Grape Seed Extract (Pycnogenol) Last updated: Nov 19, 2009

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  Grape Seed Extract (Pycnogenol)  
 

 

 
 

Grape Seed Extract (GSE) is classified as a proanthocyanidin also known as OPC’s. They are a class of compounds, which belong to the bioflavonoid family. This is the same class of compounds which pycnogenol (pine bark) belongs to. These compounds share similar properties. (In fact, grape seed extract has all the same benefits of pycnogenol). They function mainly as antioxidants, anti-inflammatories and as enhancers of connective tissue and blood vessel strength. These compounds not only are powerful antioxidants but may enhance capillary strength as well. GSE has been used to improve edema (swelling) in individuals with chronic venous insufficiency. No side effects have been reported with this compound. Most of the benefits of grape seed extract have been demonstrated in laboratory animals or in cultured cells. For example, the ingestion of grape seed extract by rabbits fed a high cholesterol diet appeared to have an inhibitory effect on atherosclerosis associated with inhibition of LDL oxidation. GSE selectively killed two human oral cancer cell lines, more efficiently than human oral normal cell lines.

The recommended adult daily dosage is 50 to 100mg, although up to 200mg (in divided doses) is a safe and effective dose. GSE should be taken with meals.

OPCs found in GSE may have some anticoagulant properties when taken in high doses. Individuals on blood-thinner drugs such as Coumadin (warfarin), heparin, Trental (pentoxifylline) and aspirin should take high doses of GSE only under medical supervision, as high doses of OPCs might cause excessive bleeding.

A study suggests that when taking Pycnogenol, more NO is provided in response to neurotransmitters allowing for better expansion of arteries to carry more blood. This process serves to meet the enhanced oxygen demand of the performing muscle and avoid anaerobic metabolism. This was reported by Dr. Yukihito Higashi, lead researcher of the study. "These results also lead me to determine that Pycnogenol will be a useful natural alternative therapy in various diseases in which oxidative stress is involved in the pathogenesis."

The double-blind, randomized, placebo study was held at the Hiroshima University Graduate School of Biomedical Sciences in Japan. Every day for two weeks young healthy men either took 180 mg Pycnogenol or a placebo. To identify Pycnogenol's effect on the release of NO, an inhibitor of the amino acid L-arginine was infused in patients, which restricts the expansion of arteries in response to the neurotransmitter acetylcholine.

After two weeks of supplementation with Pycnogenol, results revealed blood flow increased in response to acetylcholine stimulation by 42 percent. In contrast, the control group receiving the placebo did not show a pronounced blood flow increase in response to neurotransmitter stimulation.

"Acetylcholine stimulates the cells of arteries to produce NO from L-arginine faster," Dr. Higashi said. "In turn, the NO causes the muscle surrounding arteries to relax, which results in an increase of blood vessel diameters. When subjects had taken Pycnogenol the relaxation of arteries was increased by 42 percent as compared to the group taking placebo tablets."

According to Frank Schonlau, Ph.D, director of scientific communications for Horphag Research, worldwide distributors of Pycnogenol, "While more research is warranted, this is an encouraging breakthrough especially to athletes as Pycnogenol seems to allow people to move faster when exercising by satisfying the enhanced muscle oxygen demand and increasing the blood flow to active muscles. When people are performing heavy physical activity, nerves release neurotransmitter acetylcholine to arteries supplying muscles, which makes them expand, a process that requires enhanced production of NO."

A multitude of studies about Pycnogenol and sports nutrition have been conducted. Most recently, a year ago, Pycnogenol was demonstrated to improve blood circulation and support a lasting aerobic muscle activity during any kind of activity and enhance sports endurance by alleviating cramping and muscular pain in athletes. In short, Pycnogenol is effective for enhancing and prolonging muscle performance during sport, supports muscle adaptation to higher work-load and allows for faster physical recovery.

A Study published in the journal of Minerva Cardioangiologica (November 6, 2008) reveals Pycnogenol, pine bark extract from the French maritime pine tree, reduces jetlag in passengers by nearly 50%. The two-part study, consisting of a brain CT scan and a scoring system, showed Pycnogenol lowered symptoms of jetlag such as fatigue, headaches, insomnia and brain edema (swelling) in both healthy individuals and hypertensive patients. Passengers also experienced minimal lower leg edema, a common condition associated with long flights.

"This study could not have come at a better time for the upcoming holiday travel season," said Dr. Gianni Belcaro, a lead researcher of the study. Belcaro attributes Pycnogenol's combined activities for better circulation and antioxidant potency to such remarkable results. "Previous Pycnogenol flight studies have shown a reduction in jetlag; however this was the first study to solely focus on the condition."

The study, conducted at the G. D'Annunzio University in Pescara, Italy, consisted of 133 passengers who took flights that were seven to nine hours in length. Fifty mg of oral Pycnogenol was administered three times daily, for seven days, starting two days prior to the flight.

 
 

Grape Seed Extract (Pycnogenol) can help with the following:
 
 
Addictions  Current Smoker
 GSE has been shown to provide better protection on factors such as lipid peroxidation (involved in atherosclerosis), DNA damage and cell death to a type of oral cells in culture than vitamins C and E, when exposed to tobacco extract.

Aging

  Parkinson's Disease / Risk
 Flavonoids, and in particular the proanthocyanidins (grape seed and pine bark extracts) should also be excellent candidates as Parkinson's disease preventers and retarders. Proanthocyanidins are water-soluble antioxidants that are stronger than vitamin C and which readily cross into the brain fluid. Clinical trials are, however, still required to support this hypothesis.

Circulation

  Hypertension
 A study published in the October 2006 journal of Clinical and Applied Thrombosis/Hemostasis shows Pycnogenol® (pic-noj-en-all), an antioxidant plant extract from the bark of the French maritime pine tree reduced edema, a typical side-effect of antihypertensive medications, by 36 percent in patients taking these medications.

According to Dr. Gianni Belcaro, lead researcher of the study, more than 35 percent of patients taking antihypertensive medications are believed to suffer from edema as a side-effect. This happens because the antihypertensive medications cause blood vessels to dilate, which allows easier blood flow and thus lowers blood pressure. However, as a side-effect this causes blood to pool in the vessels of the lower legs. In result they stretch and liquid seeps into tissue causing swelling (edema). Hypertension is a serious risk factor for developing severe cardiovascular incidents some time in the future and thus the necessity for treatment justifies the development of edema as a side-effect.

Antihypertensive medications reduce pressure by inhibiting constriction of blood vessels. "The larger the blood vessel diameter, the easier blood will flow with less pressure," said Dr. Belcaro. "In order to avoid blood pooling in the lower legs and feet (edema), blood vessel diameters must adjust when a person changes positions from laying down to standing up. Results of this study show Pycnogenol to improve blood circulation, avoiding blood pools and reducing edema."

  Chronic Venous Insufficiency (CVI)
 Women with CVI were assisted in combating the condition in a double blind French study that utilized 150mg of oligomeric proanthocyanidins (OPCs) daily. Positive results were also obtained in another French double blind research that increased the dosage to 300mg, with each dose being 100mgs. The effectiveness of the compound was evident in just four weeks of the treatment period and all the patients showed improvement.

  Varicose Veins
 A double-blind study of 50 people with varicose veins of the legs found that doses of 150mg per day of OPCs were more effective in reducing symptoms and signs than another natural treatment: the bioflavonoid diosmin, widely used in Europe for this condition. [Gaz Med. 1985;92: pp.96-100]

A double-blind placebo-controlled study of 71 subjects with venous insufficiency found that grape seed OPCs, taken at a dose of 100mg 3 times daily, significantly improved major symptoms, including heaviness, swelling, and leg discomfort. [La Revue de Medecine. Aug/Sept.1981;no.27–28: pp.1793-1802]

  Phlebitis / Thrombophlebitis
 One month of treatment with Pycnogenol (360mg per day reduced lower limb circumference and improved subjective symptoms better than horse chestnut seed extract in a study of 40 patients with diagnosed chronic venous insufficiency. [Phytother Res 2002;16(2): pp.1-5]

Lab Values

  Elevated Total Cholesterol
 One month of treatment with Pycnogenol (360mg per day) reduced total and LDL-cholesterol levels, but had no effect on HDL-cholesterol levels, in a study of 40 patients with diagnosed chronic venous insufficiency. [Phytother Res 2002;16(2): pp.1-5]

Three months of using pycnogenol at 120mg per day improved erectile function and reduced total and LDL cholesterol levels in a double-blind, placebo-controlled study of 21 men with erectile dysfunction. [ Nutr Res 2003;23(9): pp.1189-98]

  Elevated LDL/HDL Ratio
 See the link between Elevated Total Cholesterol and Grape Seed Extract.

Metabolic

  Meniere's Disease
 Reports by doctors state that a combination of pycnogenol (pine bark extract) and shark liver oil may be useful in treating Meniere's Disease.

  Edema (Water Retention)
 One month of treatment with Pycnogenol (360mg per day reduced lower limb circumference and improved subjective symptoms better than horse chestnut seed extract in a study of 40 patients with diagnosed chronic venous insufficiency. [Phytother Res 2002;16(2): pp.1-5]

A double-blind placebo-controlled study of 71 subjects with venous insufficiency found that grape seed OPCs, taken at a dose of 100mg 3 times daily, significantly improved major symptoms, including heaviness, swelling, and leg discomfort. [La Revue de Medecine. Aug/Sept.1981;no.27–28: pp.1793-1802]

A study published in the October 2006 journal of Clinical and Applied Thrombosis/Hemostasis shows Pycnogenol® (pic-noj-en-all), an antioxidant plant extract from the bark of the French maritime pine tree reduced edema, a typical side-effect of antihypertensive medications, by 36 percent in patients taking these medications.

According to Dr. Gianni Belcaro, lead researcher of the study, more than 35 percent of patients taking antihypertensive medications are believed to suffer from edema as a side-effect. This happens because the antihypertensive medications cause blood vessels to dilate, which allows easier blood flow and thus lowers blood pressure. However, as a side-effect this causes blood to pool in the vessels of the lower legs. In result they stretch and liquid seeps into tissue causing swelling (edema). Hypertension is a serious risk factor for developing severe cardiovascular incidents some time in the future and thus the necessity for treatment justifies the development of edema as a side-effect.

Antihypertensive medications reduce pressure by inhibiting constriction of blood vessels. "The larger the blood vessel diameter, the easier blood will flow with less pressure," said Dr. Belcaro. "In order to avoid blood pooling in the lower legs and feet (edema), blood vessel diameters must adjust when a person changes positions from laying down to standing up. Results of this study show Pycnogenol to improve blood circulation, avoiding blood pools and reducing edema."

Musculo-Skeletal

  Poor Musculoskeletal Health

Nutrients

  Antioxidant Requirement / Oxidative Stress

Organ Health

  Night Blindness
 One interesting 6-week controlled (but not blinded) study evaluated the ability of grape seed OPCs to improve night vision in normal subjects. In this trial of 100 healthy volunteers, those who received 200 mg per day of OPCs showed improvements in night vision and glare recovery as compared to untreated subjects. [(English abstract) Bull Soc Ophtamol Fr. 1988;88: pp.173-174, 177-179]

Risks

  Cancer / Risk Reduction - General Measures
 A number of studies have already revealed that eating fruit and vegetables helps to prevent cancer, and that this is likely due to the presence of proanthocyanidins. The authours, Shi and colleagues have already investigated this family of antioxidant compounds in apple peel and found it triggered cell death in cancer cells but not non-cancer cells.

Studies on grape seed extract have also suggested that it reduces breast tumors in rats and skin tumors in mice, and is active in a number of laboratory human cancer cell lines (such as skin, breast, colon, lung, stomach and prostate cancer cells), but until now nobody has investigated its effect on blood cancers.

Shi and colleagues used a commercially available grape seed extract and exposed leukemia cells to various concentrations of the extract for 12 and 24 hours, and also looked at what happened when leukemia cells were exposed to 50 µg/mL of the extract over various time intervals.

The results showed that exposure to grape seed extract resulted in dose and time-dependent increase in cancer cell apoptosis. They also discovered that the extract did not affect normal cells but they weren't able to determine why.

"This is a natural compound that appears to have relatively important properties," said Shi.

He and colleagues then examined the underlying mechanisms by which the grape seed extract caused the leukemia cells to commit suicide. They found that the extract had a strong effect on the activation of JNK, which led to the up-regulation of Cip/p21 (a CDK inhibitor which controls the cell cycle).

They double checked their finding by showing that the grape seed extract didn't work when used with an agent that blocked JNK: this was a pharmacologic approach. And using a genetic approach, they showed that silencing the JNK gene also disabled the grape seed extract's ability to trigger apoptosis.

Shi told the press that "These results could have implications for the incorporation of agents such as grape seed extract into prevention or treatment of hematological malignancies and possibly other cancers."

"What everyone seeks is an agent that has an effect on cancer cells but leaves normal cells alone, and this shows that grape seed extract fits into this category," he added.

Shi said these finding were not enough to warrant advising people to start eating lots of grapes, grape seeds, or grape skin in the hope they will avoid getting cancer. It's too early to say for sure that grape seed extract has this effect, even though the results are promising, he said. [1 January 2009, Clinical Cancer Research]

Skin-Hair-Nails

  Male Hair Loss
 A mouse study has shown improved hair growth with the use of topical procyanidins (grape seed extract). [J Invest Dermatol 1999 Mar;112 (3): pp.310-6]

The active ingredients of Revivogen are natural compounds proven to inhibit of 5-alpha-reductase (the enzyme that produces DHT), block the androgen receptors and stimulate hair growth. These active ingredients include Gamma Linolenic acid (GLA), Alpha Linolenic acid (ALA), Linoleic Acid, Oleic Acid, Azaleic acid, Vitamin B6, Zinc, Saw Palmetto Extract, Beta-Sitosterol and Procyanidin Oligomers.

  Female Hair Loss
 A mouse study has shown improved hair growth with the use of topical procyanidins (grape seed extract). [J Invest Dermatol 1999 Mar;112 (3): pp.310-6]

The active ingredients of Revivogen are natural compounds proven to inhibit of 5-alpha-reductase (the enzyme that produces DHT), block the androgen receptors and stimulate hair growth. These active ingredients include Gamma Linolenic acid (GLA), Alpha Linolenic acid (ALA), Linoleic Acid, Oleic Acid, Azaleic acid, Vitamin B6, Zinc, Saw Palmetto Extract, Beta-Sitosterol and Procyanidin Oligomers.

Uro-Genital

  Erectile Dysfunction (ED, Impotence)
 Three months of using pycnogenol at 120mg per day improved erectile function and reduced total and LDL cholesterol levels in a double-blind, placebo-controlled study of 21 men with erectile dysfunction. [ Nutr Res 2003;23(9): pp.1189-98]
 
 


KEY
May do some good
Likely to help
 
Gratitude is happiness doubled by wonder. G. K. Chesterton
 
Never wrestle with a pig. You both get dirty, but the pig likes it! Anon






GLOSSARY

Acetylcholine:  A neurotransmitter widely distributed in body tissues with a primary function of mediating synaptic activity of the nervous system and skeletal muscles.

Aerobic:  Using oxygen. For example, aerobic exercises such as running, swimming, bicycling or playing tennis use up lots of oxygen and burn up lots of calories and fat.

Amino Acid:  An organic acid containing nitrogen chemical building blocks that aid in the production of protein in the body. Eight of the twenty-two known amino acids are considered "essential," and must be obtained from dietary sources because the body can not synthesize them.

Anaerobic:  Of, relating to, or being activity in which the body incurs an oxygen debt (for example weight training or resistive exercises) and does not immediately burn off a lot of calories and fat.

Anticoagulant:  A substance that prevents or delays blood clots (coagulation).

Antioxidant:  A chemical compound that slows or prevents oxygen from reacting with other compounds. Some antioxidants have been shown to have cancer-protecting potential because they neutralize free radicals. Examples include vitamins C and E, beta carotene, the minerals selenium and germanium, superoxide dismutase (SOD), coenzyme Q10, catalase, and some amino acids.

Atherosclerosis:  Common form of arteriosclerosis associated with the formation of atheromas which are deposits of yellow plaques containing cholesterol, lipids, and lipophages within the intima and inner media of arteries. This results in a narrowing of the arteries, which reduces the blood and oxygen flow to the heart and brain as well as to other parts of the body and can lead to a heart attack, stroke, or loss of function or gangrene of other tissues.

Bioflavonoid:  Vitamin P. Any of a group of colored flavones (crystalline compounds) found next to the peel in many fruits. Essential for the stability and absorption of ascorbic acid.

Cancer:  Refers to the various types of malignant neoplasms that contain cells growing out of control and invading adjacent tissues, which may metastasize to distant tissues.

Capillary:  Any of the smallest blood vessels connecting arterioles with venules and forming networks throughout the body.

Cholesterol:  A waxy, fat-like substance manufactured in the liver and found in all tissues, it facilitates the transport and absorption of fatty acids. In foods, only animal products contain cholesterol. An excess of cholesterol in the bloodstream can contribute to the development of atherosclerosis.

Chronic:  Usually Chronic illness: Illness extending over a long period of time.

Edema:  Abnormal accumulation of fluids within tissues resulting in swelling.

Low-Density Lipoprotein:  (LDL): Also known as "bad" cholesterol, LDLs are large, dense, protein-fat particles composed of a moderate proportion of protein and a high proportion of cholesterol. Higher levels of LDLs are associated with a greater risk of cardiovascular disease.

Metabolism:  The chemical processes of living cells in which energy is produced in order to replace and repair tissues and maintain a healthy body. Responsible for the production of energy, biosynthesis of important substances, and degradation of various compounds.

Milligram:  (mg): 1/1,000 of a gram by weight.

Neurotransmitters:  Chemicals in the brain that aid in the transmission of nerve impulses. Various Neurotransmitters are responsible for different functions including controlling mood and muscle movement and inhibiting or causing the sensation of pain.

pH:  A measure of an environment's acidity or alkalinity. The more acidic the solution, the lower the pH. For example, a pH of 1 is very acidic; a pH of 7 is neutral; a pH of 14 is very alkaline.

Placebo:  A pharmacologically inactive substance. Often used to compare clinical responses against the effects of pharmacologically active substances in experiments.

Proanthocyanidin:  Also called procyanidin, it is a powerful antioxidant that chemically belongs to the class of bioflavonoids. Pycnogenol from grape seed and pine bark extracts is an example. Berries, such as hawthorn berries, cherries, blueberries, and blackberries and, to a lesser extent, red wine, are natural sources.

Pycnogenol:  A trademark for specific bioflavonoids extracted from pine bark.