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Grape Seed Extract

Reference 2

PCO Sources: Grape Seed vs Pine Bark

Source Grape Seed Extract
Supplement	Grape Seed Extract
Description	Grape seed extract (GSE) is just what it sounds like – an extract from grape seeds. The seeds are typically from red grapes (instead of white), which have a high content of compounds known as oligomeric proanthocyanidins (OPCs). The OPCs are also present in a wide variety of fruits and vegetables, including pine bark (Pycnogenol) and green tea, where, like grape seed extract, they possess potent antioxidant properties The OPCs are chemically known as flavonoids or polyphenols, which can differ substantially based on their polymer arrangement. For example, polyphenols can exist in single (monomers), double (dimers), triple (trimers), quadruple (tetramers) and even longer "cyanidin" chains (tannins). Any chain length from 2-7 or so is termed and "oligomer" and longer chains are generally just called "polymers." It is generally assumed that the longer the cyanidin chain length, the less bioavailable and less active the molecule becomes. It may even be possible for the longer chain length compounds (tannins) to interfere with the absorption of other nutrients consumed at the same time. Many commercial grape seed extracts are standardized to a total OPC content, which may or may not take into account the assortment of dimers/trimers, etc. present in the final product.
Claims	Antioxidant Cardioprotection (reduces risk of athersclerosis) Reduces cancer risk Improves vascular strength (stronger blood vessels) Reduces edema (inflammation/swelling) Promotes eye health (reduces risk of macular degeneration and cataracts)
Theory	You’ve probably heard about the health phenomenon known as the "French Paradox", which attributes the low incidence of heart disease in France, despite their high fat intake, to a hearty consumption of red wine. The cardioprotective effects of red wine (and possibly for red/purple grape juice) has further been speculated to be derived from a group of compounds variously called flavonoids, catechins, tannins and proanthocyanidins which are found at high concentrations in red wine. These compounds are found at especially high levels in the seeds of the grape, where they can be extracted and concentrated for use as a dietary supplement. Research on the chemical properties of grape seed extract has shown them to be powerful antioxidants, or free radical scavengers – even more potent than the more commonly used antioxidant vitamins like C and E.
Scientific Support	Grape seed extract (GSE) and oligomeric proanthocyanidins (OPCs) clearly possess remarkable antioxidant properties. Their effects on reducing free radical damage and oxidative stress suggest that they may be particularly effective in reducing the risk of cancer, cardiovascular disease and a number of the chronic diseases associated with aging. Although the majority of the studies conducted on GSE have been done in cell culture (test tube) and animals, the results are extremely promising In one laboratory study the chemo-protective (cancer fighting) properties of GSE was tested in human breast cancer and lung cancer cells. Results indicated that GSE was effective in promoting cytotoxicity (cell death) in the cancer cells, but that the growth and viability of the normal cells was maintained. Another cell study examined the effects of GSE on preventing the cell damage, DNA damage and cell death that occurs when cells are exposed to tobacco. The results showed that tobacco exposure causes oxidative tissue damage and apoptosis (cell death), which can be reduced by 10-85% by antioxidants such as vitamins C and E and grape seed extract. GSE was about 2-5 times more effective than vitamins C or E alone and the combination of the vitamins with GSE is even more effective in preventing cell damage and death. A number of animal studies have confirmed the antioxidant potential of grape seed extract. In one study, rabbits were fed a high cholesterol diet with and without GSE. Although there was no change in cholesterol levels in the rabbits, those receiving the GSE showed a reduced level of damaging cholesteryl ester hydroperoxides and aortic malondialdehyde (MDA) – both of which can induce significant damage to the delicate blood vessel linings and lead to atherosclerosis. Immunohistochemical analysis revealed a decrease in oxidized LDL – the type of cholesterol that forms atherosclerotic lesions. In another experiment using human plasma, GSE added to the plasma also inhibited the oxidation of LDL, suggesting a possible benefit in preventing atherosclerosis. In one of the few human studies to be conducted directly on GSE, 300mg of GSE daily for 5 days caused a significant increase the total antioxidant capacity (TAC) of the blood. A number of epidemiological and case-control studies have shown that those individuals who consume 1-2 glasses of red wine per day are at reduced risk for heart disease and possibly for certain cancers. These types of studies are only suggestive of possible health effects, but other studies have shown that many of the phenolic compounds in red wine are absorbed into the blood, become associated with LDL cholesterol and reduce the susceptibility of LDL to oxidation – a logical chain of events for the cardioprotective effect of red wine. Finally, there are some small studies, primarily conducted in rabbits and rats, which suggest that GSE may also possess activity in reducing inflammation, increasing circulation (vasodilatation) and enhancing blood vessel integrity.
Safety	Grape seed extract is safe when used as directed. No adverse effects have been associated with its use.

OPC's (Oligomeric Proanthocyanidins) are a set of bioflavonoid complexes that perform as free radical scavengers in the human body. Many names refer to this set of bioflavonoids, including PCO's (Oligomeric Procyanidolic Complexes), leuco anthocyanin, anthocyanidin and still others. We will refer to them as OPC's for the duration of this discussion.
 
OPC's are types of bioflavonoids, very powerful ones. Bioflavonoids are parts of plants that are actually assimilated into our body tissues when we consume them. It was, in fact, this very ability that led to their discovery. OPC bioflavonoids were first noticed in the laboratory because they have the uncanny ability to strengthen blood vessel walls within hours after taking them! The person responsible for their discovery was a French scientist named Dr. Jacques Masquelier, who first tested bioflavonoid containing peanuts on lab animals and discovered that their blood vessel walls would double in strength only hours after eating them. His discovery was made in 1948. In 1951, this same doctor extracted OPC's from pine bark.
 
In 1970, Dr. Masquelier obtained yet another patent for these bioflavonoids - a far more potent product. It is the grape seed extract that you may have heard about, and it is a powerful substance indeed.  

Source

One of the most beneficial group of plant flavonoids are the proanthocyanidins. These flavonoids exert many health promoting effects. The most potent proanthocyanidins are those bound to other proanthocyanidins. When two proanthocyanidin molecules are linked together it is referred to as a "dimer", for three it is a "trimer", for four it is a "tetramer". Collectively mixtures of proanthocyanidin dimers, trimers, tetramers and larger molecules are referred to as proanthocyanidolic 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 barks of the maritime (Landes) pine. This article shall review these benefits of PCOs as well as answer the question "Which is better, PCOs from grape seeds or pine bark?"

In 1534, French explorer Jacques Cartier was leading an expedition up the Saint Lawrence river. Trapped by ice, Cartier and his crew was forced to survive on a ration of salted meat and biscuits. Cartier's crew began to exhibit signs and symptoms of scurvy-a 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 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 believed and concluded that pine bark must contain some Vitamin C as well as be 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 described an entire complex of proanthocyanidin complexes found in a variety of plants including pine bark, grape seed, lemon tree bark, peanuts, cranberries and citrus peels. 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 procyanidolic oligomers(PCO). In the United States (Australia???), the term Pycnogenol is a registered trademark of Horphag Ltd.,Guernsey, UK and refers to the procyanidolic oligomer (PCO) extracted from the bark of the French maritime pine.

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

Both PCOs from grape seeds and pine bark have been marketed in France for decades. Sales for the grape seed extract are roughly 400 times greater than those for the pine bark.

The most celebrated effects of PCOs in the United States are its potent antioxidant and free radical scavenging effects. Antioxidants and free radical scavengers prevent against 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 PCOs were discovered by Masquelier in 1986.

While the therapeutic potential of PCOs is quite broad due to its antioxidant activity, PCOs are used in Europe primarily in the treatment of venous and capillary disorders including venous insufficiency, varicose veins, capillary fragility and vascular disorders of the retina. A recent study has shed more light on the exact mechanisms underlying these clinical applications of PCOs.

The study featured two primary goals: (1) to determine the free radical scavenging activity of PCOs and (2) to determine the inhibitory effects of PCOs on xanthine oxidase ( the primary generator of oxygen derived free radicals) and the lysosomal enzyme system which governs the release of enzymes which can damage the connective tissue framework which acts as a protective sheath surrounding capillary walls.

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

1. Trap hydroxyl free radicals.
2. Trap lipid peroxides and free radicals.
3. Markedly delay the onset of lipid peroxidation.
4. Bind to free iron molecules, thereby preventing iron-induced lipid peroxidation.
5. Inhibit production of free radicals.
6. Inhibit the damaging effects of the enzymes (eg. hyaluronidase, elastase, collagenase etc) which can degrade connective tissue structures.

In regards to the antioxidant action of PCO, the activity of PCOs is much greater than that of Vitamin C and Vitamin E. From a cellular perspective, one of the most advantageous features of PCOs 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."

Again the primary uses of PCOs is in the treatment of venous and capillary disorders including venous insufficiency, varicose veins, capillary fragility and vascular disorders of the retina. Good clinical studies have shown positive results in the treatment of these conditions.

Based on the relatively recent demonstration of potent antioxidant activity the list of clinical uses of PCOs extract will surely increase. Perhaps the most significant use will eventually be in the prevention of Atherosclerosis( hardening of the arteries characterized by the appearance of cholesterol deposits) and its complications (heart disease and strokes).

There are now numerous studies demonstrating the level of antioxidants may be a more significant factor in determining the risk of developing heart disease than cholesterol levels. Antioxidants prevent the oxidation of cholesterol and its carrier proteins as well as prevent the initial damage to the artery which ultimately leads to the process of atherosclerosis( hardening of the arteries). Large-scale studies with Vitamin E, Vitamin C and beta-carotene have shown these antioxidants are capable of significantly reducing the risk of dying of a heart attack or a stroke. For example, in one study of 87,245 nurses it was discovered that nurses who took 100 IU of Vitamin E daily for more than two years had a 41% lower risk of heart disease compared to non-users of Vitamin E supplements. In another study, 39,910 male health care professionals produced similar results: a 37% lower risk of heart disease with the intake of more than 30 IU of supplemental Vitamin E daily.

Since PCOs has a greater antioxidant effect compared to Vitamins C and E, it is natural to assume it 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. The active components in the wine are proanthocyanidins. Also, results from a recent study in 805 men beginning in 1985 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 the artery, PCOs extracts have actually been shown to lower blood cholesterol levels and shrink the size of the cholesterol deposit in the artery in animal studies. Presumably PCOs extracts may exert similar benefits in humans. PCOs extracts, although in a supplement form, should be thought of as a necessary food in the prevention and treatment of atherosclerosis.

Grape seed and pine bark extracts of PCOs are well-defined chemically. Both are excellent sources of proanthocyanidins: grape seed extracts are available which contain a total of 92% or 95% PCOs while the pine bark extracts can vary from 80% to 85%. Although both sources can be used interchangeably, for several valid reasons PCOs extracted from grape seeds have emerged as the preferred source.

First of all, the overwhelming majority of the published clinical and experimental studies over the past twenty years have been performed on the grape seed extract, not the extract of pine bark. Professor Jacques Masquelier , the original patent holder for extraction procedures for both sources favours the grape seed extract not the extract of pine bark. It is also interesting to point out that only the PCOs extracted from grape seed is approved for medicinal use in France.

In regards to the free radical scavenging activities of PCOs, studies by Professor Masquelier have demonstrated that the grape seed extract is substantially more potent and effective compared to the extract of pine bark. 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 PCO. They are not present in the pine bark extract but they are found in the PCOs extract from the grape seed.

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

Regardless of the source, PCOs extracts can be used to support good health. As a preventive measure and as antioxidant support, a daily dose of 50 mg of either the grape seed or pine bark extract is suitable. When greater support from PCOs are desired, the daily dosage should be increased to 150 to 300mg.

Michael T. Murray, N.D. is a graduate and faculty member of the Bastyr University in Seattle,Washington. In addition to maintaining a private medical practice, Dr. Murray is an accomplished writer, educator and lecturer. He is co-author of A Textbook of Natural Medicine, the definitive textbook on naturopathic medicine for physicians, and the Encyclopaedia of Natural Medicine. He has also written twelve other books including The Healing Power of Herbs and Natural Alternatives to Over The Counter and Prescription Drugs. Dr. Murray is also the editor of The American Journal of Natural Medicine.

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