Polyphenols are naturally occurring micronutrients that are present in many food sources. Besides being potent antioxidants, these molecules may also possess anti-inflammatory properties. Many studies have highlighted their potential role in the prevention and treatment of various pathological conditions connected to oxidative stress and inflammation (e.g., cancer, and cardiovascular and neurodegenerative disorders). Neurodegenerative diseases are globally one of the main causes of death and represent an enormous burden in terms of human suffering, social distress, and economic costs. Recent data expanded on the initial antioxidant-based mechanism of polyphenols’ action by showing that they are also able to modulate several cell-signaling pathways and mediators. The proposed benefits of polyphenols, either as protective/prophylactic substances or as therapeutic molecules, may be achieved by the consumption of a natural polyphenol-enriched diet, by their use as food supplements, or with formulations as pharmaceutical drugs/nutraceuticals. It has also been proved that the health effects of polyphenols depend on the consumed amount and their bioavailability. However, their overconsumption may raise safety concerns due to the accumulation of high levels of these molecules in the organism, particularly if we consider the loose regulatory legislation regarding the commercialization and use of food supplements. This review addresses the main beneficial effects of food polyphenols, and focuses on neuroprotection and the safety issues related to overconsumption.

https://www.mdpi.com/2076-3921/9/1/61/pdf

Polyphenols from Food and Natural Products: Neuroprotection and Safety.

Polyphenols (PPs) are the naturally occurring bioactive components in fruits and vegetables, and they are the most abundant antioxidant in the human diet. Studies are suggesting that ingestion of PPs might be helpful to ameliorate metabolic syndromes that may contribute in the prevention of several chronic disorders like diabetes, obesity, hypertension, and colon cancer. PPs have structural diversity which impacts their bioavailability as they accumulate in the large intestine and are extensively metabolized through gut microbiota (GM). Intestinal microbiota transforms PPs into their metabolites to make them bioactive. Interestingly, not only GM act on PPs to metabolize them but PPs also modulate the composition of GM. Thus, change in GM from pathogenic to beneficial ones may be helpful to ameliorate gut health and associated diseases. However, to overcome the low bioavailability of PPs, various approaches have been developed to improve their solubility and transportation through the gut. In this review, we present evidence supporting the structural changes that occur after metabolic reactions in PPs (curcumin, quercetin, and catechins) and their effect on GM composition that leads to improving overall gut health and helping to ameliorate metabolic disorders.

https://www.mdpi.com/2072-6643/13/1/206/pdf

Curcumin, Quercetin, Catechins and Metabolic Diseases: The Role of Gut Microbiota.

Quercetin (QCT) is a natural polyphenolic compound enriched in human food, mainly in vegetables, fruits and berries. QCT and its main derivatives, such as rhamnetin, rutin, hyperoside, etc., have been documented to possess many beneficial effects in the human body including their positive effects in the cardiovascular system. However, clinical implications of QCT and its derivatives are still rare. In the current paper we provide a complex picture of the most recent knowledge on the effects of QCT and its derivatives in different types of cardiac injury, mainly in ischemia-reperfusion (I/R) injury of the heart, but also in other pathologies such as anthracycline-induced cardiotoxicity or oxidative stress-induced cardiac injury, documented in in vitro and ex vivo, as well as in in vivo experimental models of cardiac injury. Moreover, we focus on cardiac effects of QCT in presence of metabolic comorbidities in addition to cardiovascular disease (CVD). Finally, we provide a short summary of clinical studies focused on cardiac effects of QCT. In general, it seems that QCT and its metabolites exert strong cardioprotective effects in a wide range of experimental models of cardiac injury, likely via their antioxidant, anti-inflammatory and molecular pathways-modulating properties; however, ageing and presence of lifestyle-related comorbidities may confound their beneficial effects in heart disease. On the other hand, due to very limited number of clinical trials focused on cardiac effects of QCT and its derivatives, clinical data are inconclusive. Thus, additional well-designed human studies including a high enough number of patients testing different concentrations of QCT are needed to reveal real therapeutic potential of QCT in CVD. Finally, several negative or controversial effects of QCT in the heart have been reported, and this should be also taken into consideration in QCT-based approaches aimed to treat CVD in humans.

https://www.mdpi.com/1422-0067/21/5/1585/pdf

Potential Implications of Quercetin and its Derivatives in Cardioprotection.

As the most widely consumed fruit in the world, apple (Malus domestica Borkh.) fruits provide a high level of phenolics and have many beneficial effects on human health. The composition and content of phenolic compounds in natural apples differs according to the tissue types and cultivar varieties. The bioavailability of apple-derived phenolics, depending on the absorption and metabolism of phenolics during digestion, is the key determinant of their positive biological effects. Meanwhile, various processing technologies affect the composition and content of phenolic compounds in apple products, further affecting the bioavailability of apple phenolics. This review summarizes current understanding on the compositions, distribution, absorption, and metabolism of phenolic compounds in apple and their stability when subjected to common technologies during processing. We intend to provide an updated overview on apple phenolics and also suggest some perspectives for future research of apple phenolics.

Systematic Review of Phenolic Compounds in Apple Fruits: Compositions, Distribution, Absorption, Metabolism, and Processing Stability.

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.

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Health Benefits of Quercetin in Age-Related Diseases

Quercetin, one of the most taken flavonoid with diet, belongs to the family of flavonols in which kaempferol and myricetin are also found. Quercetin occurs as a glycoside (with linked sugars) or as an aglycone (without linked sugars). Although quercetin has many different forms in nature, the form found in plants is quercetin-3-O-glucoside, which generally functions as a pigment that gives color to a multitude of fruits and vegetables. The recent literature has been reviewed using PubMed, Science Direct, and Embase databases. In this article, we reviewed quercetin with respect to chemical properties, absorption mechanism, metabolism, bioavailability, food sources, bioactivities, and possible health-promoting mechanisms. Quercetin is known as an antioxidant, anti-inflammatory, cardioprotective, and anti-obesity compound. It is thought to be beneficial against cardiovascular diseases, cancer, diabetes, neurological diseases, obesity, allergy asthma, and atopic diseases. Further clinical studies with large sample sizes are needed to determine the appropriate dose and form of quercetin for preventing diseases.

Hande Gül Ulusoy

Papers

A minireview of quercetin: from its metabolism to possible mechanisms of its biological activities