Quercetin

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Keywords: quercetin, bees, propolis, resin, PI3K, Flavonoids, phytochemical compounds, quercetin, inflammation, immune function, dietary sources, metabolism, SARS-Cov-2, COVID-19, vitamin C, quercetin, flavonoids, antiviral, Coronavirus, immunonutrition, Quercetin, Allergy, Asthma, Senolytic, Senescent cells, Dasatinib, Quercetin, Ageing, Lifespan, COVID-19, corona virus, aging, senescence, senolytic drug therapy, prevention, viral replication, drug repurposing, antibiotic, Azithromycin, Hydroxy-chloroquine, Rapamycin, Doxycycline, Quercetin, quercetin, lipid profile, protein metabolism, metabolic fitness, boxing, anti-tyrosinase, antioxidant, niosomes, photostability, transderma

Summary of Abstracts:

Phenolic Fractions from Vaccinium vitis-idaea L. and Their Antioxidant and Anticancer Activities Assessment: [ Botanical leaves can provide significant bioactives. ] Lingonberry leaves and fruits are associated with a range of potential bioactivities related to their phenolic content and composition, but the identification of major biological activity markers remains limited. Fractions of lingonberry leaves and fruits, obtained by the last fractionation step, proved to be the most active against tested cancer cell lines and possessed the greatest antioxidant activity. In this perspective, the predominant compounds of these fractions—polymeric and mainly A-type dimeric proanthocyanidins—also quercetin can be considered to be anticancer and antioxidant activity markers of lingonberries.

Flavonol Glycosides: In Vitro Inhibition of DPPIV, Aldose Reductase and Combating Oxidative Stress are Potential Mechanisms for Mediating the Antidiabetic Activity of Cleome droserifolia: [ Compounds may help to reduce diabetes. ] Diabetes is a major health problem that is associated with high risk of various complications. Medicinal plants hold great promise against diabetes. The traditional use of Cleome droserifolia as an antidiabetic agent was correlated to its flavonol glycosides content. Moreover, these compounds showed high potential in preventing diabetes complications through inhibiting aldose reductase enzyme and combating oxidative stress. Both isorhamnetin glycoside derivatives (2, 3) exhibited the highest activities in aldose reductase inhibition and compound 2 was even more potent than standard quercetin. Additionally, these flavonols exerted excellent antioxidant capacities through (DPPH) and ferric reducing antioxidant (FRAP) assays.

Propolis Suppresses UV-Induced Photoaging in Human Skin through Directly Targeting Phosphoinositide 3-Kinase: [ Propolis shows anti-skin-aging effects through direct inhibition of PI3K activity. The PI3K/AKT/mTOR pathway is an intracellular signaling pathway important in regulating the cell cycle. Therefore, it is directly related to cellular quiescence, proliferation, cancer, and longevity. PI3K activation phosphorylates and activates AKT, localizing it in the plasma membrane. ] Propolis is a resinous substance generated by bees using materials from various plant sources. It has been known to exhibit diverse bioactivities including anti-oxidative, anti-microbial, anti-inflammatory, and anti-cancer effects. Propolis suppressed UV induced matrix metalloproteinase (MMP) 1 production in human dermal fibroblasts. The content of active compounds was quantified, and among the compounds identified from the propolis extract, caffeic acid phenethyl ester, quercetin, and apigenin were shown to attenuate PI3K activity. These results demonstrate that propolis shows anti-skin-aging effects through direct inhibition of PI3K activity.

Mechanistic Aspects and Therapeutic Potential of Quercetin against COVID-19-Associated Acute Kidney Injury: [ There is evidence of the anti-coronavirus activities of this compound, including against the target SARS CoV 2 3CLpro. ] 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.

Neuroprotective Effects of Quercetin in Pediatric Neurological Diseases: [ The neuroprotective effects of quercetin against oxidative stress applies to anti-cancer, anti-inflammatory, anti-viral, anti-obesity and anti-microbial, and appears to be a suitable adjuvant for therapy against pediatric neurological diseases. ] Oxidative stress is a crucial event underlying several pediatric neurological diseases, such as the central nervous system (CNS) tumors, autism spectrum disorder (ASD) and attention-deficit/hyperactivity disorder (ADHD). Neuroprotective therapy with natural compounds used as antioxidants has the potential to delay, ameliorate or prevent several pediatric neurological diseases. The neuroprotective effects of quercetin against oxidative stress can also be applied in the management of several neurodegenerative disorders with effects such as anti-cancer, anti-inflammatory, anti-viral, anti-obesity and anti-microbial. Therefore, quercetin appears to be a suitable adjuvant for therapy against pediatric neurological diseases.

A Novel Promising Frontier for Human Health: The Beneficial Effects of Nutraceuticals in Cardiovascular Diseases: [ A better way to contain the onset of CVDs remains prevention by use of nutraceuticals. ] Cardiovascular diseases (CVDs) such as hypertension, atherosclerosis, myocardial infarction, and diabetes are a significant public health problem worldwide. Although several novel pharmacological treatments to reduce the progression of CVDs have been discovered during the last 20 years, the better way to contain the onset of CVDs remains prevention. In this regard, nutraceuticals seem to own a great potential in maintaining human health, exerting important protective cardiovascular effects. In the last years, there has been increased focus on identifying natural compounds with cardiovascular health-promoting effects and also to characterize the molecular mechanisms involved. Although many review articles have focused on the individual natural compound impact on cardiovascular diseases, the aim of this manuscript was to examine the role of the most studied nutraceuticals, such as resveratrol, cocoa, quercetin, curcumin, brassica, berberine and Spirulina platensis, on different CVDs.

Important Flavonoids and Their Role as a Therapeutic Agent: [ Flavonoids possess a number of medicinal benefits, including anticancer, antioxidant, anti-inflammatory, and antiviral properties. They also have neuroprotective and cardio-protective effects. ] Flavonoids are phytochemical compounds present in many plants, fruits, vegetables, and leaves, with potential applications in medicinal chemistry. Flavonoids possess a number of medicinal benefits, including anticancer, antioxidant, anti-inflammatory, and antiviral properties. They also have neuroprotective and cardio-protective effects. These biological activities depend upon the type of flavonoid, its (possible) mode of action, and its bioavailability. These cost-effective medicinal components have significant biological activities, and their effectiveness has been proved for a variety of diseases. The most recent work is focused on their isolation, synthesis of their analogs, and their effects on human health using a variety of techniques and animal models. Thousands of flavonoids have been successfully isolated, and this number increases steadily.

Cell Clearing Systems as Targets of Polyphenols in Viral Infections: Potential Implications for COVID-19 Pathogenesis: The pharmacological properties of natural compounds have gained increasing attention in the field of alternative and adjunct therapeutic approaches to several diseases. In particular, several naturally-occurring herbal compounds (mostly polyphenols) are reported to produce widespread antiviral, anti-inflammatory, and anti-oxidant effects while acting as autophagy and (immuno)-proteasome modulators. This article attempts to bridge the perturbation of autophagy and proteasome pathways with the potentially beneficial effects of specific phytochemicals and flavonoids in viral infections, with a focus on the multisystem SARS CoV 2 infection.

Effects of Light-Emitting Diodes on the Accumulation of Phenolic Compounds and Glucosinolates in Brassica juncea Sprouts: [ White LED light is appropriate for glucosinolate accumulation and blue LED light is effective in increasing the production of phenolic compounds in B. juncea sprouts. ] Recent improvements in light-emitting diode (LED) technology afford an excellent opportunity to investigate the relationship between different light sources and plant metabolites. Accordingly, the goal of the present study was to determine the effect of different LED (white, blue, and red) treatments on the contents of glucosinolates. These findings indicate that white LED light is appropriate for glucosinolate accumulation, whereas blue LED light is effective in increasing the production of phenolic compounds in B. juncea sprouts.

New Oleoyl Hybrids of Natural Antioxidants: Synthesis and In Vitro Evaluation as Inducers of Apoptosis in Colorectal Cancer Cells: Nowadays, the beneficial role of a healthy lifestyle, particularly emphasizing the quality of foods and cancer management, is accepted worldwide. Polyphenols and oleic acid play a key role in this context, but are still scarcely used as anti-cancer agents due to their bio accessibility limits. Therefore, we aimed to synthesize a set of new oleoyl hybrids of quercetin, morin, pinocembrin, and catechin to overcome the low bioavailability of polyphenols, throughout a bio catalytic approach using pancreatic porcine lipase as a catalyst. We demonstrated convincing data about two novel polyphenol based hybrids displaying a highly selective anti cancer cytotoxicity and being superior compared to their reference/parental compounds.

Quercetin, Inflammation and Immunity: Quercetin is categorized as a flavonol, one of the six subclasses of flavonoid compounds. The name has been used since 1857, and is derived from quercetum (oak forest), after Quercus. It is a naturally occurring polar auxin transport inhibitor. Some animal models have shown that quercetin, a polyphenol derived from plants, has a wide range of biological actions including anti-carcinogenic, anti-inflammatory and antiviral activities; as well as attenuating lipid peroxidation, platelet aggregation and capillary permeability.

Therapeutic Potential of Quercetin: New Insights and Perspectives for Human Health: [ Nutritional flavonoids, as is the case of Que, are even more powerful antioxidants than vitamins C and E. ] Quercetin (Que) and its derivatives are naturally occurring phytochemicals with promising bioactive effects. The antidiabetic, anti-inflammatory, antioxidant, antimicrobial, anti Alzheimers, antiarthritic, cardiovascular, and wound-healing effects of Que have been extensively investigated, as well as its anticancer activity against different cancer cell lines has been recently reported. Que and its derivatives are found predominantly in the Western diet, and people might benefit from their protective effect just by taking them via diets or as a food supplement. Bioavailability related drug delivery systems of Que have also been markedly exploited, and Que nanoparticles appear as a promising platform to enhance their bioavailability. The anti inflammatory and antioxidant effects of Que are essential for its activity as oxidative, kinase, and cell cycle inhibitors, as well as for neuronal survival. Que apoptosis inducing effects are the key for its anticancer potential. There is an extraordinary attention to naturally occurring bioactive molecules, and Que is a great example of phenomenal therapeutic applications.

Quercetin and Vitamin C: An Experimental, Synergistic Therapy for the Prevention and Treatment of SARS-CoV-2 Related Disease (COVID-19): [ Vitamin C and quercetin work synergistically for both for prophylaxis in the treatment of COVID-19 patients as an adjunct to promising pharmacological agents such as Remdesivir or convalescent plasma. ] Quercetin is a well-known flavonoid whose antiviral properties have been investigated in numerous studies. There is evidence that vitamin C and quercetin co-administration exerts a synergistic antiviral action due to overlapping antiviral and immunomodulatory properties and the capacity of ascorbate to recycle quercetin, increasing its efficacy. vitamin C and quercetin both for prophylaxis in high-risk populations and for the treatment of COVID-19 patients as an adjunct to promising pharmacological agents such as Remdesivir or convalescent plasma.

Quercetin with the potential effect on allergic diseases: [ Quercetin may affect allergic diseases, such as allergic asthma, allergic rhinitis (AR), and atopic dermatitis (AD). ] Quercetin is a naturally occurring polyphenol flavonoid which is rich in antioxidants. It has anti allergic functions that are known for inhibiting histamine production and pro-inflammatory mediators. Quercetin can regulate the Th1 Th2 stability, and decrease the antigen-specific IgE antibody releasing by B cells. Quercetin has a main role in anti-inflammatory and immunomodulatory function which makes it proper for the management of different diseases. Since the effect of quercetin on allergic diseases has been widely studied, in the current article, we review the effect of quercetin on allergic diseases, such as allergic asthma, allergic rhinitis (AR), and atopic dermatitis (AD).

Antioxidant Activity of Quercetin: A Mechanistic Review: Flavones and flavonoids are known to have potent antioxidant activity due to intracellular free radical scavenging capacities. Flavonoids are found ubiquitously in plants as a member of polyphenolic compounds which share diverse chemical structure and properties. Quercetin is among the most efficient antioxidants of the flavonoids. The antioxidant property of quercetin has been highlighted in this review. These compounds have pivotal role in treatment of diabetes, cancers and some cardiovascular diseases.

Dasatinib and Quercetin: Short-Term Simultaneous Administration Improves Physical Capacity in Human: [ Quercetin resulted in remarkably outstanding improvement of physical endurance. ] It’s proven that senescent cells are the main source of intoxication for organism. Their mechanism of origin is still uncertain up to nowadays. We consider their origin through the prism of molecular genetic centriolar theory of aging. Results of Complete Blood Count (CBC), C-reactive protein and creatinine blood test performed on participants practically did not show any significant alterations. First SAT results taken a day prior to the administration of compounds showed that the systolic and diastolic blood pressure results of all participants were on the same level with just minor differences. Second SAT taken on the 21st day, showcased clear reduction of systolic blood pressure in groups D+Q and just slight reduction in D+P in comparison with unchanged results in the rest of 2 groups that administered quercetin along with placebo and placebo along with placebo. Significant reduction of Systolic Blood Pressure (SBP) was seen starting at 20 minutes and 10 minutes post-exercise respectively in the D+Q group (p<0.05), versus the rest of the groups. First group participants who orally administered once a day after meal 50 mg of dasatinib and 500 mg of quercetin during five days demonstrated the remarkably outstanding improvement of physical endurance. Senescent cells obviously are involved in the ageing process. It's becoming more clear why people normally age at the same rate. The intensity of aging and the amount of senescent cell are directly related. The more division of cells, the more senescent cells. This research also provides initial evidence that senolytics may alleviate physical dysfunction (in their case, not with practically healthy people, but with patients in IPF). We expected a reduction of senescent cells’ amount in the organism. In our opinion, it might cause a decrease in daily intoxication of tissues, organs, and body as a whole.

COVID 19 and chronological aging: senolytics and other anti-aging drugs for the treatment or prevention of corona virus infection: Question as to whether there is a functional association between COVID-19 infection and the process of chronological aging. Two host receptors have been proposed for COVID19. One is CD26 and the other is ACE 2 (angiotensin converting enzyme 2). Interestingly, both CD26 and the angiotensin system show associations with senescence. Similarly, two proposed therapeutics for the treatment of COVID 19 infection are Azithromycin and Quercetin, both drugs with significant senolytic activity. Therefore, we wish to speculate that the fight against COVID-19 disease should involve testing the hypothesis that senolytics and other anti-aging drugs may have a prominent role in preventing the transmission of the virus, as well as aid in its treatment.

Effects of Quercetin Supplementation on Lipid and Protein Metabolism after Classic Boxing Training: Conclusion: it can be concluded that quercetin plays an important role on lipid metabolism not protein.

Quercetin topical application, from conventional dosage forms to nanodosage forms: [ Quercetin is a promising drug candidate for topical applications as it possesses strong antioxidant. Due to poor solubility, Liquid Nano Capsules provide the best delivery. ] Skin is a multifunctional organ with activities in protection, metabolism and regulation. Skin is in a continuous exposure to oxidizing agents and inflammogens from the sun and from the contact with the environment. These agents may overload the skin auto-defense capacity. To strengthen skin defense mechanisms against oxidation and inflammation, supplementation of exogenous antioxidants is a promising strategy. Quercetin is a flavonoid with very pronounced effective antioxidant and antiinflammatory activities, and thus a candidate of first choice for such skin supplementation. However, due to its poor solubility, quercetin has limited skin penetration ability, and various formulation approaches were taken to increase its dermal penetration. The modified formulations enabled six-fold increase in quercetin-loaded amount and more than 5000 times increase in its apparent water solubility. Moreover, the formulation process did not require specific equipment and a higher yield compared to other nanoformulation. The preserved antioxidant activity on cells holds great promise for skin supplementation with this natural molecule. With extremely small size distribution (26 and 54 nm), a lipophilic character for a better affinity to skin lipids and a strong occlusive effect to skin tissue, LNC (Liquid Nano Capsules) as a carrier system could also hold a great interest for the dermal application of other poorly soluble molecules. LNC presents the triple benefit of increasing the apparent water solubility of quercetin, protecting it from degradation (Zvezdanovic et al., 2012) and enabling a higher occlusive effect on the skin.

Niosomal Nanocarriers for Enhanced Skin Delivery of Quercetin with Functions of Anti-Tyrosinase and Antioxidant: [ Quercetin niosomes had the advantages of sustained release and improved transdermal penetration. ] This study aimed to screen an effective flavonoid with promising whitening and antioxidant capacities, and design flavonoid loaded niosomes to improve its solubility, stability, and penetration. Niosomes remarkably improved the solubility and photostability of quercetin. Furthermore, compared to quercetin solution, quercetin niosomes had the advantages of sustained release and improved transdermal penetration, with skin retention 2.95 times higher than quercetin solution.

Quercetin, a Natural Flavonoid Interacts with DNA, Arrests Cell Cycle and Causes Tumor Regression by Activating Mitochondrial Pathway of Apoptosis: Naturally occurring compounds are considered as attractive candidates for cancer treatment and prevention. Quercetin and ellagic acid are naturally occurring flavonoids abundantly seen in several fruits and vegetables. Quercetin induced tumor regression in mice at a concentration 3-fold lower than ellagic acid. Importantly, administration of quercetin lead to ~5 fold increase in the life span in tumor bearing mice compared to that of untreated controls. Further, we found that quercetin interacts with DNA directly and could be one of the mechanisms for inducing apoptosis in both, cancer cell lines and tumor tissues by activating the intrinsic pathway. Thus, our data suggests that quercetin can be further explored for its potential to be used in cancer therapeutics and combination therapy.

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