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http://www.hfn-usa.com/articles-text/040927.htm

 

 

Grape Seed Extract Provides OPCs:

Safe and Powerful Antioxidant Support for Vascular, Cardiovascular and

Eye Health; Protects Against Cancer

 

Grape seed extract (GSE) (Vitis vinnifera) is simply an extract from

grape seeds from red grapes. Grape seeds have a high content of

compounds known as oligomeric proanthocyanidins—better known as

OPCs—which are also found in a variety of fruits and vegetables,

including cranberries, blueberries, bilberries, and green and black

tea. These naturally occurring antioxidants have been shown to exert a

broad spectrum of biological, pharmacological and therapeutic

activities against free radicals and oxidative stress.2 Also, OPCs are

distinct from other flavonoids because their simple chemical structure

allows them to be readily absorbed into the bloodstream.

 

Most OPC nutritional supplements are made from grape seed extract or

the bark of maritime pine (Pycnogenol), although GSE usually contains

a total of 92% or 95% OPCs, compared to pine bark extracts which

contain 80% to 85%. GSE has emerged as the preferred source of OPCs,

which makes sense, especially since the overwhelming majority of the

published clinical and experimental studies over the past 20 years

have been performed on GSE, not the extract of pine bark.3

The Discovery of OPCs

In 1951, Jacques Masquelier of the University of Bordeaux was inspired

to investigate the constituents of pine trees after coming across a

story that reads something like this:

 

In 1532, a French explorer and his crew were trapped by ice in the

Saint Lawrence River. A Native American suggested they make tea from

the needles and bark of a local pine tree, which saved many of the men

from developing scurvy.4

 

When Masquelier extracted OPCs from the bark of the maritime pine, he

found that they could duplicate many of the functions of vitamin C. He

named 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, cranberries and citrus peels. Instead of using the term

pycnogenols to describe these compounds, the scientific community now

uses the terms proanthocyanidins, oligomeric proanthocyanidin

complexes (OPCs) and procyanidolic oligomers(PCO).3

 

Masquelier patented the method of extracting OPCs from pine bark in

France in 1951 and from grape seeds in 1970. Extensive research on the

OPC extract from grape seeds went on between 1951 and 1971, as well as

intensive research from 1972 to 1978. The research in the 1970s was

carried out with the goal of getting the approval for grape seed

extract to be classified as a medicinal agent in France.

 

Today, although pine bark extract is still sold in France, sales for

the grape seed extract are approximately 400 times higher and it

remains the only OPC with the status of a medicinal agent3 —the

equivalent of a FDA approval.

Benefits

Grape seed extract is considered to be a powerful antioxidant that

protects the body from premature aging and disease. Research shows

that GSE is beneficial in many areas of health, and is even capable of

promoting youthful skin, cellular health, elasticity, and flexibility.

OPCs also improve blood circulation by strengthening capillaries,

arteries, and veins.1

 

A number of recent scientific studies also demonstrate that grape seed

extract OPCs reduce the risk of cancer, cardiovascular disease and a

number of the chronic diseases associated with aging. Although most of

the studies conducted on GSE have been done in vitro (cell cultures

tested in a test tube) and on animals, more studies are being done on

humans, and the results are extremely promising.

 

Grape seed extract has been shown to:

 

* Help reduce risk of cataracts 5

 

* Provide potent antioxidants 6,7

 

* Reduce risk of, and even reverse, atherosclerosis 8,9,10

 

* Provide cardiovascular support 11,12

 

* Support vascular strength and flexibility 13,14,15

 

* Reduce edema (inflammation and swelling) 16,17,18

 

* Protect against cancer 19,20,21,22

 

 

Scientific Studies

GSE offers potent antioxidant support

Human study

 

A study at the University of Milan, Italy evaluated the effect that

grape seed extract supplementation had on oxidative stress markers in

10 healthy volunteers.

 

The volunteers received a daily dose of 110 mg of OPCs for 30 days.

Fasting blood samples were taken before and at the end of the

supplementation period, and then again after 7 days of not having

taken the supplements. The results showed that the OPCs provided

antioxidant protection by increasing levels of alpha tocopherol

(liposoluble vitamin E) in red blood cells, and by reducing DNA

oxidative damage.6

Animal study

A study at the Government College of Pharmacy in Bangalore, India

found that grape seed extract produced the most optimal antioxidant

activity in laboratory rodents. The animals were first treated with a

substance that decreased the natural antioxidants catalase, superoxide

dismutase (SOD), and peroxidase by 81, 49, and 89% respectively. On

the other hand, lipid peroxidation—the break down of fats in the

arteries and veins due to free radical attack, and the main cause of

artherosclerosis in humans—increased nearly threefold.

 

Compared to the control group, the catalase, SOD, and peroxidase

levels were restored by 43.6, 73.2, and 54%, respectively, in the

rodents that were pretreated with GSE, whereas lipid peroxidation was

restored to values comparable with the control.7

 

This study indicates that GSE has the potential to offer potent

antioxidant support and help control lipid peroxidation, both key

factors in heart health, as we see below.

Grape OPCs reduce atherosclerosis risk and heart disease

A large body of evidence shows that oxidized low-density lipoprotein

(LDL - " bad " cholesterol) plays a major role in atherosclerosis and

heart disease. If this oxidative stress is not neutralized, it causes

plaque to form in the walls of the arteries in the heart. OPCs,

however, protect against free radicals and oxidative stress.

 

A French in-vitro study examined the effects of OPCs in grape seed

extract compared with whole grape and grape skin extracts. The GSE was

the most effective at preventing LDL oxidation.8

 

Scientists around the world are realizing the value of GSE in reducing

LDL oxidation associated with heart disease. Roger Corder, a scientist

from the William Harvey Research Institute, Queen Mary, University of

London gave a presentation to the American Heart Association meeting

in Chicago in November 2002, which outlined how procyanidins found in

grape seeds and grape skin appear to stall the development of

atherosclerosis.

 

The team of scientists at the William Harvey Research Institute mainly

focused their research on vascular endothelium, the flat endothelial

cells which line all blood vessels in a single layer and which have

numerous functions.

 

They established that red wine and grape seed extract appear to

inhibit the production of endothelin-1, a protein that has long been

incriminated in the formation of the early signs of artery disease.

Previous studies have shown that suppression of ET-1 can reduce the

risk of a heart attack in those with heart disease. The news is

significant because it indicates polyphenols may be beneficial for

more than just their antioxidant properties.9,10

May reduce risk of heart attack

Researchers at the University of Connecticut School of Medicine

concluded that animals fed with grape seed OPCs were resistant to

heart attack (myocardial infarction). This was demonstrated by the way

in which the heart muscle contracted after blood flow was restricted.

Grape seed extract was given to the animals before they received a

compound that restricted blood flow. The OPCs were found to exert a

cardioprotective effect against the restricted blood flow, which the

researchers attributed to grape seed's ability to directly scavenge

peroxyl and hydroxyl radicals, and to reduce oxidative stress

developed during ischemia (restricted blood flow).11

Helps protect smokers from oxidative stress

Grape seed extract has been shown to protect low-density lipoproteins

(LDL) under oxidative stress in heavy smokers. A fourteen-week

clinical study involved 24 healthy smokers over the age of 50 who

smoked more than 10 cigarettes per day. During the first four-week

stage, one group was given 150 mg/d of a GSE supplement and the other

was given 150 mg/d of placebo. The fatty component of the blood was

measured before and after the end of each phase. " Treatment with the

supplement, compared with the placebo, induced a 20-percent reduction

of the lipidic peroxidation, with a significant 15-percent increase of

LDL resistance to oxidating stress, " explained Roberto Maffei Facino,

a professor at Milan University.12 In other words, the GSE

supplementation lowered the smokers' risk for developing heart disease.

Strengthens capillary walls and reduces varicose veins

Grape seed OPCs help stabilize blood vessel walls, reduce

inflammation, and generally support tissues containing collagen and

elastin—proteins found in cartilage, tendons, blood vessels, skin, and

muscle. OPCs have also been shown to strengthen capillaries in

double-blind research using as little as 100 mg per day.13

 

A French double-blind study of 50 women with chronic venous

insufficiency (a condition where blood pools in the veins of the lower

legs and can result in varicose veins) found that GSE quickly and

effectively resolved their symptoms using 150 mg per day.14

 

Another French double-blind study of 92 patients found that GSE,

compared to placebo, significantly reduced peripheral venous

insufficiency symptoms, such as edema, pain and cramps. And

supplementation with 100 mg taken three times per day, resulted in

benefits within four weeks.15

Reduces post-op swelling

Possibly because of their effects on blood vessels, grape seed OPCs

can be useful for swelling following an injury or surgery. In

double-blind research, they have been reported to reduce the duration

of edema after face-lift surgery from 15.8 to 11.4 days.16

 

Also, a double-blind controlled study found that postoperative breast

cancer patients who took 600 milligrams of GSE daily for six months

experienced a significant reduction in swelling, pain, and sensations

known as paresthesias.17 Another double-blind controlled study found

that GSE improved the rate at which swelling disappeared following

sports injuries.18

Inhibits growth of cancer cells

Some of the latest research being done on grape seed extract has

indicated that it is a chemopreventative, protecting against the

proliferation of cancer cells.

 

A study recently published in June, 2004, discussed GSE's positive

effect on cancer cells in the human intestinal tract.19

 

Several recent studies at the University of Colorado Health Sciences

Center in Denver, have also shown that GSE inhibits the growth of

human breast cancer,20 prostate cancer,21 and cancer in endothelial

cells.22

How safe is grape seed extract?

OPCs have been extensively tested for safety and are considered to be

essentially nontoxic.23,24

Conclusion

Free radicals have been implicated in a myriad of modern day diseases

and conditions, including aging, arthritis, atherosclerosis, ischemia,

Alzheimer and Parkinson's disease, AIDS and cancer.

 

A large number of synthetic and natural antioxidants have been

demonstrated to produce beneficial effects on human health and disease

prevention. However, the bioavailability and effectiveness of the

various antioxidants are unique to each antioxidant, and some are more

effective than others.

 

As we have seen, grape seed extract's OPCs possess a broad spectrum of

biological, pharmacological and therapeutic activities against free

radicals and oxidative stress. Scientists have demonstrated that GSE

is highly bioavailable and even provides significantly greater

protection against free radicals and free radical-induced lipid

peroxidation and DNA damage than vitamins C, E and beta-carotene.25

 

While vitamins C, E and beta-carotene are certainly potent

antioxidants and necessary for overall health, if you want extra

protection against heart disease and cancer, and added support for

healthy circulation and eye health, consider taking grape seed extract

for added support and peace of mind.

References

 

1. Shi J, Yu J, Pohorly JE, Kakuda Y. Polyphenolics in grape

seeds-biochemistry and functionality. J Med Food. 2003 Winter;6(4):291-9.

Abstract

 

2. Bagchi D, Bagchi M, Stohs SJ, Das DK, Ray SD, Kuszynski CA,

Joshi SS, Pruess HG. Free radicals and grape seed proanthocyanidin

extract: importance in human health and disease prevention.

Toxicology. 2000 Aug 7;148(2-3):187-97.

Abstract

 

3. Murray, Michael T. " PCO Sources: Grape Seed vs Pine Bark. " The

Healing Power of Herbs. Prima Publishing, Rocklin, CA. 1995.

 

4. Murray M, Pizzorno J. Procyanidolic oligomers. In: Murray M,

Pizzorno J, eds. The Textbook of Natural Medicine. 2nd ed. London:

Churchill Livingston; 1999:899-902.

 

5. Yamakoshi J, Saito M, Kataoka S, Tokutake S. Procyanidin-rich

extract from grape seeds prevents cataract formation in hereditary

cataractous (ICR/f) rats. J Agric Food Chem. 2002 Aug 14;50(17):4983-8.

Abstract

 

6. Simonetti P, Ciappellano S, Gardana C, Bramati L, Pietta P.

Procyanidins from Vitis vinifera seeds: in vivo effects on oxidative

stress. J Agric Food Chem. 2002 Oct 9;50(21):6217-21.

Abstract

 

7. Chidambara Murthy KN, Singh RP, Jayaprakasha GK. Antioxidant

activities of grape (Vitis vinifera) pomace extracts. J Agric Food

Chem. 2002 Oct 9;50(21):5909-14.

Abstract

 

8. Shafiee M, Carbonneau MA, Urban N, Descomps B, Leger CL. Grape

and grape seed extract capacities at protecting LDL against oxidation

generated by Cu2+, AAPH or SIN-1 and at decreasing superoxide THP-1

cell production. A comparison to other extracts or compounds. Free

Radic Res. 2003 May;37(5):573-84.

Abstract

 

9. Hagen, Pat. " Fresh Heart for Red Wine Drinkers " The Scientist

http://www.biomedcentral.com/news/20011231/02

 

10. Institute of Food Technologists.

http://www.ift.org/cms/?pid=1000707

 

11. Sato M, Maulik G, Ray PS, Bagchi D, Das DK. Cardioprotective

effects of grape seed proanthocyanidin against ischemic reperfusion

injury. J Mol Cell Cardiol. 1999 Jun;31(6):1289-97.

Abstract

 

12. Vigna GB et al. " Effect of a standardized grape seed extract on

low-density lipoprotein susceptibility to oxidation in heavy smokers. "

Metabolism. 52, 10:1250-7, 2003. (www.ncbi.nih.gov)

 

13. Dartenuc JY, Marache P, Choussat H. Resistance Capillaire en

Geriatrie Etude d'un Microangioprotecteur. Bordeaux Médical

1980;13:903-7 [in French].

 

14. Delacroix P. Etude en Double Avengle de l'Endotelon dans

l'Insuffisance Veineuse Chronique. Therapeutique, la Revue de Medicine

1981;27-28 Sept:1793-802 [in French].

 

15. Thebaut JF, Thebaut P, Vin F. Study of Endotelon in functional

manifestations of peripheral venous insufficiency. Gazette Medicale

1985;92:96-100 [in French].

 

16. Baroch J. Effect of Endotelon in postoperative edema. Results of

a double-blind study versus placebo in 32 female patients. Ann Chir

Polast Esthet 1984;29:393-5 [in French].

 

17. Pecking A, Desprez-Curely JP, Megret G. Oligomeric grape

flavanols (Endotelon®) in the treatment of secondary upper limb

lymphedemas [translated from French]. [source unknown]. 1989:69-73.

 

18. Parienti J-J, Parienti-Amsellem J. Post-traumatic edemas in

sports: a controlled test of Endotelon® [translated from French]. Gaz

Med Fr. 1983;90:231-236.

 

19. Laurent C, Besancon P, Auger C, Rouanet JM, Caporiccio B. Grape

seed extract affects proliferation and differentiation of human

intestinal Caco-2 cells. J Agric Food Chem. 2004 Jun 2;52(11):3301-8.

Abstract

 

20. Sharma G, Tyagi AK, Singh RP, Chan DC, Agarwal R. Synergistic

anti-cancer effects of grape seed extract and conventional cytotoxic

agent doxorubicin against human breast carcinoma cells. Breast Cancer

Res Treat. 2004 May;85(1):1-12.

Abstract

 

21. Singh RP, Tyagi AK, Dhanalakshmi S, Agarwal R, Agarwal C. Grape

seed extract inhibits advanced human prostate tumor growth and

angiogenesis and upregulates insulin-like growth factor binding

protein-3. Int J Cancer. 2004 Feb 20;108(5):733-40.

Abstract

 

22. Agarwal C, Singh RP, Dhanalakshmi S, Agarwal R. Anti-angiogenic

efficacy of grape seed extract in endothelial cells. Oncol Rep. 2004

Mar;11(3):681-5.

Abstract

 

23. Wren AF, Cleary M, Frantz C, Melton S, Norris L. 90-day oral

toxicity study of a grape seed extract (IH636) in rats. J Agric Food

Chem. 2002 Mar 27;50(7):2180-92.

Abstract

 

24. Yamakoshi J, Saito M, Kataoka S, Kikuchi M. Safety evaluation of

proanthocyanidin-rich extract from grape seeds. Food Chem Toxicol.

2002 May;40(5):599-607.

Abstract

 

25. Bagchi D, et al. Free radicals and grape seed proanthocyanidin

extract: importance in human health and disease prevention.

Toxicology. 2000 Aug 7;148(2-3):187-97.

Abstract

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