A role for quercetin in coronavirus disease 2019 (COVID‐19)

Derosa, Giuseppe; Maffioli, Pamela; D’Angelo, Angela; Pierro, Francesco Di

doi:10.1002/ptr.6887

Cited by 232 publications

(207 citation statements)

References 46 publications

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“…Anti-inflammatory, antimicrobial and antioxidant activities, antiviral capacity, prevent digestion issues, reduce the risk of chronic diseases [45][46][47][48][49][50][51][52][53] Inhibition of viral replication Disruption of viral spike protein Inhibition of SARS-CoV-2 protease [26,[54][55][56][57][58][59][60][61][62][63][64][65][66][67][68][69] Bioactive lipids comprise several endogenous molecules affecting a wide array of biological processes. Typical examples of lipids include omega-3 fatty acids and their metabolic products, carotenoids, phytosterols, and fat-soluble vitamins, phenolic lipids, and acylglycerol derivatives.…”

Section: In Vitro Clinicalmentioning

confidence: 99%

Food Ingredients and Active Compounds against the Coronavirus Disease (COVID-19) Pandemic: A Comprehensive Review

Galanakis

Aldawoud

Rizou³

et al. 2020

Foods

205

127

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As media reports have noted, the COVID-19 pandemic has accelerated market mainstreaming of immune-boosting food bioactives, supplements, and nutraceuticals. However, most studies reporting on the potential of bioactives against COVID-19 transmission have been uploaded as preprints with little opportunity to revise content for benefit and impact. The current review discusses current best evidence and information underpinning the role of food ingredients and bioactive compounds in supporting immune functions in humans and animals, specifically in the prevention and treatment of COVID-19 disease. Up to now, some evidence from randomized population and clinical trials has suggested that vitamin D levels may be linked to COVID-19 transmission and severity. Numerous theoretical studies have pointed to polyphenols and particularly flavonoids as potential inhibitors of SARS-CoV-2 infection. There is also inconclusive evidence to support the future use of β-glucan to address COVID-19 due in part to variability in immune response arising from heterogeneity in polysaccharide branch and chain length for different sources and the absence of a standardized extraction method. To confirm the promising outcomes and hypotheses for bioactive compounds, more randomized and controlled clinical studies are needed. The results of such studies would have a profound effect on the prospects of food supplements and nutraceuticals as potential prophylaxis against COVID-19 and serve to help consumers to protect themselves during the post-lockdown recovery era.

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Section: In Vitro Clinicalmentioning

confidence: 99%

Food Ingredients and Active Compounds against the Coronavirus Disease (COVID-19) Pandemic: A Comprehensive Review

Galanakis

Aldawoud

Rizou³

et al. 2020

Foods

205

127

View full text Add to dashboard Cite

show abstract

“…Strong experimental evidence validated this theoretical hypothesis [ 71 ]. Concerning the SARS-CoV-2 papain-like protease (PLpro), quercetin did not result as a good binder in a theoretical study [ 72 ]. Conversely, a computational investigation evidenced it as able to bind at S protein: ACE2 receptor interface [ 73 ].…”

Section: Resultsmentioning

confidence: 99%

Current Updates on Naturally Occurring Compounds Recognizing SARS-CoV-2 Druggable Targets

et al. 2021

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The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has been identified in China as the etiologic agent of the recent COVID-19 pandemic outbreak. Due to its high transmissibility, this virus quickly spread throughout the world, causing considerable health issues. The scientific community exerted noteworthy efforts to obtain therapeutic solutions for COVID-19, and new scientific networks were constituted. No certified drugs to efficiently inhibit the virus were identified, and the development of de-novo medicines requires approximately ten years of research. Therefore, the repurposing of natural products could be an effective strategy to handle SARS-CoV-2 infection. This review aims to update on current status of the natural occurring compounds recognizing SARS-CoV-2 druggable targets. Among the clinical trials actually recruited, some natural compounds are ongoing to examine their potential role to prevent and to treat the COVID-19 infection. Many natural scaffolds, including alkaloids, terpenes, flavonoids, and benzoquinones, were investigated by in-silico, in-vitro, and in-vivo approaches. Despite the large data set obtained by a computational approach, experimental evidences in most cases are not available. To fill this gap, further efforts to validate these results are required. We believe that an accurate investigation of naturally occurring compounds may provide insights for the potential treatment of COVID-19 patients.

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“…ORF1a encodes two cysteine proteases, a papain-like protease (PLpro) and a 3 C-like protease (3CLpro). Scientists have provided evidences that main protease (3CLpro) is one of the good targets to discover new antiviral agents before vaccines are available (Derosa, Maffioli, D'Angelo, & Di Pierro, 2020). To explore more potent leading compound against SARS-Cov-2 by targeting key molecule in RNA synthesis of the virus, recombinant SARS-CoV-2 3CLpro was firstly expressed and purified from Escherichia coli (Xue et al, 2007;Yang et al, 2003).…”

Section: Crude Polysaccharide 375 Was a Potent Inhibitor Of Sars-cov-mentioning

confidence: 99%

Structural characterization of cocktail-like targeting polysaccharides fromEcklonia kuromeOkam and their anti-SARS-CoV-2 activitiesinvitro

Ding

Zhang

Chen

et al. 2021

Preprint

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Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the etiological agent responsible for the worldwide coronavirus disease 2019 (COVID-19) outbreak. Investigation has confirmed that polysaccharide heparan sulfate can bind to the spike protein and block SARS-CoV-2 infection. Theoretically, similar structure of nature polysaccharides may also have the impact on the virus. Indeed, some marine polysaccharide has been reported to inhibit SARS-Cov-2 infection in vitro, however the convinced targets and mechanism are still vague. By high throughput screening to target 3CLpro enzyme, a key enzyme that plays a pivotal role in the viral replication and transcription using nature polysaccharides library, we discover the mixture polysaccharide 375 from seaweed Ecklonia kurome Okam completely block 3Clpro enzymatic activity (IC50, 0.48 µM). Further, the homogeneous polysaccharide 37502 from the 375 may bind to 3CLpro molecule well (kD value : 4.23 × 10−6). Very interestingly, 37502 also can potently disturb spike protein binding to ACE2 receptor (EC50, 2.01 µM). Importantly, polysaccharide 375 shows good anti-SARS-CoV-2 infection activity in cell culture with EC50 values of 27 nM (99.9% inhibiting rate at the concentration of 20 µg/mL), low toxicity (LD50: 136 mg/Kg on mice). By DEAE ion-exchange chromatography, 37501, 37502 and 37503 polysaccharides are purified from native 375. Bioactivity test show that 37501 and 37503 may impede SARS-Cov-2 infection and virus replication, however their individual impact on the virus is significantly less that of 375. Surprisingly, polysaccharide 37502 has no inhibition effect on SARS-Cov-2. The structure study based on monosaccharide composition, methylation, NMR spectrum analysis suggest that 375 contains guluronic acid, mannuronic acid, mannose, rhamnose, glucouronic acid, galacturonic acid, glucose, galactose, xylose and fucose with ratio of 1.86 : 9.56 : 6.81 : 1.69 : 1.00 : 1.75 : 1.19 : 11.06 : 4.31 : 23.06. However, polysaccharide 37502 is an aginate which composed of mannuronic acid (89.3 %) and guluronic acid (10.7 %), with the molecular weight (Mw) of 27.9 kDa. These results imply that mixture polysaccharides 375 works better than the individual polysaccharide on SARS-Cov-2 may be the cocktail-like polysaccharide synergistic function through targeting multiple key molecules implicated in the virus infection and replication. The results also suggest that 375 may be a potential drug candidate against SARS-CoV-2.

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A role for quercetin in coronavirus disease 2019 (COVID‐19)

Cited by 232 publications

References 46 publications

Food Ingredients and Active Compounds against the Coronavirus Disease (COVID-19) Pandemic: A Comprehensive Review

Food Ingredients and Active Compounds against the Coronavirus Disease (COVID-19) Pandemic: A Comprehensive Review

Current Updates on Naturally Occurring Compounds Recognizing SARS-CoV-2 Druggable Targets

Structural characterization of cocktail-like targeting polysaccharides fromEcklonia kuromeOkam and their anti-SARS-CoV-2 activitiesinvitro

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