Health Care Professional Information
Quercetin is a dietary flavonoid found in fruits and vegetables including apples, black, green and buckwheat tea, onions, red grapes, cherries, raspberries, citrus fruits. It is also found in some popular medicinal plants including ginkgo biloba and St. John's Wort (5) and is used widely for its antioxidant effects.
In vitro data indicate that quercetin has anti-inflammatory(13) (14)and chemopreventive effects (15). However, quercetin can also act as an anti-apoptotic agent (5).
Studies in animal models have shown its ability to potentiate the antitumor effects of doxorubicin in liver cancer cells, while protecting normal liver cells (16). Quercetin also demonstrated neuroprotective property and induced anti-depressant effects (17); it was also shown to exert pro-oxidant effects by decreasing serum homocysteine levels (18).
Long-term supplementation with 1000 mg/day quercetin resulted in wide-ranging metabolic effects in a study of healthy subjects (19). Further research is needed to understand the implications of these effects.
Quercetin was shown to exacerbate estrogen-induced breast tumors in rats (12). But human data are lacking.
Due to its antioxidant effects, quercetin may interfere with the actions of certain chemotherapy drugs.
Teas, onions, apples, buckwheat
- Cancer prevention
- Cancer treatment
- Cardiovascular disease
Mechanism of Action
Quercetin constitutes the major bioflavonoid in the human diet. Its antioxidant effects are due its phenolic group, which reacts with free radicals to form the more stable phenoxy radicals (1). Quercetin also exerts anti-inflammatory (13) and chemopreventive (15) properties. It also has been shown to have membrane-stabilizing capabilities and inhibits aldose reductase and low-density lipoprotein oxidation (8). The anti-cancer effects of quercetin are via down regulation of mutant p53 proteins; G1 phase arrest (1); tyrosine kinase inhibition (10); and down regulation of cell survival, proliferative and anti-apoptotic proteins (15). Preclinical data support the concept of quercetin as an anti-cancer compound (15). However, clinical studies that support these uses are few and the results are mixed (7) (9).
Following oral administration, quercetin glycosides are absorbed from the gut. These glycosides may then undergo hydrolysis in the enterocyte via b-glucosidases before draining into the portal vein. Absorption rate from dietary sources is influenced by the position and chemical nature of the glycoside in combination with the various compounds in the food matrix (1).
Quercetin is found predominantly in plasma in the form of its conjugates (e.g., quercetin glucuronides and/or sulfates) and small amounts of unconjugated quercetin aglycone. Maximum plasma concentrations are achieved within the first two hours of administration. This suggests that the absorption site is in the upper gut compartment, and may rule out intestinal bacterial degradation (2) (3).
Previous pharmacokinetic studies using intravenous administration suggest that quercetin is quickly eliminated in humans, with an approximate elimination half-life of less than two hours. Several studies report that quercetin is present in urine as a conjugate of glucuronic acid and sulfate groups (2).
Papain and Bromelain: May assist the absorption of Quercetin in the intestine (6).
Quinolone antibiotic: Quercetin may compete for DNA gyrase binding sites in bacteria (5).
CYP 3A4: Quercetin was shown to significantly inhibit the constitutive CYP3A4 activity (11).
Literature Summary and Critique
Dosage (Inside MSKCC Only)
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- Lamson DW, Brignall MS. Antioxidant and cancer III: quercetin. Altern Med Rev 2000;5:196-208.
- Graefe EU, et al. Pharmacokinetics and bioavailability of the flavonol quercetin in humans. Int J Clin Pharmacol Therapy 1999;37:219-33.
- Erlund I, et al. Pharmacokinetics of quercetin aglycone and rutin in healthy volunteers. Eur J Clin Pharmacol 2000;56:545-53.
- Sampson S, et al. Flavonol and flavone intakes in US health professionals. J Am Diet Assoc 2002;102:1414-20.
- Akan Z, Garip AI. Antioxidants May Protect Cancer Cells from Apoptosis Signals and Enhance Cell Viability. Asian Pac J Cancer Prev. 2013;14(8):4611-4614.
- Shoskes D, et al. Quercetin in men with category III chronic prostatitis: a preliminary prospective, double-blind, placebo-controlled trial. Urology 1999;54:960-3.
- Janssen K, et al. Effects of the flavonoids quercetin and apigenin on hemostasis in healthy volunteers: results from an in vitro and dietary supplement study. Am J Clin Nutr 1998;67:255-62.
- Chopra M, et al. Nonalcoholic red wine extract and quercetin inhibit LDL oxidation without affecting plasma antioxidant vitamin and carotenoid concentrations. Clin Chem 2000;46:1162-70.
- Beatty ER, et al. Effect of dietary quercetin on oxidative DNA damage in healthy human subjects. Br J Nutr 2000;84:919-25.
- Ferry DR, et al. Phase I clinical trial of the flavonoid quercetin: pharmacokinetics and evidence for in vivo tyrosine kinase inhibition. Clin Cancer Res 1996;2:659-68.
- Sergent T, Dupont I, Van der Heiden E, et al. CYP1A1 and CYP3A4 modulation by dietary flavonoids in human intestinal Caco-2 cells. Toxicol Lett. 2009 Dec 15;191(2-3):216-22.
- Singh B, Mense SM, Bhat NK, et al. Dietary quercetin exacerbates the development of estrogen-induced breast tumors in female ACI rats. Toxicol Appl Pharmacol. 2010 Sep 1;247(2):83-90.
- Askari G, Ghiasvand R, Feizi A, Ghanadian SM, Karimian J. The effect of quercetin supplementation on selected markers of inflammation and oxidative stress. J Res Med Sci. 2012 Jul;17(7):637-41.
- Chen YW, Chou HC, Lin ST, et al. Cardioprotective Effects of Quercetin in Cardiomyocyte under Ischemia/Reperfusion Injury. Evid Based Complement Alternat Med. 2013;2013:364519.
- Sharmila G, Bhat FA, Arunkumar R, et al. Chemopreventive effect of quercetin, a natural dietary flavonoid on prostate cancer in in vivo model. Clin Nutr. 2013 Sep 3. [Epub ahead of print]
- Wang G, Zhang J, Liu L, Sharma S, Dong Q. Quercetin potentiates doxorubicin mediated antitumor effects against liver cancer through p53/Bcl-xl. PLoS One. 2012;7(12):e51764.
- Rinwa P, Kumar A. Quercetin suppresses the microglial neuroinflammatory response and induces anti-depressant like effect in olfactory bulbectomized rats. Neuroscience. 2013 Oct 1. [Epub ahead of print]
- Meng B, Gao W, Wei J, et al. Quercetin reduces serum homocysteine level in rats fed a methionine-enriched diet. Nutrition. 2013 Apr;29(4):661-6.
- Cialdella-Kam L, Nieman DC, Sha W, et al. Dose-response to 3 months of quercetin-containing supplements on metabolite and quercetin conjugate profile in adults. Br J Nutr. 2013 Jun;109(11):1923-33.
How It Works
Bottom Line: Quercetin has not been shown to treat cancer or other diseases.
Quercetin belongs to a family of compounds called bioflavonoids, which are largely responsible for the bright colors and medicinal activities of many plants. Quercetin is the most common bioflavonoid that people consume, and is the most active of the bioflavonoids in laboratory experiments. It is known to act as an antioxidant, neutralizing free radicals that can cause cellular and DNA damage. Quercetin is thought to have anti-inflammatory properties by inhibiting the release of substances that mediate the inflammatory response, such as histamine. Presently, considerable laboratory data support the concept of quercetin as an anticancer compound, but it is still unclear from clinical trials whether this effect occurs in the human body.
Becasue of its antioxidant effects, quercetin may interfere with the actions of certain chemotherapy drugs.
- To treat allergies
Laboratory studies show an anti-inflammatory effect of quercetin, including inhibition of histamine release. Clinical trials have not been conducted.
- To prevent and treat cancer
Laboratory studies indicate anti-cancer activity of quercetin against a wide range of cancer cell types. But human data are lacking.
- To treat heart disease
One study showed that quercetin, in combination with red wine extract, lowered LDL oxidation (which may contribute to atherosclerosis) in healthy volunteers. However, it is unclear how much of this effect was due to quercetin alone, and other similar studies have not found the same effect.
Chronic prostatitis (chronic pelvic pain syndrome)
Thirty men with category III chronic prostatitis (chronic pelvic pain syndrome) took part in a study about the effects of quercetin. They were randomly assigned to take either 500 mg of quercetin or a placebo pill by mouth twice a day for one month. Men who took quercetin reported significant improvements in quality of life and symptoms (67%) compared to those on the placebo pill (20%). This study also suggested that bromelain and papain can increase the absorption of quercetin. But larger studies are needed to confirm these results.
Do Not Take If
- You are taking quinolone antibiotics (Quercetin may lessen their effects).
- You are taking drugs that are substrates of CYP 3A4 (Quercetin may increase the risk of side effects of such drugs).
- The fruit extracts papain and bromelain may help increase the absorption of Quercetin in the intestine.
- Quercetin was shown to worsen estrogen-induced breast tumors in rats.
Last updated: October 11, 2013