OPC is unique among biological nutrients contained in nutritional supplements in that extensive laboratory and clinical research has been ongoing for more than fifty years to support the structure and function claims made for its multiple potential health benefits. Summarized here are some of the most important health benefits of OPC that are found in greater detail in the more than 100 research articles reviewed in the new book by Glen A. Halvorson M.D. "OPC: The Real Story About Nature's Most Powerful Antioxidant."

OPC has not been prominently featured in cancer research since it has been found to have overwhelmingly positive effects on cardiovascular and musculoskeletal health. Its potential chemopreventive properties are currently under review because of the renewed interest in flavonoids as chemopreventive agents. Key research includes the following:

Huynh, et al., showed that Pycnogenol® inhibits nitrogen- containing compounds from causing cancer in the gastro- intestinal tract of rats. Nitrogen compounds are known to increase risk in humans for both gut and lung cancers.

Nelson, et al., found that Pycnogenol® protected DNA single and double strands from breaking in the presence of oxygen free radical species. This breakage of genetic material is thought to be a possible factor in carcinogenesis (creation of cancer).

Jang, et al., review the properties of the chemical trans- Resveratrol (or Resveretrol) found recently in red wine and the skin of grapes. Cancer studies at the University of Illinois found Resveratrol prevented cancer from starting in normal cells, stopped already cancerous cells from growing, and caused already cancerous cells to revert back to normal.

Grape skin contained the highest amount of Resveratrol of over 1000 plants studied. The OPC in EIF comes from red grapes grown in the Rhone Valley of France that have a comparatively higher content of Resveratrol.

Please keep in mind Resveratrol was tested in cultured cells from mice with induced cancer; there have been no studies in humans. This does not mean Resveratrol doesn't fight cancer, but as of today, realistically speaking, there is more evidence to support its role in reducing heart disease than cancer. Resveratrol prevents platelet aggregation--another reason or excuse to drink red wine! Epidemiological studies do present strong evidence for a reduced risk of both cancer and heart disease in populations consuming higher than normal amounts of red wine on a daily basis (2-4 glasses per day).

Packer, et al., cite many references that support cancer- protective properties of flavonoids and polyphenols including OPC. Flavonoids in numerous studies inhibit the growth of tumor cells by various mechanisms including antioxidant properties, inhibition of enzymes that facilitate cellular metabolism, and ability to inhibit telomerase, an enzyme essential for promoting rapid growth of tumor cells.

A brief review of the multiple benefits of OPC should convince even the most skeptical scientist of the value of increasing daily intake of bioflavonoids, including OPC.

OPC inhibits damage to blood vessels and inhibits abnormal clotting of blood, both of which are related to heart disease. OPC inhibits excessive metabolizing of nitric oxide, a process linked to inflammation, arthritis, and Alzheimer's disease (Fitzpatrick).

OPC 100 mg given to smokers two hours after smoking inhibited clotting of platelets more effectively and faster than 500 mg of aspirin. A 200 mg dose of OPC was even more effective with effects lasting a week after the OPC was stopped (Watson, Putter). OPC corrects some forms of infertility in males by increasing the number of structurally normal sperm, a more cost effective treatment than expensive fertility drugs (Roseff)!

OPC is one of nature's most powerful antioxidants, inhibiting superoxide and hydroxyl forms of oxygen free radicals more effectively than either Vitamin C or E (Bagchi).

OPC inhibits lipid peroxidation of blood fats more effectively than Vitamin E (Bagchi).

OPC inhibits growth of cancer cells in the laboratory while simultaneously enhancing the growth and viability of normal human gastric mucosal cells (Ye).

OPC inhibits acetaminophen-induced liver death in lab mice (Ray).

OPC improved venous insufficiency in 80% of patients treated for just 10 days with 100 mg of OPC. Itching, heaviness and pain disappeared with rapid reduction of the swelling in lower limbs. Symptom improvement correlated with objective changes in videocapillaroscope examination of blood flow (Constantini).

Resveratrol, a chemical found in the skin of grapes, was shown to protect lipid and protein membranes against copper- induced oxidation (Fremont).

OPC binds to both collagen and elastin fibers in connective tissue to reduce their rate of degradation by inflammatory enzymes (Tixier).

OPC protects the lining of blood vessel walls from free radical damage (Rong).

OPC reduces diabetic retinal bleeding and improves vision within a few weeks on as little as 100 mg per day (Froantin).

OPC reduces peripheral edema in several studies involving over 4,000 patients (Henreit).

OPC increases capillary resistance, resulting in lower systolic blood pressure (Lagrue).

OPC reduces severity and duration of soft tissue injuries in soccer players treated immediately following injury with 400 mg per day tapering over several weeks to 200 mg per day of OPC from grape seed extract (Parienti).

OPC reduces symptoms in gastric ulcers (Saito).

OPC reduces post-surgical swelling and pain and speeds soft tissue recovery when elective facial surgery patients were pre- treated before and after surgery (Baruch).

OPC reduced symptoms of PMS in over 60% of patients treated with 200 mg of OPC for three months and in 80% of patients treated for six months (Amsellem).

OPC is an acronym for "oligomeric proanthocyanidins", a polyphenolic phytochemical extracted from many different plants of which the highest concentrations for supplement use are found in grape seed extract, entire grape extract, and pine bark extract.

OPC is distinct from other plant flavonoids because it is a flavan-3-ol. Flavanols differ from flavonoids in that flavanols are highly water-soluble, absorbable and bioavailable. OPC is quickly and readily distributed throughout the body within minutes to a few hours of oral ingestion. OPC also contains ellagitannins in lesser amounts than red raspberries.

OPC is a potent scavenger of free radicals. It is one of nature's most potent antioxidants. OPC contains multiple electron donor sites (hydroxyl sites) that allow it to bind to unstable molecules called free radicals by donating its hydrogen atoms. OPC also recycles other antioxidants such as Vitamin C and glutathione by removing the free radicals they bind with and freeing them up to interact again with other free radicals.

Examples of free radical scavenging activities of OPC include: traps hydroxyl and superoxide radicals; inhibits or delays onset of lipid peroxidation; chelates free iron molecules and inhibits iron-induced lipid peroxidation; reduces free radical production by inhibiting the enzyme xanthine oxidase; and inhibits degradative enzymes that produce free radicals through soft tissue damage (hyaluronidase, elastase, collagenase, protease).

OPC from grape seed extract contains the most potent antioxidant activity of the various polyphenols studied. In one study rat blood vessel walls were exposed to free radicals and the ability of grape seed extract, pine bark, and bilberry to protect the blood vessel walls from damaged was measured. Grape seed extract provided the best arterial wall defense against the damaging effects of free radicals and on an absolute scale, was 22% stronger than pine bark extract and 15% greater than bilberry extract (Jonadet).

OPC binds to protein tissue such as collagen, producing a wide range of benefits to health and anti-aging. OPC binds to the collagen in blood vessel walls, making capillaries stronger and more elastic, improving circulation, and reducing blood pressure. Since joint capsules, ligaments, and tendons are also made up of collagen, OPC typically improves joint elasticity and range of motion. Since skin is also predominantly collagen, OPC is billed in France as the internal cosmetic, making skin more elastic, softening wrinkles, and giving skin over time a more youthful appearance.

The protein-binding properties of OPC also affect protein receptor sites that control enzymes of inflammation and allergy. OPC blocks the release of histamine, resulting in reduced symptoms in allergies, ulcers, and asthma. OPC blocks the release of proteases and collagenases, resulting in reduced swelling, inflammation, and pain in arthritis.

OPC reduces pain, inflammation, swelling, and stiffness in joints made symptomatic from arthritis or injury in several documented ways. OPC is a potent anti-inflammatory that inhibits the release of degradative enzymes including collagenases, proteases, and elastases that damage soft tissues including joint cartilage and synovial joint linings. OPC is a potent antioxidant that inhibits free radical damage and inflammatory response following injury. OPC speeds recovery from acute injury by inhibiting or reducing the formation of soft tissue edema secondary to acute inflammation. OPC reduces symptoms of chronic joint stiffness and restores functional mobility by improving elasticity of connective tissues. OPC speeds up healing by increasing circulation to joints.

OPC may be the ultimate anti-aging nutrient. OPC improves the appearance of skin. OPC increases circulation to the brain and enhances cognitive functions such as memory and mood. OPC reduces joint stiffness associated with wear and tear of aging.OPC is a potent antioxidant that slows aging by inhibiting the damaging effects of free radicals.

Diabetics experienced reduced diabetic retinopathy and improved retinal appearance and clinical visual acuity after taking as little as 100 mg of OPC per day for six weeks. OPC may enhance peripheral circulation and reduce symptoms of diabetic neuropathy.

OPC has no known side effects such as mutagenecity, carcinogenecity, cellular toxicity or allergic reactions in over fifty years of clinical and laboratory research. Toxicity studies in animals indicate OPC has an extremely high LD50. This means that humans would have to take literally hundreds of thousands of milligrams daily to be adversely effected. OPC is safe to take during pregnancy and breast feeding, unless combined with other herbal ingredients that may be contraindicated during pregnancy.

OPC works best when taken at saturation levels of at least one milligram per pound of body weight per day. A person weighing 200 pounds would take 100 mg twice daily for a total daily dose of 200 milligrams. Therapeutic levels, 300-600 mg of OPC per day, are frequently prescribed by European physicians for medical conditions they think might respond to OPC. Maintenance levels of 100 mg per day are recommended for healthy, younger individuals taking OPC along with other supplements for nutritional insurance.

Selected References

Amsellem M et al. Endotelon in the treatment of venolymphatic problems in premenstrual syndrome. Multicentered study on 165 patients. Tempo Medical 282: Nov 1987.

Bagchi D et al. Oxygen free radical scavenging abilities of vitamins C and E, and a grape seed extract proanthocyanidin extract in vitro. Molecular Pathology and Pharmacology 95: 179-189, 1997.

Baruch J. Effet de 'Endotelon dans les oedemes post-chirurgicaux. Resultats d'une etude en double aveugle contre placebo sur trente-dewx patientes. Ann Chir Plast Estbet 29: 4, 1984.

Chen G et al. Ability of m-chloroperoxybenzoic acid to induce the ornithine decarboxylase marker of skin tumor promotion and inhibition of this response by gallotannins, oligomeric proanthocyanidins, and their monomeric units in mouse epidermis in vivo. Anticancer Res 15(4): 1183- 1189, 1995.

Constantini A et al. Clinical and capillaroscopic evaluation of chronic uncomplicated venous insufficiency with procyanidins extracted from vitis vinifera. Minerva Cardioangiol 47(1-2): 39-46, 1999.

Fitzpatrick DF et al. Endothelium-dependent vascular effects of Pycnogenol. J Cardiovasc Pharmacol 32(4): 509-515, 1998.

Froantin M. Les oligomeres procyanidoliques dans le traitement de la fragilite capillaire et de la retinopathie chez les diabetiques. A propos de 26 cas. Med Int 16(11): 432-434, 1981.

Groult N et al. Study of the effect of procyanidole oligomers on cultured mesenchymatous cells. Size and shape of cells and nuclei. Quantitative morphological study. Path Biol 39(4): 277-282, 1991.

Hagerman AE et al. The specificity of proanthocyanidin-protein interactions. J Biol Chem 256(9): 4494-4497.

Henreit JP. Veno-lymphatic insufficiency. 4,729 patients undergoing hormonal and procyanidole oligomer therapy. Phlebologie 46: 313-325, 1993.

Huynh HT et al. Effects of intragastrically administered Pycnogenol on NNK metabolism in F344 rats. Anticancer Res 19: 2095-2099, 1999.

Huynh HT et al. Effects of pycnogenol on the microsomal metabolism of the tobacco-specific nitrosamine NNK as a function of age. Cancer Lett 132(1-2): 135-139, 1998.

Jonadet M et al. Anthocyanosides extracted from Vitis vinifera, Vaccinium myrtillus and Pinus maritimus. I. Elastase-inhibiting activities in vitro. II. Compared angioprotective activities in vivo. J Pharm Belg 38(1): 41-46, 1983.

Lagrue G et al. A study of the effects of procyanidole oligomers on capillary resistance in hypertension and in certain nephropathies. Sem Hop Paris 57: 1399-1401, 1981.

Liviero L et al. Antimutagenic activity of procyanidins from Vitis vinifera. Fitother 65: 203-209, 1994. Maffei Facino R et al. Free radical scavenging action and anti-enzyme activities of procyanidins from Vitis vinifera. A mechanism for capillary- protective action. Drug Res 44: 592-601, 1994.

Mangiapane H et al. The inhibition of the oxidation of low density lipoprotein by (+)-catechin, a naturally occurring flavonoid. Biochemical Pharmacology 43(3): 445-450, 1992.

Masquelier J et al. Stabilization of collagen by procyanidolic oligomers. Acta Therap. 7: 101-105, 1981.

Meunier MT et al. Free radical scavenger activity of procyanidolic oligomers and anthocyanosides with respect to superoxide anion and lipid peroxidation. Plant Med Phytother 23(4): 267-274, 1989.

Nelson AB et al. Pycnogenol inhibits macrophage oxidative burst, lipoprotein oxidation and hydroxyl radical induced DNA damage. Drug Develop Ind Med 24: 1-6, 1998.

Nuttall SL et al. An evaluation of the antioxidant activity of a standardized grape seed extract, Leucoselect. J Clin Pharm Ther 23(5): 385-389, 1998.

Packer L et al. Antioxidant activity and biological properties of a procyanidin-rich extract from pine (Pinus maritima) bark, pycnogenol. Free Rad Biol Med 27(5-6): 704-724, 1999.

Parienti JJ et al. Post-traumatic edema in athletes: controlled study of Endotelon. Gaz. Med. de France 90(3): 1, 1983.

Plumb GW et al. Antioxidant properties of catechins and proanthocyanidins: effect of polymerisatin, galloylation and glycosylation. Free Radic Res 29(4): 351-358, 1998.

Putter M et al. Inhibition of smoking-induced platelet aggregation by aspirin and pycnogenol. Thromb Res 15(4): 155-156, 1999.

Rao AV and MT Yatcilla. Bio-absorption and in vivo antioxidant properties of BioVin® polyphenols: A human intervention study. Submitted to J of Medicinal Plants, July 2, 1999.

Ray SD et al. A novel proanthocyanidin IH636 grape seed extract increases in vivo Bcl-X1 expression and prevents acetaminophen-induced programmed and unprogrammed cell death in mouse liver. Arch Biochem Biophys 369(1): 42-58, 1999.

Rong Y et al. Pycnogenol protects vascular endothelial cells from t-butyl hydroperoxide induced oxidant injury. Biotechnol Ther 5(3-4): 117-126, 1994.

Saito M et al. Anti-ulcer activity of grape seed extract and procyanidins. J Agric Food Chem 46: 1460-1464, 1998.

Tixier JM et al. Evidence by in vivo and in vitro studies that binding of pycnogenols to elastin affects its rate of degradation by elastases. Biochem Pharmacol 33(24): 3933-3939, 1984.

Virgili F et al. Procyanidins extracted from Pinus maritima (Pycnogenol): scavengers of free radical species and modulators of nitrogen monoxide metabolism in activated murine RAW 264.7 macrophages. Free Radic Biol Med 24: 1120-1129, 1998.

Ye X et al. The cytotoxic effects of a novel IH 636 grape seed proanthocyanidin extract on cultured human cancer cells. Mol Cell Biochem 196(1-2): 99-108, 1999.