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THE CHEMOPREVENTATIVE PROPERTIES OF PHYTOCHEMICALS

Featuring The ELLAGIC INSURANCE FORMULA

By GLEN A. HALVORSON M.D.

 

 

 

The Ellagic Insurance Formula is a unique nutraceutical formula based on ground-breaking research suggesting that concentrated extracts of certain plant phytochemicals may therapeutically impact health in ways greater than possible from eating the average daily amount of fruits and vegetables consumed in the American diet.

 

 

The Ellagic Insurance Formula combines therapeutic levels of three polyphenolic plant chemicals, ellagitannins from raspberries (Ellagic acid), oligomeric proanthocyanidins (OPC’s) from whole grape extract, and catechins from green tea together with vitamins A, C, E and the mineral Selenium. Synergistically formulated in our PhytoBioä base of Amino Acids and Digestive Plant Enzymes to create a Potent Antioxidant Formula.

 

 

We review both the scientific laboratory evidence and the known clinical medical research supporting the protective effects of these nutrients in multiple areas of health concern, including their potent actions against the two most feared killers of our time, cardiovascular disease and cancer.

 

 

This booklet will review why and how catechins, procyanidins (proanthocyanidins), ellagitannins, and other phytochemicals are being recommended in preventative and treatment protocols for cardiovascular disease, cancer, inflammatory conditions, asthma, periodontal disease, diabetes, liver disease, cataracts and macular degeneration, just to name a few.

 

 

Cancer kills on average 500,000 Americans EACH year!

 

Would you rather fight it or prevent it?

 

 

ARE WE WINNING THE WAR ON CANCER?

 

During the past thirty years and the WAR ON CANCER, tens of billions of US dollars have been spent on finding a cure for cancer.

 

How successful has this war been?

 

One answer: After 30 years and $40,000,000,000 we now have a higher incidence of cancer, higher death rates, and about the same five-year survival rates.

 

Another answer: About as successful as the war on drugs.

 

During the past thirty or more years, the emphasis in cancer treatment has been to destroy cancer cells by surgery, radiotherapy and cytotoxic chemotherapy.

 

This aggressive "curative" medical and surgical approach has done little to reduce the overall mortality rate from cancer and even less to prevent cancer. 

 

Evidence clearly indicates that if not all cancerous cells are destroyed or removed, in time cancer will recur.

 

The need for more effective treatment and a cure for cancer has turned scientists more recently toward an emphasis on more biological strategies of preventing and dealing with cancers.

 

This is indicated by the proliferation of research documenting the effects of nutritional and environmental factors upon cancer prevention and treatment, as well as significant progress in understanding the molecular basis for the initiation and promotion of cancer.

 

Scientists are unraveling the role of various genes critical to cancer oncogenes, in which mutations promote malignancy; and suppressor or regulatory genes, in which mutations create a loss of regulatory control, enabling cancerous cells to divide uncontrollably.

 

Suppressor genes for many common cancers have been identified and mapped to particular chromosomal locations.

 

There has also been a perceptible shift away from the search and destroy methods of toxic chemotherapy to investigating and understanding the natural processes of cell death and cell suicide, referred to as cellular apoptosis.

 

This area of molecular biology is now the rage in cancer research, with everyone lining up to discover and unravel the complex array of genes involved in orchestrating life and death cycles of normal cells.

 

If the mutations occurring in genes that prevent normal cell death can be prevented, then the ability of cancer cells to grow and divide uncontrollably can be prevented.

 

Nutritional Factors

 

Finally, there is increasing evidence that nutritional factors, particularly antioxidants, interact with cancer oncogenes and suppressor genes.

 

Vitamins A, C and E are strong regulatory factors of cancer cellular differentiation, regression, membrane biogenesis, DNA, RNA, protein and collagen synthesis and the transformation of precancerous into cancer cells.

 

These vitamins exert cytotoxic and cytostatic effects and may cause the cancer to regress to its normal phenotype.

 

The interaction of vitamins A, C and E with oncogenes and growth factors is of considerable importance to cancer cell biology, and may be instrumental in eventual cancer prevention and treatment. 

 

Even more exciting is new research on the many health benefits of potent phytochemical antioxidants, including chemopreventative properties of ellagic acids, oligomeric proanthocyanidins, and green tea catechins, all phenolic flavonoids, which form the basis for Ellagic Insurance Formula

 

PROVEN HEALTH BENEFITS OF FLAVONOIDS

 

Ellagic acid, OPC, and green tea catechins are all members of related chemical families known as flavonoids and flavanols.  These bioflavinoids are polyphenolic compounds and are found in high concentrations in various plants that have potent physiological and biochemical actions within the human body to account for many of the known health benefits associated with eating fresh fruits and vegetables. Because they are such potent antioxidants and because they represent most of the plant polyphenols, flavonoids were quickly isolated by research scientists as the most promising compounds in fruits and vegetables to provide protection from disease-causing agents. To date, hundreds of published articles have reported on the broad protective health benefits of flavonoids.

 

Flavonoids have clearly emerged as protective phytonutrients, and current research focuses on their role in helping to prevent disease.

 

 

Epidemiological research continues to show that greater fruit and vegetable consumption is linked to a lower risk of developing disease. At the same time, it is evident that in many parts of the world, intake of fruits and vegetables is far from recommended levels. Less than 10% of Americans, for example, eat the recommended amount of fresh fruits and vegetables daily, only 20% eat enough vegetables, and only 40% eat enough fruit. Since fruits and vegetables supply most of the flavonoids in our diet, it is clear that our intake of flavonoids is dangerously low, increasing general risk for illness and disease.

 

Bioflavinoids have been shown in a number of studies to be potent antioxidants, capable of scavenging hydroxyl radicals, superoxide anions, and lipid peroxy radicals.  Scientists have learned how to extract and provide many of these bioactive compounds in concentrated form as nutritional supplements.  Fortunately, many of these potent polyphenols account for a significant percentage of the chemical constituents of many plants with known health benefits. For example, of the three flavonoid components found in Ellagic Insurance Formula, dried green tea leaves contain approximately 30% flavonoids by weight, grape seed extracts contain about 40% oligomeric proanthocyanidins, and red raspberries contain approximately 60-100 mg of phenolic compounds per 100 grams, including 1500 micrograms of ellagic acid per gram of dry weight. Phenolic compounds like green tea catechins, grape proanthocyanidins, and raspberry ellagitannins also have proven antibacterial, anti-inflammatory, antiallergic, antimutagenic, antiviral, antineoplastic, anti-thrombotic, and vasodilatory activity.

 

The potent antioxidant activity of flavonoids and their ability to reduce hydroxyl radicals, superoxide anions, and lipid peroxy radicals is considered by many scientists to be among their most important functions as it relates to their effects on human health.

 

Ellagitannins, OPC, and green tea catechins, as indicated above, have many additional potential effects that provide for an even greater range of health benefits than those ascribed to their potent antioxidant properties. 

 

OPC, for example, binds to collagen and is a potent anti-aging supplement that revitalizes connective tissue secondary to its effects on collagen. OPC strengthens capillary walls and improves circulation, lowers blood pressure, reduces peripheral edema, and enhances function in vital organs. 

 

Green tea catechins as well as OPC reduce risk of cardiovascular disease through synergistic actions that reduce blood pressure, prevent oxidation of LDL cholesterol, inhibit platelet aggregation, and reduce capillary fragility. 

 

Each of these phytochemicals may play a major role in cancer prevention through prevention of nitrosamine conversion into carcinogenic substances, prevention of free radical damage to DNA, inhibition of enzymes critical to the conversion of normal cells to precancerous states, and a host of other mechanisms currently under investigation in various clinical trials to be reviewed.

 

It is clearly evident that ellagic acids, oligomeric proanthocyanidins, and catechins are among the most potent antioxidants currently known to man.

 

Oxidative damage is implicated in most disease processes, and epidemiological, clinical, and laboratory research on flavonoids and other antioxidants support their use in the prevention and treatment of a number of acute and chronic degenerative and life-threatening conditions.

 

ELLAGIC ACID

 

Exhaustive research is being conducted in major centers worldwide on ellagic acid because of growing evidence that this extract from berries is a potent antioxidant that may also prove to be an effective chemopreventative agent.

 

Ellagic acid is a naturally occurring phytonutrient, chemically belonging to the phenol family of compounds. It is a phenolic lactone compound found in a variety of fruits and vegetables.

 

It occurs in particularly high concentrations in raspberries, strawberries, cranberries, grapes and many other berries, and in nuts such as walnuts and pecans (Daniel). It is present in plants in the form of hydrolyzable tannins called ellagitannins. Ellagitannins are esters of glucose with hexahydroxydiphenic acid; when hydrolyzed, they yield ellagic acid in numerous plants such as those mentioned above.

 

Ellagic acid is not the only phenolic compound found in fruit and vegetables (phytonutrients) that may have preventive or therapeutic activities on the cancer process, but it may be one of the most potent. Hydroxycinnamic acids also possess potential chemopreventative properties. However, ferulic acid, caffeic acid and related compounds are only minimally effective inhibitors of experimentally induced tumor (Shugar).

 

Initial studies of the antitumor activity of ellagic acid were conducted in animals using esophagus, tongue, lung, colon, liver, and skin tumors. Inhibition of carcinogenesis by ellagic acid appears to occur through a number of mechanisms. Ellagic acid inhibits the initiation of tumors by inhibiting metabolic activation of carcinogenic compounds (such as polycyclic hydrocarbons, nitroso-containing chemicals or food preservatives, and aflatoxins) into forms that induce cell DNA damage (Muktar, Singletary).

 

Ellagic acid is also being considered as a possible chemopreventative agent in human carcinogenesis.

 

Ellagic acid promotes carcinogen detoxification by stimulating the activity of various isoforms of the enzyme glutathione-S-transferase in hepatoma (liver cancer) (Barch).  Another mechanism by which ellagic acid could inhibit tumor initiation is through its potential role as scavenger of the reactive metabolites of carcinogens.

 

Ellagic acid slows the growth of abnormal colon cells in humans, prevents the development of cells infected with human papilloma virus (HPV), which is linked to cervical cancer, and promotes apoptotic growth (natural death) of prostate cancer cells.

 

The apoptotic process triggered by ellagic acid may also have beneficial effects on breast, lung, esophageal, and skin cancer (melanoma).

 

NOTE: Apoptosis is a mechanism by which the body destroys imperfect cells. During the cell cycle, a cell can become damaged, and rather than let this cell continue to divide into additional imperfect cells, the apoptosis mechanism simply destroys the imperfect cell. There are two popular pronunciations; ap-o-to'sis and ap'op-to'sis.  A more technical definition is that apoptosis is the single deletion of scattered cells by fragmentation into membrane-bound particles which are phagocytosed by other cells; believed to be due to programmed cell death. The targeted cells quickly shrink and shed tiny vesicles that are ingested and destroyed by neighboring cells without leaving a mess to cause inflammation. In this orderly and efficient process, the cell materials can be disassembled and the building block used over again. The apoptosis process takes only a few minutes which markedly contrasts with cell necrosis, which is cell death resulting from injury or poisoning. In cell necrosis, the cells swell over a period of several hours until they burst, spilling their contents over neighboring cells eliciting an inflammatory response.

 

 

 

Unpublished research by Dr. Daniel Nixon at the Medical University of South Carolina (Hollings Cancer Center) shows that one cup of raspberries per week will stop prostate cancer growth for a period of up to one week.  Their studies reveal that ellagic acid from red raspberries is readily absorbed through the gastrointestinal tract. Additional tests reveal that the Ellagic acid retains its potency after heating, freezing and concentration processing. So whether consumed fresh, in juices, fruit spreads, preserves or sorbets, red raspberry has been recommended by researchers at the Hollings Cancer Center as a beneficial addition to any healthy diet. (See also: Nixon DW. Alternative and complementary therapies in oncology care. J Clin Oncol  17(11 Suppl):35-7, 1999. Nixon DW. Prostate cancer and nutrition.  JSC Med Assoc 96(2): 85-6, 2000. Nixon DW. Preventive medicine in the year 2000.  Prev Med 30(1): 1-2, 2000.)

 

Medical findings in Europe further show that Ellagic acid reduces the incidence of birth defects, promotes wound healing, reduces and reverses chemically induced liver fibrosis, and is helpful in the fight against heart disease!

Animal tests suggest that red raspberry may reduce levels of glucose (blood sugar) in animals, and therefore may help in the management of diabetes.

 

As noted above, research studies on Ellagic acid have been extensive, especially in vitro studies and studies in laboratory animals.  Although yet to prove conclusively in humans that red raspberries will reduce risk of cancer or even cause remission of active disease, this research does represent a substantial body of evidence to support the protective effects of ellagitannins in humans in combination with other chemopreventative nutrients. 

 

WHAT IS ELLAGIC ACID?

 

Description and Constituents:

 

Ellagic acid is a phenolic compound found in plants in the form of hydrolyzable tannins called ellagitannins. Ellagitannins are esters of glucose with hexahydroxydiphenic acid; when hydrolyzed, they yield ellagic acid, the dilactone of hexahydroxydiphenic acid. Ellagic acid is a very stable compound, moderately soluble in dimethysulfoxide, slightly soluble in other organic solvents, and relatively insoluble in water. It is readily absorbed through the gastrointestinal system in mammals, including humans.

 

 

Mechanism of Action:

 

Ellagic acid is pharmacologically active and has been found to control hemorrhage in animals and in humans, presumably as a result of its ability to activate Hageman factor.

 

Ellagic acid acts as a scavenger to "bind" cancer-causing chemicals, making them inactive. It inhibits the ability of other chemicals to cause mutations in bacteria. In addition, Ellagic acid from red raspberries prevents binding of carcinogens to DNA, and reduces the incidence of cancer in cultured human cells exposed to carcinogens.

 

Ellagic acid from raspberries causes apoptosis (normal cell death) of human cervical cancer cells (human papilloma virus), induces G1 inhibition of cancer cell division, and prevents destruction of the P53 gene by cancer cells.  P53 is regarded as a safeguard against mutagenic activity (cancer causing changes) in cervical cells (Nixon).

 

Additional studies suggest that one of the mechanisms by which ellagic acid inhibits mutagenesis and carcinogenesis is by forming adducts with DNA, thus masking binding sites to be occupied by the mutagen or carcinogen.

 

Ellagic acid induces G arrest, inhibits growth, and induces apoptosis in human cervical cancer cells in laboratory studies (Narayanan).

 

Ellagic acid is active in antimutagenesis assays, and has been shown to inhibit chemically induced cancer in the lung, liver, skin and esophagus of rodents, and TPA-induced tumor promotion in mouse skin (Stoner).

 

Ellagic acid elicits a dose-dependent bactericidal effect in H. pylori cultures, the bacteria thought primarily responsible for the development of gastric ulcers (Chung).

 

Ellagic acid is an effective inhibitor of lung and esophageal tumors in mice (Stoner).

 

Ellagic acid significantly reduces the elevated levels of enzymes, lipid peroxide and liver hydroxy proline and rectifies liver pathology in laboratory animal hepatotoxcity induced by carbon tetrachloride (Thresiamma).

 

Ellagic acid inhibits lipid peroxidation necrosis of skin flaps, enhancing preservation of grafting procedures (Ashoori).

 

Ellagic acid has a marked inhibitory effect on acid secretion and the occurrence of stress-induced gastric lesions (Murakami).

 

One method by which cancer affects DNA is through covalent bonding of the carcinogen to the DNA molecule. Ellagic acid inhibits mutagenesis and carcinogenesis by forming adducts with DNA, thus masking binding sites to be occupied by the mutagen or carcinogen (Teel).

 

Ellagic acid treatment of preweanling mice before an injection of B(a)P diol-epoxide caused a 44-75% inhibition in the number of diol-epoxide-induced lung tumors (Chang).

 

Ellagic acid inhibits N-nitrosomethylbenzylamine (NMBA) tumorigenesis in the esophagus of F-344 rats. Ellagic acid inhibited the development of both preneoplastic and neoplastic lesions by 25-50% (Daniel and Stoner).

 

Ellagic acid reduced the number of altered foci and the incidence of hepatocellular neoplasms in rats with liver cancer induced by N-2-fluorenylacetamide (Tanaka). 

 

Ellagic acid in strawberries prevented esophagus cancer in rats when they are given high doses of carcinogens and then treated by feeding on lyophilized strawberries.

 

Laboratory tests reveal ellagic acid exerts similar chemopreventative effects on breast, pancreas, esophageal, skin, colon, and prostate cancer cells.

 

Toxicity, Side Effects, and Allergic Reactions:

 

No adverse side effects have been recorded in the scientific literature from taking ellagic acids in the form of an extract. No allergies to the extracts have been described.

 

Suggested Usage:

 

Consuming one cup (150 grams) of red raspberries per day prevents the development of cancer cells in unpublished studies.  Most extract formulas recommend from 500-2000 mg of ellagitannins per day.  The amount of Ellagic acid found in red raspberries is 1500 micrograms per gram of dry weight.  If one cup contains 150 grams by dry weight, then each cup of red raspberries would average 225 mg of ellagic acids as well as up to 90 mg of anthocyanidins and less than 40 mg of other polyphenols including flavanols.

 

OPC

 

OPC is unique among biological nutrients contained in nutritional supplements in that extensive laboratory and clinical research has been ongoing for more than fifty years to support the structure and function claims made for its multiple potential health benefits.

 

Let's put it this way--research has really found only the tip of the iceberg with respect to plant phytochemicals and cancer.  There is enough evidence to convince anyone to take OPC as part of a good program of preventive nutrition that should also include at least seven servings of fresh fruits and vegetables daily.

 

OPC is added to Ellagic Insurance Formula because it is a proven source of potent phenolic compounds that have many positive effects on health, including a significant effect on cardiovascular function.  OPC also contains ellagitannins, although in lesser quantities than red raspberries.  A brief review of the multiple benefits of OPC will quickly convince even the most skeptical scientist of the value of increasing daily intake of bioflavinoids, including OPC in particular.

 

Description and Constituents:

 

OPC is an acronym for "oligomeric proanthocyanidins", a polyphenolic phytochemical extracted from many different plants of which the highest concentrations for supplement use are found in grape seed extract, entire grape extract, and pine bark extract. 

 

OPC is distinct from other plant flavonoids because it is a flavan-3-ol.  Flavanols differ from flavonoids in that flavanols are highly water-soluble, absorbable and bioavailable. OPC is quickly and readily distributed throughout the body within minutes to a few hours of oral ingestion.  OPC flavanols are technically polyphenols: OPC consists of many different shapes and sizes of catechin and epicatechin molecules bonded together to form the unique chemical properties of OPC distinct from fruit and vegetable bioflavinoids.

 

OPC extracted from the stems, leaves, seeds and bark of plants also contains various organic acids and sugars as well as more complex polymers called tannins.  Unlike other flavonoids, OPC is colorless until enzymatically broken down into red, purple, and blue anthocyanidins.  The original researchers on OPC coined the nickname "pycnogenols" for OPC, meaning "products of condensation", to describe the way OPC forms in plants from the basic catechin molecules into dimers, trimers, and other polymers.  As a result, OPC exerts many unique effects on the chemistry and physiology of the human body.

 

Resveratrol is a chemical found in the skin of grapes and is present in red wines and in OPC that is extracted from the whole grape.  Resveratrol is a phenolic compound thought responsible for some of the cardioprotective and cancer-protective properties of red wine.

 

Mechanisms of Action:

 

OPC is a potent scavenger of free radicals.  It is one of nature's most potent antioxidants.  OPC contains multiple electron donor sites (hydroxyl sites) that allow it to bind to unstable molecules called free radicals by donating its hydrogen atoms.  OPC also recycles other antioxidants such as vitamin C and glutathione by removing the free radicals they bind with and freeing them up to interact again with other free radicals.

 

Examples of free radical scavenging activities of OPC include: traps hydroxyl and superoxide radicals, inhibits or delays onset of lipid peroxidation, chelates free iron molecules and inhibits iron-induced lipid peroxidation, reduces free radical production by inhibiting the enzyme xanthine oxidase, and inhibits degradative enzymes that produce free radicals through soft tissue damage (hyaluronidase, elastase, collagenase, protease).

 

OPC from grape seed extract contains the most potent antioxidant activity of the various polyphenols studied. In one study rat blood vessel walls were exposed to free radicals and the ability of grape seed extract, pine bark, and bilberry to protect the blood vessel walls from damage was measured.  Grape seed extract provided the best arterial wall defense against the damaging effects of free radicals and on an absolute scale, was 22% stronger than pine bark extract and 15% greater than bilberry extract (Jonadet).

 

OPC binds to protein tissue.  For example, OPC binds to collagen to make the spiral coils of collagen stronger and more elastic. Since collagen is the support structure for blood vessel walls, joint cartilage, joint capsules, tendons, ligaments, and skin, OPC therefore improves capillary resistance, reduces blood pressure, reduces soft tissue edema, improves circulation, improves joints flexibility, softens skin wrinkles, and may even produce a more youthful appearance.  Another example, OPC binds to protein receptor sites that control the release of various inflammatory and enzymatically harmful enzymes.  OPC blocks the release of histamine, resulting in reduced symptoms in allergies, ulcers, and asthma.  OPC blocks the release of proteases and collagenases, resulting in reduced swelling, inflammation, and pain in arthritis.

 

OPC reduces platelet aggregation.  OPC is more effective than aspirin at inhibiting clumping of platelets, thus reducing atherosclerosis and the risk of heart attack and stroke.

 

OPC inhibits oxidation of LDL cholesterol.  OPC also reduces LDL cholesterol levels, thereby reducing the risk of cardiovascular disease.

 

OPC inhibits swelling (edema) and inflammation.

 

OPC decreases capillary fragility.  This is another way of stating that OPC binds to collagen tissue.  Improving capillary fragility improves blood pressure, reduces leakage of blood constituents into the extravascular tissue, enhances cellular metabolism, and decreases peripheral edema.

 

OPC inhibits damage to blood vessels and inhibits abnormal clotting of blood, both of which are related to heart disease.  OPC inhibits excessive metabolizing of nitric oxide, a process linked to inflammation, arthritis, and Alzheimer's disease (Fitzpatrick).

 

100 mg of OPC given to smokers two hours after smoking inhibited clotting of platelets more effectively and faster than 500 mg of aspirin.  A 200 mg dose of OPC was even more effective with effects lasting a week after the OPC was stopped (Watson, Putter).

 

OPC as a potent antioxidant corrects some forms of infertility in males by increasing the number of structurally normal sperm, providing a more cost effective treatment than expensive fertility drugs (Roseff).

 

OPC is one of nature's most powerful antioxidants, inhibiting superoxide and hydroxyl forms of oxygen free radicals more effectively than either vitamin C or E (Bagchi).

 

OPC inhibits lipid peroxidation of blood fats more effectively than vitamin E (Bagchi).

 

OPC inhibits growth of cancer cells in the laboratory while simultaneously enhancing the growth and viability of normal human gastric mucosal cells (Ye).

 

OPC inhibits acetaminophen-induced liver death in lab mice (Ray).

 

OPC improved venous insufficiency in 80% of patients treated with 100 mg of OPC after just ten days of treatment.  Itching, heaviness and pain disappeared with rapid reduction of the swelling in lower limbs.  Symptom improvement correlated with objective changes in videocapillaroscope examination (Constantini).

 

Resveratrol, a chemical found in the skin of grapes,(and in our OPC) was shown to protect lipid and protein membranes against copper-induced oxidation (Fremont).

 

OPC binds to both collagen and elastin fibers in connective tissue to reduce their rate of degradation by inflammatory enzymes (Tixier).

 

OPC protects the lining of blood vessel walls from free radical damage (Rong).

 

OPC inhibits the enzymatic reduction of tobacco specific nitrogen-containing compounds to their carcinogenic derivatives in the gut and liver (Huynh).

 

OPC reduces diabetic retinal bleeding and improves vision within a few weeks on as little as 100 mg per day (Froantin).

 

OPC reduces peripheral edema in several studies involving over 4,000 patients (Henreit).

 

OPC increases capillary resistance, resulting in lower systolic blood pressure (Lagrue).

 

OPC reduces severity and duration of soft tissue injuries in soccer players treated immediately following injury with 400 mg per day tapering over several weeks to 200 mg per day of OPC from grape seed extract (Parienti).

 

OPC reduces symptoms in gastric ulcers (Saito).

 

OPC reduces post-surgical swelling and pain and speeds soft tissue recovery when elective facial surgery patients were pre-treated before and after surgery (Baruch).

 

OPC reduced symptoms of PMS in over 60% of patients treated with 200 mg of OPC for three months and in 80% of patients treated for six months (Amsellem).

 

Resveratrol from grape extract was found to inhibit the growth of cancer cells, lower blood pressure, inhibit oxidation of LDL cholesterol, and inhibit platelet aggregation.

 

Clinical Indications:

 

OPC has multiple potential health benefits described in the literature.  Profound effects on health have been documented with multiple clinical studies outlined in the references.  OPC has been found particularly effective in microvascular disorders including venous insufficiency, capillary fragility, varicose veins, and retinal disorders such as macular degeneration and diabetic retinopathy.  It has more recently been identified as an inhibitor of atherogenesis and platelet aggregation, making it a potentially important treatment for reduced risk of cardiovascular disease.  Further studies are also being conducted on the anti-inflammatory and immunostimulant properties that result in reduced symptoms in allergies, trauma, and arthritis.  

 

OPC and cardiovascular disease: OPC improves general circulation secondary to its effects on collagen. OPC reduces blood pressure, inhibits oxidation of LDL cholesterol, and inhibits aggregation of platelets more effectively than aspirin.  OPC may reduce risk of heart attack or stroke because oxidation of LDL cholesterol, for example, is the first step in atherogenesis, hardening of the arteries.  Sticking of platelets is necessary for blood clots to form and shut off blood flow. OPC reduces peripheral edema.

 

OPC reduces risk of heart attack and stroke by preventing oxidation of blood fats. Frankel noted that polyphenols in red wine inhibit oxidation of cholesterol, exposing again the secret of the "French Paradox", why red wine drinkers have lower rates of heart attack and stroke. Other studies (Meunier, Mangiapane) have identified the ability of OPC to prevent free radical damage to cholesterol.  Recent studies of the relationship between cholesterol and risk of heart disease suggest it is not the total amount of cholesterol that increases risk of heart disease, as much as whether that cholesterol is damaged by free radicals and sticks to blood vessel walls to increase risk of blockage.

 

Musculoskeletal: OPC reduces pain, inflammation, swelling, and stiffness in joints made symptomatic from arthritis or injury in several documented ways.  OPC is a potent anti-inflammatory that inhibits the release of degradative enzymes including collagenases, proteases, and elastases that damage soft tissues including joint cartilage and synovial joint linings.  OPC is a potent antioxidant that inhibits free radical damage and inflammatory response following injury.  OPC speeds recovery from acute injury by inhibiting or reducing the formation of soft tissue edema secondary to acute inflammation. OPC reduces symptoms of chronic joint stiffness and restores functional mobility by improving elasticity of connective tissues by binding to collagen and elastin. OPC speeds up healing by increasing circulation to joints. 

 

Aging: OPC improves the appearance of skin.  OPC increases circulation to the brain and may enhance cognitive functions such as memory and mood.  OPC reduces joint stiffness associated with wear and tear of aging.  OPC may slow the aging process by inhibiting excess damage to cell walls secondary to free radicals.

 

Allergies, ulcers and asthma: OPC inhibits allergic histamine responses and reduces symptoms from the above conditions. OPC appears to reduce inflammatory skin lesions associated with psoriasis and eczema.

 

Immunity: OPC may enhance immune system function in several direct and indirect ways.  OPC reduces free radical damage to immune cells.  OPC increases circulatory function.  OPC aids in detoxification of the liver and gut by reducing the free radical load on these organs of detoxification.  OPC binds to toxic inorganic trace metals.