Health Care Professional Information
Common Name
Dwarf bilberry, bog bilberry, European blueberry, huckleberry, and whortleberry
Clinical Summary
Bilberry is derived from the fruit of the tree. It is available as a dietary supplement to help improve eyesight. Several human studies suggest that bilberry anthocyanosides prevent diabetic retinopathy and improve visual acuity and retinal function (1) (2) (3) (4) . One human study also suggested that bilberry extract may significantly reduce the proliferation of colorectal cancer tumor tissue (5). In vitro studies have also indicated that bilberry may have anticancer activities(6) (7) (8) (9) (10). Coumarins present in bilberry may interact with platelets and have an additive effect with blood thinners (11). Bilberry fruit should not be confused with bilberry leaf, which may have hypoglycemic effect.
Purported Uses
- Cancer prevention
- Cataracts
- Circulatory disorders
- Diabetic retinopathy
- Diarrhea
- Glaucoma
- Hemorrhoids
- Macular degeneration
- Mucositis
- Varicose veins
- Visual acuity
Constituents
- Tannins: 5-10% catechin tannins
- Carbohydrates: 30% invert sugar and pectins
- Flavonols: Flavonol glycosides including astragalin, hyperoside, isoquercitrin and quercetin
- Phenolic acids
- Anthocyanosides
(12)
Mechanism of Action
The anthocyanins in bilberry contribute to most of its pharmacological activities. Anthocyanin has anti-inflammatory, vasoprotective (13), and antioxidant effects (14). It has demonstrated free radical scavenging and inhibition of cAMP phosphodiesterase actions. Extract of bilberry can inhibit human leukemia cells and human colon carcinoma cells growth through the induction of apoptosis (6). Another in vitro study investigated the effect of bilberry extract on MCF-7 human breast cancer cells and also found that it inhibited cell proliferation and induced apoptosis (15). In vitro and in vivo clinical studies show inhibition of platelet aggregation and stimulation of vascular prostacyclin. Bilberry anthocyanins regenerate rhodopsin and are indicated in treatment of poor night vision, macular degeneration, glaucoma and cataracts (1) (2) (3) (4) (16) (17)
Pharmacokinetics
Pharmacokinetic studies in humans have found that the anthocyanins in bilberry extract are excreted in the urine either Intact or as methylated or glucuronidated metabolites (5) (8). One of these studies suggested that the stomach is the primary site for anthocyanin absorption (16). Intravenous and oral studies of bilberry anthocyanosides have also been performed in male rats (19). Oral administration showed moderate GI absorption with bioavailability less than 2%. Peak levels were achieved within 15 minutes with a three-compartment distribution and elimination shown. Elimination was primarily through urine and bile.
Herb-Drug Interactions
Anticoagulants / Antiplatelets: Bilberry may potentiate the risk of bleeding if used concurrently due to platelet aggregation inhibition and prostaglandin modulation.
Herb Lab Interactions
Coumarin content in bilberry may increase PT/PTT and inhibit platelet activity (11).
Literature Summary and Critique
Dosage (Inside MSKCC Only)
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References
- Muth ER, et al. The effect of bilberry nutritional supplementation on night visual acuity and contrast sensitivity. Altern Med Rev 2000;5:164-73.
- Zadok D, et al. The effect of anthocyanosides on night vision tests. Invest Ophthalmol Vis Sci 1997;38(suppl):633.
- Boniface R,et al. Pharmacological properties of mytillus anthocyanosides: correlation with results of treatment of diabetic microangiopathy. Flavonoids Bioflavonoids. Ireland: Elsevier; 1985, 293-301.
- Perossini M, et al. Diabetic and hypertensive retinopathy therapy with anthocyanosides double blind placebo-controlled clinical trial. Ann Ottal Clin Ocul 1987;113:1173-90.
- Thomasset S, Berry DP, Cai H, et al. Pilot study of oral anthocyanins for colorectal cancer chemoprevention. Cancer Prev Res (Phila). 2009 Jul;2(7):625-33.
- Katsube N, et al. Induction of apoptosis in cancer cells by Bilberry (Vaccinium myrtillus) and the anthocyanins. J Agric Food Chem. 2003 Jan 1;51(1):68-75.
- Bagchi D, Sen CK, Bagchi M, Atalay M. Anti-angiogenic, antioxidant, and anti-carcinogenic properties of a novel anthocyanin-rich berry extract formula. Biochemistry (Mosc). 2004 Jan;69(1):75-80
- Lala G, Malik M, Zhao C, et al. Anthocyanin-rich extracts inhibit multiple biomarkers of colon cancer in rats. Nutr Cancer. 2006;54(1):84-93.
- Misikangas M, Pajari AM, Päivärinta E, et al. Three Nordic berries inhibit intestinal tumorigenesis in multiple intestinal neoplasia/+ mice by modulating beta-catenin signaling in the tumor and transcription in the mucosa. J Nutr. 2007 Oct;137(10):2285-90.
- Teller N, Thiele W, Marczylo TH, et al. Suppression of the kinase activity of receptor tyrosine kinases by anthocyanin-rich mixtures extracted from bilberries and grapes. J Agric Food Chem. 2009 Apr 22;57(8):3094-101.
- Brinker F. Herb Contraindications and Drug Interactions 3rd ed. Sandy (OR): Eclectic Medical; 2001.
- Bisset NG, et al. Herbal Drugs and Phytopharmaceuticals, 2nd ed. Boca Raton: Medpharm CRC Press; 1994.
- Lietti A, et al. Studies on Vaccinium myrtillus anthocyanosides. I. Vasoprotective and antiinflammatory activity. Arzneimittelforschung. 1976;26(5):829-32.
- Laplaud PM, et al. Antioxidant action of Vaccinium myrtillus extract on human low density lipoproteins in vitro: initial observations. Fundam Clin Pharmacol. 1997;11(1):35-40.
- Nguyen V, Tang J, Oroudjev E, et al. Cytotoxic effects of bilberry extract on MCF7-GFP-tubulin breast cancer cells. J Med Food. 2010 Apr;13(2):278-85.
- Blumenthal, et al. Herbal Medicine Expanded Commission E Monographs, 1st ed. Austin: American Botanical Council; 2000.
- Bruneton, J. Pharmacognosy, Phytochemistry, Medicinal Plants. Paris: Lavoisier Publishing; 1995.
- Cai H, Thomasset SC, Berry DP, et al. Determination of anthocyanins in the urine of patients with colorectal liver metastases after administration of bilberry extract. Biomed Chromatogr. 2010 Aug 31.
- Morazzoni P, et al. Vaccinium myrtillus anthocyanosides pharmacokinetics in rats. Arzneimittel-Forschung 1991;41:128-31.
Consumer Information
How It Works
Bottom Line: Bilberry may help improve vision in people with cataracts and macular degeneration. There is insufficient evidence to support its other uses.
In laboratory studies, bilberry reduces inflammation and edema (accumulation of fluid in the tissues), acts as an antioxidant, inhibits blood clotting, and strengthens the walls of the blood vessels. The extracts of bilberry can inhibit the growth of cancer cells in the lab. Preliminary clinical trials indicate that bilberry strengthens and protects the walls of the blood vessels in humans. More clinical trials are needed to confirm these effects in humans.
In addition, compounds isolated from bilberry called anthocyanins are able to regenerate rhodopsin, the pigment found in retina cells responsible for eyesight. This finding explains bilberry's success in improving vision in patients with macular degeneration, glaucoma and cataracts.
Purported Uses
- To prevent cancer
Laboratory studies and one clinical study suggest anti-cancer effects. Further study is needed to confirm these effects.
- To treat cataracts
Several clinical trials support this use.
- To treat diabetic retinopathy (degeneration of the retina due to diabetes)
Several clinical trials support this use.
- To treat glaucoma
Several studies support this use.
- To prevent the progression of macular degeneration
Several studies support this use.
- To reduce inflammation in conditions such as hemorrhoids or mucositis
Laboratory studies suggest anti-inflammatory effects, but there is no proof from clinical trials that bilberry can reduce inflammation in humans.
- To improve vision, especially at night
Clinical trials show that bilberry improves eyesight in patients with certain disorders, but do not support this use in individuals with good vision.
- To treat diarrhea
No scientific evidence supports this use.
- To treat circulatory disorders
Laboratory studies show that bilberry may protect blood vessels and decrease the risk of blood clots. Human data are needed.
- To improve the appearance of varicose veins
No scientific evidence supports this use.
Research Evidence
Colorectal Cancer
One study in humans suggests that bilberry extract may decrease tumor growth in colorectal cancer. However, additional studies are needed to confirm this effect.
Patient Warnings
- Bilberry fruit should not be confused with bilberry leaf, which may lower blood sugar levels.
Do Not Take If
- You use warfarin or other blood thinners (bilberry may increase the risk of bleeding).
- You have a blood clotting disorder such as hemophilia (bilberry may increase the risk of bleeding).
Last updated: March 9, 2012
absorption (ub-SORP-shun)
The process of taking nutrients from the digestive system into the blood so they can be used in the body.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
administration (ad-MIH-nih-STRAY-shun)
In medicine, the act of giving a treatment, such as a drug, to a patient. It can also refer to the way it is given, the dose, or how often it is given.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
anti-inflammatory (AN-tee-in-FLA-muh-TOR-ee)
Having to do with reducing inflammation.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
antioxidant (AN-tee-OK-sih-dent)
A substance that protects cells from the damage caused by free radicals (unstable molecules made by the process of oxidation during normal metabolism). Free radicals may play a part in cancer, heart disease, stroke, and other diseases of aging. Antioxidants include beta-carotene, lycopene, vitamins A, C, and E, and other natural and manufactured substances.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
apoptosis (A-pop-TOH-sis)
A type of cell death in which a series of molecular steps in a cell leads to its death. This is the body’s normal way of getting rid of unneeded or abnormal cells. The process of apoptosis may be blocked in cancer cells. Also called programmed cell death.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
bile (bile)
A fluid made by the liver and stored in the gallbladder. Bile is excreted into the small intestine, where it helps digest fat.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
biopsy (BY-op-see)
The removal of cells or tissues for examination by a pathologist. The pathologist may study the tissue under a microscope or perform other tests on the cells or tissue. There are many different types of biopsy procedures. The most common types include: (1) incisional biopsy, in which only a sample of tissue is removed; (2) excisional biopsy, in which an entire lump or suspicious area is removed; and (3) needle biopsy, in which a sample of tissue or fluid is removed with a needle. When a wide needle is used, the procedure is called a core biopsy. When a thin needle is used, the procedure is called a fine-needle aspiration biopsy.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
blood (blud)
A tissue with red blood cells, white blood cells, platelets, and other substances suspended in fluid called plasma. Blood takes oxygen and nutrients to the tissues, and carries away wastes.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
blood sugar (blud SHUH-ger)
Glucose (a type of sugar) found in the blood. Also called glycemia.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
breast (brest)
Glandular organ located on the chest. The breast is made up of connective tissue, fat, and breast tissue that contains the glands that can make milk. Also called mammary gland.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
cancer (KAN-ser)
A term for diseases in which abnormal cells divide without control and can invade nearby tissues. Cancer cells can also spread to other parts of the body through the blood and lymph systems. There are several main types of cancer. Carcinoma is a cancer that begins in the skin or in tissues that line or cover internal organs. Sarcoma is a cancer that begins in bone, cartilage, fat, muscle, blood vessels, or other connective or supportive tissue. Leukemia is a cancer that starts in blood-forming tissue such as the bone marrow, and causes large numbers of abnormal blood cells to be produced and enter the blood. Lymphoma and multiple myeloma are cancers that begin in the cells of the immune system. Central nervous system cancers are cancers that begin in the tissues of the brain and spinal cord. Also called malignancy.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
carcinoma (KAR-sih-NOH-muh)
Cancer that begins in the skin or in tissues that line or cover internal organs.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
cell (sel)
The individual unit that makes up the tissues of the body. All living things are made up of one or more cells.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
clinical (KLIH-nih-kul)
Having to do with the examination and treatment of patients.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
clinical study (KLIH-nih-kul STUH-dee)
A type of research study that tests how well new medical approaches work in people. These studies test new methods of screening, prevention, diagnosis, or treatment of a disease. Also called clinical trial.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
colon (KOH-lun)
The longest part of the large intestine, which is a tube-like organ connected to the small intestine at one end and the anus at the other. The colon removes water and some nutrients and electrolytes from partially digested food. The remaining material, solid waste called stool, moves through the colon to the rectum and leaves the body through the anus.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
colorectal (KOH-loh-REK-tul)
Having to do with the colon or the rectum.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
colorectal cancer (KOH-loh-REK-tul KAN-ser)
Cancer that develops in the colon (the longest part of the large intestine) and/or the rectum (the last several inches of the large intestine before the anus).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
coumarin (KOO-muh-rin)
A substance used to make drugs that prevent and treat blood clots in blood vessels and treat certain heart conditions. Coumarin is taken from certain plants and can also be made in the laboratory. It is a type of anticoagulant.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
dose (dose)
The amount of medicine taken, or radiation given, at one time.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
edema (eh-DEE-muh)
Swelling caused by excess fluid in body tissues.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
ER
A protein found inside the cells of the female reproductive tissue, some other types of tissue, and some cancer cells. The hormone estrogen will bind to the receptors inside the cells and may cause the cells to grow. Also called estrogen receptor.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
extract (EK-strakt)
In medicine, a preparation of a substance obtained from plants, animals, or bacteria and used as a drug or in drugs.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
fluid (FLOO-id)
A substance that flows smoothly and takes the shape of its container. Liquids and gases are fluids.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
free radical (free RA-dih-kul)
A type of unstable molecule that is made during normal cell metabolism (chemical changes that take place in a cell). Free radicals can build up in cells and cause damage to other molecules, such as DNA, lipids, and proteins. This damage may increase the risk of cancer and other diseases.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
GI
Refers to the stomach and intestines. Also called gastrointestinal.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
glaucoma (glaw-KOH-muh)
A condition in which there is a build-up of fluid in the eye, which presses on the retina and the optic nerve. The retina is the layer of nerve tissue inside the eye that senses light and sends images along the optic nerve to the brain. Glaucoma can damage the optic nerve and cause loss of vision or blindness.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
growth factor (grothe FAK-ter)
A substance made by the body that functions to regulate cell division and cell survival. Some growth factors are also produced in the laboratory and used in biological therapy.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
herbal (ER-bul)
Having to do with plants.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
in vitro (in VEE-troh)
In the laboratory (outside the body). The opposite of in vivo (in the body).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
in vivo (in VEE-voh)
In the body. The opposite of in vitro (outside the body or in the laboratory).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
inflammation (IN-fluh-MAY-shun)
Redness, swelling, pain, and/or a feeling of heat in an area of the body. This is a protective reaction to injury, disease, or irritation of the tissues.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
intravenous (IN-truh-VEE-nus)
Into or within a vein. Intravenous usually refers to a way of giving a drug or other substance through a needle or tube inserted into a vein. Also called IV.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
leukemia (loo-KEE-mee-uh)
Cancer that starts in blood-forming tissue such as the bone marrow and causes large numbers of blood cells to be produced and enter the bloodstream.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
liver (LIH-ver)
A large organ located in the upper abdomen. The liver cleanses the blood and aids in digestion by secreting bile.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
macular degeneration (MA-kyoo-ler dee-JEH-neh-RAY-shun)
A condition in which there is a slow breakdown of cells in the center of the retina (the light-sensitive layers of nerve tissue at the back of the eye). This blocks vision in the center of the eye and can cause problems with activities such as reading and driving. Macular degeneration is most often seen in people who are over the age of 50. Also called age-related macular degeneration, AMD, and ARMD.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
oral (OR-ul)
By or having to do with the mouth.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
pigment (PIG-ment)
A substance that gives color to tissue. Pigments are responsible for the color of skin, eyes, and hair.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
plasma (PLAZ-muh)
The clear, yellowish, fluid part of the blood that carries the blood cells. The proteins that form blood clots are in plasma.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
platelet (PLAYT-let)
A tiny piece of a cell found in the blood that breaks off from a large cell found in the bone marrow. Platelets help wounds heal and prevent bleeding by forming blood clots. Also called thrombocyte.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
primary tumor (PRY-mayr-ee TOO-mer)
The original tumor.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
prostaglandin (PROS-tuh-GLAN-din)
One of several hormone-like substances made by the body. Different prostaglandins control blood pressure, contraction of smooth muscles, and other processes within tissues where they are made. Certain prostaglandins are being studied as cancer biomarkers. Also called PG.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
randomized
Describes an experiment or clinical trial in which animal or human subjects are assigned by chance to separate groups that compare different treatments.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
reduction (ree-DUK-shun)
A chemical reaction that takes place when a substance comes into contact with hydrogen or another reducing substance.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
resection (ree-SEK-shun)
Surgery to remove tissue or part or all of an organ.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
retina (REH-tih-nuh)
The light-sensitive layers of nerve tissue at the back of the eye that receive images and sends them as electric signals through the optic nerve to the brain.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
stomach (STUH-muk)
An organ that is part of the digestive system. The stomach helps digest food by mixing it with digestive juices and churning it into a thin liquid.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
surgery (SER-juh-ree)
A procedure to remove or repair a part of the body or to find out whether disease is present. An operation.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
tissue (TIH-shoo)
A group or layer of cells that work together to perform a specific function.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
tumor (TOO-mer)
An abnormal mass of tissue that results when cells divide more than they should or do not die when they should. Tumors may be benign (not cancer), or malignant (cancer). Also called neoplasm.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
urine (YOOR-in)
Fluid containing water and waste products. Urine is made by the kidneys, stored in the bladder, and leaves the body through the urethra.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)