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Quercetin: From Structure to Health Issues
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Quercetin: From Structure to Health Issues

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

Deadline for manuscript submissions: closed (30 September 2022) | Viewed by 35264

Special Issue Editors

Dr. Natalie Lenard

E-Mail Website
Guest Editor
Biology Department, Franciscan Missionaries of Our Lady University, Baton Rouge, LA 70808, USA
Interests: quercetin; inflammation; browning; mulilocular adipocyte; red onion extract; botanical extract; adipose tissue; adipocyte; adipokine
Special Issues, Collections and Topics in MDPI journals
Dr. Tara M. Henagan

E-Mail Website
Guest Editor
LSU Health Shreveport, 1501 Kings Hwy, Shreveport, LA, USA
Interests: epigenetics; short-chain fatty acids; mitochondria; adipose tissue; exercise; skeletal muscle

Special Issue Information

Dear Colleagues,

The plant pigment quercetin is well-known as a potent flavonol antioxidant abundantly found in a wide variety of fruits and vegetables, especially onions and berries. The aim of this Special Issue of Molecules is to showcase the breadth and depth of research conducted on the properties of this important potential therapeutic phytochemical. Multiple disciplines have contributed to the understanding of quercetin, such as botany, chemistry molecular modelling and structure–activity relationships, and pharmacokinetics and pharmacodynamics in both basic research and clinical trials, to name a few. We envision this Special Issue as not only a collection of recent studies, but also as a means to support scientists in disparate fields in identifying potential interdisciplinary collaborations.

You are cordially invited to contribute a review or original research to this Special Issue of Molecules.

Dr. Natalie Lenard
Dr. Tara M. Henagan
Guest Editors

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 submissions that pass pre-check are 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 2700 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

  • bioactive natural compound
  • antioxidant
  • structure-activity relationship
  • pharmacotherapeutics
  • anti-inflammatory

Published Papers (5 papers)

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Research

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13 pages, 1151 KiB  
Article
Different Effects of Quercetin Glycosides and Quercetin on Kidney Mitochondrial Function—Uncoupling, Cytochrome C Reducing and Antioxidant Activity
by Kristina Zymone, Raimondas Benetis, Darius Trumbeckas, Ingrida Baseviciene and Sonata Trumbeckaite
Molecules 2022, 27(19), 6377; https://doi.org/10.3390/molecules27196377 - 27 Sep 2022
Cited by 10 | Viewed by 1593
Abstract
Flavonols are found in plants as aglycones and as glycosides. Antioxidant activity of flavonols may occur via several mechanisms within the cell, and mitochondria as a target may play an important role. There is a lack of information about the influence of the [...] Read more.
Flavonols are found in plants as aglycones and as glycosides. Antioxidant activity of flavonols may occur via several mechanisms within the cell, and mitochondria as a target may play an important role. There is a lack of information about the influence of the sugar moiety on biological activity of flavonoid glycosides. The aims of study were to investigate the effects of quercetin and its glycosides on mitochondrial respiration rates at various metabolic states, and to evaluate their antioxidant potential using chemical and biological approaches. Mitochondrial function was measured using an oxygraphic method, cytochrome c reduction spectrophotometrically, H2O2 generation in mitochondria fluorimetrically, and antioxidant activity of flavonoids using an HPLC-post column system. Our data revealed that quercetin and its glycosides isoquercitrin, rutin, and hyperoside uncouple kidney mitochondrial respiration (increasing the State 2 respiration rate) and significantly reduce cytochrome c. Moreover, quercetin, and its glycosides decrease the production of mitochondrial H2O2 and possess radical scavenging and ferric reducing capacities. The highest activity was characteristic for quercetin, showing that the sugar moiety significantly diminishes its activity. In conclusion, our results show the efficient radical scavenging, ferric and cytochrome c reducing capacities, and uncoupling properties of quercetin and its glycosides, as well as the importance of the sugar residue and its structure in the regulation of kidney mitochondrial function. Full article
(This article belongs to the Special Issue Quercetin: From Structure to Health Issues)
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18 pages, 3006 KiB  
Article
PLA Nanofibers for Microenvironmental-Responsive Quercetin Release in Local Periodontal Treatment
by Francesca Di Cristo, Anna Valentino, Ilenia De Luca, Gianfranco Peluso, Irene Bonadies, Anna Calarco and Anna Di Salle
Molecules 2022, 27(7), 2205; https://doi.org/10.3390/molecules27072205 - 28 Mar 2022
Cited by 18 | Viewed by 3089
Abstract
The management of periodontitis remains a vital clinical challenge due to the interplay between the microorganisms of the dental biofilm and the host inflammatory response leading to a degenerative process in the surrounding tissues. Quercetin (QUE), a natural flavonol found in many foods, [...] Read more.
The management of periodontitis remains a vital clinical challenge due to the interplay between the microorganisms of the dental biofilm and the host inflammatory response leading to a degenerative process in the surrounding tissues. Quercetin (QUE), a natural flavonol found in many foods, including apples, onions and tea, has exhibited prolonged and strong antibiofilm and anti-inflammatory effects both in vitro and in vivo. However, its clinical application is limited by its poor stability and water solubility, as well as its low bioavailability. Thus, in the present study, electrospun polylactic acid (PLA) nanofibers loaded with different amounts (5–10% w/w) of QUE were produced to rapidly respond to the acidic microenvironment typical of periodontal pockets during periodontal disease. This strategy demonstrated that PLA-QUE membranes can act as a drug reservoir releasing high QUE concentrations in the presence of oral bacterial infection (pH < 5.5), and thus limiting Pseudomonas aeruginosa PAO1 and Streptococcus mutans biofilm maturation. In addition, released QUE exerts antioxidant and anti-inflammatory effects on P. gingivalis Lipopolysaccharide (LPS)-stimulated human gingival fibroblast (HGFs). The reported results confirmed that PLA-QUE membranes could inhibit subgingival biofilm maturation while reducing interleukin release, thereby limiting host inflammatory response. Overall, this study provided an effective pH-sensitive drug delivery system as a promising strategy for treating periodontitis. Full article
(This article belongs to the Special Issue Quercetin: From Structure to Health Issues)
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Review

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20 pages, 2402 KiB  
Review
Quercetin’s Effects on Glutamate Cytotoxicity
by Kade Riche and Natalie R. Lenard
Molecules 2022, 27(21), 7620; https://doi.org/10.3390/molecules27217620 - 7 Nov 2022
Cited by 7 | Viewed by 3453
Abstract
The potentially therapeutic effects of the naturally abundant plant flavonoid quercetin have been extensively studied. An extensive body of literature suggests that quercetin’s powerful antioxidant effects may relate to its ability to treat disease. Glutamate excitotoxicity occurs when a neuron is overstimulated by [...] Read more.
The potentially therapeutic effects of the naturally abundant plant flavonoid quercetin have been extensively studied. An extensive body of literature suggests that quercetin’s powerful antioxidant effects may relate to its ability to treat disease. Glutamate excitotoxicity occurs when a neuron is overstimulated by the neurotransmitter glutamate and causes dysregulation of intracellular calcium concentrations. Quercetin has been shown to be preventative against many forms of neuronal cell death resulting from glutamate excitotoxicity, such as oncosis, intrinsic apoptosis, mitochondrial permeability transition, ferroptosis, phagoptosis, lysosomal cell death, parthanatos, and death by reactive oxygen species (ROS)/reactive nitrogen species (RNS) generation. The clinical importance for the attenuation of glutamate excitotoxicity arises from the need to deter the continuous formation of tissue infarction caused by various neurological diseases, such as ischemic stroke, seizures, neurodegenerative diseases, and trauma. This review aims to summarize what is known concerning glutamate physiology and glutamate excitotoxic pathophysiology and provide further insight into quercetin’s potential to hinder neuronal death caused by cell death pathways activated by glutamate excitotoxicity. Quercetin’s bioavailability may limit its use clinically, however. Thus, future research into ways to increase its bioavailability are warranted. Full article
(This article belongs to the Special Issue Quercetin: From Structure to Health Issues)
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14 pages, 1643 KiB  
Review
Health Benefits of Quercetin in Age-Related Diseases
by Deepika and Pawan Kumar Maurya
Molecules 2022, 27(8), 2498; https://doi.org/10.3390/molecules27082498 - 13 Apr 2022
Cited by 122 | Viewed by 15026
Abstract
Polyphenols are the known group of phytochemicals that essentially consists of phenolic rings. These are the plant product present in varied fruits and vegetables. These secondary metabolites perform a protective function in plants from environmental and biological stress. When consumed as a human [...] Read more.
Polyphenols are the known group of phytochemicals that essentially consists of phenolic rings. These are the plant product present in varied fruits and vegetables. These secondary metabolites perform a protective function in plants from environmental and biological stress. When consumed as a human diet these are also known to prevent various age-associated diseases. Polyphenols are known to possess antioxidant properties and protect against oxidative stress. The literature survey was carried out using databases such as PubMed, Science direct and Springer. The research articles from last 10–12 years were selected for this review based on its relevancy with the topic. The articles selected was mainly focused on quercetin and its health benefits. The present review highlights the main functions of a flavonoid, quercetin. Quercetin is among the widely occurring polyphenol, found abundantly in nature. It is commonly present in different plant products. Onion is known to have the highest quantity of quercetin. This plant compound is possessed antioxidant properties and is considered to have a protective function against aging. It is known to be present in both free and conjugated forms. Quercetin has anti-oxidative, anti-inflammatory, anti-proliferative, anti-carcinogenic, anti-diabetic, and anti-viral properties. The molecule is lipophilic and can easily cross the BBB (Blood-Brain Barrier) and hence protects from neurodegenerative diseases. Various in vivo and in vitro studies have demonstrated the role of quercetin and here a detailed review of quercetin as a curative agent in neurodegeneration, diabetes, cancer, and inflammation has been carried out. Studies have proved that quercetin plays a crucial role in the prevention of age-related disorders. Quercetin is a potent antioxidant which is currently being used in various pharmaceuticals. Properties of quercetin can be further explored in various other disorders. Nanoformulations and liposomal formulations of quercetin can be made to treat other age associated diseases. Full article
(This article belongs to the Special Issue Quercetin: From Structure to Health Issues)
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13 pages, 1472 KiB  
Review
Antimicrobial Activity of Quercetin: An Approach to Its Mechanistic Principle
by Thi Lan Anh Nguyen and Debanjana Bhattacharya
Molecules 2022, 27(8), 2494; https://doi.org/10.3390/molecules27082494 - 12 Apr 2022
Cited by 143 | Viewed by 10842
Abstract
Quercetin, an essential plant flavonoid, possesses a variety of pharmacological activities. Extensive literature investigates its antimicrobial activity and possible mechanism of action. Quercetin has been shown to inhibit the growth of different Gram-positive and Gram-negative bacteria as well as fungi and viruses. The [...] Read more.
Quercetin, an essential plant flavonoid, possesses a variety of pharmacological activities. Extensive literature investigates its antimicrobial activity and possible mechanism of action. Quercetin has been shown to inhibit the growth of different Gram-positive and Gram-negative bacteria as well as fungi and viruses. The mechanism of its antimicrobial action includes cell membrane damage, change of membrane permeability, inhibition of synthesis of nucleic acids and proteins, reduction of expression of virulence factors, mitochondrial dysfunction, and preventing biofilm formation. Quercetin has also been shown to inhibit the growth of various drug-resistant microorganisms, thereby suggesting its use as a potent antimicrobial agent against drug-resistant strains. Furthermore, certain structural modifications of quercetin have sometimes been shown to enhance its antimicrobial activity compared to that of the parent molecule. In this review, we have summarized the antimicrobial activity of quercetin with a special focus on its mechanistic principle. Therefore, this review will provide further insights into the scientific understanding of quercetin’s mechanism of action, and the implications for its use as a clinically relevant antimicrobial agent. Full article
(This article belongs to the Special Issue Quercetin: From Structure to Health Issues)
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