The Consumer Guide to Grape Seed Extract

In this guide...
  Traditional Use
  Modern Perspective
  Daily Requirement
  Types Of Products
  Recent Findings
  Safety
  Abstract
  References
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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.

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.

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.

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.

 

Recent 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 activityresults consistent with and expanding upon earlier experiments (see Abstract, below).

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.

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