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. |
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- Traditional use
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- 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
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- 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
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- 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
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- 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
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- 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
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 | 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).
-
- 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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Product Recommendations |
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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.  |
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- Safety
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- 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 lEndotélon [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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