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Quercetanus (1607) was one of the first medieval scientists to recognise the existence of the essential oil industry for lavender and juniper oils leading to the discovery of another group - the terpenes. Quercetin has earned a controversial reputation, first as a mutagen and then as one of the strongest anti-cancer agents known, according to Terence Leighton, Ph.D., professor of biochemistry at the University of California at Berkeley.

Quercetin is widely distributed in the plant kingdom and is the most abundant of the flavonoid molecules. It is found in many often-consumed foods, including apple, onion, tea, berries, and brassica vegetables, as well as many seeds, nuts, flowers, barks, and leaves. It is also found in medicinal botanicals, including Ginkgo biloba, Hypericum perforatum (St. John's Wort), Sambucus canadensis (Elder), and many others. It is often a major component of the medicinal activity of the plant, and has been shown in experimental studies to have numerous effects on the body.

It occurs very predominantly in red onions and broccoli. However if you think you should immediately take it off your menu because of its mutagenicity, bear in mind that in a study published by the National Cancer Institute and the Beijing Institute for Cancer Research in the People's Republic of China, persons with diets high in onions and garlic, which at dry weight have qercetin levels of 3% to 4%, have a 20-fold lower cancer risk than persons who don't eat these vegetables.

Note also that particular vegetables such as broccoli are renowned for other anti-cancer substances. Broccoli in particular has both mustard oils as allyl isothiocyanates and indoles such as carbinol which have their own toxicity, balanced by a pronounced anti-cancer potential.

Quercetin's anti-tumor action appears diverse and includes inhibition of inoculated cancer cells, chemical and virally induced cancers leukaemia and ovarian cancer. Related flavonoids also give protection against UV-B damage. Despite being a mutagen under test conditions, quercetin does not appear to be a carcinogen in hamsters, or in rats.

Quercetin is a member of a group of naturally occurring compounds, the flavonoids, which have a common flavone nucleus composed of two benzene rings linked through a heterocyclicpyrone ring. Quercetin is found in various plants, food products, and dyes of natural origin. The estimated average daily intake of quercetin by an individual in the United States is 25 mg. The Food and Drug Administration nominated quercetin for toxicity and carcinogenicity studies in the rat because it is a chemical that is widely distributed in foods. Quercetin was administered to rats by dosed feed since human exposure is by dietary consumption.

Information in the literature showed that quercetin administered in the diet to rats at levels up to approximately 4% caused a minor body weight effect, whereas higher dose levels produced greater than 10% reduction in body weight gains relative to controls. Based on this information, the NTP 2-year studies were conducted by administering 0, 1,000, 10,000, or 40,000 ppm quercetin (>95% pure) in feed to groups of 50 male and female rats for 104 weeks. Ten additional animals per dose group were evaluated at 6 and 15 months.

Under the conditions of these 2-year feed studies there was some evidence of carcinogenic activity of quercetin in male F344/N rats based on an increased incidence of renal tubule cell adenomas. There was no evidence of carcinogenic activity of quercetin in female F344/N rats receiving 1,000, 10,000 or 40,000 ppm.

Studies in experimental models indicate significant influence against diabetic complication, viral infection, inflammatory and allergic conditions and cancer.

Quercetin's aldose reductase-inhibiting properties make it a useful addition to diabetic nutritional supplementation, to prevent cataract and neurovascular complications.

Quercetin's anti-inflammatory activity appears to be due to its antioxidant and inhibitory effects on inflammation-producing enzymes (cyclooxygenase, lipoxygenase) and the subsequent inhibition of inflammatory mediators, including leukotrienes and prostaglandins. Inhibition of histamine release by mast cells and basophils also contributes to quercetin's anti-inflammatory activity.

Quercetin is a strong antioxidant and a major dietary flavonoid. Epidemiological studies suggest that consumption of quercetin protects against cardiovascular disease, but its absorption in man is controversial. We fed nine subjects a single large dose of onions, which contain glucose conjugates of quercetin, apples, which contain both glucose and non-glucose quercetin glycosides, or pure quercetin-3-rutinoside, the major quercetin glycoside in tea. Plasma levels were then measured over 36 h. Bioavailability of quercetin from apples and of pure quercetin rutinoside was both 30% relative to onions. Peak levels were achieved less than 0.7 h after ingestion of onions, 2.5 h after apples and 9 h after the rutinoside. Half-lives of elimination were 28 h for onions and 23 h for apples. We conclude that conjugation with glucose enhances absorption from the small gut. Because of the long half-lives of elimination, repeated consumption of quercetin-containing foods will cause accumulation of quercetin in blood.

Red wine contains one of the strongest anti-cancer angents known to man, which "directly blocks the proliferation of cancer cells", according to Terance Leighton, PhD, professor of microbiology at the University of California in Berkeley. The agent quercetin is not found in white or rose wine, brandies or in red or white grape juices in any significant levels.

Quercetin was initially discovered in red wine because of its trait as a mutagen (a subtance that mutates cells). Subsequent studies found that the substance, even in large quantities, did not promote the development of cancer. Instead, it emerged as a powerful natural anti-cancer agent that "simply overwhelms its danger as a mutagen", Dr. Lieghton said.

Buy Aller-Response from Source Naturals delivers seasonal support for the sinuses, lungs and immune system. Aller-Response features quercetin along with other powerful herbs including ginger, ginkgo biloba, amla, and andrographis, which have been used traditionally for lung, bronchial, and immune health. Vitamins A and C, along with Zinc, provide additional immune support. Aller-Response $23.99 plus $5.99 Shipping and Handling
Aller-Response addresses 5 body systems that are critical to achieving seasonal health Histamine Response. Aller-Response contains plant constituents that modify the release of histamine. Human cell culture studies with quercetin have demonstrated its ability to inhibit the release of histamine from immune cells. Ginkgo inhibits Platelet-Activating Factor,which stimulates histamine secretion from platelets: Ginkgo, Quercetin

Dr. Leighton, speaking at the 1989 American Chemical Society National Meeting, said that in a study of 250 red wines from throughout the world, quercetin levels varied from very low (less than 0.1 mg/L) to very high (greater than 7.0 mg/L).

Dr. Leighton and his team could not link the presence of quercetin to a specific region, grape variety, vintage, cask, aging method or length of aging in the bottle. Instead, they found it was directly related to the fining process. Young red wines, particularly those exposed to high pressure pressing, contain high concentrations of substances that impart bitter and astrigent flavours, and therefore are removed by fining with such agents as gelatine, casein or polyvinylpolypyrrolidone. At levels of 5 pounds per 1,000 gallons of wine, 85-90% of the quercetin is removed. At levels of 20 pounds per 1,000 gallons of wine, all the quercetin was removed from wines with even the highest levels. That explains why, within even a single variety of grapes and even among closely localized wineries, you have great variations in mutagenicity (presence of quercetin) from producer to producer, Dr. Leighton said. If other fining methods are used, the quercetin remains in the wine.

Resveratrol and quercetin are polyphenols which have been detected in significant amounts in green vegetables, citrus fruits and red grape wines. Beneficial effects attributed to these compounds include anti-inflammatory, antiviral and antitumor properties. The effect of resveratrol and quercetin on growth of human oral cancer cells is unknown... Combining 50 microM of resveratrol with 10, 25 and 50 microM of quercetin resulted in a gradual and significant increase in the inhibitory effect of quercetin on cell growth and DNA synthesis. We conclude that resveratrol or a combination of resveratrol and quercetin, in concentrations equivalent to that present in red wines, are effective inhibitors of oral squamous carcinoma cell (SCC-25) growth and proliferation, and warrant further investigation as cancer chemopreventive agents.

Flavonoids, particularly quercetin, are inhibitors of allergic (IgE-mediated) mediator release from mast cells and basophils. In previous studies reported from our laboratories (Hope et al., 1983) quercetin inhibited not only IgE-mediated allergic mediator release from mast cells but also IgG-mediated histamine and SRS-A (peptidoleukotriene) release from chopped lung fragments from actively sensitized guinea pigs. Interestingly, quercetin was much more potent as an inhibitor of the release of SRS-A than histamine, suggesting that it might also inhibit the biosynthesis of SRS-A. Subsequently we demonstrated that quercetin was an effective inhibitor of Æ5-lipoxygenase. This property of the compound most likely accounts for its effect on peptidoleukotriene biosynthesis. The studies reported herein further expand on these observations by evaluating the activities of a variety of standard flavonoids on Æ5-lipoxygenase and other enzymes known to be involved in the metabolism of arachidonic acid in cells. Compounds such as the flavonoid, quercetin, which exhibit both allergic mediator release activity and selective inhibition of the biosynthesis of proinflammatory arachidonic acid metabolites may be interesting prototypes which will lead to the discovery of very effective antiallergic and antiinflammatory agents.

See also: Flavonoids

  • TR-409 Toxicology and Carcinogenesis Studies of Quercetin (CAS No. 117-39-5) in F344 Rats (Feed Studies). National Institute of Environmental Health Sciences
  • Hollman PC; van Trijp JM. Et al. Relative bioavailability of the antioxidant flavonoid quercetin from various foods in man. FEBS Lett, 418(1-2):152-6 1997 Nov 24
  • Ferrandiz ML, and Alcaraz MJ, Anti-inflammatory activity and inhibition of arachidonic acid metabolism by flavonoids. Agents Action 32, 283-287, 1991
  • Stavric B, Quercetin in our diet: from potent mutagen to probable anticarcinogen. Clin Biochem 27, 245-248, 1994
  • ElAttar TM; Virji AS. Modulating effect of resveratrol and quercetin on oral cancer cell growth and proliferation. Anticancer Drugs 1999 Feb;10(2):187-93
  • Gail Finlayson. Wines & Vines Inc. July 1991.
  • Welton AF, Tobias LD, Fiedler-Nagy C, et al. Effect of flavonoids on arachidonic acid metabolism. Prog Clin Biol Res 213:231-242; 1986.