What Is Grape Seed Extract?
Grapes have been cultivated and eaten for a long time. But grapes, along with other parts of the Vitis vinifera plant such as the leaves and sap, have also been used in traditional medicine in Europe for thousands of years. From the Egyptians to the ancient Greeks, the healing power of grapes and wine were realized, and grapes and grapevines were used to treat a variety of conditions including inflammation, pain, constipation, infections, and even various diseases.
Today, grape seed extract is made primarily from the seeds of wine grapes. Grape seed extract has a rich antioxidant content, and these antioxidants have been studied for a number of therapeutic effects. Below we discuss what these antioxidants do in your body and highlight clinical data that supports the various uses of grape seed extract.
What Are The Active Ingredients In Grape Seed Extract?
The predominant class of molecules found in grape seed extract is polyphenols. Polyphenols are a broad group of substances found in plants. They include tannins, lignins, flavonoids such as quercetin (a flavonol found in many fruits and vegetable) and EGCG (epigallocatechin-3-gallate, a catechin found in green tea), cinnamic acids such as caffeic acid (found in coffee and other plants), coumarins, and stilbenoids such as resveratrol (present in grapes and also other berries).
More specifically, in grape seed extract one type of polyphenol called oligomeric proanthocyanidin (OPC) is present at higher concentrations than all the others. OPC is a powerful antioxidant responsible for most of the beneficial therapeutic effects of grape seed extract. Proanthocyanidins are also found in other common foods and spices like fruits and especially berries, nuts, cinnamon, cocoa, and tea (EGCG is also a proanthocyanidin). Like these other foods, proanthocyanidins are found in grape skins and juice, but grape seed extract contains a much higher concentration. In fact, 70-90% of grape seed extract may be proanythocyanidins. The rest of grape seed extract contains procyanidin, different forms of catechins, and other bioactives in smaller amounts.
What Do The Ingredients In Grape Seed Extract Do?
The polyphenols in grape seed extract, especially proanthocyanidin, have been shown to have a number of beneficial effects. By increasing the levels of antioxidants in your blood stream (and body), grape seed extract can help counteract the harmful effects of free radicals.
As a strong antioxidant, proanthocyanidin protects from free radicals such as reactive oxygen species, defending your body from free radical damage from such factors as sun exposure, pollution, and stress. Standardized extracts of grape seeds have also been shown to have a positive effect in treating a wide range of health problems related to free radical damage.
Research has implicated that grape seed extract may help:
- Protect heart tissue and the cardiovascular system
- Defend against the damaging effects of diabetes
- Prevent bacterial and viral infections
- Decrease the incidence of various tumors
- Promote your defenses against the effects of sun exposure
- Mitigate aging effects in the skin by protecting collagen and elastin
- Reduce inflammation
- Improve cholesterol levels
- Increase fat metabolism
- Prevent dental cavities
- Protect neurons
- Treat hypertension (high blood pressure)
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Research: Clinical Studies Showing the Effectiveness of Grape Seed Extract
There has been an extensive amount of clinical research conducted with grape seed extract (GSE) on a wide range of conditions. Here is a sample of some of the benefits that have been shown in each of the following areas:
Cardiovascular
One study demonstrated that active compounds in GSE help blood vessels relax. The researchers concluded that these compounds present in grape seed extract “individually or in the form of wines, juices, or nutritional supplements, may be useful in preventing or treating cardiovascular diseases.” Other studies have found that GSE aids relaxation of the circulatory system and helps regulate blood pressure. And still others have shown that GSE can protect heart tissue from toxins and even lead exposure. 1,2,3,4
The antioxidant properties of GSE have also been known to exert cardio-protective effects that defend against the adverse effects of various cardiac disorders. One study indicated that “grape seed polyphenols (GSP) could protect against cardiac cell apoptosis via the induction of endogenous antioxidant enzymes.” 5
Diabetes
A study found GSE ameliorated certain types of cardiac damage in diabetic animals. The study “may provide a new recognition of natural medicine for the treatment of diabetic cardiomyopathy.” In fact, GSE may be beneficial to everyone (especially those with high blood sugar levels) by reducing oxidative damage to the entire cardiovascular system. 6,7,8
Fat And Cholesterol
GSE has been shown to help burn stored fat (increase lipolysis) and also to reduce food intake. In one study, GSE was shown to reduce the amount of food overweight individuals consumed by 4%. The authors conclude that “grape seed could be effective in reducing 24 hour energy intake in normal to overweight dietary unrestrained subjects, and could, therefore, play a significant role in body-weight management.” 9
One study in animals also showed that procyanidins from grape seeds lowered plasma triglycerides, free fatty acids, apolipoprotein B (apoB), LDL-cholesterol, and other types of cholesterol while slightly increasing HDL-cholesterol. Another study also showed that “oral administration of a grape seed procyanidin extract (GSPE) drastically decreases plasma levels of triglycerides (TG) and apolipoprotein B (ApoB).” And a further study in humans concluded that “a combination of chromium and GSE can decrease total cholesterol and LDL levels significantly” in people with high cholesterol. 10,11,12
Inflammation
A study was also run with GSE to test its effect on inflammatory mediators in rats fed a high-fat diet. The results showed that the procyanidins from grape seeds had a beneficial effect on low-grade inflammatory disease by inhibiting certain pro-inflammatory proteins and enhancing the production of an anti-inflammatory cytokine. Another study also demonstrated the anti-inflammatory properties of grape seed procyanidins and concluded they have potential health benefits in certain inflammatory conditions. 13,14
Oral Hygiene
Unfriendly bacteria in your mouth has been shown to cause cavities and various oral diseases, but also to release toxins that enter the blood stream and even damage the cardiovascular system. One study found grape seed extract can reduce the harm caused by these bacterial toxins and concluded that proanthocyanidins from grape seeds “have potent antioxidant properties and should be considered a potential agent in the prevention of periodontal diseases.” 15
Wounds
Topically, grape seed extract has been shown to help wounds heal faster and more completely by accelerating wound contraction and closure, increasing cell density and connective tissue deposition, and via multiple other mechanisms. In summary, the “study provides firm evidence to support that topical application of GSPE (grape seed proanthycyanidin extract) represents a feasible and productive approach to support dermal wound healing. 16
Melasma (Chloasma)
A study conducted in Japan showed that oral administration of grape seed extract is “effective in reducing the hyperpigmentation of women with chloasma.” The beneficial effects were achieved after 6 months of use. The study also found that “GSE intake for 5 months may prevent chloasma from becoming worse prior to the summer season.” 17
Protection From Sun Exposure And Photoaging
GSE has also been shown to fight oxidative stress and preserve important natural antioxidants in the body. In turn, it was shown to significantly reduce the incidence of skin tumors in mice exposed to UVB light after receiving supplemental grape seed extract. The lead author concludes that grape seed extract inhibits the process of skin aging and photoaging. Dr. Katiyar says: “Clinically, the photoaging component of skin aging accounts for the development in sun-exposed areas of wrinkling, mottled hyperpigmentation and depigmentation, coarsening of the skin, roughness, poor elastic recoil, and bruisability…Polyphenols [including those in grape seed extract] have anti-inflammatory and antioxidant properties. Because of these characteristics, polyphenols have been shown to inhibit, reverse, or slow down the risk of UV-induced skin carcinogenesis.” 18
A study in the Journal of Medicinal Food summarized many of the beneficial effects of grape seed extract that have been studied so far. In general, GSE is a powerful antioxidant with properties that have been shown to protect the body from disease and premature aging. The researchers summarize the remarkable power and properties of GSE by saying, “Scientific studies have shown that the antioxidant power of proanthocyanidins is 20 times greater than vitamin E and 50 times greater than vitamin C. Extensive research suggests that grape seed extract is beneficial in many areas of health because of its antioxidant effect to bond with collagen, promoting youthful skin, cell health, elasticity, and flexibility. Other studies have shown that proanthocyanidins help to protect the body from sun damage, to improve vision, to improve flexibility in joints, arteries, and body tissues such as the heart, and to improve blood circulation by strengthening capillaries, arteries, and veins.” 19
In another study, oligomeric proanthocyanidins (OPCs) from grape seeds were shown to be potent antioxidants that effectively protect skin cells from oxidative stress; the researchers demonstrated via a number of different mechanisms that OPCs have the potential to protect human melanocytes from UV light and inhibit skin damage and melanogenesis. 20
Ultraviolet-radiation-induced immunosuppression has been linked with the risk of developing skin cancer. In this study, administration of grape seed proanthocyanidins significantly inhibited the development of UV-induced skin tumors as well as reduced immune system suppression. The researchers conclude that this information has “important implications for the use of GSPs as a dietary supplement in chemoprevention of UV-induced immunosuppression as well as photocarcinogenesis.” 21
The results of another study, “suggest that GSPs could be useful in the attenuation of UV-radiation-induced oxidative stress-mediated skin diseases in human skin.” 22
Further results showed that red grape seed extract (from Vitis vinifera L of the Burgund Mare variety) “reduced the formation of sunburn cells in skin” and suggest that grape seed extract “might be a potential chemo-preventive candidate in reducing the oxidative stress and apoptosis induced by multiple doses of UVB in skin.” 23
Additionally, the results from another study “clearly suggest that dietary GSPs inhibit photocarcinogenesis in mice through the inhibition of UVB-induced inflammation and mediators of inflammation in mouse skin.” 24
Safety and Dosing
Studies with grape seed extract have shown efficacy with a wide range of doses. GSE is commonly taken in capsules or tablets containing serving sizes of 50 to 100mg, and may be sold by itself or in combination with other ingredients, including in this anti-aging product. Grape seed extract is generally considered very safe to consume, even at higher doses. Grape seed extract and grape seed proanthocyanidins haven’t shown any short or long-term toxicity.
People allergic to grapes should not take grape seed extract. Because proanthocyanidins can limit platelet adhesion, grape seed extract may act as a blood-thinner, increasing clotting time. While this has cardio-protective benefits, people taking blood thinners should ask their doctors about any potential effects. Interactions between grape seed extract and other supplements and medications have not been extensively studied.
Summary
Grape seed extract contains healthy ingredients called polyphenols, including a powerful antioxidant called proanthocyanidin. To date, research has shown a variety of benefits of grape seed extract, due in part to its powerful free-radical-fighting properties. In particular, data show grape seed extract to be useful in preventing or treating many different conditions, including those in areas involving cardio-protection, decreasing inflammation, the prevention of sun damage and skin aging, and fat metabolism and the maintenance of healthy blood sugar levels. Ongoing research will undoubtedly reveal additional benefits.
References
1. Ann N Y Acad Sci. 2002 May;957:78-89. Vasodilating procyanidins derived from grape seeds. Fitzpatrick DF1, Bing B, Maggi DA, Fleming RC, O’Malley RM. http://www.ncbi.nlm.nih.gov/pubmed/12074963
2. Clin Sci (Lond). 2008 Feb;114(4):331-7. Mechanism of the endothelium-dependent relaxation evoked by a grape seed extract. Edirisinghe I1, Burton-Freeman B, Tissa Kappagoda C. http://www.ncbi.nlm.nih.gov/pubmed/17927567
3. Life Sci. 2007 Nov 30;81(23-24):1615-21. Epub 2007 Oct 10. Grape seed proanthocyanidins ameliorates isoproterenol-induced myocardial injury in rats by stabilizing mitochondrial and lysosomal enzymes: an in vivo study. Karthikeyan K1, Sarala Bai BR, Niranjali Devaraj S. http://www.ncbi.nlm.nih.gov/pubmed/17991491
4. Pak J Biol Sci. 2008 Mar 15;11(6):882-7. Effect of grape seed extract on lead induced hypertension and heart rate in rat. Badavi M1, Mehrgerdi FZ, Sarkaki A, Naseri MK, Dianat M. http://www.ncbi.nlm.nih.gov/pubmed/18814650
5. J Agric Food Chem. 2007 Mar 7;55(5):1695-701. Epub 2007 Feb 13. Grape seed polyphenols protect cardiac cells from apoptosis via induction of endogenous antioxidant enzymes. Du Y1, Guo H, Lou H. http://www.ncbi.nlm.nih.gov/pubmed/17295515
6. J Agric Food Chem. 2007 Mar 7;55(5):1695-701. Epub 2007 Feb 13. Grape seed polyphenols protect cardiac cells from apoptosis via induction of endogenous antioxidant enzymes. Du Y1, Guo H, Lou H. http://www.ncbi.nlm.nih.gov/pubmed/17295515
7. J Cardiovasc Pharmacol. 2007 Nov;50(5):503-9. Cardioprotective effects of grape seed proanthocyanidins extracts in streptozocin induced diabetic rats. Cheng M1, Gao HQ, Xu L, Li BY, Zhang H, Li XH. http://www.ncbi.nlm.nih.gov/pubmed/18030059
8. J Cardiovasc Pharmacol. 2007 Oct;50(4):434-40. Inhibitory effect of GSPE on RAGE expression induced by advanced glycation end products in endothelial cells. Zhang FL1, Gao HQ, Shen L. http://www.ncbi.nlm.nih.gov/pubmed/18049312
9. Eur J Clin Nutr. 2004 Apr;58(4):667-73. The effect of grape-seed extract on 24 h energy intake in humans. Vogels N1, Nijs IM, Westerterp-Plantenga MS. http://www.ncbi.nlm.nih.gov/pubmed/15042136
10. FASEB J. 2005 Mar;19(3):479-81. Epub 2005 Jan 6. Grape seed procyanidins improve atherosclerotic risk index and induce liver CYP7A1 and SHP expression in healthy rats. Del Bas JM1, Fernández-Larrea J, Blay M, Ardèvol A, Salvadó MJ, Arola L, Bladé C. http://www.ncbi.nlm.nih.gov/pubmed/15637110
11. Mol Nutr Food Res. 2008 Oct;52(10):1172-81. doi: 10.1002/mnfr.200800054. Dietary procyanidins lower triglyceride levels signaling through the nuclear receptor small heterodimer partner. Del Bas JM1, Ricketts ML, Baiges I, Quesada H, Ardevol A, Salvadó MJ, Pujadas G, Blay M, Arola L, Bladé C, Moore DD, Fernandez-Larrea J. http://www.ncbi.nlm.nih.gov/pubmed/18720348
12. J Med. 2000;31(5-6):227-46. Effects of niacin-bound chromium and grape seed proanthocyanidin extract on the lipid profile of hypercholesterolemic subjects: a pilot study. Preuss HG1, Wallerstedt D, Talpur N, Tutuncuoglu SO, Echard B, Myers A, Bui M, Bagchi D. http://www.ncbi.nlm.nih.gov/pubmed/11508317
13. J Nutr Biochem. 2009 Mar;20(3):210-8. doi: 10.1016/j.jnutbio.2008.02.005. Epub 2008 Jul 7. Grape-seed procyanidins prevent low-grade inflammation by modulating cytokine expression in rats fed a high-fat diet. Terra X1, Montagut G, Bustos M, Llopiz N, Ardèvol A, Bladé C, Fernández-Larrea J, Pujadas G, Salvadó J, Arola L, Blay M. http://www.ncbi.nlm.nih.gov/pubmed/18602813
14. J Agric Food Chem. 2007 May 30;55(11):4357-65. Epub 2007 Apr 27. Grape-seed procyanidins act as antiinflammatory agents in endotoxin-stimulated RAW 264.7 macrophages by inhibiting NFkB signaling pathway. Terra X1, Valls J, Vitrac X, Mérrillon JM, Arola L, Ardèvol A, Bladé C, Fernandez-Larrea J, Pujadas G, Salvadó J, Blay M. http://www.ncbi.nlm.nih.gov/pubmed/17461594
15. J Periodontol. 2006 Aug;77(8):1371-9. Protective effects of grape seed proanthocyanidins against oxidative stress induced by lipopolysaccharides of periodontopathogens. Houde V1, Grenier D, Chandad F. http://www.ncbi.nlm.nih.gov/pubmed/16881806
16. Free Radic Biol Med. 2002 Oct 15;33(8):1089-96. Dermal wound healing properties of redox-active grape seed proanthocyanidins. Khanna S1, Venojarvi M, Roy S, Sharma N, Trikha P, Bagchi D, Bagchi M, Sen CK. http://www.ncbi.nlm.nih.gov/pubmed/12374620
17. Phytother Res. 2004 Nov;18(11):895-9. Oral intake of proanthocyanidin-rich extract from grape seeds improves chloasma. Yamakoshi J1, Sano A, Tokutake S, Saito M, Kikuchi M, Kubota Y, Kawachi Y, Otsuka F. http://www.ncbi.nlm.nih.gov/pubmed/15597304
18. Sharma SD, Meeran SM, Katiyar SK. Dietary grape seed proanthocyanidins inhibit UVB-induced oxidative stress and activation of mitogen-activated protein kinases and nuclear factor-{kappa}B signaling in in vivo SKH-1 hairless mice. Mol Cancer Ther. 2007 Mar;6(3):995-1005 http://www.ncbi.nlm.nih.gov/pubmed/17363493
19. J Med Food. 2003 Winter;6(4):291-9. Polyphenolics in grape seeds-biochemistry and functionality. Shi J1, Yu J, Pohorly JE, Kakuda Y. http://www.ncbi.nlm.nih.gov/pubmed/14977436
20. Int J Mol Med. 2009 Feb;23(2):197-204. Oligomeric proanthocyanidins from grape seeds effectively inhibit ultraviolet-induced melanogenesis of human melanocytes in vitro. Zi SX1, Ma HJ, Li Y, Liu W, Yang QQ, Zhao G, Lian S. http://www.ncbi.nlm.nih.gov/pubmed/19148543
21. Photochem Photobiol. 2015 Jan-Feb;91(1):156-62. doi: 10.1111/php.12330. Epub 2014 Sep 8. Proanthocyanidins from grape seeds inhibit UV-radiation-induced immune suppression in mice: detection and analysis of molecular and cellular targets. Katiyar SK. http://www.ncbi.nlm.nih.gov/pubmed/25112437
22. Free Radic Biol Med. 2006 May 1;40(9):1603-14. Epub 2006 Jan 26. Grape seed proanthocyanidins inhibit UV-radiation-induced oxidative stress and activation of MAPK and NF-kappaB signaling in human epidermal keratinocytes. Mantena SK1, Katiyar SK. http://www.ncbi.nlm.nih.gov/pubmed/16632120
23. J Photochem Photobiol B. 2011 Nov 3;105(2):133-42. doi: 10.1016/j.jphotobiol.2011.08.002. Epub 2011 Aug 26. The effects of grape seeds polyphenols on SKH-1 mice skin irradiated with multiple doses of UV-B. Filip A1, Daicoviciu D, Clichici S, Bolfa P, Catoi C, Baldea I, Bolojan L, Olteanu D, Muresan A, Postescu ID. http://www.ncbi.nlm.nih.gov/pubmed/21925895
24. Pharm Res. 2010 Jun;27(6):1092-102. doi: 10.1007/s11095-010-0050-9. Epub 2010 Feb 9. Dietary grape seed proanthocyanidins inhibit UVB-induced cyclooxygenase-2 expression and other inflammatory mediators in UVB-exposed skin and skin tumors of SKH-1 hairless mice. Sharma SD1, Katiyar SK. http://www.ncbi.nlm.nih.gov/pubmed/20143255
Additional References
Baliga, Manjeshwar S.; Katiyar, Santosh K. (2006). “Chemoprevention of photocarcinogenesis by selected dietary botanicals”. Photochemical & Photobiological Sciences 5 (2): 243–53. doi:10.1039/b505311k. PMID 16465310.
Mantena SK, Katiyar SK. Grape seed proanthocyanidins inhibit UV-radiation-induced oxidative stress and activation of MAPK and NF-kappaB signaling in human epidermal keratinocytes. Free Radic Biol Med. 2006 June 1;40(9):1603-14.
Katiyar, Santosh K. (2008). “Grape seed proanthocyanidines and skin cancer prevention: Inhibition of oxidative stress and protection of immune system”. Molecular Nutrition & Food Research. 52 Suppl 1: S71–6. doi:10.1002/mnfr.200700198. PMC 2562900. PMID 18384090.
Smullen, J.; Koutsou, G.A.; Foster, H.A.; Zumbé, A.; Storey, D.M. (2007). “The Antibacterial Activity of Plant Extracts Containing Polyphenols against Streptococcus mutans”. Caries Research 41 (5): 342–9. doi:10.1159/000104791. PMID 17713333
Su, X; d’Souza, DH (2011). “Grape seed extract for control of human enteric viruses”. Applied and environmental microbiology 77 (12): 3982–7. doi:10.1128/AEM.00193-11. PMC 3131668. PMID 21498749.
Nair, Madhavan P; Kandaswami, Chithan; Mahajan, Supriya; Nair, Harikrishna N; Chawda, RAM; Shanahan, Thomas; Schwartz, Stanley A (2002). “Grape seed extract proanthocyanidins downregulate HIV- 1 entry coreceptors, CCR2b, CCR3 and CCR5 gene expression by normal peripheral blood mononuclear cells”. Biological Research 35 (3–4): 421–31. doi:10.4067/S0716-97602002000300016. PMID 12462994.
Al-Habib A, Al-Saleh, E (2010). “Bactericidal effect of grape seed extract on methicillin-resistant Staphylococcus aureus (MRSA)”. Journal of Toxicology Science 357 (3): 357–64. PMID 20519844.
Eur J Clin Nutr. 2006 Oct;60(10):1201-6. Epub 2006 May 3. Effect of a novel dietary supplement on skin aging in post-menopausal women. Skovgaard GR1, Jensen AS, Sigler ML.
Biosci Biotechnol Biochem. 2003 May;67(5):1140-3. Procyanidin B1 is detected in human serum after intake of proanthocyanidin-rich grape seed extract. Sano A1, Yamakoshi J, Tokutake S, Tobe K, Kubota Y, Kikuchi M.
J Agric Food Chem. 2011 Oct 12;59(19):10594-603. doi: 10.1021/jf202697j. Epub 2011 Sep 12. Analysis of Flavan-3-ols and procyanidins in food samples by reversed phase high-performance liquid chromatography coupled to electrospray ionization tandem mass spectrometry (RP-HPLC-ESI-MS/MS). Rzeppa S1, Von Bargen C, Bittner K, Humpf HU.
Concentrations of Proanthocyanidins in Common Foods and Estimations of Normal Consumption1,2 Liwei Gu, Mark A. Kelm*, John F. Hammerstone*, Gary Beecher†, Joanne Holden†, David Haytowitz†, Susan Gebhardt†, and Ronald L. Prior3 The Journal of Nutrition March 1, 2004
Chapla Agarwal, Rana P. Singh, and Rajesh Agarwal, Grape seed extract induces apoptotic death of human prostate carcinoma DU145 cells via caspases activation accompanied by dissipation of mitochondrial membrane potential and cytochrome c release, Carcinogenesis (2002) 23 (11): 1869-1876. doi: 10.1093/carcin/23.11.1869.
Sharma SD, Meeran SM, Katiyar SK. Dietary grape seed proanthocyanidins inhibit UVB-induced oxidative stress and activation of mitogen-activated protein kinases and nuclear factor-{kappa}B signaling in in vivo SKH-1 hairless mice. Mol Cancer Ther. 2007 Mar;6(3):995-1005
J Physiol Pharmacol. 2011 Jun;62(3):385-92. Chemopreventive effects of Calluna vulgaris and Vitis vinifera extracts on UVB-induced skin damage in SKH-1 hairless mice. Filip A1, Clichici S, Daicoviciu D, Catoi C, Bolfa P, Postescu ID, Gal A, Baldea I, Gherman C, Muresan A. http://www.ncbi.nlm.nih.gov/pubmed/21893700
Mini Rev Med Chem. 2011 Dec;11(14):1200-15. Polyphenols: skin photoprotection and inhibition of photocarcinogenesis. Afaq F1, Katiyar SK. http://www.ncbi.nlm.nih.gov/pubmed/22070679
Arch Dermatol Res. 2010 Mar;302(2):71-83. doi: 10.1007/s00403-009-1001-3. Epub 2009 Nov 7. Skin photoprotection by natural polyphenols: anti-inflammatory, antioxidant and DNA repair mechanisms. Nichols JA1, Katiyar SK. http://www.ncbi.nlm.nih.gov/pubmed/19898857
