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Special Issue "Flavonoids and Their Disease Prevention and Treatment Potential 2021"

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

Deadline for manuscript submissions: 31 July 2021.

Special Issue Editor

Prof. Dr. H.P. Vasantha Rupasinghe
E-Mail Website
Guest Editor
Faculty of Agriculture, Dalhousie University, Halifax, Canada
Interests: dietary antioxidants; phytochemicals; polyphenols; flavonoids and their derivatives; chemoprevention; molecular mechanisms of action; DNA damage signaling and DNA repair
Special Issues and Collections in MDPI journals

Special Issue Information

Dear Colleagues,

In recent years, the interest in flavonoids as dietary bioactives to prevent human diseases, as well as their candidacy as pharmaceutical leads, has been exponentially expanded. Flavonoids are a sub-class of plant polyphenols that have been shown to possess numerous health-promoting physiological benefits  in a wide range of investigations, from cell-based assays to epidemiological and human intervention studies.

Flavonoids are ubiquitously present in plant-based foods, traditional herbal remedies, and natural health products. Scientific evidence has strongly shown that regular intake of dietary flavonoids in efficacious amounts reduces the risk of oxidative-stress- and chronic inflammation-mediated pathogenesis of human diseases, such as cardiovascular disease, certain cancers, and neurological disorders. The physiological benefits of dietary flavonoids have been demonstrated to be due to multiple mechanisms of action, including regulating redox homeostasis, epigenetic regulations, the activation of survival genes and signaling pathways, the regulation of mitochondrial function and bioenergetics, and the modulation of inflammation response. The role of flavonoids on gut microbiota and impact of microbial metabolites of flavonoids on optimal health have begun to unravel. The complex biological activities of flavonoid molecules are due to their structural diversity. However, some flavonoids are not absorbed well, and their bioavailability could be enhanced through structural modifications and the application of nanotechnologies such as encapsulation.

Therefore, this Special Issue is dedicated to original research articles, which cover the latest findings on the role of dietary flavonoids and their derivatives in disease prevention and treatment. Review articles could discuss the advancement of our knowledge within the mechanisms of action of specific flavonoids, the interaction of flavonoids with microbiota, and the enhancement of flavonoid bioavailability and bio-efficacy, etc.

Prof. Dr. H.P. Vasantha Rupasinghe
Guest Editor

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 papers will be 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. Molecules is an international peer-reviewed open access semimonthly 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 2000 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

  • Flavonoids and their derivatives
  • Chronic and metabolic diseases
  • Prevention and treatment
  • Mechanisms of action
  • Functional foods and nutraceuticals
  • Drug discovery

Published Papers (6 papers)

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Research

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Article
Gossypitrin, A Naturally Occurring Flavonoid, Attenuates Iron-Induced Neuronal and Mitochondrial Damage
Molecules 2021, 26(11), 3364; https://doi.org/10.3390/molecules26113364 - 02 Jun 2021
Viewed by 498
Abstract
The disruption of iron homeostasis is an important factor in the loss of mitochondrial function in neural cells, leading to neurodegeneration. Here, we assessed the protective action of gossypitrin (Gos), a naturally occurring flavonoid, on iron-induced neuronal cell damage using mouse hippocampal HT-22 [...] Read more.
The disruption of iron homeostasis is an important factor in the loss of mitochondrial function in neural cells, leading to neurodegeneration. Here, we assessed the protective action of gossypitrin (Gos), a naturally occurring flavonoid, on iron-induced neuronal cell damage using mouse hippocampal HT-22 cells and mitochondria isolated from rat brains. Gos was able to rescue HT22 cells from the damage induced by 100 µM Fe(II)-citrate (EC50 8.6 µM). This protection was linked to the prevention of both iron-induced mitochondrial membrane potential dissipation and ATP depletion. In isolated mitochondria, Gos (50 µM) elicited an almost complete protection against iron-induced mitochondrial swelling, the loss of mitochondrial transmembrane potential and ATP depletion. Gos also prevented Fe(II)-citrate-induced mitochondrial lipid peroxidation with an IC50 value (12.45 µM) that was about nine time lower than that for the tert-butylhydroperoxide-induced oxidation. Furthermore, the flavonoid was effective in inhibiting the degradation of both 15 and 1.5 mM 2-deoxyribose. It also decreased Fe(II) concentration with time, while increasing O2 consumption rate, and impairing the reduction of Fe(III) by ascorbate. Gos–Fe(II) complexes were detected by UV-VIS and IR spectroscopies, with an apparent Gos-iron stoichiometry of 2:1. Results suggest that Gos does not generally act as a classical antioxidant, but it directly affects iron, by maintaining it in its ferric form after stimulating Fe(II) oxidation. Metal ions would therefore be unable to participate in a Fenton-type reaction and the lipid peroxidation propagation phase. Hence, Gos could be used to treat neuronal diseases associated with iron-induced oxidative stress and mitochondrial damage. Full article
(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)
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Article
Anti-Melanogenic Properties of Velutin and Its Analogs
Molecules 2021, 26(10), 3033; https://doi.org/10.3390/molecules26103033 - 19 May 2021
Viewed by 338
Abstract
Velutin, one of the flavones contained in natural plants, has various beneficial activities, such as skin whitening, as well as anti-inflammatory, anti-allergic, antioxidant, and antimicrobial activities. However, the relationship between the structure of velutin and its anti-melanogenesis activity is not yet investigated. In [...] Read more.
Velutin, one of the flavones contained in natural plants, has various beneficial activities, such as skin whitening, as well as anti-inflammatory, anti-allergic, antioxidant, and antimicrobial activities. However, the relationship between the structure of velutin and its anti-melanogenesis activity is not yet investigated. In this study, we obtained 12 velutin derivatives substituted at C5, C7, C3′, and C4′ of the flavone backbone with hydrogen, hydroxyl, and methoxy functionalities by chemical synthesis, to perform SAR analysis of velutin structural analogues. The SAR study revealed that the substitution of functional groups at C5, C7, C3′, and C4′ of the flavone backbone affects biological activities related to melanin synthesis. The coexistence of hydroxyl and methoxy at the C5 and C7 position is essential for inhibiting tyrosinase activity. However, 1,2-diol compounds substituted at C3′ and C4′ of flavone backbone induce apoptosis of melanoma cells. Further, substitution at C3′ and C4′ with methoxy or hydrogen is essential for inhibiting melanogenesis. Thus, this study would be helpful for the development of natural-derived functional materials to regulate melanin synthesis. Full article
(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)
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Article
Iridin Induces G2/M Phase Cell Cycle Arrest and Extrinsic Apoptotic Cell Death through PI3K/AKT Signaling Pathway in AGS Gastric Cancer Cells
Molecules 2021, 26(9), 2802; https://doi.org/10.3390/molecules26092802 - 10 May 2021
Viewed by 304
Abstract
Iridin is a natural flavonoid found in Belamcanda chinensis documented for its broad spectrum of biological activities like antioxidant, antitumor, and antiproliferative effects. In the present study, we have investigated the antitumor potential of iridin in AGS gastric cancer cells. Iridin treatment decreases [...] Read more.
Iridin is a natural flavonoid found in Belamcanda chinensis documented for its broad spectrum of biological activities like antioxidant, antitumor, and antiproliferative effects. In the present study, we have investigated the antitumor potential of iridin in AGS gastric cancer cells. Iridin treatment decreases AGS cell growth and promotes G2/M phase cell cycle arrest by attenuating the expression of Cdc25C, CDK1, and Cyclin B1 proteins. Iridin-treatment also triggered apoptotic cell death in AGS cells, which was verified by cleaved Caspase-3 (Cl- Caspase-3) and poly ADP-ribose polymerase (PARP) protein expression. Further apoptotic cell death was confirmed by increased apoptotic cell death fraction shown in allophycocyanin (APC)/Annexin V and propidium iodide staining. Iridin also increased the expression of extrinsic apoptotic pathway proteins like Fas, FasL, and cleaved Caspase-8 in AGS cells. On the contrary, iridin-treated AGS cells did not show variations in proteins related to an intrinsic apoptotic pathway such as Bax and Bcl-xL. Besides, Iridin showed inhibition of PI3K/AKT signaling pathways by downregulation of (p-PI3K, p-AKT) proteins in AGS cells. In conclusion, these data suggest that iridin has anticancer potential by inhibiting PI3K/AKT pathway. It could be a basis for further drug design in gastric cancer treatment. Full article
(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)
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Article
Modulation of Oxidative Stress and Hemostasis by Flavonoids from Lentil Aerial Parts
Molecules 2021, 26(2), 497; https://doi.org/10.3390/molecules26020497 - 18 Jan 2021
Cited by 2 | Viewed by 587
Abstract
While specific metabolites of lentil (Lens culinaris L.) seeds and their biological activity have been well described, other organs of this plant have attracted little scientific attention. In recent years, green parts of lentils have been shown to contain diverse acylated flavonoids. [...] Read more.
While specific metabolites of lentil (Lens culinaris L.) seeds and their biological activity have been well described, other organs of this plant have attracted little scientific attention. In recent years, green parts of lentils have been shown to contain diverse acylated flavonoids. This work presents the results of the research on the effect of the crude extract, the phenolic fraction, and seven flavonoids obtained from aerial parts of lentils on oxidative damage induced by H2O2/Fe to lipid and protein constituents of human plasma. Another goal was to determine their effect on hemostasis parameters of human plasma in vitro. Most of the purified lentil flavonoids had antioxidant and anticoagulant properties. The crude extract and the phenolic fraction of lentil aerial parts showed antioxidant activity, only at the highest tested concentration (50 μg/mL). Our results indicate that aerial parts of lentils may be recommended as a source of bioactive substances. Full article
(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)
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Review

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Review
Potential Benefits of Flavonoids on the Progression of Atherosclerosis by Their Effect on Vascular Smooth Muscle Excitability
Molecules 2021, 26(12), 3557; https://doi.org/10.3390/molecules26123557 - 10 Jun 2021
Viewed by 328
Abstract
Flavonoids are a group of secondary metabolites derived from plant-based foods, and they offer many health benefits in different stages of several diseases. This review will focus on their effects on ion channels expressed in vascular smooth muscle during atherosclerosis. Since ion channels [...] Read more.
Flavonoids are a group of secondary metabolites derived from plant-based foods, and they offer many health benefits in different stages of several diseases. This review will focus on their effects on ion channels expressed in vascular smooth muscle during atherosclerosis. Since ion channels can be regulated by redox potential, it is expected that during the onset of oxidative stress-related diseases, ion channels present changes in their conductive activity, impacting the progression of the disease. A typical oxidative stress-related condition is atherosclerosis, which involves the dysfunction of vascular smooth muscle. We aim to present the state of the art on how redox potential affects vascular smooth muscle ion channel function and summarize if the benefits observed in this disease by using flavonoids involve restoring the ion channel activity. Full article
(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)
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Review
Mechanistic Aspects and Therapeutic Potential of Quercetin against COVID-19-Associated Acute Kidney Injury
Molecules 2020, 25(23), 5772; https://doi.org/10.3390/molecules25235772 - 07 Dec 2020
Cited by 3 | Viewed by 1294
Abstract
The inflammatory mediator and oxidant agent storm caused by the SARS-CoV-2 infection has been strongly associated with the failure of vital organs observed in critically ill patients with coronavirus disease 2019 (COVID-19) and the death of thousands of infected people around the world. [...] Read more.
The inflammatory mediator and oxidant agent storm caused by the SARS-CoV-2 infection has been strongly associated with the failure of vital organs observed in critically ill patients with coronavirus disease 2019 (COVID-19) and the death of thousands of infected people around the world. Acute kidney injury (AKI) is a common renal disorder characterized by a sudden and sustained decrease in renal function with a critical influence on poor prognosis and lethal clinical outcomes of various etiologies, including some viral infection diseases. It is known that oxidative stress and inflammation play key roles in the pathogenesis and development of AKI. Quercetin is a natural substance that has multiple pharmacological properties, such as anti-inflammatory action, and is used as a dietary supplement. There is evidence of the anti-coronavirus activities of this compound, including against the target SARS-CoV-2 3CLpro. The ability to inhibit coronavirus and its inflammatory processes is strongly desired in a new drug for the treatment of COVID-19. Therefore, in this review, the dual effect of quercetin is discussed from a mechanistic perspective in relation to AKI kidney injury and its nephroprotective potential to SARS-CoV-2 patients. Full article
(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)
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