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Flavonoids and Their Impact on Human Health

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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 (25 April 2023) | Viewed by 34856

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Prof. Dr. Davide Barreca

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Department of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, 98168 Messina, Italy
Interests: plant biochemistry; isolation and identification of polyphenols; evaluation of biological potentials of polyphenols on isolate cells in culture; identification of molecular mechanisms of antioxidants action
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Dear Colleagues,

There is an enormous growth of worldwide interest in nutraceutical compounds in both developed and developing countries over the last two decades, increasing the interest of pharmaceutical companies, which has in turn motivated preclinical pharmacological studies as well as controlled and randomized clinical trials to prove the safety and efficacy of these products. Flavonoids are the most studied class of nutraceutical compounds for their impact on human health due to the unquestionable promising biological and pharmacological activities, as shown by epigenetic research, too. These compounds are able to modulate the intracellular signal cascade, and in addition to their well-known antioxidant activity, they can be utilized to promote cell survival or death, focusing their action on a well-defined biological target. USDA, NIH, and several other government and health agencies encourage people to consume a variegated and healthy balanced diet, rich in polyphenols, taking into account the potential health-promoting effects and supported by the evidence supplied by numerous epidemiological studies. Taken together, these characteristics make the daily assumptions of flavonoids a natural defense weapon to promote organisms’ wellness. Taking into account the strong interest in polyphenols as an emerging challenge for the development of health-promoting compounds and potential biotechnological applications, this Special Issue will cover a wide variety of areas, aiming to contribute to the overall knowledge of the molecular mechanism of flavonoids action by multiple points of view on both in producers and in consumers.

Please do note that papers that only focus on extraction do not qualify for this IJMS Special Issue. The focus is not only on the chemical composition of these ingredients, but, more specifically, on describing their mechanism of action in improving human nutrition

Prof. Dr. Davide Barreca
Guest Editor

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Keywords

flavonoids
antioxidants
activation/block of signal cascade
modulation of key metabolic enzymes
oxidative stress
biological potentials
antimicrobial activity
antiviral potential
anticancer activity
anti-aggregative activity
anti-inflammatory activity

Related Special Issue

Flavonoids and Their Impact on Human Health 2.0 in International Journal of Molecular Sciences (1 article)

Published Papers (14 papers)

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Research

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17 pages, 9476 KiB

Open AccessArticle

GB1a Activates SIRT6 to Regulate Lipid Metabolism in Mouse Primary Hepatocytes

by Yongzhi Sun, Congmin Zheng, Ting Li, Xinqian He, Fan Yang, Wenfeng Guo, Jianping Song, Yong Gao, Changsheng Deng and Xinan Huang

Int. J. Mol. Sci. 2023, 24(11), 9540; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24119540 - 31 May 2023

Cited by 2 | Viewed by 1499

Abstract

Lipid accumulation, oxidative stress, and inflammation in hepatocytes are features of nonalcoholic fatty liver disease (NAFLD). Garcinia biflavonoid 1a (GB1a) is a natural product capable of hepatic protection. In this study, the effect of GB1a on anti-inflammatory, antioxidant, and regulation of the accumulation in HepG2 cells and mouse primary hepatocytes (MPHs) was investigated, and its regulatory mechanism was further explored. The result showed that GB1a reduced triglyceride (TG) content and lipid accumulation by regulating the expression of SREBP-1c and PPARα; GB1a reduced reactive oxygen species (ROS) and improved cellular oxidative stress to protect mitochondrial morphology by regulating genes Nrf2, HO-1, NQO1, and Keap1; and GB1a reduced the damage of hepatocytes by inhibiting the expression of inflammatory cytokines interleukin-6 (IL-6), interleukin-1β (IL-1β), tumor necrosis factor-alpha (TNF-α), and nuclear factor kappa B (NF-κB) p65. The activities of GB1a were lost in liver SIRT6-specific knockout mouse primary hepatocytes (SIRT6-LKO MPHs). This indicated that activating SIRT6 was critical for GB1a to perform its activity, and GB1a acted as an agonist of SIRT6. It was speculated that GB1a may be a potential drug for NAFLD treatment. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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20 pages, 2688 KiB

Open AccessArticle

Investigation of Flavonoid Scaffolds as DAX1 Inhibitors against Ewing Sarcoma through Pharmacoinformatic and Dynamic Simulation Studies

by Muhammad Yasir, Jinyoung Park, Eun-Taek Han, Won Sun Park, Jin-Hee Han, Yong-Soo Kwon, Hee-Jae Lee, Mubashir Hassan, Andrzej Kloczkowski and Wanjoo Chun

Int. J. Mol. Sci. 2023, 24(11), 9332; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24119332 - 26 May 2023

Cited by 4 | Viewed by 1021

Abstract

Dosage-sensitive sex reversal, adrenal hypoplasia critical region, on chromosome X, gene 1 (DAX1) is an orphan nuclear receptor encoded by the NR0B1 gene. The functional study showed that DAX1 is a physiologically significant target for EWS/FLI1-mediated oncogenesis, particularly Ewing Sarcoma (ES). In this study, a three-dimensional DAX1 structure was modeled by employing a homology modeling approach. Furthermore, the network analysis of genes involved in Ewing Sarcoma was also carried out to evaluate the association of DAX1 and other genes with ES. Moreover, a molecular docking study was carried out to check the binding profile of screened flavonoid compounds against DAX1. Therefore, 132 flavonoids were docked in the predicted active binding pocket of DAX1. Moreover, the pharmacogenomics analysis was performed for the top ten docked compounds to evaluate the ES-related gene clusters. As a result, the five best flavonoid-docked complexes were selected and further evaluated by Molecular Dynamics (MD) simulation studies at 100 ns. The MD simulation trajectories were evaluated by generating RMSD, hydrogen bond plot analysis, and interaction energy graphs. Our results demonstrate that flavonoids showed interactive profiles in the active region of DAX1 and can be used as potential therapeutic agents against DAX1-mediated augmentation of ES after in-vitro and in-vivo evaluations. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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14 pages, 2510 KiB

Open AccessArticle

Isoquercitrin Attenuates Steatohepatitis by Inhibition of the Activated NLRP3 Inflammasome through HSP90

by Ji Ma, Maoru Li, Tingting Yang, Yang Deng, Yadong Ding, Tiantian Guo and Jing Shang

Int. J. Mol. Sci. 2023, 24(10), 8795; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24108795 - 15 May 2023

Cited by 3 | Viewed by 1420

Abstract

Non-alcoholic fatty liver disease (NAFLD) is a chronic liver disease with a global prevalence of 25%. However, the medicines approved by the FDA or EMA are still not commercially available for the treatment of NAFLD. The NOD-like receptor thermal protein domain-associated protein 3 (NLRP3) inflammasome plays a crucial role in inflammatory responses, and the mechanisms related to steatohepatitis have been sufficiently clarified. NLRP3 has been widely evaluated as a potential target for multiple active agents in treating NAFLD. As a quercetin glycoside, isoquercitrin (IQ) has a broad inhibitory effect on oxidative stress, cancers, cardiovascular diseases, diabetes, and allergic reactions in vitro and in vivo. This study aimed to investigate the undercover mechanism of IQ in the treatment of NAFLD, particularly in anti-steatohepatitis, by suppressing the NLRP3 inflammasome. In this study, a methionine-choline-deficient induced steatohepatitis mice model was used to explore the effect of IQ on NAFLD treatment. Further mechanism exploration based on transcriptomics and molecular biology revealed that IQ inhibited the activated NLRP3 inflammasome by down-regulating the expression of heat shock protein 90 (HSP90) and suppressor of G-two allele of Skp1 (SGT1). In conclusion, IQ could alleviate NAFLD by inhibiting the activated NLRP3 inflammasome by suppressing the expression of HSP90. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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20 pages, 4570 KiB

Open AccessArticle

Differential Modulation of Dendritic Cell Biology by Endogenous and Exogenous Aryl Hydrocarbon Receptor Ligands

by Atefeh Sadeghi Shermeh, Dmytro Royzman, Christine Kuhnt, Christina Draßner, Lena Stich, Alexander Steinkasserer, Ilka Knippertz and Andreas B. Wild

Int. J. Mol. Sci. 2023, 24(9), 7801; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24097801 - 25 Apr 2023

Cited by 2 | Viewed by 1336

Abstract

The aryl hydrocarbon receptor (AhR) is a decisive regulatory ligand-dependent transcription factor. It binds highly diverse ligands, which can be categorized as either endogenous or exogenous. Ligand binding activates AhR, which can adjust inflammatory responses by modulating immune cells such as dendritic cells (DCs). However, how different AhR ligand classes impact the phenotype and function of human monocyte-derived DCs (hMoDCs) has not been extensively studied in a comparative manner. We, therefore, tested the effect of the representative compounds Benzo(a)pyrene (BP), 6-formylindolo[3,2-b]carbazole (FICZ), and Indoxyl 3-sulfate (I3S) on DC biology. Thereby, we reveal that BP significantly induces a tolerogenic response in lipopolysaccharide-matured DCs, which is not apparent to the same extent when using FICZ or I3S. While all three ligand classes activate AhR-dependent pathways, BP especially induces the expression of negative immune regulators, and subsequently strongly subverts the T cell stimulatory capacity of DCs. Using the CRISPR/Cas9 strategy we also prove that the regulatory effect of BP is strictly AhR-dependent. These findings imply that AhR ligands contribute differently to DC responses and incite further studies to uncover the mechanisms and molecules which are involved in the induction of different phenotypes and functions in DCs upon AhR activation. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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14 pages, 1851 KiB

Open AccessArticle

The Emerging Importance of Cirsimaritin in Type 2 Diabetes Treatment

by Abdelrahim Alqudah, Rabaa Y. Athamneh, Esam Qnais, Omar Gammoh, Muna Oqal, Rawan AbuDalo, Hanan Abu Alshaikh, Nabil AL-Hashimi and Mohammad Alqudah

Int. J. Mol. Sci. 2023, 24(6), 5749; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24065749 - 17 Mar 2023

Cited by 3 | Viewed by 1791

Abstract

Cirsimaritin is a dimethoxy flavon that has different biological activities such as antiproliferative, antimicrobial, and antioxidant activities. This study aims to investigate the anti-diabetic effects of cirsimaritin in a high-fat diet and streptozotocin-(HFD/STZ)-induced rat model of type 2 diabetes mellitus (T2D). Rats were fed HFD, followed by a single low dose of STZ (40 mg/kg). HFD/STZ diabetic rats were treated orally with cirsimaritin (50 mg/kg) or metformin (200 mg/kg) for 10 days before terminating the experiment and collecting plasma, soleus muscle, adipose tissue, and liver for further downstream analysis. Cirsimaritin reduced the elevated levels of serum glucose in diabetic rats compared to the vehicle control group (p < 0.001). Cirsimaritin abrogated the increase in serum insulin in the treated diabetic group compared to the vehicle control rats (p < 0.01). The homeostasis model assessment of insulin resistance (HOMA-IR) was decreased in the diabetic rats treated with cirsimaritin compared to the vehicle controls. The skeletal muscle and adipose tissue protein contents of GLUT4 (p < 0.01 and p < 0.05, respectively) and pAMPK-α1 (p < 0.05) were upregulated following treatment with cirsimaritin. Cirsimaritin was able to upregulate GLUT2 and AMPK protein expression in the liver (p < 0.01, <0.05, respectively). LDL, triglyceride, and cholesterol were reduced in diabetic rats treated with cirsimaritin compared to the vehicle controls (p < 0.001). Cirsimaritin reduced MDA, and IL-6 levels (p < 0.001), increased GSH levels (p < 0.001), and reduced GSSG levels (p < 0.001) in diabetic rats compared to the vehicle control. Cirsimaritin could represent a promising therapeutic agent to treat T2D. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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18 pages, 1556 KiB

Open AccessArticle

Anti-Inflammatory, Antimicrobial, Antioxidant and Photoprotective Investigation of Red Propolis Extract as Sunscreen Formulation in Polawax Cream

by Thalita Marcolan Valverde, Bruna Nayane Goncalves de Souza Soares, Andréa Mendes do Nascimento, Ângela Leão Andrade, Lucas Resende Dutra Sousa, Paula Melo de Abreu Vieira, Vagner Rodrigues Santos, Janaína Brandão Seibert, Tatiane Cristine Silva de Almeida, Caio Fabrini Rodrigues, Samantha Roberta Machado de Oliveira, Flaviano dos Santos Martins, Jeronimo Geraldo Ferreira Júnior and Viviane Martins Rebello dos Santos

Int. J. Mol. Sci. 2023, 24(6), 5112; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24065112 - 07 Mar 2023

Cited by 6 | Viewed by 2477

Abstract

Many activities have been described for propolis, including, antiviral, antibacterial, antifungal, anti-inflammatory, immunoregulatory, antioxidant and wound healing properties. Recently, propolis has been highlighted due to its potential application in the pharmaceutical and cosmetic industries, motivating a better understanding of its antioxidant and anti-inflammatory activities. Propolis and its main polyphenolic compounds presented high antioxidant activity, and effectiveness as broad spectrum UVB and UVA photoprotection sunscreens. Through a qualitative phytochemical screening, the ethanolic red propolis extracts (EEPV) (70% at room temperature and 70% at a hot temperature) presented a positive result for flavonoids and terpenoids. It presented an antioxidant activity for reducing 50% of DPPH of 17 and 12 μg/mL for extraction at room temperature and at a hot temperature, respectively. The UPLC-QTOF-MS/MS analysis allowed the annotation of 40 substances for EEPV-Heated and 42 substances for EEPV-Room Temperature. The IC₅₀ results of the ABTS scavenging activity was 4.7 μg/mL for both extractions, at room temperature and at a hot temperature. Additionally, we also evaluated the cytotoxic profile of propolis extracts against macrophage (RAW 264.7 cells) and keratinocytes (HaCaT cells), which showed non-cytotoxic doses in cell viability assays even after a long period of exposure. In addition, propolis extracts showed antibacterial activity for Gram-positive bacteria (Staphylococcus aureus and Staphylococcus epidermidis), demonstrating potential biological activity for the creation of formulations aimed at disease control and prevention. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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14 pages, 8786 KiB

Open AccessArticle

Effects of Luteolin on Biofilm of Trueperella pyogenes and Its Therapeutic Effect on Rat Endometritis

by Luyao Zhang, Yitong Cai, Lishuang Li, Chen Chen, Hanyu Zhao, Zehui Zhang, Yaochuan Liu, Yingyu Wang, Chunlian Tian and Mingchun Liu

Int. J. Mol. Sci. 2022, 23(22), 14451; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232214451 - 21 Nov 2022

Cited by 4 | Viewed by 1314

Abstract

Trueperella pyogenes is an opportunistic pathogen that causes suppurative infections in animals. The development of new anti-biofilm drugs will improve the current treatment status for controlling T. pyogenes infections in the animal husbandry industry. Luteolin is a naturally derived flavonoid compound with antibacterial properties. In this study, the effects and the mechanism of luteolin on T. pyogenes biofilm were analyzed and explored. The MBIC and MBEC of luteolin on T. pyogenes were 156 μg/mL and 312 μg/mL, respectively. The anti-biofilm effects of luteolin were also observed by a confocal laser microscope and scanning electron microscope. The results indicated that 312 μg/mL of luteolin could disperse large pieces of biofilm into small clusters after 8 h of treatment. According to the real-time quantitative PCR detection results, luteolin could significantly inhibit the relative expression of the biofilm-associated genes luxS, plo, rbsB and lsrB. In addition, the in vivo anti-biofilm activity of luteolin against T. pyogenes was studied using a rat endometritis model established by glacial acetic acid stimulation and T. pyogenes intrauterine infusion. Our study showed that luteolin could significantly reduce the symptoms of rat endometritis. These data may provide new opinions on the clinical treatment of luteolin and other flavonoid compounds on T. pyogenes biofilm-associated infections. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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13 pages, 3483 KiB

Open AccessArticle

Molecular Basis for Luteolin as a Natural TatD DNase Inhibitor in Trueperella pyogenes

by Zehui Zhang, Yuru Guo, Yueting Guo, Luyao Zhang, Shengli Niu, Chunlian Tian, Limei Han, Dexian Zhang and Mingchun Liu

Int. J. Mol. Sci. 2022, 23(15), 8374; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23158374 - 29 Jul 2022

Cited by 1 | Viewed by 1488

Abstract

TatD960 and TatD825 are DNases that contribute to biofilm formation and virulence in Trueperella pyogenes (T. pyogenes). Luteolin is a natural flavonoid commonly found in plants that exhibits antimicrobial capacity. Our study aims to investigate the effects of luteolin on TatD DNases as a natural inhibitor. In this research, the expression of tatD genes and TatD proteins in T. pyogenes treated with luteolin was detected, and then the effect of luteolin on the hydrolysis of DNA by TatD DNases was analyzed using agarose gel electrophoresis. Moreover, the interactions between luteolin and TatD DNases were tested using surface plasmon resonance (SPR) assays and molecular docking analysis. After 1/2 MIC luteolin treatment, the transcription of tatD genes and expression of TatD proteins appeared to be reduced in 80–90% of T. pyogenes (n = 20). The gel assay revealed that luteolin can inhibit the activity of TatD DNases. The SPR assay showed that the KD values of luteolin to TatD960 and TatD825 were 6.268 × 10⁻⁶ M and 5.654 × 10⁻⁶ M, respectively. We found through molecular docking that hydrogen bonding is predominant in the interaction of luteolin and TatD DNases. Our data indicate that luteolin inhibited the ability of TatD DNases by decreasing their binding to DNA. The current study provides an insight into the development of luteolin as a DNase inhibitor in preventing biofilm formation and virulence in T. pyogenes. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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22 pages, 5605 KiB

Open AccessArticle

Anti-Inflammatory Activity of Mulberry Leaf Flavonoids In Vitro and In Vivo

by Ziwei Lin, Tiantian Gan, Yanzhen Huang, Lijun Bao, Shuang Liu, Xiaopeng Cui, Hexin Wang, Feng Jiao, Minjuan Zhang, Chao Su and Yonghua Qian

Int. J. Mol. Sci. 2022, 23(14), 7694; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23147694 - 12 Jul 2022

Cited by 14 | Viewed by 3025

Abstract

Mulberry (Morus alba L.) is a flowering tree traditionally used in Chinese herbal medicine. Mulberry leaf flavonoids (MLFs) have been reported to exert important anti-inflammatory and antioxidant properties. The purpose of this study was to select the MLF with the best anti-inflammatory and antioxidative activities from MLFs eluted by different ethanol concentrations (30%, 50%, and 75%) and explore its pharmacological properties. Three types of MLFs inhibited the production of nitric oxide (NO), prostaglandin E2 (PGE2), inducible nitric oxide synthase (iNOS), cyclooxygenase-2 (COX-2), and inflammatory cytokines in lipopolysaccharide (LPS)-induced RAW 264.7 cells. All MLFs boosted the antioxidative capacity by decreasing the reactive oxygen species (ROS) production and the scavenging of 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radicals and improving the metal ion chelating activity and reducing power. The results revealed that the MLFs eluted by 30% ethanol exhibited the best anti-inflammatory and antioxidative activities. A nontargeted metabolomic analysis was used to analyze 24 types of differential flavonoids between the MLFs. Quercetin, kaempferol, and their derivatives in 30%MLF were more abundant than the other two MLFs. Furthermore, we evaluated the pharmacological activities of 30%MLF in dextran sodium sulfate (DSS)-induced ulcerative colitis (UC) mice. The 30%MLF could alleviate the clinical symptoms, reduce the secretion of inflammatory cytokines, and inhibit the activation of the inflammatory pathway in DSS-induced colitis mice. This study will provide valuable information for the development of MLFs eluted by 30% ethanol as a functional food. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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Review

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13 pages, 2620 KiB

Open AccessReview

Consideration for Flavonoid-Containing Dietary Supplements to Tackle Deficiency and Optimize Health

by Julia Solnier, Chuck Chang and Joseph Pizzorno

Int. J. Mol. Sci. 2023, 24(10), 8663; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms24108663 - 12 May 2023

Cited by 2 | Viewed by 2303

Abstract

Randomized clinical trials (RCT) and observational studies have highlighted the importance of flavonoid consumption for human health. Several studies have associated a high intake of dietary flavonoids with (a) enhanced metabolic and cardiovascular health, (b) enhanced cognitive and vascular endothelial functions, (c) an improved glycemic response in type 2 diabetes mellitus, and (d) a reduced risk of breast cancer in postmenopausal women. Since flavonoids belong to a broad and diverse family of polyphenolic plant molecules—with more than 6000 compounds interspersed in the human diet—researchers are still uncertain whether the intake of single, individual polyphenols or a large combination of them (i.e., synergistic action) can produce the greatest health benefits for humans. Furthermore, studies have reported a poor bioavailability of flavonoid compounds in humans, which presents a major challenge for determining their optimal dosage, recommended intake, and, consequently, their therapeutic value. Especially because of their scarce bioavailability from foods—along with the overall declining food quality and nutrient density in foods—the role of flavonoid supplementation may become increasingly important for human health. Although research shows that dietary supplements can be a highly useful tool to complement diets that lack sufficient amounts of important nutrients, some caution is warranted regarding possible interactions with prescription and non-prescription drugs, especially when taken concurrently. Herein, we discuss the current scientific basis for using flavonoid supplementation to improve health as well as the limitations related to high intakes of dietary flavonoids. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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22 pages, 3444 KiB

Open AccessReview

The Neuroprotective Potentiality of Flavonoids on Alzheimer’s Disease

by Antonella Calderaro, Giuseppe Tancredi Patanè, Ester Tellone, Davide Barreca, Silvana Ficarra, Francesco Misiti and Giuseppina Laganà

Int. J. Mol. Sci. 2022, 23(23), 14835; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232314835 - 27 Nov 2022

Cited by 31 | Viewed by 4849

Abstract

Alzheimer’s disease (AD), due to its spread, has become a global health priority, and is characterized by senile dementia and progressive disability. The main cause of AD and other neurodegenerations (Huntington, Parkinson, Amyotrophic Lateral Sclerosis) are aggregated protein accumulation and oxidative damage. Recent research on secondary metabolites of plants such as polyphenols demonstrated that they may slow the progression of AD. The flavonoids’ mechanism of action in AD involved the inhibition of acetylcholinesterase, butyrylcholinesterase, Tau protein aggregation, β-secretase, oxidative stress, inflammation, and apoptosis through modulation of signaling pathways which are implicated in cognitive and neuroprotective functions, such as ERK, PI3-kinase/Akt, NFKB, MAPKs, and endogenous antioxidant enzymatic systems. This review focuses on flavonoids and their role in AD, in terms of therapeutic potentiality for human health, antioxidant potential, and specific AD molecular targets. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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35 pages, 11541 KiB

Open AccessReview

Flavonoids as Antidiabetic and Anti-Inflammatory Agents: A Review on Structural Activity Relationship-Based Studies and Meta-Analysis

by Nur Farisya Shamsudin, Qamar Uddin Ahmed, Syed Mahmood, Syed Adnan Ali Shah, Murni Nazira Sarian, Muhammad Muzaffar Ali Khan Khattak, Alfi Khatib, Awis Sukarni Mohmad Sabere, Yusnaini Md Yusoff and Jalifah Latip

Int. J. Mol. Sci. 2022, 23(20), 12605; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms232012605 - 20 Oct 2022

Cited by 46 | Viewed by 4138

Abstract

Flavonoids are a group of naturally occurring polyphenolic secondary metabolites which have been reported to demonstrate a wide range of pharmacological properties, most importantly, antidiabetic and anti-inflammatory effects. The relationship between hyperglycaemia and inflammation and vascular complications in diabetes is now well established. Flavonoids possessing antidiabetic properties may alleviate inflammation by reducing hyperglycaemia through different mechanisms of action. It has been suggested that the flavonoids’ biochemical properties are structure-dependent; however, they are yet to be thoroughly grasped. Hence, the main aim of this review is to understand the antidiabetic and anti-inflammatory properties of various structurally diverse flavonoids and to identify key positions responsible for the effects, their correlation, and the effect of different substitutions on both antidiabetic and anti-inflammatory properties. The general requirement of flavonoids for exerting both anti-inflammatory and antidiabetic effects is found to be the presence of a C2–C3 double bond (C-ring) and hydroxyl groups at the C3’, C4’, C5, and C7 positions of both rings A and B of a flavonoid skeleton. Furthermore, it has been demonstrated that substitution at the C3 position of a C-ring decreases the anti-inflammatory action of flavonoids while enhancing their antidiabetic activity. Correlation is discussed at length to support flavonoids possessing essential pharmacophores to demonstrate equipotent effects. The consideration of these structural features may play an important role in synthesizing better flavonoid-based drugs possessing dual antidiabetic and anti-inflammatory effects. A meta-analysis further established the role of flavonoids as antidiabetic and anti-inflammatory agents. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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21 pages, 1043 KiB

Open AccessReview

Molecular Pathways Involved in the Anti-Cancer Activity of Flavonols: A Focus on Myricetin and Kaempferol

by Maria Rosa Felice, Alessandro Maugeri, Giovambattista De Sarro, Michele Navarra and Davide Barreca

Int. J. Mol. Sci. 2022, 23(8), 4411; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms23084411 - 16 Apr 2022

Cited by 25 | Viewed by 3229

Abstract

Natural compounds have always represented valuable allies in the battle against several illnesses, particularly cancer. In this field, flavonoids are known to modulate a wide panel of mechanisms involved in tumorigenesis, thus rendering them worthy candidates for both cancer prevention and treatment. In particular, it was reported that flavonoids regulate apoptosis, as well as hamper migration and proliferation, crucial events for the progression of cancer. In this review, we collect recent evidence concerning the anti-cancer properties of the flavonols myricetin and kaempferol, discussing their mechanisms of action to give a thorough overview of their noteworthy capabilities, which are comparable to those of their most famous analogue, namely quercetin. On the whole, these flavonols possess great potential, and hence further study is highly advised to allow a proper definition of their pharmaco-toxicological profile and assess their potential use in protocols of chemoprevention and adjuvant therapies. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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15 pages, 429 KiB

Open AccessReview

Zapotin, a Polymethoxyflavone, with Potential Therapeutic Attributes

by Jakub W. Strawa, Katarzyna Jakimiuk and Michał Tomczyk

Int. J. Mol. Sci. 2021, 22(24), 13227; https://0-doi-org.brum.beds.ac.uk/10.3390/ijms222413227 - 08 Dec 2021

Cited by 12 | Viewed by 2877

Abstract

The use of plants as traditional medicines is common and has prevailed in many different cultures over time. Polymethoxyflavones (PMFs) are natural polyphenols from the group of flavonoids. Zapotin, a member of the PMFs, is found mainly in citrus plants and is almost exclusively limited to their peels. The chemical structure of zapotin has been questioned from the very beginning, since the structure of flavonoids with a single oxygen atom in the C2′ position is extremely rare in the plant kingdom. To clarify this, the structural determination and bio-inspired synthesis of zapotin are discussed in detail in this review. Due to the broad biological potential of PMFs, the complication in the isolation process and characterization of PMFs, as well as their purification, have been estimated by adapting various chromatographic methods. According to available data from the literature, zapotin may be a promising curative agent with extensive biological activities, especially as a chemopreventive factor. Apart from that, zapotin acts as an antidepressant-like, anticancer, antifungal, and antioxidant agent. Finally, accessible studies about zapotin metabolism (absorption, distribution, metabolism, excretion, and toxicity) underline its potential in use as a therapeutic substance. Full article

(This article belongs to the Special Issue Flavonoids and Their Impact on Human Health)

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