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Grape seeds are the primary commercial source of a group of antioxidant, collagen-protective pigments called oligomeric proanthocyanidins (OPCs or PCO), which are concentrated in pine bark and grapes. OPCs and related phenolic flavonols are also found in berries, blackcurrant, green tea, black tea, and many other plants.

On This Page
Traditional Use
Modern Perspective
Daily Requirement
Facts About Grape Seed and Aging
Recent Findings
Safety
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Traditional use
There are no traditional medicinal uses of OPCs, except to the extent that berries, grapes, and other food sources have been perceived as generally healthful.
 
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Modern perspective
For more than 50 years, European biochemists have been conducting research into OPCs, which are also generically termed pycnogenol. (When capitalized, the term Pycnogenol refers to a patented pine bark extract.) Supplemental OPCs are used in Europe to treat weak blood capillaries (chronic venous insufficiency), post-surgical edema (swelling), cirrhosis, varicose veins and diabetic retinopathy.

OPCs restore the antioxidant function of vitamin C molecules worn out by their free radical scavenging activities. In one experiment, OPCs boosted vitamin C activity by 1,000%. Test tube studies indicate that OPCs are 18 times more effective than vitamin C, and 50 times more potent than Vitamin E, for neutralizing free oxygen radicals.

OPCs’ anti-inflammatory properties have been proved in laboratory studies on test animals and in human clinical trials involving sports injuries and post-surgical recovery. Given their mode of anti-inflammatory action and affinity for collagen, OPCs may be useful in reducing rheumatic inflammations.

OPCs promote healthy cartilage by normalizing "collagen cross-linkage." Collagen consists of twin, ladder-like spirals of proteins connected by step-like cross links. In osteoarthritis and rheumatoid arthritis, excess cross-linkage is caused by internal production of excess free radicals, and release of excess amounts of collagenase enzyme.

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Daily requirement
Flavonols, including grape seed OPCs and green tea catechins, are not classified as essential nutrients, since their absence does not produce a deficiency state. However, OPCs may have many health benefits, and anyone not eating a wide variety of plants will not derive these benefits.

Medically, OPCs are usually prescribed at a dosage level of 300 mg per day, and a reasonable preventive health regimen would range from 50 to 100 mg per day.

Types of products: Currently, pine bark extracts rich in OPCs (i.e., Pycnogenol) dominate the U.S. market. But grape skin/seed extracts contain equivalent amounts, including a unique antioxidant (B2-3’-o-gallate) that makes them a more desirable source of OPCs. Most research has been done on grape skin/seed extract, and it is less expensive.

OPCs are reported to produce better antioxidant effects in body tissues when packaged in a patented chemical envelope called a phytosome. OPC phytosomes may be twice as effective as straight OPC extract, but this enhanced efficiency per milligram must be weighed against the cost differential.

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Facts About Grape Seed and Aging
Grape Seed Extract contains oligomeric proanthocyanidins (OPCs) which are a class of flavonoids (water-soluble compounds) found in a wide variety of plants. OPCs have powerful antioxidant activity and destroy free radicals.* Free radicals are highly reactive compounds generated by air pollution, cigarette smoke and many other sources and also naturally-occurring in the body.* Free radicals can damage fats, protein, and DNA in the body disturbing normal function in the process.*26
 
Collagen and elastin are critical structural proteins in connective tissue, blood vessels, and muscle. OPCs help maintain healthy collagen and elastin and contribute to the integrity and strength of blood vessels and capillaries.*32, 28 OPCs inhibit potentially harmful enzymes, such as hyaluronidase and histidine decarboxylase, which are implicated in the breakdown of muscle fiber and the release of histamine in the inflammation process.*33 OPCs also inhibit several glycosidases and glucosidases, enzymes which help break down synovial fluid in the joints.*27 This ability to inhibit these destructive enzymes helps to reduce the body's natural inflammatory response.*28
 
The abnormal accumulation of fluid in the body's tissues can result from malfunction of the capillaries (the smallest of the blood vessels).* Grape seed extract supports normal circulation in the veins, according to human clinical trials.*29 Other human research adds evidence that OPCs strengthen the capillaries when compared to placebo. *30 Animal research reinforces the idea that grape seed extract inhibits fluid accumulation by preventing abnormal capillary permeability.*31 According to preliminary laboratory research, grape seed extract has been shown to inhibit the binding of cholesterol to blood vessel walls.*32
 
bulletRecent findings
In test tube and animal experiments published in 1998, which compared grape seed proanthocyanidin extract (GSPE) to vitamin C, Vitamin E succinate and beta carotene (Bagchi D et al.), GSPE showed significantly more antioxidant activity—results consistent with and expanding upon earlier experiments (see Abstract, below).
 
A large body of research documents the antioxidant abilities of flavonoids in general,*23 while a growing number of studies have focused exclusively on OPCs. Research shows that grape seed extract inhibits the formation of free radicals and neutralizes existing free radicals.*23 In fact, one study found grape seed extract to have a stronger antioxidant effect than vitamin E.*24 An animal experiment validates this antioxidant capability of OPCs by suggesting that it is equivalent to vitamin E for preventing lipid peroxidation of liver cells.*25

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OPC's scavenge oxygen free radicals at a greater rate than Vitamin C or E.   Contain 50 mg of Grape Seed, dried extract. Buy Tru-OPCs

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Safety
Flavonols, including proanthocyanidins, are free of side effects. As water-soluble nutrients, unusable excess intake is eliminated through urination.

 Abstract:
Authors: Bagchi D et al.
Title: Protective effects of grape seed proanthocyanidins and selected antioxidants against TPA-induced hepatic and brain lipid peroxidation and DNA fragmentation, and peritoneal macrophage activation in mice.
Source: Gen Pharmacol 1998 May;30(5):771-6.

Treatment of mice with GSPE (100 mg/kg), vitamin C, VES and beta-carotene decreased TPA-induced production of reactive oxygen species, as evidenced by decreases in the chemiluminescence response in peritoneal macrophages by approximately 70%, 18%, 47% and 16%, respectively, and cytochrome c reduction by approximately 65%, 15%, 37% and 19%, respectively, compared with controls. 3. GSPE, vitamin C, VES and beta-carotene decreased TPA-induced DNA fragmentation by approximately 47%, 10%, 30% and 11%, respectively, in the hepatic tissues, and 50%, 14%, 31% and 11%, respectively, in the brain tissues, at the doses that were used. Similar results were observed with respect to lipid peroxidation in hepatic mitochondria and microsomes and in brain homogenates. 4. GSPE exhibited a dose-dependent inhibition of TPA-induced lipid peroxidation and DNA fragmentation in liver and brain, as well as a dose-dependent inhibition of TPA- induced reactive oxygen species production in peritoneal macrophages. 5. GSPE and other antioxidants provided significant protection against TPA-induced oxidative damage, with GSPE providing better protection than did other antioxidants at the doses that were employed.

References:

Bagchi D et al. Protective effects of grape seed proanthocyanidins and selected antioxidants against TPA-induced hepatic and brain lipid peroxidation and DNA fragmentation, and peritoneal macrophage activation in mice. Gen Pharmacol 1998 May;30(5):771-6.
Bagchi D et al. Oxygen free radical scavenging abilities of vitamins C and E, and a grape seed proanthocyanidin extract in vitro. Res Commun Mol Pathol Pharmacol 1997 Feb;95(2):179-89.
Mitcheva M, et al. Biochemical and morphological studies on the effects of anthocyans and vitamin E on carbon tetrachloride induced liver injury. Cell Mol Bio 1993;39(4):443-8.
Maffei F. et al. Free radical scavenging action and anti-enzyme activities of procyanidines from Vitis vinifera. A mechanism for their capillary protective action. Arzn Forsch 1994;44:592-601.
Gabor M, Razga Z. Effect of benzopyrone derivatives on simultaneously induced croton oil ear oedema and carrageenin paw oedema in rats. Acta Physiol Hung 1991;77(3-4):197-207.
Dubos G, et al. La Revue de la Gériatrie, Tome 5, no. 6, September 1980 — Schwitters p. 112;
Beylot C, et al. Gaz Med de France - 87, no. 22, June 13, 1980.
Pfister A, et al. Acta Therapeutica no. 8, 1982.
Masquelier J, et al. Acta Therapeutica no. 7, 1981 101-105.
Tixier, JM, et al. Laboratoire de Biochimie du Tissue Connectif, Univ of Paris, June 25, 1984.
Kuttan, R, et al. Collagen treated with (+) catechin becomes resistant to the action of mammalian collagenases. Experientia 37, 1981, Berhauser Verlag, Basel, Switzerland.
Tixier, JM, et al. Laboratoire de Biochimie du Tissue Connectif, Univ of Paris, June 25, 1984.
Kakegawa, et al, Inhibitory effects of tannins on hyaluronidase activation and on the degranulation from rat mesentry mast cells. Chem Pharm Bulletin, 33(11)5079-3082, 1985.
Mori, et al. Med Sci Res 1987, 15, 831-2.
US Patent # 4,698, 360. Oct 6, 1987.
Masquelier J, Michaud J, Laparra J, Dumon MC. [Flavonoids and pycnogenols]. Int J Vitam Nutr Res 1979;49(3):307-11 [Article in French]
Laparra, et al, Travaux originaux, Université de Bordeaux, 1976.
Parienti J, et al. Means of controlling post traumatic edema in sports injuries with l’Endotélon [OPCS]. Gaz Med de France - 90, No. 3, Jan 21, 1983.
" Pycnogenols: Recent Advances in the Therapeutical Actitivy of Procyanidins," by Prof. Jacques Masquelier, Hyppocrates Verlag, 1981.
Blaszo G, Gabor, M. Edema-inhibiting effect of procyanidin. Acta Physiologica Academiae Hungaricae, Tomus 65 (2), 235-240,1985.
Kakegawa, et al, Inhibitory effects of tannins on hyaluronidase activation and on the degranulation from rat mesentry mast cells. Chem Pharm Bulletin, 33(11)5079-3082, 1985.
Bombardelli E, et al. Botanical derivatives in functional cosmetics. Drug Cosmet Ind 1994, (155) 44-51.
Rice-Evans CA and Miller NJ. Antioxidant activities of flavonoids as bioactive components of food. Biochem Soc Trans 1996;24:790-795.
Maffei F, Facino R, Carinin M, et al. Free radicals scavenging action and anti-enzyme activities of procyanidines from Vitis vinifera. A mechanism for their capillary protective action. Arzn Forsch 1994;44(5):592- 601
Mitcheva M, Astroug H, Drenska D, et al. Biochemical and morphological studies on the effects of anthocyans and vitamin E on carbon tetrachloride induced liver injury. Cell Mol Bio 1993;39(4):443-8
Ames BN, Shigenaga MK, and Hagen TM. Oxidants, antioxidants, and the degenerative diseases of aging. Proc Natl Acad Sci USA 1993;90:7915-1922 
Jonadet M, et al. Flavonoids extracted from Ribes nigrum L. and Alchemilla vulgaris L.: 1. In vitro inhibitory activities on elastase, trypsin and chymotrypsin. 2. Angioprotective activities compared in vivo. Journal de Pharmacologie 1986;17:21-27
Delacrois P. Double-blind study of endotelon in chronic venous insufficiency. La Revue de Medecine 1981;27:28-31
Lagrue G, et al. A study of the effects of procyanidol oligomers on capillary resistance in hypertension and in certain nephropathies. Semaine des Hopitaux 1981;57:33-36
Zafirov D, et al. Antiexudative and capillaritonic effects of procyanidines isolated from grape seeds (V. vinifera). Acta Phys Pharm Bulg 1990;16(3):50-54
Wegrowski J, et al. The effect of procyanidolic oligomers on the composition of normal and hypercholesterolemic rabbit aortas. Biochem Pharm 1984;33:3491-3497
Tixier J, et al. Evidence by in vivo and in vitro studies that binding of pycnogenols to elastin affects its rate of degradation by elastases. Biochem Pharm 1984;33:3933-3939
Kakegawa H, Matsumoto H, Endo K, et al. Inhibitory effects of tannins on hyaluronidase activation and on the degranulation from rat mesentery mast cells. Chem Pharm Bull 1985;33(11):5079-5082 7. Bombardelli E and Morazzoni P. Vitis vinifera L. Fitoterapia 1995;LXVI(4):291-317
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