Health Care Professional Information
Scientific Name
Vitis vinifera, Vitis coignetiae
Common Name
Grape Seed Oil, Grape Seed Extract, muskat
Brand Name
ActiVin® eganaturalTM Leucoselect®
Clinical Summary
Obtained as a by-product of wine production, grape seeds are ground to produce grape seed oil. Traditionally, grape seed oil and grape seed extract (GSE) have been used as a laxative, antacid, cholagogic agent, to treat burns, ulcers, and as a hand cleanser (1) (2). Studies of grape seed proanthocyanidin extract (GSPE) in mice have shown effectiveness in minimizing cardiotoxicity induced by doxorubicin (15) , cyclosporine (22); and drug-induced nephro- and pulmonary toxicities (3) (23). GSPE also inhibits atherosclerosis (4) (5).
Small human trials have shown possible efficacy in decreasing LDL (6) and increasing total serum antioxidant activity (7). Conclusions from a meta analysis indicate that grape seed extract significantly lowers systolic blood pressure and heart rate, but does not affect lipid or CRP levels (24).
Topical application of GSPE has been shown to accelerate wound contraction and closure (8).
In vitro studies have shown GSPE to have anticancer effects (16) (17) and synergistic effects with doxorubicin (13). Supplementation with grape seed may be associated with decreased risk of hematologic malignancies (21).
But orally administered GSPE was not effective for breast induration following radiotherapy in patients with breast cancer (14).
Purported Uses
- Atherosclerosis
- Burns
- Cancer prevention
- Constipation
- GI disorders
- High cholesterol
- Wound healing
Constituents
- Oligomeric proanthocyanidins (OPC): dimeric, trimeric and tetrameric OPCs, cathechin derivatives, other flavonoids
- Lipids: palmitic, stearic, oleic, linoleic, sitosterol and tocopherols. Phosphatidylserine, phosphatidylinositol, lecithin, cephalin, cerebrosides and phosphatic acid are bound to seed lipoproteins.
- Proteins: leucine, arginine, cystine, phenylalanine, valine
- Tocopherol
- Tannins
(3)
Mechanism of Action
Proanthocyanidins and minor phenolic compounds found in GSPE are also found naturally in many foods including fruits, vegetables, chocolate and tea. People generally consume 460-1000 mg/day of these combined substances (9). GPSE has protective effects on doxorubin-induced cardiotoxicity (3). Cardioprotective effects may be due to its ability to modulate anti-apoptotic genes and modify molecular targets such as DNA damage and repair, lipid peroxidation and intracellular calcium homeostasis (5).
Herb-Drug Interactions
- Cytochrome P450 3A4 substrates: Grape seed extract inhibits CYP3A4 and can affect the intracellular concentration of drugs metabolized by this enzyme (18).
- Warfarin (Coumadin): Due to its anticoagulant effects, grape seed can enhance the activity of warfarin (11) (12) (19).
- UGT (Uridine 5'-diphospho-glucuronosyltransferase) substrates: Grape seed modulates UGT enzymes in vitro and can increase the side effects of drugs metabolized by them (20).
Literature Summary and Critique
Feringa HH, Laskey DA, Dickson JE, Coleman CI. The effect of grape seed extract on cardiovascular risk markers: a meta-analysis of randomized controlled trials.J Am Diet Assoc. 2011 Aug;111(8):1173-81.
Nine randomized controlled trials involving 390 patients were included in this meta analysis. The studies had to report efficacy data on at least one of the following end points: systolic or diastolic blood pressure, heart rate, total cholesterol, low-density or high-density lipoprotein cholesterol, triglycerides, or CRP. Results showed that grape seed extract significantly lowered systolic blood pressure (P=0.02]), and heart rate (P=0.01]). No significant effect on diastolic blood pressure, lipid levels, or CRP was found. Larger randomized, double-blinded trials are warranted to evaluate different dosages of grape seed extract and for longer follow-up periods.
Dosage (Inside MSKCC Only)
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References
- DerMarderosian A. The Review of Natural Products. St. Louis: Facts and Comparisons, 1999.
- Bombardelli E,.Morazzoni P. Vitis vinifera L. Fitoterapia 1995;66:291-317.
- Ray SD, Patel D, Wong V, Bagchi D. In vivo protection of dna damage associated apoptotic and necrotic cell deaths during acetaminophen-induced nephrotoxicity, amiodarone-induced lung toxicity and doxorubicin-induced cardiotoxicity by a novel IH636 grape seed proanthocyanidin extract. Res Commun. Mol. Pathol. Pharmacol. 2000;107:137-66.
- Yu H, Wang SE, Zhao C, Xu G. [Study of anti-atherosclerosic effect of grape seed extract and its mechanism]. Wei Sheng Yan. Jiu. 2002;31:263-5.
- Bagchi D, Sen CK, Ray SD, Das DK, Bagchi M, Preuss HG et al. Molecular mechanisms of cardioprotection by a novel grape seed proanthocyanidin extract. Mutat. Res 2003;523-524:87-97.
- Preuss HG, Wallerstedt D, Talpur N, Tutuncuoglu SO, Echard B, Myers A et al. Effects of niacin-bound chromium and grape seed proanthocyanidin extract on the lipid profile of hypercholesterolemic subjects: a pilot study. J Med 2000;31:227-46.
- Nuttall SL, Kendall MJ, Bombardelli E, Morazzoni P. An evaluation of the antioxidant activity of a standardized grape seed extract, Leucoselect. J Clin Pharm. Ther. 1998;23:385-9.
- Khanna S, Venojarvi M, Roy S, Sharma N, Trikha P, Bagchi D et al. Dermal wound healing properties of redox-active grape seed proanthocyanidins. Free Radic. Biol Med 2002;33:1089-96.
- Bentivegna SS,.Whitney KM. Subchronic 3-month oral toxicity study of grape seed and grape skin extracts. Food Chem. Toxicol. 2002;40:1731-43.
- Yamakoshi J, Saito M, Kataoka S, Kikuchi M. Safety evaluation of proanthocyanidin-rich extract from grape seeds. Food Chem. Toxicol. 2002;40:599-607.
- Kim JM,.White RH. Effect of vitamin E on the anticoagulant response to warfarin. Am J Cardiol. 1996;77:545-6.
- Corrigan JJ, Jr.,.Marcus FI. Coagulopathy associated with vitamin E ingestion. JAMA 1974;230:1300-1.
- Sharma G, Tyagi AK, Singh RP, Chan DC, Agarwal R. Synergistic anti-cancer effects of grape seed extract and conventional cytotoxic agent doxorubicin against human breast carcinoma cells. Breast Cancer Res Treat. 2004;85:1-12.
- Brooker S, Martin S, Pearson A, et al. Double-blind, placebo-controlled, randomised phase II trial of IH636 grape seed proanthocyanidin extract (GSPE) in patients with radiation-induced breast induration. Radiother Oncol. 2006;79(1):45-51.
- Li W, Xu B, Xu J, Wu XL. Procyanidins produce significant attenuation of doxorubicin-induced cardiotoxicity via suppression of oxidative stress. Basic Clin Pharmacol Toxicol. 2009 Mar;104(3):192-7.
- Song X, Siriwardhana N, Rathore K, Lin D, Wang HC. Grape seed proanthocyanidin suppression of breast cell carcinogenesis induced by chronic exposure to combined 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone and benzo[a]pyrene. Mol Carcinog. 2010 May;49(5):450-63.
- Kaur M, Tyagi A, Singh RP, et al. Grape seed extract upregulates p21 (Cip1) through redox-mediated activation of ERK1/2 and posttranscriptional regulation leading to cell cycle arrest in colon carcinoma HT29 cells. Mol Carcinog. 2011. [Epub ahead of print]
- Etheridge AS, Black SR, Patel PR, So J, Mathews JM. An in vitro evaluation of cytochrome P450 inhibition and P-glycoprotein interaction with goldenseal, Ginkgo biloba, grape seed, milk thistle, and ginseng extracts and their constituents. Planta Med. 2007 Jul;73(8):731-41.
- Bijak M, Bobrowski M, Borowiecka M, et al. Anticoagulant effect of polyphenols-rich extracts from black chokeberry and grape seeds. Fitoterapia. 2011 May 6. [Epub ahead of print]
- Mohamed ME, Frye RF. Effects of herbal supplements on drug glucuronidation. Review of clinical, animal, and in vitro studies. Planta Med. 2011 Mar;77(4):311-21.
- Walter RB, Brasky TM, Milano F, White E. Vitamin, mineral, and specialty supplements and risk of hematologic malignancies in the prospective VITamins And Lifestyle (VITAL) study.Cancer Epidemiol Biomarkers Prev. 2011;20(10):2298-308.
- Ozkan G, Ulusoy S, Alkanat M, et al. Antiapoptotic and antioxidant effects of GSPE in preventing cyclosporine A-induced cardiotoxicity. Ren Fail. 2012;34(4):460-6.
- Ulusoy S, Ozkan G, Ersoz S, et al. The effect of grape seed proanthocyanidin extract in preventing amikacin-induced nephropathy. Ren Fail. 2012;34(2):227-34.
- Feringa HH, Laskey DA, Dickson JE, Coleman CI. The effect of grape seed extract on cardiovascular risk markers: a meta-analysis of randomized controlled trials. J Am Diet Assoc. 2011 Aug;111(8):1173-81.
Consumer Information
How It Works
Bottom Line: Grape seed has not been shown to treat or prevent cancer.
Grape Seed Extract is derived from the oil that comes from ground red wine grapes. The extract contains a substance called proanthocyanidin which has antioxidant activities. Proanthocyanidins have also been shown to reduce cholesterol in patients with high cholesterol. Other substances within the grape seed may also help protect teeth from decay.
Purported Uses
- To lower high cholesterol
One study showed a combination of Grape Seed Extract and chromium to be effective at lowering cholesterol levels.
- As an antioxidant
One small study showed Grape Seed Extract to increase antioxidant levels in the blood.
- To treat atherosclerosis
Although studies have shown that substances found within grape seeds may have an effect in reducing the thickening of arteries, further study is needed to determine whether Grape Seed Extract will reduce atherosclerosis in humans.
- As a topical wound treatment
Animal studies have shown a possible effect, but further study is required to determine its effect in humans.
- As a laxative
No scientific evidence supports this use.
- As an antacid
This claim is not supported by research.
- To treat ulcers
There is no evidence to back this claim.
Research Evidence
Cardiovascular Health:
Nine randomized controlled trials involving 390 patients were included in this meta analysis. The studies had to report efficacy data on at least one of the following end points: systolic or diastolic blood pressure, heart rate, total cholesterol, low-density or high-density lipoprotein cholesterol, triglycerides, or CRP. Results showed that grape seed extract significantly lowered systolic blood pressure. No significant effect on diastolic blood pressure, lipid levels, or CRP was found.
Do Not Take If
- You are taking drugs that are substrates of Cytochrome P450 3A4 (Grape seed may increase the risk of side effects of these drugs).
- You are taking Warfarin or other blood thinners (Grape seed can increase the risk of bleeding).
- You are taking drugs that are substrates of UGT (Uridine 5'-diphospho-glucuronosyltransferase) enzymes (grape seed may increase the risk of side effects of these drugs).
Last updated: October 15, 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)acid (A-sid)
A chemical that gives off hydrogen ions in water and forms salts by combining with certain metals. Acids have a sour taste and turn certain dyes red. Some acids made by the body, such as gastric acid, can help organs work the way they should. An example of an acid is hydrochloric acid. Acidity is measured on a scale called the pH scale. On this scale, a value of 7 is neutral, and a pH value of less than 7 to 0 shows increasing acidity.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)analysis (uh-NA-lih-sis)
A process in which anything complex is separated into simple or less complex parts.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)anticoagulant (AN-tee-koh-A-gyuh-lunt)
A substance that is used to prevent and treat blood clots in blood vessels and the heart. Also called blood thinner.
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)arginine (AR-jih-neen)
One of the twenty common amino acids (building blocks of proteins). Arginine is being studied as a nutritional supplement in the treatment and prevention of cancer and other conditions. Also called L-arginine.
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)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 pressure (blud PREH-sher)
The force of circulating blood on the walls of the arteries. Blood pressure is taken using two measurements: systolic (measured when the heart beats, when blood pressure is at its highest) and diastolic (measured between heart beats, when blood pressure is at its lowest). Blood pressure is written with the systolic blood pressure first, followed by the diastolic blood pressure (for example 120/80).
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)breast cancer (brest KAN-ser)
Cancer that forms in tissues of the breast, usually the ducts (tubes that carry milk to the nipple) and lobules (glands that make milk). It occurs in both men and women, although male breast cancer is rare.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)calcium (KAL-see-um)
A mineral needed for healthy teeth, bones, and other body tissues. It is the most common mineral in the body. A deposit of calcium in body tissues, such as breast tissue, may be a sign of disease.
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)cardiotoxicity (KAR-dee-oh-tok-SIH-sih-tee)
Toxicity that affects the heart.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)cholesterol (koh-LES-teh-rol)
A waxy, fat-like substance made in the liver, and found in the blood and in all cells of the body. Cholesterol is important for good health and is needed for making cell walls, tissues, hormones, vitamin D, and bile acid. Cholesterol also comes from eating foods taken from animals such as egg yolks, meat, and whole-milk dairy products. Too much cholesterol in the blood may build up in blood vessel walls, block blood flow to tissues and organs, and increase the risk of developing heart disease and stroke.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)cyclosporine (SY-kloh-SPOR-een)
A drug used to help reduce the risk of rejection of organ and bone marrow transplants by the body. It is also used in clinical trials to make cancer cells more sensitive to anticancer drugs.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)DNA
The molecules inside cells that carry genetic information and pass it from one generation to the next. Also called deoxyribonucleic acid.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)double-blinded (DUH-bul BLINE-ded)
A clinical trial in which the medical staff, the patient, and the people who analyze the results do not know the specific type of treatment the patient receives until after the clinical trial is over.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)doxorubicin (DOK-soh-ROO-bih-sin)
A drug that is used to treat many types of cancer and is being studied in the treatment of other types of cancer. Doxorubicin comes from the bacterium . It damages DNA and may kill cancer cells. It is a type of anthracycline antitumor antibiotic. Also called Adriamycin PFS, Adriamycin RDF, doxorubicin hydrochloride, hydroxydaunorubicin, and Rubex.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)efficacy (EH-fih-kuh-see)
Effectiveness. In medicine, the ability of an intervention (for example, a drug or surgery) to produce the desired beneficial effect.
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)feces (FEE-seez)
The material in a bowel movement. Feces is made up of undigested food, bacteria, mucus, and cells from the lining of the intestines. Also called stool.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)follow-up (FAH-loh-up)
Monitoring a person's health over time after treatment. This includes keeping track of the health of people who participate in a clinical study or clinical trial for a period of time, both during the study and after the study ends.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)gastrointestinal (GAS-troh-in-TES-tih-nul)
Refers to the stomach and intestines. Also called GI.
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)homeostasis (HOH-mee-oh-STAY-sis)
A state of balance among all the body systems needed for the body to survive and function correctly. In homeostasis, body levels of acid, blood pressure, blood sugar, electrolytes, energy, hormones, oxygen, proteins, and temperature are constantly adjusted to respond to changes inside and outside the body, to keep them at a normal level.
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)intracellular (IN-truh-SEL-yoo-ler)
Inside a cell.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)lipid (LIH-pid)
Fat.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)modulate (MAH-juh-layt)
To adjust, or change.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)pulmonary (PUL-muh-NAYR-ee)
Having to do with the lungs.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)radiotherapy (RAY-dee-oh-THAYR-uh-pee)
The use of high-energy radiation from x-rays, gamma rays, neutrons, protons, and other sources to kill cancer cells and shrink tumors. Radiation may come from a machine outside the body (external-beam radiation therapy), or it may come from radioactive material placed in the body near cancer cells (internal radiation therapy). Systemic radiotherapy uses a radioactive substance, such as a radiolabeled monoclonal antibody, that travels in the blood to tissues throughout the body. Also called irradiation and radiation therapy.
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.
(http://www.cancer.gov/dictionary)serum (SEER-um)
The clear liquid part of the blood that remains after blood cells and clotting proteins have been removed.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)significant (sig-NIH-fih-kunt)
In statistics, describes a mathematical measure of difference between groups. The difference is said to be significant if it is greater than what might be expected to happen by chance alone. Also called statistically significant.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)supplementation (SUH-pleh-men-TAY-shun)
Adding nutrients to the diet.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)synergistic (SIH-ner-JIS-tik)
In medicine, describes the interaction of two or more drugs when their combined effect is greater than the sum of the effects seen when each drug is given alone.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)topical (TAH-pih-kul)
On the surface of the body.
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)warfarin (WOR-fuh-rin)
A drug that prevents blood from clotting. It belongs to the family of drugs called anticoagulants (blood thinners).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)will (wil)
A legal document in which a person states what is to be done with his or her property after death, who is to carry out the terms of the will, and who is to care for any minor children.
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)wound (woond)
A break in the skin or other body tissues caused by injury or surgical incision (cut).
Source: The National Cancer Institute's Dictionary of Cancer Terms
(http://www.cancer.gov/dictionary)
