PROANTHOCYANIDINS: RESVERATROL, GRAPE SEED EXTRACT AND PYCNOGENOL Resveratrol

THE WINE WHEN IT’S RED
by Lynn Hinderliter CN, L
DN

Proanthocyanidins, Resveratrol and Pycnogenol are not snappy words, I agree, but we would do well to know and pay attention to them , particularly when it comes to its presence or absence in our diets! These are the molecules which are responsible for the pigmentation in the fruits and vegetables we eat, the carrots, the broccoli, the berries and grapes,  present in high concentrations in red wine and red grape juice.

Most of us are familiar with the term “the French Paradox”.

This refers to the surprise of dietitians and scientists when confronted with the fact that, although the French in many cases eat diets which are extremely high in fat, the rate of heart disease and cancer does not reflect this excess. Many scientists have now come to believe that the flavonoids (of which Proanthocyanidins are one) in red wine provide the antioxidants which give this unexpected protection. 

Dr. John Folts M.D., at the University of Wisconsin Medical School, has been focusing on the connection between grapes and heart disease. His research has suggested that grapes may have a more protective anti-clotting effect than aspirin – the figures showed that aspirin and red wine both had anti-clotting activity of 45%, but then went on to show a whopping 75% effect from ordinary grape juice!

This is great news, because while no one wants to be encouraging people to drink regular amounts of alcohol for fear that they might succumb to the negative effects that alcohol sometimes has, the beneficial effects of wine cannot be denied. Now, we have many alternatives: we can eat plenty of grapes  (be aware that commercial grapes are likely to be contaminated with many different pesticides, so wash them well!), make our own grape juice, buy commercial grape juice, take capsules of grape extracts, take capsules of red wine extract, or drink moderate amounts of red wine.

The antioxidants these fruits contain have other potential benefits besides the effect on blood clotting: they protect collagen and elastin in the skin, and we are now seeing some cosmetic creams containing Pycnogenol, for example. I have tried one, and found it very effective. They also stabilize capillary walls, helping with micro-circulation, and showing possible benefits for varicose veins. A Dutch study followed 552 men for 15 years, tracking the incidence of stroke and correlating that with their intake of flavonoids. He found that men with the highest intake of flavonoids had 73% fewer strokes than men with low intake. (This being a Dutch study, the sources of the flavonoids were black tea and apples).

There has recently been much anecdotal evidence about the effect Proanthocyanidins have on allergies, a use for them that is already widespread in Europe: they appear to block the production of histamine and to the extent that allergies are involved in ADHD, this may provide a possible explanation for their successful use in that problem.

PYCNOGENOL   is available from two sources, the French Maritime Pine, and Grape Seeds

both developed by Dr. Masquelier.  Much of the impressive research, however, has been done using the Pine source. I leave it to you, therefore, to decide whether to go for the proven but more expensive Pycnogenol, or the less proven, less expensive but frequently effective grape seed extract, also sometimes called OPCs.  

To this add Resveratrol.

There is some impressive research being done  with respect to its effect on cancer cells. In fact, Cancer Research published a study in its July 2000 issue showed that Resveratrol also helps cancer cells be more receptive to chemotherapy. 

More recently, researchers reported that Resveratrol is converted in the body to a known anti-cancer agent that can selectively target and destroy cancer cells. Although previous studies have suggested that this phytoestrogen might prevent cancer, they said it was the first time that scientists had gained an insight into the underlying mechanism of the chemical’s anticancer properties. Resveratrol is a defensive molecule against fungus in grapes and other crops, and is found at higher levels in those which have not been treated with man-made fungicides.

In 2008, a study at P. Wilmot Cancer Center at the University of Rochester Medical Center showed for the first time that a natural antioxidant found in grape skins and red wine can help destroy pancreatic cancer cells by reaching the cell’s core energy source, or mitochondrion, and crippling its function. The study is published in the March  2008 edition of the journal, Advances in Experimental Medicine and Biology.The study also showed that when the pancreatic cancer cells were doubly assaulted (pre-treated with the antioxidant, resveratrol, and then irradiated) the combination induced a type of cell death called apoptosis, an important goal of cancer therapy.Mounting evidence shows red wine antioxidant kills cancer, read more at http://www.eurekalert.org/pub_releases/2008-03/uorm-mes032508.phpThe latest good news about red wine, is that  Resveratrol, may be helpful in preventing breast cancer.

“Scientists know that many breast cancers are fueled by increased estrogen, which collects and reacts with DNA molecules to form adducts.

Professor Rogan and her colleagues found that resveratrol was able to suppress the formation of these DNA adducts and she says this is dramatic because fairly low concentrations of resveratrol were used.

Although the researchers experimented with up to 100 µmol/L of resveratrol, the suppression of DNA adducts was seen with 10 µmol/L… a glass of red wine contains between 9 and 28 µmol/L of resveratrol.”

Full text at http://www.news-medical.net/?id=39811- compound in red wine may prevent breast cancer

Resveratrol is now being shown in animal studies to be beneficial in protecting against injury from stroke – see the study in RESOURCES at bottom.

Resveratrol also appears to fight against plaques in the brain that can lead to Alzheimer’s disease, according to 2005 research (Journal of Biological Chemistry 2005, vol.280, no.45: 37,377-37,382).

In the study, researchers added Resveratrol to cells that produce human amyloid-beta peptides, which cause the plaques. They found that levels of amyloid-beta in the treated cells were much lower than those in untreated cells. The researchers noted that concentrations of resveratrol in grapes and other plants were probably not high enough to reach the effect seen in this study. However, they added that because grapes and wine contain more than 600 components, including well-characterized antioxidants, very possibly the synergy between these compounds works  to slow the progression of the neurodegenerative process.

 Interestingly, the Muscadine grape, grown right here in the US, is the highest grape source of Resveratrol, up to 40 mg per liter of wine or juice, as opposed to between 2 and 12 mg in others. Who would have guessed that the humble peanut is also a good source of Resveratrol?  Around 250 mcg per cup, more for boiled peanuts. Blueberries are also a good source of Resveratrol and many other antioxidants also.

“What we’re talking about is a single pill that you can take every day that would ward off most diseases,” says David Sinclair, Ph.D., a pathologist at Harvard Medical School and co-founder of Sirtris Pharmaceuticals.What new mighty drug is this? What strange chemical rising on our horizon?  What magnificent new discovery?

Ta dah!  Resveratrol.  But not as we know it, no – a PATENTABLE form of the extra-condensed synthetic molecule, which as we know is where the money is.  And also, all too often, the side effects … the developers point out that it would take 1,000 glasses of red wine to equal the resveratrol found in just one pill. …  let’s wait and see what the hangover is like.

Develop wisdom, health and age together:  drink red wine or take Resveratrol, the plant.

Eliminating Disease – http://www.ivanhoe.com/channels/p_channelstory.cfm?storyid=17362

Grapeseed Extract in and of itself has many interesting properties, not least being recent research which shows it to induce and support apoptosis in Leukemia cells ( Gao N, et al “Induction of apoptosis in human leukemia cells by grape seed extract occurs via activation of c-Jun NH2-terminal kinase” Clin Cancer Res 2009; 15(1): 140-149.)

I personally use the Muscadine grape powder in my juice each day. You can see it here.

A group of FFH Program scientists led by Dr. John Pezzuto in the College of Pharmacy at the UIC campus has recently shown that  Resveratrol  is one of a group of compounds (called phytoalexins) that are produced in plants during times of environmental stress such as adverse weather or insect, animal or pathogenic attack.

Resveratrol has been identified in more than 70 species of plants, including mulberries and peanuts. Grapes, however are particularly good sources. Resveratrol is found in the skin (not flesh) of grapes. Fresh grape skin contains about 50 to 100 micrograms of Resveratrol per gram, while red wine concentrations range from 1.5 to 3 milligrams per liter. This compound is also thought to be responsible, in part, for the cholesterol-lowering effects of red wine and may also explain why those consuming a Mediterranean-type diet (of which red wine consumption is characteristic) may have a reduced risk of heart disease.

In the current study, Pezzuto and colleagues were able to show that Resveratrol was effective during all three phases of the cancer process: initiation, promotion and progression. Resveratrol was found to have antioxidant and antimutagenic activity and also increased levels of the phase II drug-metabolizing enzyme quinone reductase, an enzyme capable of metabolically detoxifying carcinogens, thereby ridding them from the body.

All three of these physiological effects are indicative of Resveratrol preventing cancer initiation–the initial, irreversible stage of the cancer process. Resveratrol also demonstrated antiinflammatory effects and inhibited the activity of the cyclooxygenase and hydroperoxidase enzymes (suggestive of antipromotion activity) in addition to causing the differentiation of human promyelocytic leukemia cells, indicating that this compound may also depress the progression phase of cancer. Finally, Resveratrol inhibited the development of preneoplastic lesions in mouse mammary glands treated with a carcinogen in culture and inhibited tumor formation in mice. No toxic effects were observed.

The researchers found that Resveratrol is processed by the enzyme CYP1B1, which is found in a variety of different tumors. This converts Resveratrol into piceatannol, a closely related phytoestrogen with known anticancer activity. Resveratrol was found to have antioxidant and antimutagenic activity and also increased levels of the phase II drug-metabolizing enzymes that are capable of metabolically detoxifying carcinogens, thereby ridding them from the body. All three of these physiological effects are indicative of Resveratrol preventing cancer initiation — the initial, irreversible stage of the cancer process. Resveratrol also demonstrated antiinflammatory effects and inhibited the activity of the cyclooxygenase and hydroperoxidase enzymes (suggestive of antipromotion activity) in addition to causing the differentiation of human promyelocytic leukemia cells, indicating that this compound may also depress the progression phase of cancer.
British Journal of Cancer 2002;5.
 

What these various sources have in common is a high concentration of a form of Flavonoids called Proanthocyanidins.

These are the substances which make your fruits and vegetables the colorful foods that they are, but more important than the visual are the health benefits. The first flavonoids were identified by Nobel prize winner Dr. Albert Szent Gyorgi in 1936. He discovered and identified Vitamin C, and determined that the flavonoids assisted Vitamin C in its task of supporting the integrity of blood vessel walls, preventing damage to the endothelium, the inner lining of the blood vessels.

Much of the most recent research into Pycnogenol has focused on its role in circulation: in May of this year, for example, a study by Dr. Hans Ruve was presented to the American Society for Biochemistry and Molecular Biology showing that Pycnogenol “significantly” reduced platelet aggregation , which is a leading cause of heart attacks and strokes. It was particularly effective in protecting smokers, as shown by Dr. Watson at Arizona University: smoking can aggravate a tendency to platelet aggregation. Since Pycnogenol is also an extremely effective antioxidant and free radical scavenger, this may be an important protective supplement for people who cannot stop smoking.

Dr. Ruve also found that Pycnogenol had an inhibitory effect on angiotensin converting enzyme: this enzyme is involved in constricting blood vessels, a key factor in high blood pressure. This is very interesting to me, since it is the first direct link between eating more fruits and vegetables, and lowering blood pressure. For years there have been studies that show a positive effect from changing one’s diet and lowering blood pressure, but now we know WHY it works!  See RESOURCES at right.

Pycnogenol and Alzheimer’s Disease: some research is under way showing that the formation of a toxic protein (beta amyloid) which is present in Alzheimer patients is inhibited. Dr. Packer in his studies is finding o that Pycnogenol regulates Nitric Oxide production, excessive amounts of which also play a part in A.D.

Pycnogenol , Fibromyalgia and Chronic Fatigue syndrome: it has been noted that in these conditions the mitochondria of the cells are damaged.  Pycnogenol’s free radical quenching properties make it of particular benefit, since it can cross the blood/ brain barrier . Dr. Martin, D.C in Ontario Canada uses doses of from 200 to 400 mg daily, and finds it brings a decrease in symptoms in from 3 to 6 weeks.

Pycnogenol and inflammation: since Pycnogenol reduces the production of histamine and promotes microcirculation it can be very helpful both for joint problems, and for athletic injuries. Inflammation can also be a result of excessive Nitric Oxide radicals produced by white blood cells – see comment on Alzheimer’s above.

Pycnogenol and Cancer: Dr. Packer is doing research at Berkeley that shows Pycnogenol interacts with DNA at a very basic, transcription level. This is going to be interesting research to watch, since cancer at its simplest is cells running amuck. If regulating this process at an early stage could be a part of the cure – what a boon to mankind this would be! Factors in Pycnogenol have also been shown in some tests to inhibit the formation , and in some cases reverse the growth of, certain tumors.

Grape Seed Extract and Cancer – in 2006, a study in the October 18 issue of Clinical Cancer Research documented a significant effect on colorectal cancer cells:  not only was growth inhibited, but levels of Cip1/p21 protein, which also controls apoptosis( programmed cell death) rose in a dose-dependent manner

Pycnogenol and Aging: Dr. Arnold Fox, M.D. points out that the most common theory of aging is accumulated damage from free radicals and oxidative stress. This causes such problems as cataracts, retinal degeneration, coronary heart disease, heart attacks, strokes, kidney failure, diabetes mellitus type 11. He says “Pycnogenol is a very strong antioxidant and free radical quencher, perhaps the strongest one discovered. As an antioxidant it is 50 times more powerful than Vitamin E and 20 times more powerful than Vitamin C. Furthermore, – it – is able to cross the blood/brain barrier and get into the brain to extend its beneficial effects in reducing the ravages of aging on the brain”.

A study presented at the 54th Annual Meeting for the American Society of Reproductive Medicine (16th World Congress on Fertility and Sterility) showed that Pycnogenol – the study used maritime pine bark – may have an effect on sperm health. Dr. S. Roseff (West Essex center for Advanced Reproductive Endocrinology, West Orange N.J.) had 4 sub fertile men with high numbers of deformed sperm in a low overall sperm count take daily supplements of Pycnogenol. After 3 months, the percentage of structurally normal sperm increased by an average of 99% while the sperm count and activity remained the same.

As I have said many times before, no pill in and of itself is going to take the place of a better diet. In other words, please don’t expect to be able to continue eating an inadequate diet, thinking one pill will make the difference between sickness and health. However, for people who have already developed health conditions of the types mentioned above, or who wish to take out some extra insurance, these new extracts of Proanthocyanidins certainly appear to have a lot going for them, and adding more of those colorful fruits and vegetables will help, too.

Find the recommended supplements here

Grape juice and coronary artery  disease – http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10477529&dopt=Abstract

Press release from Cancer Research UK on Resveratrol – http://info.cancerresearchuk.org/news/pressreleases/2002/february/40684

Resveratrol and Stroke Protection – http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=12470882&dopt=Abstract

Pycnogenol and platelet aggregation – http://www.ahsc.arizona.edu/opa/news/may98/watson.htm

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