Mediterranean Crops: From Molecular Aspects to Field.
Balestrini, R, Brunetti, C, Cammareri, M, Caretto, S, Cavallaro, V, Cominelli, E, De Palma, M, Docimo, T, Giovinazzo, G, Grandillo, S, et al
International journal of molecular sciences. 2021;(6)
Abstract
Plant specialized metabolites (SMs) play an important role in the interaction with the environment and are part of the plant defense response. These natural products are volatile, semi-volatile and non-volatile compounds produced from common building blocks deriving from primary metabolic pathways and rapidly evolved to allow a better adaptation of plants to environmental cues. Specialized metabolites include terpenes, flavonoids, alkaloids, glucosinolates, tannins, resins, etc. that can be used as phytochemicals, food additives, flavoring agents and pharmaceutical compounds. This review will be focused on Mediterranean crop plants as a source of SMs, with a special attention on the strategies that can be used to modulate their production, including abiotic stresses, interaction with beneficial soil microorganisms and novel genetic approaches.
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Can Natural Polyphenols Help in Reducing Cytokine Storm in COVID-19 Patients?
Giovinazzo, G, Gerardi, C, Uberti-Foppa, C, Lopalco, L
Molecules (Basel, Switzerland). 2020;25(24)
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Plain language summary
During covid-19 infection the body experiences a hyper-immune reaction resulting in an extreme inflammatory response known as cytokine release syndrome (CRS), which correlates with poor prognosis and severe illness. There are no effective treatments for CRS, although there are ongoing trials. The use of natural plant chemicals known as polyphenols have been shown in previous trials to improve inflammation This review of over 90 studies aimed to summarise the use of polyphenols to fight severe covid-19 infection. The paper began by reviewing current drug therapies, which have been shown in studies to be of benefit to inflammation, with tocilizumab being heavily reviewed. The authors then reviewed several plant polyphenols and reviewed how they can modulate inflammation through inhibiting inflammatory molecules and viral activity. It was concluded that human studies are lacking data and so phytochemicals may be promising for the treatment of covid-19. This study could be used by health care professionals to understand the importance of recommending a whole food, plant rich diet with many different coloured foods for individuals who are suffering from covid-19.
Abstract
SARS-CoV-2 first emerged in China during late 2019 and rapidly spread all over the world. Alterations in the inflammatory cytokines pathway represent a strong signature during SARS-COV-2 infection and correlate with poor prognosis and severity of the illness. The hyper-activation of the immune system results in an acute severe systemic inflammatory response named cytokine release syndrome (CRS). No effective prophylactic or post-exposure treatments are available, although some anti-inflammatory compounds are currently in clinical trials. Studies of plant extracts and natural compounds show that polyphenols can play a beneficial role in the prevention and the progress of chronic diseases related to inflammation. The aim of this manuscript is to review the published background on the possible effectiveness of polyphenols to fight SARS-COV-2 infection, contributing to the reduction of inflammation. Here, some of the anti-inflammatory therapies are discussed and although great progress has been made though this year, there is no proven cytokine blocking agents for COVID currently used in clinical practice. In this regard, bioactive phytochemicals such as polyphenols may become promising tools to be used as adjuvants in the treatment of SARS-CoV-2 infection. Such nutrients, with anti-inflammatory and antioxidant properties, associated to classical anti-inflammatory drugs, could help in reducing the inflammation in patients with COVID-19.
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Gut Microbiota Modulation and Anti-Inflammatory Properties of Dietary Polyphenols in IBD: New and Consolidated Perspectives.
Santino, A, Scarano, A, De Santis, S, De Benedictis, M, Giovinazzo, G, Chieppa, M
Current pharmaceutical design. 2017;(16):2344-2351
Abstract
BACKGROUND Polyphenols represent a great variety of compounds occurring in fruits, vegetables and plant-derived products. Dietary polyphenols have been found displaying several biological properties, such as anti-inflammatory, antioxidant and anti-aging activities, cardiovascular and neuro-protection, and reduction of the risk of intestinal diseases. The bio-efficacy of polyphenols is tightly linked to their bioavailability, to structural complexity and composition of food matrix in which they are present. Since most of the polyphenols are naturally stored in food matrices as glycosylated and/or variously decorated forms, they need an intestinal bio-conversion in more absorbable forms. Recent findings are highlighting the polyphenols-gut microbiota interplay in the health benefits linked to these compounds. Furthermore, the prebiotic-like activities of polyphenols on microbiota and their potential use in preventive/therapeutic strategies for gastrointestinal disorders are recently emerging. CONCLUSION In this review, we will focus on the dietary flavonols, anthocyanins and stilbenes, as widely occurring polyphenols in human diet, their metabolism mediated by gut microbiota and their protective effects on inflammatory bowel diseases (IBDs).
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5.
Functional Properties of Grape and Wine Polyphenols.
Giovinazzo, G, Grieco, F
Plant foods for human nutrition (Dordrecht, Netherlands). 2015;(4):454-62
Abstract
Grape berries polyphenols are mainly synthesized in the skin tissues and seeds and they are extracted during the winemaking process. These substances have a potentially positive effect, on human health, thus giving to grape and red wine "functional properties" that can contribute to prevent a number of human illness. Nevertheless, the research community is showing that the real effect is a result of a combination of different factors, notably daily intake, bioavailability, or in vivo antioxidant activity that are yet to be resolved. Viticulture and winemaking practices, determine the concentration of polyphenols in grape and wine. To date, reduced knowledge is existing on the effects of different yeast strains on the final concentration of polyphenols in red wine. We summarize the recent findings concerning the effects of polyphenols on human chronic disease and the future directions for research to increase the amount of these compounds in wine.
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Resveratrol biosynthesis: plant metabolic engineering for nutritional improvement of food.
Giovinazzo, G, Ingrosso, I, Paradiso, A, De Gara, L, Santino, A
Plant foods for human nutrition (Dordrecht, Netherlands). 2012;(3):191-9
Abstract
The plant polyphenol trans-resveratrol (3, 5, 4'-trihydroxystilbene) mainly found in grape, peanut and other few plants, displays a wide range of biological effects. Numerous in vitro studies have described various biological effects of resveratrol. In order to provide more information regarding absorption, metabolism, and bioavailability of resveratrol, various research approaches have been performed, including in vitro, ex vivo, and in vivo models. In recent years, the induction of resveratrol synthesis in plants which normally do not accumulate such polyphenol, has been successfully achieved by molecular engineering. In this context, the ectopic production of resveratrol has been reported to have positive effects both on plant resistance to biotic stress and the enhancement of the nutritional value of several widely consumed fruits and vegetables. The metabolic engineering of plants offers the opportunity to change the content of specific phytonutrients in plant - derived foods. This review focuses on the latest findings regarding on resveratrol bioproduction and its effects on the prevention of the major pathological conditions in man.