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Flavonoids and Their Disease Prevention and Treatment Potential 2021

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

Deadline for manuscript submissions: closed (31 December 2021) | Viewed by 49435

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Special Issue Editor

Prof. Dr. H. P. Vasantha Rupasinghe

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Guest Editor

Department of Plant, Food, and Environmental Sciences, Faculty of Agriculture, Dalhousie University, Truro, NS B2N 5E3, Canada
Interests: dietary antioxidants; phytochemicals; polyphenols; flavonoids and their derivatives; chemoprevention; molecular mechanisms of action; DNA damage signaling and DNA repair; postbiotics of polyphenols
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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

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Keywords

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

Published Papers (14 papers)

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Research

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24 pages, 2860 KiB

Open AccessArticle

Optimization of the Extraction of Proanthocyanidins from Grape Seeds Using Ultrasonication-Assisted Aqueous Ethanol and Evaluation of Anti-Steatosis Activity In Vitro

by Wasitha P. D. W. Thilakarathna and H. P. Vasantha Rupasinghe

Molecules 2022, 27(4), 1363; https://doi.org/10.3390/molecules27041363 - 17 Feb 2022

Cited by 10 | Viewed by 4570

Abstract

Conventional extraction methods of proanthocyanidins (PAC) are based on toxic organic solvents, which can raise concerns about the use of extracts in supplemented food and nutraceuticals. Thus, a PAC extraction method was developed for grape seeds (GS) and grape seed powder using food-grade ethanol by optimizing the extraction conditions to generate the maximum yield of PAC. Extraction parameters, % ethanol, solvent: solid (s:s) ratio, sonication time, and temperature were optimized by the central composite design of the response surface method. The yields of PAC under different extraction conditions were quantified by the methylcellulose precipitable tannin assay. The final optimum conditions were 47% ethanol, 10:1 s:s ratio (v:w), 53 min sonication time, and 60 °C extraction temperature. High-performance liquid chromatography analysis revealed the presence of catechin, procyanidin B2, oligomeric and polymeric PAC in the grape seed-proanthocyanidin extracts (GS-PAC). GS-PAC significantly reduced reactive oxygen species and lipid accumulation in the palmitic-acid-induced mouse hepatocytes (AML12) model of steatosis. About 50% of the PAC of the GS was found to be retained in the by-product of wine fermentation. Therefore, the developed ethanol-based extraction method is suitable to produce PAC-rich functional ingredients from grape by-products to be used in supplemented food and nutraceuticals. Full article

(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)

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13 pages, 2854 KiB

Open AccessArticle

Flavonoids: Antiplatelet Effect as Inhibitors of COX-1

by Cristina Zaragozá, Miguel Ángel Álvarez-Mon, Francisco Zaragozá and Lucinda Villaescusa

Molecules 2022, 27(3), 1146; https://doi.org/10.3390/molecules27031146 - 08 Feb 2022

Cited by 12 | Viewed by 2521

Abstract

Flavonoids are compounds with a benzopyranic structure that exhibits multiple pharmacological activities. They are known for their venotonic activity, but their mechanism of action remains unclear. It is thought that, as this mechanism is mediated by prostaglandins, these compounds may interfere with the arachidonic acid (AA) cascade. These assays are designed to measure the antiplatelet aggregation capacity of quercetin, rutin, diosmetin, diosmin, and hidrosmin, as well as to evaluate a potential structure−activity ratio. In this paper, several studies on platelet aggregation at different concentrations (from 0.33 mM to 1.5 mM) of different flavone compounds are conducted, measuring platelet aggregation by impedance aggregometry, and the cyclooxygenase (COX) activity by metabolites generated, including the activity of the pure recombinant enzyme in the presence of these polyphenols. The results obtained showed that quercetin and diosmetin aglycones have a greater antiplatelet effect and inhibit the COX enzyme activity to a greater extent than their heterosides; however, the fact that greater inhibition of the pure recombinant enzyme was achieved by heterosides suggests that these compounds may have difficulty in crossing biological membranes. In any case, in view of the results obtained, it can be concluded that flavonoids could be useful as coadjuvants in the treatment of cardiovascular pathologies. Full article

(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)

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12 pages, 2720 KiB

Open AccessArticle

Proteomic Analysis of Protective Effects of Epimedium Flavonoids against Ethanol-Induced Toxicity in Retinoic Acid-Treated SH-SY5Y Cells

by Xiaohua Yang, Huafeng Zhang, Lu Li, Xuexue Zhou, Yichao Liu and Jianghua Lai

Molecules 2022, 27(3), 1026; https://doi.org/10.3390/molecules27031026 - 02 Feb 2022

Cited by 3 | Viewed by 1726

Abstract

Alcohol (ethanol) is one of the most common addictive psychoactive substances in the world, and alcoholism may result in harmful effects on human health, especially on the nervous system. Flavonoids are regarded as the main active constituent in Epimedium, which has been used to cure some nervous system diseases such as amnesia for over 1000 years. Here, the protective effects of Epimedium flavonoids against ethanol-induced toxicity in retinoic acid (RA)-treated SH-SY5Y cells were investigated. Their mechanism was explored by a label-free proteomic approach combined with bioinformatic analysis for the first time. The results showed that ethanol treatment decreased cell viability by 18%, whereas the viability increased significantly after intervention with Epimedium flavonoids (p < 0.01). According to proteomic and bioinformatic analyses, hundreds of differentially expressed proteins (DEPs) were identified and classified as biological process (GO_BP), cellular component (GO_CC) and molecular function (GO_MF). Among them, GO_MF of DEPs, especially molecular function relevant to G proteins, greatly changed in SH-SY5Y cells pretreated by Epimedium flavonoids. In the alcoholism pathway, the expression of the Gi protein was up-regulated under the influence of ethanol, whereas Epimedium flavonoids could reverse the expression profile, both of which were validated by Western blot assay. In conclusion, Gi protein seemed to be an important factor in the alcoholism pathway to suppress the ethanol-induced toxicity of SH-SY5Y cells. These findings suggest a protective potential of Epimedium flavonoids against ethanol-induced toxicity to neurons via the regulation of Gi protein function. Full article

(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)

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16 pages, 3201 KiB

Open AccessArticle

Structural Design, Synthesis and Antioxidant, Antileishmania, Anti-Inflammatory and Anticancer Activities of a Novel Quercetin Acetylated Derivative

by Saul Vislei Simões da Silva, Orlando Maia Barboza, Jéssica Teles Souza, Érica Novaes Soares, Cleonice Creusa dos Santos, Luciano Vasconcellos Pacheco, Ivanilson Pimenta Santos, Tatiana Barbosa dos Santos Magalhães, Milena Botelho Pereira Soares, Elisalva Teixeira Guimarães, Cássio Santana Meira, Silvia Lima Costa, Victor Diógenes Amaral da Silva, Lourenço Luís Botelho de Santana and Aníbal de Freitas Santos Júnior

Molecules 2021, 26(22), 6923; https://doi.org/10.3390/molecules26226923 - 17 Nov 2021

Cited by 10 | Viewed by 2476

Abstract

Quercetin (Q) is a bioflavonoid with biological potential; however, poor solubility in water, extensive enzymatic metabolism and a reduced bioavailability limit its biopharmacological use. The aim of this study was to perform structural modification in Q by acetylation, thus, obtaining the quercetin pentaacetate (Q5) analogue, in order to investigate the biological potentials (antioxidant, antileishmania, anti-inflammatory and cytotoxicity activities) in cell cultures. Q5 was characterized by FTIR, ¹H and ¹³C NMR spectra. The antioxidant potential was evaluated against the radical ABTS^•+. The anti-inflammatory potential was evaluated by measuring the pro-inflammatory cytokine tumor necrosis factor (TNF) and the production of nitric oxide (NO) in peritoneal macrophages from BALB/c mice. Cytotoxicity tests were performed using the AlamarBlue method in cancer cells HepG2 (human hepatocarcinoma), HL-60 (promyelocytic leukemia) and MCR-5 (healthy human lung fibroblasts) as well as the MTT method for C6 cell cultures (rat glioma). Q and Q5 showed antioxidant activity of 29% and 18%, respectively, which is justified by the replacement of hydroxyls by acetyl groups. Q and Q5 showed concentration-dependent reductions in NO and TNF production (p < 0.05); Q and Q5 showed higher activity at concentrations > 40µM when compared to dexamethasone (20 µM). For the HL-60 lineage, Q5 demonstrated selectivity, inducing death in cancer cells, when compared to the healthy cell line MRC-5 (IC₅₀ > 80 µM). Finally, the cytotoxic superiority of Q5 was verified (IC₅₀ = 11 µM), which, at 50 µM for 24 h, induced changes in the morphology of C6 glioma cells characterized by a round body shape (not yet reported in the literature). The analogue Q5 had potential biological effects and may be promising for further investigations against other cell cultures, particularly neural ones. Full article

(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)

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10 pages, 1068 KiB

Open AccessCommunication

Active Flavonoids from Colubrina greggii var. greggii S. Watson against Clinical Isolates of Candida spp.

by Elda M. Melchor-Martínez, Juan F. Tamez-Fernández, Gloria María González-González, David A. Silva-Mares, Noemí Waksman-Minsky, Luis Alejandro Pérez-López and Verónica M. Rivas-Galindo

Molecules 2021, 26(19), 5760; https://doi.org/10.3390/molecules26195760 - 23 Sep 2021

Cited by 4 | Viewed by 2157

Abstract

Candida albicans is the most commonly implicated agent in invasive human fungal infections. The disease could be presented as minimal symptomatic candidemia or can be fulminant sepsis. Candidemia is associated with a high rate of mortality and high healthcare and hospitalization costs. The surveillance programs have reported the distribution of other Candida species reflecting the trends and antifungal susceptibilities. Previous studies have demonstrated that C. glabrata more frequently presents fluconazole-resistant strains. Extracts from Mexican plants have been reported with activity against pulmonary mycosis, among them Colubrina greggii. In the present study, extracts from the aerial parts (leaves, flowers, and fruits) of this plant were evaluated against clinical isolates of several species of Candida (C. albicans, C. glabrata, C. parapsilosis, C. krusei, and C. tropicalis) by the broth microdilution assay. Through bioassay-guided fractionation, three antifungal glycosylated flavonoids were isolated and characterized. The isolated compounds showed antifungal activity only against C. glabrata resistant to fluconazole, and were non-toxic toward brine shrimp lethality bioassay and in vitro Vero cell line assay. The ethyl acetate and butanol extracts, as well as the fractions containing the mixture of flavonoids, were more active against Candida spp. Full article

(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)

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12 pages, 2206 KiB

Open AccessArticle

Hairy Roots of Scutellaria spp. (Lamiaceae) as Promising Producers of Antiviral Flavones

by Anna Yurievna Stepanova, Aleksandra Ivanovna Solov’eva, Maria Victorovna Malunova, Svetlana Andreevna Salamaikina, Yury Mikhailovich Panov and Andrey Aleksandrovich Lelishentsev

Molecules 2021, 26(13), 3927; https://doi.org/10.3390/molecules26133927 - 27 Jun 2021

Cited by 18 | Viewed by 2707

Abstract

We measured and studied the growth parameters and the qualitative and quantitative composition of the flavones of hairy roots of the Scutellaria genus: S. lateriflora, S. przewalskii and S. pycnoclada. Hairy roots were obtained using wild-type Agrobacterium rhizogenes A4 by co-cultivation of explants (cotyledons) in a suspension of Agrobacterium. The presence of the rol-genes was confirmed by PCR analysis. The hairy roots of the most studied plant from the Scutellaria genus, S. baicalensis, were obtained earlier and used as a reference sample. HPLC-MS showed the predominance of four main flavones (baicalin, baicalein, wogonin and wogonoside) in the methanol extracts of the studied hairy roots. In addition to the four main flavones, the other substances which are typical to the aerial part of plants were found in all the extracts: apigenin, apigetrin, scutellarin and chrysin-7-O-β-d-glucuronide. According to the total content of flavones, the hairy roots of the studied skullcaps form the following series: S. przewalskii (33 mg/g dry weight) > S. baicalensis (17.04 mg/g dry weight) > S. pycnoclada (12.9 mg/g dry weight) > S. lateriflora (4.57 mg/g dry weight). Therefore, the most promising producer of anti-coronavirus flavones is S. przewalskii. Full article

(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)

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17 pages, 1896 KiB

Open AccessArticle

Gossypitrin, A Naturally Occurring Flavonoid, Attenuates Iron-Induced Neuronal and Mitochondrial Damage

by María Ángeles Bécquer-Viart, Adonis Armentero-López, Daniel Alvarez-Almiñaque, Roberto Fernández-Acosta, Yasser Matos-Peralta, Richard F. D’Vries, Javier Marín-Prida and Gilberto L. Pardo-Andreu

Molecules 2021, 26(11), 3364; https://doi.org/10.3390/molecules26113364 - 02 Jun 2021

Cited by 4 | Viewed by 2704

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 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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13 pages, 3468 KiB

Open AccessArticle

Anti-Melanogenic Properties of Velutin and Its Analogs

by Se-Hui Jung, Hee-Young Heo, Jung-Won Choe, Jaehyun Kim and Kooyeon Lee

Molecules 2021, 26(10), 3033; https://doi.org/10.3390/molecules26103033 - 19 May 2021

Cited by 5 | Viewed by 2701

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 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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12 pages, 3605 KiB

Open AccessArticle

Iridin Induces G2/M Phase Cell Cycle Arrest and Extrinsic Apoptotic Cell Death through PI3K/AKT Signaling Pathway in AGS Gastric Cancer Cells

by Pritam-Bhagwan Bhosale, Preethi Vetrivel, Sang-Eun Ha, Hun-Hwan Kim, Jeong-Doo Heo, Chung-Kil Won, Seong-Min Kim and Gon-Sup Kim

Molecules 2021, 26(9), 2802; https://doi.org/10.3390/molecules26092802 - 10 May 2021

Cited by 16 | Viewed by 2446

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 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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15 pages, 2483 KiB

Open AccessArticle

Modulation of Oxidative Stress and Hemostasis by Flavonoids from Lentil Aerial Parts

by Jerzy Żuchowski, Agata Rolnik, Weronika Adach, Anna Stochmal and Beata Olas

Molecules 2021, 26(2), 497; https://doi.org/10.3390/molecules26020497 - 18 Jan 2021

Cited by 7 | Viewed by 2221

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. 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

Jump to: Research

12 pages, 1283 KiB

Open AccessReview

Insight into Potential Anticancer Activity of Algal Flavonoids: Current Status and Challenges

by Umme Tamanna Ferdous and Zetty Norhana Balia Yusof

Molecules 2021, 26(22), 6844; https://doi.org/10.3390/molecules26226844 - 13 Nov 2021

Cited by 30 | Viewed by 3789

Abstract

Flavonoids are some of the most precious phytochemicals, believed to be found largely in terrestrial plants. With the advancement of phytochemical research and marine bioprospecting, flavonoids have also been reported by the research of microalgae and macroalgae. High growth rate with minimal nutritional and growth requirement, saving arable land and rich metabolic profile make microalgae an excellent repertoire of novel anticancer compounds, such as flavonoids. In addition, marine algae, especially seaweeds contain different types of flavonoids which are assumed to have unique chemical structures and bioactivities than their terrestrial counterparts. Flavonoids are not only good antioxidants but also have the abilities to kill cancer cells by inducing apoptosis and autophagy. However, the study of the anticancer properties of flavonoids is largely limited to terrestrial plants. This review offers an insight into the distribution of different classes of flavonoids in eukaryotic microalgae, cyanobacteria and seaweeds with their possible anticancer activities. In addition, extraction and purification methods of these flavonoids have been highlighted. Finally, prospects and challenges to use algal flavonoids as anticancer agents have been discussed. Full article

(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)

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24 pages, 2010 KiB

Open AccessReview

Dietary Flavonoids: Cardioprotective Potential with Antioxidant Effects and Their Pharmacokinetic, Toxicological and Therapeutic Concerns

by Johra Khan, Prashanta Kumar Deb, Somi Priya, Karla Damián Medina, Rajlakshmi Devi, Sanjay G. Walode and Mithun Rudrapal

Molecules 2021, 26(13), 4021; https://doi.org/10.3390/molecules26134021 - 30 Jun 2021

Cited by 124 | Viewed by 7464

Abstract

Flavonoids comprise a large group of structurally diverse polyphenolic compounds of plant origin and are abundantly found in human diet such as fruits, vegetables, grains, tea, dairy products, red wine, etc. Major classes of flavonoids include flavonols, flavones, flavanones, flavanols, anthocyanidins, isoflavones, and chalcones. Owing to their potential health benefits and medicinal significance, flavonoids are now considered as an indispensable component in a variety of medicinal, pharmaceutical, nutraceutical, and cosmetic preparations. Moreover, flavonoids play a significant role in preventing cardiovascular diseases (CVDs), which could be mainly due to their antioxidant, antiatherogenic, and antithrombotic effects. Epidemiological and in vitro/in vivo evidence of antioxidant effects supports the cardioprotective function of dietary flavonoids. Further, the inhibition of LDL oxidation and platelet aggregation following regular consumption of food containing flavonoids and moderate consumption of red wine might protect against atherosclerosis and thrombosis. One study suggests that daily intake of 100 mg of flavonoids through the diet may reduce the risk of developing morbidity and mortality due to coronary heart disease (CHD) by approximately 10%. This review summarizes dietary flavonoids with their sources and potential health implications in CVDs including various redox-active cardioprotective (molecular) mechanisms with antioxidant effects. Pharmacokinetic (oral bioavailability, drug metabolism), toxicological, and therapeutic aspects of dietary flavonoids are also addressed herein with future directions for the discovery and development of useful drug candidates/therapeutic molecules. Full article

(This article belongs to the Special Issue Flavonoids and Their Disease Prevention and Treatment Potential 2021)

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22 pages, 4001 KiB

Open AccessReview

Potential Benefits of Flavonoids on the Progression of Atherosclerosis by Their Effect on Vascular Smooth Muscle Excitability

by Rosa Edith Grijalva-Guiza, Aura Matilde Jiménez-Garduño and Luis Ricardo Hernández

Molecules 2021, 26(12), 3557; https://doi.org/10.3390/molecules26123557 - 10 Jun 2021

Cited by 7 | Viewed by 2966

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 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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19 pages, 881 KiB

Open AccessReview

Mechanistic Aspects and Therapeutic Potential of Quercetin against COVID-19-Associated Acute Kidney Injury

by Lúcio Ricardo Leite Diniz, Marilia Trindade de Santana Souza, Allana Brunna Sucupira Duarte and Damião Pergentino de Sousa

Molecules 2020, 25(23), 5772; https://doi.org/10.3390/molecules25235772 - 07 Dec 2020

Cited by 29 | Viewed by 6546

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. 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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