Quercetin, a natural polyphenolic flavonoid substance present in a variety of food plants, has been shown in vitro and in animal studies to have widespread health and performance benefits resulting from a combination of biological properties, including antioxidant and anti-inflammatory activity, as well as the ability to increase mitochondrial biogenesis. Little is known about these effects in humans, however, especially with respect to exercise performance. The authors determined whether quercetin ingestion would enhance maximal aerobic capacity and delay fatigue during prolonged exercise in healthy but untrained participants. Twelve volunteers were randomly assigned to 1 of 2 treatments: (a) 500 mg of quercetin twice daily dissolved in vitamin-enriched Tang or (b) a nondistinguishable placebo (Tang). Baseline VO2max and bike-ride times to fatigue were established. Treatments were administered for a period of 7 days using a randomized, double-blind, placebo-controlled, crossover study design. After treatment both VO2max and ride time to fatigue were determined. Seven days of quercetin feedings were associated with a modest increase in VO2max (3.9% vs.

PURPOSE:: To determine the influence of 2-weeks quercetin (Q) (1000 mg/day) compared to placebo (P) supplementation on exercise performance and skeletal muscle mitochondrial biogenesis in untrained, young adult males (N=26, age 20.2+/-0.4 y, VO2max 46.3+/-1.2 ml.kg.min). METHODS:: Utilizing a randomized, crossover design with a 2-week washout period, subjects provided blood and muscle biopsy samples pre- and post-supplementation periods, and were given 12-minute time trials on 15% graded treadmills following 60-min moderate exercise pre-loads at 60% VO2max. RESULTS:: Plasma quercetin levels rose significantly in Q vs. P during the 2-week supplementation period (interaction P-value<0.001). During the 12-minute trial, the net change in distance achieved was significantly greater during Q (2.9%) compared to P (-1.2%) (29.5+/-11.5 vs. -11.9+/-16.0 m, respectively, P=0.038). Skeletal muscle mRNA expression tended to increase (range of 16% to 25%) during Q vs. P for SIRT1 (interaction effect, P=0.152), PGC-1alpha (P=0.192), cytochrome C oxidase (P=0.081), and citrate synthase (P=0.166).

The natural compounds genistein (G), quercetin (Q), and resveratrol (R) have been reported to each exhibit anti-adipogenic activities in adipocytes and antiproliferative and pro-apoptotic activities in several cell types. We studied the combined effects of G, Q, and R on adipogenesis and apoptosis in primary human adipocytes (HAs) and 3T3-L1 murine adipocyte (MAs). Combined treatment with 6.25 microM G, 12.5 microM Q, and 12.5 microM R during the 14-day differentiation period caused an enhanced inhibition of lipid accumulation in maturing HAs that was greater than the responses to individual compounds and to the calculated additive response. Glycerol 3-phosphate dehydrogenase activity, a marker of late adipocyte differentiation, was decreased markedly in HAs treated with the combination of G+Q+R. In addition, combined treatment with 50 microM G, 100 microM Q, and 100 microM R for 3 days decreased cell viability and induced apoptosis in early- and mid- phase maturing and lipid-filled mature HAs. In contrast, no compound alone induced apoptosis. Oil Red O stain and Hoechst 33342 stain were performed to confirm the effects on lipid accumulation and apoptosis, respectively.

Glioma is the most frequent and malignant primary human brain tumor with dismal prognosis despite multimodal therapy. Resveratrol and quercetin, two structurally related and naturally occurring polyphenols, are proposed to have anticancer effects. We report here that resveratrol and quercetin decreased the cell number in four glioma cell lines but not in rat astrocytes. Low doses of resveratrol (10 microM) or quercetin (25 microM) separately had no effect on apoptosis induction, but had a strong effect on caspase 3/7 activation when administered together. Western blot analyses showed that resveratrol (10 microM) and quercetin (25 microM) caused a reduction in phosphorylation of Akt, but this reduction was not sufficient by itself to mediate the effects of these polyphenols. Most important, resveratrol and quercetin chronically administered presented a strong synergism in inducing senescence-like growth arrest. These results suggest that the combination of polyphenols can potentialize their antitumoral activity, thereby reducing the therapeutic concentration needed for glioma treatment

Prostate cancer (CaP) is a significant cause of death in American men. While men residing in Asia show a lower incidence of hormone-refractory prostate cancer (HRPC) compared to Caucasian males, Asian men who move to and live in the United States and adopt a western lifestyle have HRPC rates indistinguishable from Caucasian males. These findings suggest that Asian diets contain ingredients that might protect against the development of HRPC. The identity and mechanisms of such HRPC protective agents remain to be elucidated. An Asian diet may confer protection against HRPC owing to functional synergy between bioactive dietary agents, thus broadening the chemopreventive index, with increased distinct anticancer properties and decreased untoward effects. Here, whether or not a combination of epigallocatechin gallate (EGCG), genistein and quercetin, phytochemicals present in a traditional Asian diet, might exert synergy in controlling proliferation and gene expression was investigated in CWR22Rv1 CaP cells, an in vitro model mimicking CaP transition from AD (androgen dependence) to HRPC.

Athens, Ga. – The antioxidant quercetin is increasingly being marketed as a supplement that boosts athletic performance, but a new University of Georgia study finds that it is no better than a placebo.

Professor Kirk Cureton, head of the department of kinesiology in the UGA College of Education, and his colleagues tested quercetin in a double-blind, placebo-controlled study that assessed a variety of measures, including the ability of muscles to synthesize energy, cycling performance, perceived exertion and strength loss following exercise.

The researchers, whose results appear in the early online edition of the Journal of Applied Physiology, found that quercetin did not improve athletic performance in any of the measures they examined.“We did not see any performance enhancing effect of quercetin,” Cureton said. “To a certain extent that was disappointing because our hypothesis, based on previous studies in mice, was that we would see positive effects. But our findings are important because they suggest that results from the animal studies shouldn’t be generalized to humans.”

Loss of synapses has been correlated with dementia in Alzheimer's disease (AD) as an early event during the disease progression. Hence, synaptogenesis and neurogenesis in adulthood could serve as a therapeutic target for the prevention and treatment of AD. Recently, we have demonstrated enhanced hippocampal neurogenesis by oral administration of Ginkgo biloba extract (EGb 761) to a mouse model of AD. This study aims to identify the constituents that contribute to EGb 761-induced neurogenesis. Among the constituents tested, bilobalide and quercetin significantly increased cell proliferation in the hippocampal neurons in a dose-dependent manner. Bilobalide and quercetin also enhanced phosphorylation of cyclic-AMP Response Element Binding Protein (CREB) in these cells, and elevated the levels of pCREB and, brain-derived neurotrophic factor in mice brain. Immunofluorescence staining of synaptic markers shows remarkable dendritic processes in hippocampal neurons treated with either quercetin or bilobalide. Furthermore, both constituents restored amyloid-beta oligomers (also known as ADDL)-induced synaptic loss and phosphorylation of CREB.

For the purposes of inhibiting ACE and reducing cytokines, the following foods and compounds seem to be the best choices:

• Green tea (ACE inhibitor, reduces cytokines)
• Black tea (ACE inhibitor, reduces cytokines)
• Quercetin (possible ACE inhibitor, reduces cytokines)
• Pomegranate juice (ACE inhibitor)
• Red wine (ACE inhibitor)
• Turmeric (reduces cytokines)
• Black pepper (reduces cytokines)
• Raw crushed garlic (reduces cytokines)
• Red palm oil (reduces cytokines)
• Vitamin E (reduces cytokines)
• Coconut oil (reduces cytokines)

The following foods, while beneficial in many other ways, may not be a good idea in terms of reducing cytokine levels:

• Olive oil (may increase cytokines)
• Fish oil (may increase cytokines)
• Chocolate (ACE inhibitor, increases cytokines)

In addition, it seems that vitamin D3 could be on either list, depending on the dosage. Average blood levels of vitamin D may be worse than very low or high levels.

Exercise stress is associated with increased risk for upper respiratory tract infection. We have shown that exercise stress can increase susceptibility to infection. Quercetin, a flavonoid present in a wide variety of fruits and vegetables, has been reported to inhibit infectivity and replication of a broad spectrum of viruses and may offset the increase in susceptibility to infection associated with stressful exercise. This study examined the effects of quercetin feedings on susceptibility to the influenza virus A/Puerto Rico/8/34 (H1N1) following stressful exercise. Mice were randomly assigned to one of four treatment groups: exercise-placebo, exercise-quercetin, control-placebo, or control-quercetin. Exercise consisted of a run to fatigue (approximately 140 min) on a treadmill for 3 consecutive days. Quercetin (12.5 mg/kg) was administered via gavage for 7 days before viral challenge. At 30 min after the last bout of exercise or rest, mice (n=23-30) were intranasally inoculated with a standardized dose of influenza virus (0.04 hemagglutinating units). Mice were monitored daily for morbidity (time to sickness), symptom severity, and mortality (time to death) for 21 days.

PURPOSE:: To test the influence of 1000 mg of quercetin (Q) with or without 120 mg of epigallocatechin 3-gallate (EGCG), 400 mg of isoquercetin, and 400 mg of eicosapentaenoic acid and docosahexaenoic acid (Q-EGCG) on exercise performance, muscle mitochondrial biogenesis, and changes in measures of immunity and inflammation before and after a 3-d period of heavy exertion. METHODS:: Trained cyclists (N = 39) were randomized to placebo (P), Q, or Q-EGCG and ingested supplements in a double-blinded fashion for 2 wk before, during, and 1 wk after a 3-d period in which subjects cycled for 3 h.d at approximately 57% Wmax. Blood, saliva, and muscle biopsy samples were collected before and after 2 wk of supplementation and immediately after the exercise bout on the third day. Blood and saliva samples were also collected 14 h after exercise. RESULTS:: Two-week supplementation resulted in a significant increase in plasma quercetin for Q and Q-EGCG and granulocyte oxidative burst activity (GOBA) in Q-EGCG.

PURPOSE OF REVIEW: Quercetin is discussed since several decades as a multipotent bioflavonoid with great potential for the prevention and treatment of disease. In the current review, we present the most recent findings on quercetin with regard to the pharmacology, the in-vitro and in-vivo effects in different cell systems and animal models, and the clinical effects in humans. RECENT FINDINGS: Quercetin bioavailability has been underestimated in the past and can be improved by food matrix components or particular delivery forms. Among the biological effects of particular relevance, the antihypertensive effects of quercetin in humans and the improvement of endothelial function should be emphasized. Together with its antithrombotic and anti-inflammatory effects, the latter mainly mediated through the inhibition of cytokines and nitric oxide, quercetin is a candidate for preventing obesity-related diseases. Most exiting are the findings that quercetin enhances physical power by yet unclear mechanisms. The anti-infectious and immunomodulatory activities of quercetin might be related to this effect.

e flavonoid quercetin is considered to have beneficial effects on human health. We recently have shown that quercetin-enriched foods reduced the duration of immobility time in a rat forced swimming test, indicating that dietary quercetin is promising as an antidepressant-like factor, whereas its mechanism of action is poorly understood. The aim of this study is to investigate the effects of quercetin on water immersion-restraint (WIR), stress-induced hypothalamic-pituitary-adrenal (HPA) axis activation, which is a major component of stress response and plays an important role in the pathology of depression. Quercetin administration to rats significantly suppressed WIR stress-induced increase of plasma corticosterone and adrenocorticotropic hormone levels as well as the mRNA expression of corticotropin-releasing factor (CRF) in the hypothalamic region.

The risk of an avian influenza pandemic has put oseltamivir (Tamiflu) in the spotlight and has given rise to rumors that shikimic acid (SK), which is used for the synthesis of Tamiflu, possesses therapeutic activity. This study was undertaken to determine whether SK, either alone or in combination with quercitin (QT) is able to modulate the release of IL-6 and IL-8 from peripheral blood mononuclear cells (PBMCs). The experiments were conducted comparing the properties of SK, both alone and in combination, with those of Tamiflu. The incubation of PBMCs with 100 nM Tamiflu or SK at two concentrations (10 nM; 100 nM) did not produce any change in IL-6 and IL-8 baseline levels (data expressed as incremental change vs. baseline). On the contrary, incubation with SK and QT at both concentrations (10 and 100 nM) produced a significant increase in the release of IL-8 as compared to other groups (4.19 +/- 0.82, SK-QT 10 nM; 3.83 +/- 1.17 SK-QT 100 nM, P < 0.05 vs. baseline 1.00 +/- 0.10, Tamiflu 100 nM 1.35 +/- 0.16, SK 10 nM 1.68 +/- 0.15 and SK 100 nM 1.80 +/- 0.48).

The spectre of an influenza pandemic is being widely mooted. Most of the strategies explored to date for controlling or treating the condition have centred on controlling the spread of the infection, the use of vaccines or anti-viral agents. There has been relatively little discussion about treating the lung and systemic inflammatory reactions that occur during influenza infection. In this review a range of therapeutic agents are proposed to treat the inflammatory reactions, principally in the lung as well as the systemic cytokine-mediated immuno-inflammatory reactions that may be a major cause of the morbidity and mortality associated with influenza infections. Among these are pentoxifylline, the statins, the macrolide antibiotics (e.g.