Life Extension Magazine

Life Extension Magazine September 2012

Report

Quercetin: Broad-Spectrum Protection

By Anne Buckley

Quercetin Lowers Cholesterol, Fights Atherosclerosis

Many of our most powerful medicines, including those for diabetes, chemotherapy, and cardiovascular health, are derived from plant extracts. One reason that plants hold so much potential for human health is that they are able to withstand a variety of destructive forces such as environmental radiation, oxidative damage, and chemical toxins due to their unique ability to manufacture complex molecules called flavonoids.1-4 For humans, these same conditions can be lethal. Yet when we consume plants as food and beverages, the protective benefits of these same flavonoids are readily transferred to our bodies!5

One flavonoid in particular, quercetin, is found in a broad range of foods, from grape skins and red onions to green tea and tomatoes. Quercetin is attracting intense scientific interest for its unique anti-aging and immune-boosting activities.6 Several recent studies show that organisms exposed to high levels of quercetin live longer, healthier lives.6--12 Laboratory models of aging, ranging from simple yeasts and primitive worms to cultured human cells, demonstrate that quercetin alone produces up to a 60% increase in life span!6,8-12 In addition, quercetin has been found to be cancer chemopreventive as well as reduce allergic reactions, boost immunity, and protect the cardiovascular system.

Due to its synergies with resveratrol, health-conscious people often obtain some quercetin in science-based resveratrol formulas they already use.

Quercetin Lowers Cholesterol, Fights Atherosclerosis

Quercetin is naturally abundant in plant foods and as a result is highly bioavailable.13 Nonetheless, most people do not obtain sufficient quercetin levels through their daily diets.14 This is unfortunate because large-scale epidemiological studies show that sustained high intake of quercetin and related flavonoids provides substantial protection against cardiovascular disease.15

In a study of 805 men aged 65-84 years, those with the highest quercetin and other flavonoid intake were 68% less likely to die from coronary heart disease than those with the lowest intake.14 A similar study found a reduction in death rates from all causes of 31% for women and 24% for men, with a 46% reduction in coronary death rates for women and a 22% reduction for men in those with the highest intakes.16

This dramatic cardiovascular protection is the result of a concerted synergy between several basic quercetin mechanisms, including its ability to lower cholesterol and reduce dangerous accumulations of abdominal and liver fat.

In one study on quercetin's impact on cholesterol levels, a group of otherwise healthy male smokers took 100 mg/day of quercetin or a placebo for 10 weeks, with blood tests done at baseline and at the end of the study.17 The supplemented group, but not the placebo group, had significant reductions in total and LDL cholesterol, and an increase in HDL cholesterol. They also had a significant reduction in blood sugar, another cardiovascular risk factor.

A larger study of non-smokers showed similar results, with an 18% reduction in total cholesterol, a 27% reduction in LDL, and an important 33% increase in beneficial HDL cholesterol.18

Animal and human studies also suggest that quercetin supplementation can reduce dangerous accumulations of abdominal and liver fat, the result of decreased oxidative stress and inflammation.19,20

Lowering cholesterol and reducing body fat are important first steps, but quercetin's cardiovascular benefits go farther, lowering blood pressure and increasing plasma levels of nitric oxide, thus providing more of the synergy mentioned earlier.

By blocking oxidation of LDL cholesterol, quercetin counteracts a major source of the blood vessel inflammation that precedes atherosclerosis.21,22 One human study found a 28% reduction in the rate of LDL oxidation following two weeks of supplementation with quercetin at just 30 mg/day.23

Higher doses of quercetin have shown the ability to modestly lower blood pressure.22,24 Quercetin supplements of 730 mg/day reduced hypertensive people's systolic (top number) blood pressure by 7 units (mmHg), and diastolic (bottom number) pressure by 5 units (mmHg).25 Those with normal blood pressure retained their healthy levels and did not experience a dangerous drop in blood pressure as is often the case with the use of anti-hypertensive medications. These results have been confirmed in other studies, with lower doses in the range of 100 - 200 mg/day.17,20,22,26

Quercetin also appears to exert its blood pressure-lowering effects by improving the health of your endothelium, the lining layer of the arteries that controls blood flow and pressure. Supplemental quercetin in hypertensive rats allowed "tight" blood vessels to relax, reducing their blood pressure.27

Quercetin supplements of 200 mg/day in healthy men increased blood levels of nitric oxide, a substance produced in endothelial cells that's required for vessels to dilate and lower blood pressure.28 Heart muscle that is overloaded by excess blood pressure loses its responsiveness to nitric oxide.29,30 It becomes overgrown, or hypertrophied and eventually loses its ability to pump blood effectively. This can lead to early death or disability.30 Quercetin completely blocks pressure overload-induced cardiac hypertrophy in animal models of hypertension which is the result of beneficial changes in gene expression in heart muscle tissue.30

Another of quercetin's cardiovascular benefits is its ability to inhibit platelet aggregation or "stickiness" in platelets. Oxidant stress and inflammation trigger this excessive "stickiness" in platelets and blood vessel walls. Untreated, the result can lead to a stroke or a heart attack following blood clot formation.

Human volunteers taking a highly bioavailable form of quercetin at both 150 and 300 mg/day rapidly (within 30 minutes) inhibited platelet aggregation.31 This effect proved to be the result of multiple changes in biochemical signaling pathways and gene expression, resulting in a healthier, "non-sticky" condition of the platelets.

Healthy arterial blood flow
Healthy arterial blood flow

Quercetin Shuts Down Cancer Cells Early

Cancers of all kinds are the second leading cause of death in the US, behind cardiovascular disease.32 Faced with the overwhelming challenge of achieving a cure, oncologists are increasingly turning to "chemoprevention" with nutrients as the most effective way to battle malignancies.33

Quercetin's multitargeted disease-fighting capabilities make it a natural choice as a chemopreventive compound. Strong evidence from epidemiological studies have shown that people with the highest quercetin intake enjoy substantially reduced risks for many of the leading causes of cancer death:

  • For lung cancer, the top cause of cancer deaths,34 a 51% overall risk reduction, and a 65% reduction among smokers35
  • For colon cancer, the second cause of cancer deaths,36 a 32% reduction in risk37
  • For gastric (stomach) cancer, a 43% overall risk reduction and an impressive 80% reduction in risk among female smokers38
  • And there's compelling laboratory evidence for quercetin's role in reducing risk of breast, prostate, and liver cancers as well.39-41

At the cellular level, quercetin interferes with the processes that turn healthy cells into malignant cancer cells. Quercetin's antioxidant and anti-inflammatory properties protect cellular DNA from dangerous cancer-inducing mutations.42 Quercetin "freezes" rapidly reproducing cancer cells into an early, non-productive phase of the cell replication cycle.43 This not only stops tumor growth but also triggers cell death by apoptosis—the innate programming healthy cells use to stop excessive reproduction.44 And quercetin favorably modulates chemical signaling pathways that are abnormal in cancer cells.45,46

Quercetin Combats Major Causes of Aging
Quercetin Combats Major Causes of Aging
  • Nature provides plants with powerful environmental protection in the form of phyto-molecules such as quercetin.
  • That protection, against age-inducing factors such as oxidant stress, radiation, DNA damage, and toxins, is surprisingly transferrable when we consume plant matter.
  • Quercetin extends life span in laboratory studies of simple animals and even human cells.
  • Detailed studies confirm that quercetin's life-extending effects arise from combating many of the major causes of aging and chronic disease.
  • Quercetin supplementation shows promise in lowering cardiovascular risk by normalizing cholesterol levels and in reducing cancer risk by blocking fundamental cancer-inducing processes.
  • Quercetin also favorably modifies immune function, reducing the impact of allergies and related lung diseases, while boosting our responses to dangerous viruses and bacteria.
  • Quercetin is readily absorbed and has no reported side effects; it belongs in your supplement plan as a natural way to prolong life's quality and quantity.

All of these separate actions can dramatically reduce the chances that any given cancer cell will successfully form a real tumor. And that is precisely how chemoprevention is meant to work.

Here are details about quercetin's impact on some of the most common and dangerous human cancer types, from laboratory studies:

  • Quercetin reduces the growth of colon cancer and its predecessors. Colon cancer involves both genetic predisposition and chronic inflammation in the intestinal tract. Quercetin reduces the amount of fat oxidation and inflammation of the intestine in animal studies.47,48 That reduces not only the incidence of tumors in lab animals, but also tumor size and the number of tumors per animal.49
  • Quercetin decreases the number and size of pre-cancerous lesions in the colon. These lesions are called "aberrant crypt foci," which are one of the danger signs your gastroenterologist looks for during a colonoscopy.44,50
  • Quercetin interferes with early lung cancer lesions. Laboratory studies demonstrate that quercetin traps developing cancer cells in the early phases of their replication cycle, effectively preventing further malignant development and promoting cancer cell death.43

In one dramatic study, laboratory rats were treated with quercetin before exposure to the powerful environmental carcinogen, benzo(a)pyrene.33 This compound is found in cigarette smoke, charbroiled foods, and automobile (particularly diesel) exhaust, making it among the most common pollutants in our environment. Untreated rats developed lung cancers but rats supplemented first with quercetin showed no such findings.33

  • Quercetin prevents development of liver cancer cells. Your liver is your body's "toxic waste dump," receiving and detoxifying the bulk of the poisons it is exposed to every day. As a result, liver cells are at the epicenter of toxin-induced cancer development. Studies show that quercetin ramps up human liver cells' production of protective proteins and enzyme systems, blocks the cancer replicative cell cycle, and reduces toxin-induced DNA mutations.41,51

Many of the gravest cancer-related threats to liver tissue come from increased oxidant damage. Quercetin mitigates that damage by sharply increasing liver cells' production of natural protective antioxidant enzyme systems.51 The result, again, is a marked reduction in formation and replication of cancerous liver cells.

  • Quercetin interferes with sex hormone receptors on reproductive system cancers. It blocks the androgen receptors used to sustain growth by prostate cancer cells, potentially preventing such cells from forming tumors.52 In breast cancer cells, on the other hand, quercetin stimulates estrogen receptors, but only the so-called "beta," or cancer-suppressing receptors, not the "alpha," or cancer-promoting ones.53
These cumulative effects put quercetin at the top of the list of potential cancer chemopreventive supplements.