Quercetin Overview

1) Conditions Studied

• Cardiovascular Diseases
• Allergies
• Inflammatory Disorders
• Diabetes
• Chronic Prostatitis
• Cancer
• Viral Infections

2) Efficacy in Treating Conditions

• Some studies suggest potential benefits in reducing inflammation and allergy symptoms, but more research is needed.
• Evidence for cardiovascular benefits, such as lowering blood pressure, is inconclusive.
• The impact on cancer and viral infections is not well-established and requires further clinical studies.

3) Health Benefits

• Antioxidant properties that may protect cells from free radical damage.
• Anti-inflammatory effects that could help with conditions like arthritis.
• Potential to enhance endurance and athletic performance by increasing mitochondrial biogenesis.

4) Downsides

• May interact with various medications, such as antibiotics and blood thinners.
• Possible side effects include headaches and tingling in the arms and legs.
• High doses can potentially damage the kidneys.

5) Impact on Genetic Variations

• Individuals with certain genetic profiles may metabolize quercetin differently, affecting its efficacy and safety.
• Research is ongoing, and there is currently no conclusive evidence that quercetin is particularly beneficial or harmful for specific genetic variations.

Quercetin Research Summary

Quercetin's Biological Effects

Quercetin, a widely studied flavonoid, exhibits various biological effects. In BV-2 microglial cells, it reduces nitric oxide production and iNOS gene transcription, influenced by LPS and IFN-gamma. Quercetin's anti-inflammatory properties are also evident in its ability to downregulate several cellular signaling pathways, including IKK, NF-kappaB, AP-1, STAT1, and IRF-1. Additionally, quercetin stimulates the expression of heme oxygenase-1, contributing to the inhibition of iNOS.

Quercetin and Neuroprotection

Quercetin has therapeutic potential for neurodegenerative diseases by reducing inflammation-related neuronal damage. Its neuroprotective abilities extend to the inhibition of aromatase and CYP19 activity, potentially impacting estrogen synthesis and offering insights into the structure-activity relationships of these compounds in human cells.

Quercetin's Bioavailability and Therapeutic Effects

The bioavailability of quercetin is enhanced through alpha-oligoglucosylation, as seen with enzymatically modified isoquercitrin (EMIQ), which exhibits higher absorption efficiency compared to other forms of quercetin glucosides. Quercetin's ability to cross the blood-brain barrier and its effects on brain cancer cells, such as decreasing cell proliferation and increasing apoptosis, highlight its potential as a therapeutic agent.

Quercetin and Physical Performance

In the context of endurance exercise performance under heat stress, quercetin does not appear to enhance performance, despite its known health benefits. However, it may influence cognitive function and memory in normal mice by suppressing the expression of proteins crucial for hippocampal function.

Quercetin and Cardiovascular Health

Quercetin shows cardiovascular benefits, as demonstrated in studies with LDL receptor-deficient mice. Mulberry leaves, particularly due to the presence of quercetin 3-(6-malonylglucoside) (Q3MG), can reduce atherosclerotic lesion development by increasing LDL resistance to oxidative stress.

Quercetin and Reproductive Health

In rat models, quercetin demonstrates protective effects against damage to testes caused by toxins like TCDD, improving antioxidant levels and mitigating adverse effects on sperm quality and testosterone levels.

Quercetin and Heat Acclimation

Quercetin's role in inhibiting the heat shock response suggests it can delay or prevent the body from properly adapting to high temperatures, impacting both cellular and systemic adaptations to heat stress.

Quercetin and Mitochondrial Biogenesis

Quercetin supplementation may boost physical performance without exercise training by enhancing mitochondrial biogenesis, as indicated by increased levels of PGC-1alpha, SIRT1, mitochondrial DNA, and cytochrome c in muscle and brain tissue.

Quercetin and Inflammation

Studies also indicate that quercetin can reduce the expression of proinflammatory genes in activated glial cells, potentially offering therapeutic benefits for conditions like Parkinson's disease where neuroinflammation leads to neuronal death.

Quercetin in Diet and Pharmacology

Quercetin's presence in dietary sources such as onions and its antioxidant properties are recognized, but its impact on the absorption and metabolism of drugs and activation of potential carcinogens in the body needs to be considered when consuming flavonoid-rich supplements or foods.

References:

1. Inhibition of iNOS gene expression by quercetin is mediated by the inhibition of IkappaB kinase, nuclear factor-kappa B and STAT1, and depends on heme oxygenase-1 induction in mouse BV-2 microglia
2. alpha-Oligoglucosylation of a sugar moiety enhances the bioavailability of quercetin glucosides in humans
3. Anxiolytic natural and synthetic flavonoid ligands of the central benzodiazepine receptor have no effect on memory tasks in rats
4. No effect of nutritional adenosine receptor antagonists on exercise performance in the heat
5. Protein synthesis and memory: a review
6. [Quercetin permeability across blood-brain barrier and its effect on the viability of U251 cells]
7. Mulberry (Morus alba L.) leaves and their major flavonol quercetin 3-(6-malonylglucoside) attenuate atherosclerotic lesion development in LDL receptor-deficient mice
8. Quercetin prevents 2,3,7,8-tetrachlorodibenzo-p-dioxin-induced testicular damage in rats
9. Thermotolerance and heat acclimation may share a common mechanism in humans
10. Quercetin increases brain and muscle mitochondrial biogenesis and exercise tolerance
11. Dietary polyphenols protect dopamine neurons from oxidative insults and apoptosis: investigations in primary rat mesencephalic cultures
12. Inhibition of the activation of heat shock factor in vivo and in vitro by flavonoids
13. Flavonoid permeability across an in situ model of the blood-brain barrier
14. Pharmacophore model of the quercetin binding site of the SIRT6 protein
15. Resveratrol and quercetin, two natural polyphenols, reduce apoptotic neuronal cell death induced by neuroinflammation
16. [Study of flavanoids extracted from onion on the blood-brain barrier permeation and neuroprotective effects]
17. Astra Award Lecture. Adenosine, adenosine receptors and the actions of caffeine
18. Modulation of suppressive activity of lipopolysaccharide-induced nitric oxide production by glycosidation of flavonoids
19. Fractionation of polyphenol-enriched apple juice extracts to identify constituents with cancer chemopreventive potential
20. Flavonoid transport across RBE4 cells: A blood-brain barrier model
21. Characterization of the thermotolerant cell. I. Effects on protein synthesis activity and the regulation of heat-shock protein 70 expression
22. Effects of 2 adenosine antagonists, quercetin and caffeine, on vigilance and mood
23. Direct HPLC analysis of quercetin and trans-resveratrol in red wine, grape, and winemaking byproducts
24. Effect of quercetin supplementation on repeated-sprint performance, xanthine oxidase activity, and inflammation
25. Physiologically relevant increase in temperature causes an increase in intestinal epithelial tight junction permeability
26. Protective effects of quercetin and chrysin against 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) induced oxidative stress, body wasting and altered cytokine productions in rats
27. CREB is a regulatory target for the protein kinase Akt/PKB
28. Cellular and molecular mechanisms of heat stress-induced up-regulation of occludin protein expression: regulatory role of heat shock factor-1
29. Tissue distribution of quercetin in rats and pigs
30. Pharmacokinetics and bioavailability of quercetin glycosides in humans
31. Sulfotransferase inhibition: potential impact of diet and environmental chemicals on steroid metabolism and drug detoxification
32. CREB, synapses and memory disorders: past progress and future challenges
33. Daily quercetin supplementation dose-dependently increases plasma quercetin concentrations in healthy humans
34. Determination of quercetin and kaempferol in human urine after orally administrated tablet of ginkgo biloba extract by HPLC
35. The dietary flavonoid quercetin increases VO(2max) and endurance capacity
36. Quantification of quercetin glycosides in 6 onion cultivars and comparisons of hydrolysis-HPLC and spectrophotometric methods in measuring total quercetin concentrations
37. Phytoestrogens and their low dose combinations inhibit mRNA expression and activity of aromatase in human granulosa-luteal cells
38. Effects of naturally occurring compounds on fibril formation and oxidative stress of beta-amyloid
39. Protective effects of quercetin on testicular torsion/detorsion-induced ischaemia-reperfusion injury in rats
40. Dose translation from animal to human studies revisited
41. Inhibition of human liver and duodenum sulfotransferases by drugs and dietary chemicals: a review of the literature
42. Translational control of long-lasting synaptic plasticity and memory
43. Dietary antioxidant supplementation combined with quercetin improves cycling time trial performance
44. Microwave-assisted extraction of rutin and quercetin from the stalks of Euonymus alatus (Thunb.) Sieb
45. Influence of the metabolic profile on the in vivo antioxidant activity of quercetin under a low dosage oral regimen in rats
46. Synthesis and characterization of SIRT6 protein coated magnetic beads: identification of a novel inhibitor of SIRT6 deacetylase from medicinal plant extracts
47. Ameliorating effects of quercetin and chrysin on 2,3,7,8-tetrachlorodibenzo- p-dioxin-induced nephrotoxicity in rats
48. CYP1A1 and CYP3A4 modulation by dietary flavonoids in human intestinal Caco-2 cells
49. Effect of a conjugated quercetin metabolite, quercetin 3-glucuronide, on lipid hydroperoxide-dependent formation of reactive oxygen species in differentiated PC-12 cells
50. Quercetin impairs learning and memory in normal mice via suppression of hippocampal phosphorylated cyclic AMP response element-binding protein expression
51. Comparison of quercetin pharmacokinetics following oral supplementation in humans
52. Flavonoids in vegetable foods commonly consumed in Brazil and estimated ingestion by the Brazilian population
53. Induction and inhibition of aromatase (CYP19) activity by natural and synthetic flavonoid compounds in H295R human adrenocortical carcinoma cells
54. Protective effects of flavonoids on the cytotoxicity of linoleic acid hydroperoxide toward rat pheochromocytoma PC12 cells
55. Cell death and neuronal arborization upon quercetin treatment in rat neurons
56. Saponins in yerba mate tea ( Ilex paraguariensis A. St.-Hil) and quercetin synergistically inhibit iNOS and COX-2 in lipopolysaccharide-induced macrophages through NFkappaB pathways
57. Simultaneous determination of quercetin and its glycosides from the leaves of Nelumbo nucifera by reversed-phase high-performance liquid chromatography
58. Interactions of flavonoids and other phytochemicals with adenosine receptors
59. Protective effects of heat shock protein70 induced by geranylgeranylacetone in atrophic gastritis in rats
60. Inhibitory constituents of Euonymus alatus leaves and twigs on nitric oxide production in BV2 microglia cells
61. Non-selective inhibition of mammalian protein kinases by flavinoids in vitro
62. Evaluation of androgenic activity of allium cepa on spermatogenesis in the rat

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