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Grape Benefits Article

Used for : 

  • Antioxidant supplementation
  • Atherosclerosis prevention
  • Capillary fragility and easy bruising
  • Diabetes
  • Retinopathy (macular degeneration and diabetic retinopathy)
  • Varicose veins
  • Wound healing

General description

    Grape seed extract is a rich source of one of the most beneficial groups of plant flavonoids. These flavonoids exert many health-promoting effects. The most potent proanthocyanidins are those bound to other proanthocyanidins. Collectively, mixtures of proanthocyanidin dimers, trimers, tetramers, and larger molecules are referred to as procyanidolic oligomers, or PCOs for short.

    Although PCOs exist in many plants as well as red wine, commercially available sources of PCOs include extracts from grape seeds and the bark of the maritime (Landes) pine). This chapter reviews these benefits of PC0s from grape seeds and pine bark.

History and folk use

    In 1534, French explorer Jacques Cartier was leading an expedition up the Saint Lawrence river. Trapped by ice, Cartier and his crew were forced to survive on a ration of salted meat and biscuits. Cartier's crew began to exhibit signs and symptoms of scurvyma severe deficiency of vitamin C. At the time, the cause of scurvy was unknown. Fortunately for Cartier and the surviving members of his crew, they came across a native American who told them to make a tea from the bark and needles of pine trees. As a result, Cartier and his men survived.

    More than 400 years later, Professor Jacques Masquelier of the University of Bordeaux, France, read the book Cartier wrote detailing his expedition. Intrigued by Cartier's story,Masquelier and others concluded that pine bark must contain some vitamin C as well as being a good source of bioflavonoids, which can exert vitamin C-like effects.

    Masquelier termed the active components of the pine bark "pycnogenols." This term was used to describe an entire complex of proanthocyanidin complexes found in a variety of plants including pine bark, grape seed, lemon tree bark, peanuts, cranberries, and citrus peel. The term "pycnogenols" is now considered obsolete in the scientific community to describe these compounds giving way to the terms proanthocyanidins, oligomeric proanthocyanidin complexes (OPCs), and/or procyanidolic oligomers (PCO). In the United States, the term Pycnogenol® is a registered trademark of Horphag Research, Limited, Guernse), UK and refers to the PCO extracted from the bark of the French maritime pine.

    Masquelier patented the method of extracting PCO from pine bark in France in 1951 and from grape seeds in 1970. The PCO extract from grape seed emerged as the preferred source based on research between 1951 and 1971, as well as intensive research from 1972 to 1978. The research in the 1970s was conducted with the goal of gaining the approval of PCOs as a medicinal agent by the French equivalent of the Food and Drug Administration (FDA). Detailed analytical, toxicity, pharmacological, and clinical studies were performed on the PCO derived from grape seeds.

    PCOs from both grape seeds and pine bark have been marketed in France for decades. Sales for the grape seed extract in France are roughly 400 times greater than those for the pine bark. Owing to aggressive advertising and some misinformation, in the United States the pine bark extract currently out-sells the grape seed extract.

Pharmacology

    PCO extracts demonstrate a wide range of pharmacological activity. Their effects include an ability to increase intracellular vitamin C levels, decrease capillary permeability and fragility, scavenge oxidants and free radicals, and inhibit destruction of collagen.TM Collagen, the most abundant protein of the body, is responsible for maintaining the integrity of "ground substance" as well as the integrity of tendons, ligaments, and cartilage. Collagen also is the support structure of the dermis and blood vessels. PCO extracts are remarkably effective in supporting collagen structures and preventing collagen destruction: (1) They cross-link collagen fibers, resulting in reinforcement of the natural cross-linking of collagen that forms the so-called collagen matrix of connective tissue, they prevent free radical damage by their potent antioxidant and free radical scavenging action and inhibit cleavage of collagen by enzymes secreted by leukocytes during inflammation, by microbes during infection. PCO extracts also prevent the release and synthesis of compounds that promote inflammation and allergies, such as histamine, serine proteases, prostaglandins, and leukotrienes.

    Perhaps the most celebrated effects of PCO in the United States are their potent antioxidant and free radical-scavenging effects. Antioxidants and free radical scavengers prevent free radical or oxidative damage. Free radical damage has been linked to the aging process and virtually every chronic degenerative disease including heart disease, arthritis, and cancer. Fats and cholesterol are particularly susceptible to free radical damage. When damaged, fats and cholesterol form toxic derivatives known as lipid peroxides and cholesterol epoxides, respectively. The antioxidant and free radical-scavenging effects of PCO were discovered by Masquelier in 1986. A recent study has shed more light on the antioxidant activities and exact mechanisms underlying the primary clinical applications (e.g., varicose veins, capillary fragility, and easy bruising) of PCOs. The study featured two primary goals: (1) to determine the free radical-scavenging activity of PCO and (2) to determine the inhibitory effects of PCO on xanthine oxidase (the primary generator of oxygen-derived free radicals) and the lysosomal enzyme system, which governs the release of enzymes that can damage the connective tissue framework surrounding capillary walls.

    The results of some very sophisticated tests provide a detailed explanation of the vascular protective action of PCO and provide a strong rationale for their use in vascular disease. In these studies, PCOs demonstrated an ability to:

  • Trap hydroxyl free radicals
  • Trap lipid peroxides and free radicals
  • Markedly delay the onset of lipid peroxidation
  • Chelate to free iron molecules, thereby preventing iron-induced lipid peroxidation
  • Inhibit production of free radicals by noncompetitively inhibiting xan-thine oxidase
  • Inhibit the damaging effects of the enzymes (e.g., hyaluronidase, elastase, and collagenase) that can degrade connective tissue structures.

    The activity of PCOs is approximately fifty times greater than that of vitamin C and vitamin E, in terms of antioxidant action. From a cellular perspective, one of the most advantageous features of PCO free radical-scavenging activity is that, because of its chemical structure, it is incorporated within cell membranes. This physical characteristic along with its ability to protect against both water- and fat-soluble free radicals provides incredible protection to the cells against free radical damage.

    The researchers concluded their discussion with the following comment: "These findings, together [with] those of other investigators, provide a strong rationale for using these compounds in the therapeutic managements of microvascular disorders" (Facino et al., 1994).

Uses of extracts

    The primary uses of PCO extracts are in the treatment of venous and capillary disorders including venous insufficiency, varicose veins, capillary fragility, and disorders of the retina including diabetic retinopathy and macular degeneration. Clinical studies have shown positive results in the treatment of these conditions.

    It appears that most individuals can benefit from an increased intake of PCOs. This suggestion is perhaps best illustrated by studies investigating the ability of grape seed PCO extract to improve visual function in healthy subjects. In these studies, 100 normal volunteers with no retinal disorder received 200 milligrams per day of PCOs or placebo for 5 or 6 weeks and a control group received no treatment. The group receiving PCOs demonstrated significant improvement in visual performance in the dark and after glare tests compared to the placebo group. The improvement is related to improved retinal function.

    On the basis of the relatively recent demonstration of potent antioxidant activity and vasculoprotective effects, the list of clinical uses of PCO extracts will surely increase. Perhaps the most significant use will eventually be in the prevention of atherosclerosis (hardening of the arteries) and its complications (heart attacks and strokes).

    Numerous studies now demonstrate that the level of antioxidants may be a more significant factor than cholesterol levels in determining the risk of developing heart disease. Antioxidants prevent the oxidation of cholesterol and its carrier proteins as well as prevent the initial damage to the artery that ultimately leads to the process of atherosclerosis. Large-scale studies with vitamin E, vitamin C, and beta-carotene have shown that these antioxidants are capable of significantly reducing the risk of dying of a heart attack or a stroke. For example, one study of 87,245 nurses discovered that nurses who took 100 international units (IU) of vitamin E daily for more than 2 years had a 41 percent lower risk of heart disease compared to nonusers of vita-min E supplements. In another study, 39,910 male health care professionals produced similar results: a 37 percent lower risk of heart disease with the in-take of more than 30 IU of supplemental vitamin E daily.

    Since PCOs have a greater antioxidant effect compared to vitamins C and E, it is only natural to assume PCOs could offer greater protective effects. There is support for this contention. For example, several studies have shown the protective effects of red wine against heart disease and stroke by protecting against low-density lipoprotein (LDL) oxidation.is The active components in the wine are proanthocyanidins. A 7-year stud~ which began in 1985 and included 805 men, demonstrated an inverse correlation between flavonoid intake and death from a heart attack. That is to say, when flavonoid intake was high the risk of having a heart attack was quite low. Conversely, if flavonoid intake was low, the risk of a heart attack was quite high.

    In addition to preventing damage to cholesterol and the lining of arteries, PCO extracts have been shown in animal studies, to lower blood cholesterol levels and shrink the size of the cholesterol deposit in arteries. Additional ways in which PCOs prevent atherosclerosis include inhibition of platelet aggregation and inhibition of angiotensin I-converting enzyme. Presumably PCO extracts may exert similar benefits in humans. PCO extracts, although in a supplement form, should be thought of as a necessary food in the prevention and treatment of atherosclerosis.

Grape seed versus pine bark

    Grape seed and pine bark extracts are excellent sources of proanthocyanidins. Although both sources can be used interchangeably, for several valid reasons PCOs extracted from grape seeds have emerged as the preferred source.

  • Most of the published clinical and experimental studies of the past 20 years have been performed on the grape seed extract, not the extract of
    pine bark.

  • Masquelier and others have demonstrated that grape seed extract may be more potent and effective than pine bark extract, in terms of free radical-scavenging activity. The reason? Only the grape seed extract contains the gallic esters of proanthocyanidins (in particular: proanthocyanidin B2-3'-0-gallate)). These compounds are the most active free radical-scavenging PCOs. They are found only in grape seed.

  • It is far more economical to extract PCO from grape seeds than it is from pine bark. As a result, the grape seed extract provides greater value at a lower price.

Procyanidolic oligomers bound to phosphatidylcholine

    The most beneficial PCO products may be those that utilize a special process to bind one part of the grape seed PCO extract with two parts of phosphatidylcholine. This process is referred to as the "PhytosomeTM process." The result is a completely new molecule composed of a central molecule of PCO encased by two phosphatidylcholine molecules. The PCO-phosphatidylcholine complex offers significant advantages over unbound PCO.

    The major advantage is improved absorption from the gastrointestinal tract. The phosphatidylcholine molecules envelope the PCO molecule, improving absorption and protecting the PCO molecules from degradation by digestion and gut bacteria. Absorption studies on unbound PCO indicate that only about 28 percent of an orally administered dose is retained in the body after 24 hours. The majority (72 percent) is excreted in the feces (45 percent), urine (19 percent), or exhaled as carbon dioxide (6 percent). By binding the PCO to phosphatidylcholine, more PCO is absorbed.

    Another advantage of the PCO-phosphatidylcholine complex is its improved utilization and incorporation into biological membranes: more PCOs are delivered to body tissue. Once delivered to the tissue, the bound PCOs exert much greater antioxidant effects compared to unbound PCOs.

    One 50-milligram capsule of phosphatidylcholine-bound PCO, in terms of absorption only, is equivalent to about 50 milligrams of unbound PCO whether they are derived from grape seed or pine bark. However, in terms of biological activity, one 50-milligram capsule of PCO-Phytosome may be as effective as 150 milligrams of unbound PCO.

Dosage

    Regardless of the source, PCO extracts can be used to support good health. As a preventive measure and as antioxidant support, a daily dose of 50 milligrams of either the grape seed or pine bark extract is suitable. For comparison, it is now estimated that the average daily intake of total flavonoids in the United States is about 25 milligrams. An intake greater than 30 milligrams significantly reduces the risk of cardiovascular mortality. Products related to this article.

    PCO extracts exert no side effects

 
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