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Efficacy of Flavonoids in Chronic Diseases

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A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: closed (31 October 2022) | Viewed by 37919

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Prof. Dr. Nada Orsolic

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Department of Animal Physiology, Faculty of Science, University of Zagreb, 10000 Zagreb, Croatia
Interests: oxidative stress-induced diseases; natural products; chemoprevention and tumor therapy; bee products and health; radioprotection
Special Issues, Collections and Topics in MDPI journals

Dr. Maja Jazvinšćak Jembrek

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1. Division of Molecular Medicine, Rudjer Boskovic Institute, 10000 Zagreb, Croatia
2. School of Medicine, Catholic University of Croatia, 10000 Zagreb, Croatia
Interests: neuroprotection; neurotoxicity; neurodegenerative diseases; oxidative stress; polyphenols; neuropharmacology
Special Issues, Collections and Topics in MDPI journals

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Dear Colleagues,

Chronic diseases are the leading causes of death and disability worldwide. However, the quality of treatment, treatment options, and management of chronic diseases remain low in many aspects. The existing therapies for most chronic conditions sometimes have more debilitating effects than the disease itself. The question is, can we slow down or prevent the onset of chronic diseases using cost-effective therapeutic alternatives, such as readily available, less toxic, antioxidant-rich foods? Numerous scientific data indicate that foods rich in flavonoids can prevent the development of chronic diseases and maintain homeostasis and genetic stability of an organism in both health and disease. Almost 25 centuries ago, Hippocrates, the father of medicine, stated that foods rich in antioxidants could have beneficial effects on human health. He proclaimed: “Let food be thy medicine and medicine be thy food.” Flavonoids, as a sub-class of plant polyphenols, possess a 15-carbon skeleton usually abbreviated as C6-C3-C6. They are composed of two benzene rings (A and B) linked via a heterocyclic pyran ring (C) and are usually classified into flavones, flavonols, flavanones, flavanonols, flavans, flavanols, isoflavones, and chalcones.

Flavonoids, as bioactive compounds with powerful antioxidant and anti-inflammatory properties, could be useful for reducing the risk of oxidative stress and chronic inflammation-mediated pathogenesis of human diseases such as cancer, diabetes, obesity, ischemic heart disease, cardiovascular disorders, cerebrovascular diseases, Alzheimer’s disease and other dementias, osteoarthritis, osteoporosis, chronic obstructive pulmonary disease (COPD), neck pain, chronic kidney disease, cirrhosis of the liver, allergy, autoimmune diseases, atherosclerosis, inflammatory bowel diseases, and neurodegenerative and other disorders which emerge as a result of tissue injury and genomic changes induced by ongoing low-grade inflammation in and around the affected tissue or organ. The antioxidative, anti-inflammatory, antimutagenic, and anticarcinogenic effects of flavonoids are mediated by modulatory actions on multifaceted cell signaling pathways related to inflammatory transcription factors, cytokines, redox status, protein kinases, and enzymes that generally promote inflammation. Flavonoids reduce the symptoms of various chronic diseases due to multiple biological mechanisms of action, including their effects on the activation of survival genes and signaling pathways, epigenetic regulations, gut microbiota and microbial metabolites, regulation of mitochondrial functions and bioenergetics, and modulation of inflammatory response. Dietary supplementation with flavonoids may offer additional protection against oxidative stress and prevention of DNA damage caused by ionizing and UV radiations, carcinogenic agents, and various chemicals and toxins. Flavonoids, through their free radical scavenging properties, inhibition of prooxidative enzymes, metal chelation, inhibition of CYP enzymes, enhanced synthesis of antioxidant enzymes, activation of Nrf2, and inhibition of NF-κB pathways, may participate in the DNA repair mechanism or DNA damage tolerance and in the process of detoxification of toxins and carcinogens. Furthermore, flavonoids play important roles in the prevention of metabolic abnormalities such as dyslipidemia, insulin resistance, hypertension, and glucose intolerance. However, they also show pro-oxidant activity and can induce DNA damage and mutagenic effects. Pro-oxidative and mutagenic properties of flavonoids are dependent on their structure, concentration, and environmental conditions. However, the pro-oxidant activity of flavonoids can contribute to their health-promoting activity by inducing important detoxifying enzymes, suggesting potential beneficial effects of a chemical reaction presumed to be toxic.

Currently, many studies are directed toward better understanding of the pharmacological properties of flavonoids and their potential as health-promoting products capable of exerting physiological benefits, reducing chronic disease risk or otherwise optimizing health. Unfortunately, due to their poor bioavailability, the risk of some chronic diseases may be reduced only at high intake of dietary flavonoids. This problem could be overcome by structural modifications and application of nanotechnology, such as encapsulation. Nanotechnology could be a promising approach for applying flavonoids with greater therapeutic efficacy and with fewer side effects in comparison with commercially available anti-inflammatory drugs.

This Special Issue aims to bring comprehensive insight into the most recent discoveries and benefits of dietary flavonoids and their derivatives in the prevention and treatment of chronic disease. Our goal is to highlight the structural diversity of flavonoids, modulatory effects on intracellular signaling cascades, target molecules and mechanisms of action of flavonoids, current trends in the research and development of flavonoids, function and application of flavonoids as potential drugs in the prevention of chronic disease, as well as future research directions and challenges.

We cordially invite authors to contribute original articles as well as review papers that bring new insights into scientific progress and the exact mechanisms of flavonoid action, and which will hopefully contribute to potential clinical application of flavonoids in the prevention and therapy of numerous chronic diseases.

Prof. Dr. Nada Orsolic
Dr. Maja Jazvinšćak Jembrek
Guest Editors

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Keywords

flavonoids and oxidative stress-related diseases
chronic diseases
metabolic syndrome
natural bioactive compounds
chronic inflammation-mediated pathogenesis of human diseases
biological and pharmacological activity
health benefits of flavonoids
side effects of flavonoids

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Published Papers (9 papers)

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Research

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21 pages, 2276 KiB

Open AccessArticle

Hesperetin from Root Extract of Clerodendrum petasites S. Moore Inhibits SARS-CoV-2 Spike Protein S1 Subunit-Induced NLRP3 Inflammasome in A549 Lung Cells via Modulation of the Akt/MAPK/AP-1 Pathway

by Punnida Arjsri, Kamonwan Srisawad, Sariya Mapoung, Warathit Semmarath, Pilaiporn Thippraphan, Sonthaya Umsumarng, Supachai Yodkeeree and Pornngarm Dejkriengkraikul

Int. J. Mol. Sci. 2022, 23(18), 10346; https://doi.org/10.3390/ijms231810346 - 7 Sep 2022

Cited by 12 | Viewed by 2645

Abstract

Inhibition of inflammatory responses from the spike glycoprotein of SARS-CoV-2 (Spike) by targeting NLRP3 inflammasome has recently been developed as an alternative form of supportive therapy besides the traditional anti-viral approaches. Clerodendrum petasites S. Moore (C. petasites) is a Thai traditional medicinal plant possessing antipyretic and anti-inflammatory activities. In this study, C. petasites ethanolic root extract (CpEE) underwent solvent-partitioned extraction to obtain the ethyl acetate fraction of C. petasites (CpEA). Subsequently, C. petasites extracts were determined for the flavonoid contents and anti-inflammatory properties against spike induction in the A549 lung cells. According to the HPLC results, CpEA significantly contained higher amounts of hesperidin and hesperetin flavonoids than CpEE (p < 0.05). A549 cells were then pre-treated with either C. petasites extracts or its active flavonoids and were primed with 100 ng/mL of spike S1 subunit (Spike S1) and determined for the anti-inflammatory properties. The results indicate that CpEA (compared with CpEE) and hesperetin (compared with hesperidin) exhibited greater anti-inflammatory properties upon Spike S1 induction through a significant reduction in IL-6, IL-1β, and IL-18 cytokine releases in A549 cells culture supernatant (p < 0.05). Additionally, CpEA and hesperetin significantly inhibited the Spike S1-induced inflammatory gene expressions (NLRP3, IL-1β, and IL-18, p < 0.05). Mechanistically, CpEA and hesperetin attenuated inflammasome machinery protein expressions (NLRP3, ASC, and Caspase-1), as well as inactivated the Akt/MAPK/AP-1 pathway. Overall, our findings could provide scientific-based evidence to support the use of C. petasites and hesperetin in the development of supportive therapies for the prevention of COVID-19-related chronic inflammation. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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13 pages, 3028 KiB

Open AccessArticle

Comparison of the Modulating Effect of Anthocyanin-Rich Sour Cherry Extract on Occludin and ZO-1 on Caco-2 and HUVEC Cultures

by Judit Remenyik, Attila Biró, Ágnes Klusóczki, Krisztián Zoltán Juhász, Tímea Szendi-Szatmári, Ádám Kenesei, Erzsébet Szőllősi, Gábor Vasvári, László Stündl, Ferenc Fenyvesi, Judit Váradi and Arnold Markovics

Int. J. Mol. Sci. 2022, 23(16), 9036; https://doi.org/10.3390/ijms23169036 - 12 Aug 2022

Cited by 11 | Viewed by 3201

Abstract

Increased permeability of the epithelial and endothelial cell layers results in the onset of pathogenic mechanisms. In both cell types, cell–cell connections play a regulatory role in altering membrane permeability. The aim of this study was to investigate the modulating effect of anthocyanin-rich extract (AC) on TJ proteins in inflammatory Caco-2 and HUVEC monolayers. Distribution of Occludin and zonula occludens-1 (ZO-1) were investigated by immunohistochemical staining and the protein levels were measured by flow cytometry. The mRNA expression was determined by quantitative real-time PCR. The transepithelial electrical resistance (TEER) values were measured during a permeability assay on HUVEC cell culture. As a result of inflammatory induction by TNF-α, redistribution of proteins was observed in Caco-2 cell culture, which was reduced by AC treatment. In HUVEC cell culture, the decrease in protein and mRNA expression was more dominant during inflammatory induction, which was compensated for by the AC treatment. Overall, AC positively affected the expression of the examined cell-binding structures forming the membrane on both cell types. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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19 pages, 6292 KiB

Open AccessArticle

Systemic Dietary Hesperidin Modulation of Osteoclastogenesis, Bone Homeostasis and Periodontal Disease in Mice

by Vinícius de Paiva Gonçalves, Marta Liliana Musskopf, Angeliz Rivera-Concepcion, Christina Yu, Sing Wai Wong, Stephen A. Tuin, Yizu Jiao, Cristiano Susin, Luís Carlos Spolidorio and Patricia Almeida Miguez

Int. J. Mol. Sci. 2022, 23(13), 7100; https://doi.org/10.3390/ijms23137100 - 26 Jun 2022

Cited by 3 | Viewed by 2236

Abstract

This study aimed to evaluate the effects of hesperidin (HE) on in vitro osteoclastogenesis and dietary supplementation on mouse periodontal disease and femoral bone phenotype. RAW 264.7 cells were stimulated with RANKL in the presence or absence of HE (1, 100 or 500 µM) for 5 days, and evaluated by TRAP, TUNEL and Western Blot (WB) analyses. In vivo, C57BL/6 mice were given HE via oral gavage (125, 250 and 500 mg/kg) for 4 weeks. A sterile silk ligature was placed between the first and second right maxillary molars for 10 days and microcomputed tomography (μCT), histopathological and immunohistochemical evaluation were performed. Femoral bones subjected or not to dietary HE (500 mg/kg) for 6 and 12 weeks were evaluated using μCT. In vitro, HE 500 µM reduced formation of RANKL-stimulated TRAP-positive(+) multinucleated cells (500 µM) as well as c-Fos and NFATc1 protein expression (p < 0.05), markers of osteoclasts. In vivo, dietary HE 500 mg/kg increased the alveolar bone resorption in ligated teeth (p < 0.05) and resulted in a significant increase in TRAP+ cells (p < 0.05). Gingival inflammatory infiltrate was greater in the HE 500 mg/kg group even in the absence of ligature. In femurs, HE 500 mg/kg protected trabecular and cortical bone mass at 6 weeks of treatment. In conclusion, HE impaired in vitro osteoclastogenesis, but on the contrary, oral administration of a high concentration of dietary HE increased osteoclast numbers and promoted inflammation-induced alveolar bone loss. However, HE at 500 mg/kg can promote a bone-sparing effect on skeletal bone under physiological conditions. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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14 pages, 3595 KiB

Open AccessArticle

Screening Anti-Inflammatory Effects of Flavanones Solutions

by Paola Bustos-Salgado, Berenice Andrade-Carrera, Valeri Domínguez-Villegas, Natalia Díaz-Garrido, María J. Rodríguez-Lagunas, Josefa Badía, Laura Baldomà, Mireia Mallandrich, Ana Calpena-Campmany and María Luisa Garduño-Ramírez

Int. J. Mol. Sci. 2021, 22(16), 8878; https://doi.org/10.3390/ijms22168878 - 18 Aug 2021

Cited by 13 | Viewed by 2740

Abstract

There are a large number of remedies in traditional medicine focused on relieving pain and inflammation. Flavanones have been a potential source in the search for leading compounds and biologically active components, and they have been the focus of much research and development in recent years. Eysenhardtia platycarpa is used in traditional medicine for the treatment of kidney diseases, bladder infections, and diabetes mellitus. Many compounds have been isolated from this plant, such as flavones, flavanones, phenolic compounds, triterpenoid acids, chalcones, sugars, and fatty acids, among others. In this paper, natural flavanone 1 (extracted from Eysenhardtia platycarpa) as lead compound and flavanones 1a–1d as its structural analogues were screened for anti-inflammatory activity using Molinspiration^® and PASS Online in a computational study. The hydro alcoholic solutions (FS) of flavanones 1, 1a–1d (FS1, FS1a–FS1d) were also assayed to investigate their in vivo anti-inflammatory cutaneous effect using two experimental models, a rat ear edema induced by arachidonic acid (AA) and a mouse ear edema induced by 12-O-tetradecanoylphorbol acetate (TPA). Histological studies and analysis of pro-inflammatory cytokines TNF-α, IL-1β, and IL-6 were also assessed in AA-inflamed rat ear tissue. The results showed that the flavanone hydro alcoholic solutions (FS) caused edema inhibition in both evaluated models. This study suggests that the evaluated flavanones will be effective when used in the future in skin pathologies with inflammation, with the results showing 1b and 1d to be the best. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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17 pages, 4148 KiB

Open AccessArticle

Anti-Inflammatory and Anti-Allergic Effects of Saponarin and Its Impact on Signaling Pathways of RAW 264.7, RBL-2H3, and HaCaT Cells

by Seon-Young Min, Che-Hwon Park, Hye-Won Yu and Young-Jin Park

Int. J. Mol. Sci. 2021, 22(16), 8431; https://doi.org/10.3390/ijms22168431 - 5 Aug 2021

Cited by 25 | Viewed by 5234

Abstract

Saponarin{5-hydroxy-2-(4-hydroxyphenyl)-6-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]-7-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-4-one}, a flavone found in young green barley leaves, is known to possess antioxidant, antidiabetic, and hepatoprotective effects. In the present study, the anti-inflammatory, anti-allergic, and skin-protective effects of saponarin were investigated to evaluate its usefulness as a functional ingredient in cosmetics. In lipopolysaccharide-induced RAW264.7 (murine macrophage) cells, saponarin (80 μM) significantly inhibited cytokine expression, including tumor necrosis factor (TNF)-α, interleukin (IL)-1β, inducible nitric oxide synthase, and cyclooxygenase (COX)-2. Saponarin (80 μM) also inhibited the phosphorylation of extracellular signal-regulated kinase (ERK) and p38 involved in the mitogen-activated protein kinase signaling pathway in RAW264.7 cells. Saponarin (40 μM) significantly inhibited β-hexosaminidase degranulation as well as the phosphorylation of signaling effectors (Syk, phospholipase Cγ1, ERK, JNK, and p38) and the expression of inflammatory mediators (tumor necrosis factor [TNF]-α, IL-4, IL-5, IL-6, IL-13, COX-2, and FcεRIα/γ) in DNP-IgE- and DNP-BSA-stimulated RBL-2H3 (rat basophilic leukemia) cells. In addition, saponarin (100 μM) significantly inhibited the expression of macrophage-derived chemokine, thymus and activation-regulated chemokine, IL-33, thymic stromal lymphopoietin, and the phosphorylation of signaling molecules (ERK, p38 and signal transducer and activator of transcription 1 [STAT1]) in TNF-α- and interferon (IFN)-γ-stimulated HaCaT (human immortalized keratinocyte) cells. Saponarin (100 μM) also significantly induced the expression of hyaluronan synthase-3, aquaporin 3, and cathelicidin antimicrobial peptide (LL-37) in HaCaT cells, which play an important role as skin barriers. Saponarin remarkably inhibited the essential factors involved in the inflammatory and allergic responses of RAW264.7, RBL-2H3, and HaCaT cells, and induced the expression of factors that function as physical and chemical skin barriers in HaCaT cells. Therefore, saponarin could potentially be used to prevent and relieve immune-related skin diseases, including atopic dermatitis. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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Review

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25 pages, 3433 KiB

Open AccessReview

Participation of the Serotonergic System and Brain-Derived Neurotrophic Factor in the Antidepressant-like Effect of Flavonoids

by León Jesús German-Ponciano, Gilberto Uriel Rosas-Sánchez, Jonathan Cueto-Escobedo, Rafael Fernández-Demeneghi, Gabriel Guillén-Ruiz, César Soria-Fregozo, Emma Virginia Herrera-Huerta and Juan Francisco Rodríguez-Landa

Int. J. Mol. Sci. 2022, 23(18), 10896; https://doi.org/10.3390/ijms231810896 - 17 Sep 2022

Cited by 7 | Viewed by 3692

Abstract

Depressive disorders are among the most disabling diseases experienced around the world, and their incidence has significantly increased over the last few decades due to multiple environmental, social, and biological factors. The search for new pharmacological alternatives to treat depression is a global priority. In preclinical research, molecules obtained from plants, such as flavonoids, have shown promising antidepressant-like properties through several mechanisms of action that have not been fully elucidated, including crossing of the blood brain barrier (BBB). This review will focus on discussing the main findings related to the participation of the serotonergic system and brain-derived neurotrophic factor (BDNF) on the antidepressant-like effect of some flavonoids reported by behavioral, neurochemical, and molecular studies. In this sense, evidence shows that depressive individuals have low levels of serotonin and BDNF, while flavonoids can reverse it. Finally, the elucidation of the mechanism used by flavonoids to modulate serotonin and BDNF will contribute to our understanding of the neurobiological bases underlying the antidepressant-like effects produced by these natural compounds. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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68 pages, 3926 KiB

Open AccessReview

Molecular and Cellular Mechanisms of Propolis and Its Polyphenolic Compounds against Cancer

by Nada Oršolić and Maja Jazvinšćak Jembrek

Int. J. Mol. Sci. 2022, 23(18), 10479; https://doi.org/10.3390/ijms231810479 - 9 Sep 2022

Cited by 33 | Viewed by 5696

Abstract

In recent years, interest in natural products such as alternative sources of pharmaceuticals for numerous chronic diseases, including tumors, has been renewed. Propolis, a natural product collected by honeybees, and polyphenolic/flavonoid propolis-related components modulate all steps of the cancer progression process. Anticancer activity of propolis and its compounds relies on various mechanisms: cell-cycle arrest and attenuation of cancer cells proliferation, reduction in the number of cancer stem cells, induction of apoptosis, modulation of oncogene signaling pathways, inhibition of matrix metalloproteinases, prevention of metastasis, anti-angiogenesis, anti-inflammatory effects accompanied by the modulation of the tumor microenvironment (by modifying macrophage activation and polarization), epigenetic regulation, antiviral and bactericidal activities, modulation of gut microbiota, and attenuation of chemotherapy-induced deleterious side effects. Ingredients from propolis also ”sensitize“ cancer cells to chemotherapeutic agents, likely by blocking the activation of the transcription factor nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB). In this review, we summarize the current knowledge related to the the effects of flavonoids and other polyphenolic compounds from propolis on tumor growth and metastasizing ability, and discuss possible molecular and cellular mechanisms involved in the modulation of inflammatory pathways and cellular processes that affect survival, proliferation, invasion, angiogenesis, and metastasis of the tumor. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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21 pages, 1370 KiB

Open AccessReview

Targeting Mitochondria by Plant Secondary Metabolites: A Promising Strategy in Combating Parkinson’s Disease

by Sajad Fakhri, Sadaf Abdian, Seyede Nazanin Zarneshan, Esra Küpeli Akkol, Mohammad Hosein Farzaei and Eduardo Sobarzo-Sánchez

Int. J. Mol. Sci. 2021, 22(22), 12570; https://doi.org/10.3390/ijms222212570 - 22 Nov 2021

Cited by 7 | Viewed by 3121

Abstract

Parkinson’s disease (PD) is one of the most prevalent and debilitating neurodegenerative conditions, and is currently on the rise. Several dysregulated pathways are behind the pathogenesis of PD; however, the critical targets remain unclear. Accordingly, there is an urgent need to reveal the key dysregulated pathways in PD. Prevailing reports have highlighted the importance of mitochondrial and cross-talked mediators in neurological disorders, genetic changes, and related complications of PD. Multiple pathophysiological mechanisms of PD, as well as the low efficacy and side effects of conventional neuroprotective therapies, drive the need for finding novel alternative agents. Recently, much attention has been paid to using plant secondary metabolites (e.g., flavonoids/phenolic compounds, alkaloids, and terpenoids) in the modulation of PD-associated manifestations by targeting mitochondria. In this line, plant secondary metabolites have shown promising potential for the simultaneous modulation of mitochondrial apoptosis and reactive oxygen species. This review aimed to address mitochondria and multiple dysregulated pathways in PD by plant-derived secondary metabolites. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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33 pages, 1137 KiB

Open AccessReview

Anticancer Activity of Natural and Synthetic Chalcones

by Teodora Constantinescu and Claudiu N. Lungu

Int. J. Mol. Sci. 2021, 22(21), 11306; https://doi.org/10.3390/ijms222111306 - 20 Oct 2021

Cited by 107 | Viewed by 7239

Abstract

Cancer is a condition caused by many mechanisms (genetic, immune, oxidation, and inflammatory). Anticancer therapy aims to destroy or stop the growth of cancer cells. Resistance to treatment is theleading cause of the inefficiency of current standard therapies. Targeted therapies are the most effective due to the low number of side effects and low resistance. Among the small molecule natural compounds, flavonoids are of particular interest for theidentification of new anticancer agents. Chalcones are precursors to all flavonoids and have many biological activities. The anticancer activity of chalcones is due to the ability of these compounds to act on many targets. Natural chalcones, such as licochalcones, xanthohumol (XN), panduretin (PA), and loncocarpine, have been extensively studied and modulated. Modification of the basic structure of chalcones in order to obtain compounds with superior cytotoxic properties has been performed by modulating the aromatic residues, replacing aromatic residues with heterocycles, and obtaining hybrid molecules. A huge number of chalcone derivatives with residues such as diaryl ether, sulfonamide, and amine have been obtained, their presence being favorable for anticancer activity. Modification of the amino group in the structure of aminochalconesis always favorable for antitumor activity. This is why hybrid molecules of chalcones with different nitrogen hetercycles in the molecule have been obtained. From these, azoles (imidazole, oxazoles, tetrazoles, thiazoles, 1,2,3-triazoles, and 1,2,4-triazoles) are of particular importance for the identification of new anticancer agents. Full article

(This article belongs to the Special Issue Efficacy of Flavonoids in Chronic Diseases)

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