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Y2K Antioxidants
The Emergence of Phytochemicals

By Dr. John M Berardi, Ph.D.
First published at www.fitnessheaven.com, 2000.

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It's August 2000 and eight months have passed since our exaggeratedly ceremonious induction into the new millennium. While the rather anti-climactic nature of those post-midnight hours left many disappointed, the ticking of the millennial clock presented a very real marker for the passage of time.

On a smaller scale, the aging process also provides such markers in our own lives. These markers, some of which are very positive, also denote the passage of time in a unique and very personal way. Unfortunately however, the aging process also brings a host of negatives with regard to health and wellness.

Science, with increasing fervor, has focused its considerable energies toward the daunting task of studying the aging process and the diseases associated with it. One current scientific theory dictates that there is an interaction between aging and disease in which one perpetuates the other. In other words, diseases can make us age and aging can bring on disease. Many are surprised that one potential link between the two is oxygen. Ironically, although humans need to consume oxygen for survival, they grow progressively sensitive to the very oxygen that sustains their existence. Thus, as individuals grow older, their reliance on oxygen is one of their greatest liabilities in the quest for youth, quality and quantity of life. Let me explain.

Free Radical Theory and Anitoxidant Protection

Once taken in the body, oxygen is processed metabolically. This metabolism makes the oxygen available to perform its vital functions in the cells. This is a good thing. However, as a result of this processing, derivatives of oxygen known as reactive oxygen species (ROS) are formed. It is these ROS molecules that we need to worry about since they have been implicated in a number of pathological conditions including cancer, myocardial infarction (heart attack), inflammatory diseases (arthritis), and other diseases of aging.

If you haven't heard about ROS before that's because most writers focus on the by-products of ROS metabolism, free radicals. Both are extremely volatile and potentially dangerous as they react with cellular components such as proteins (both enzymatic and structural), membrane lipids, and the nucleotides within DNA and RNA. Since these represent all the functional and regulatory stations within the cells, this places virtually every part of the cell at risk for radical induced damage. And this damage can lead to poor cell structure, function, and even altered genetic patterns.

Fortunately, our bodies have developed defense mechanisms (natural antioxidants) to compensate for ROS and free radical formation. Antioxidants act to attract the ROS and free radicals in order to spare the cell's machinery. The problem, however, is that stress, exercise, pollution, aging, and a number of disease states can lead to an overwhelming of these natural antioxidant defenses. In such situations, additional antioxidants in the form of foods or supplements may be necessary to preserve the integrity of our cells.

The New Generation of Antioxidants

Assuming an adequate diet, most nutritionists have suggested that people do not need supplemental antioxidants in the form of vitamins or herbs. This advice, however, seems much too conservative. Traditionally nutrition research has focused on the prevention of deficiency. Today, however, we are interested in optimal function. In light of recent scientific discoveries on the therapeutic benefits of moderate doses of vitamins C and E, as well as other antioxidants, it appears that both diet and supplementation may be necessary to promote optimal health. It may be impossible to consume enough nutrients for optimal health with dietary means alone. In addition, very few individuals actually consume a diet that is actually adequate and varied.

With this said, a new generation of supplements have been investigated. These supplements, including antioxidants, have been discovered in interesting places. The most interesting thing about these nutrients, however, is the fact that they have been found within our food. That's right, aside from the major vitamins, minerals, and macronutrients (proteins, carbs, and fats) in most foods; there is emerging a new group of food substances known as phytochemicals. Very little is known about what the exact human value of phytochemicals may be, but with each year more is discovered about these intriguing nutrients and how they may impact health.

Phyochemicals

There are hundreds of known phytochemicals. Some of the most researched, however, are a group of nutrients known as polyphenols (including their derivatives including the flavonoids, tannins, and catechins). These molecules are derived from plants or their fruits and have great potential benefit for human health. One of the many proposed benefits of the polyphenols and their derivatives is their potential for antioxidant effects. Due to their structural similarities, the polyphenols act as antioxidants by donating electrons to the electron-poor free radicals. This prevents the free radicals from taking electrons from the cellular machinery and thereby damaging the cell. In addition to scavenging free radicals, polyphenols are associated with prevention of diseases such as atherosclerosis and cancer among others. Some of the more well-documented foods and food derivatives rich in polyphenols are listed below and include grape seed extract, green tea, and ginkgo biloba, milk thistle, and pine bark.

Ginkgo Biloba

The leaves and fruit of this tree have been used as therapeutic agents in China for over 5000 years. More recently, ginkgo biloba extracts have been used in western medicine in the treatment of minor defects in brain function including poor concentration, short-term memory loss, dizziness, headache, and emotional hypersensitivity and anxiety. Ginkgo has also been used in peripheral artery disease to increase blood flow to tissues supplied by the damaged arteries. While many of ginkgo's beneficial actions are due to its ability to increase blood flow, it has been speculated that further beneficial actions of this extract are due to the antioxidant properties of its ingredients, especially its variety of polyphenols including flavonoids and terpenes. These antioxidant properties may help to protect blood vessels as well as brain and nerve cells from the free radicals associated with poor blood flow and inflammation. These properties demonstrate that ginkgo might be as useful in the prevention of vascular/arterial disease as well as cerebral problems as it is in the treatment of such problems. Typically 120 mg per day is recommended take in 3, 40mg doses.

Grape Seed Extract

Grapes and red wine have been receiving much attention lately due to their proposed health benefits, including the reduction of the incidence of mortality and morbidity from coronary heart disease. The polyphenols that are found in grape seeds, skin, and stems are known as proanthocyanidins. These phytochemicals have been shown to be more potent free radical scavengers than vitamins C, E, and beta-carotene and are thought to serve many favorable biological roles with respect to heart disease. Grape seeds extracts are useful in the prevention of arterial wall damage, in the lowering of blood-cholesterol levels, and in the shrinking of cholesterol deposits in arteries. These antioxidants may also prevent the formation of excessive blood clots and the constriction of blood vessels. These benefits are thought to be due, in part, to the antioxidant properties of the extract. In addition to potent free radical scavenging abilities, grape seed extract appears to protect against cell membrane and DNA damage in the liver and brain. Further, it appears this phytochemical is active in protecting the heart itself from free radicals associated with poor oxygen delivery. Typically 50mg per day is recommended for antioxidant protection, while 150-200 mg per day is recommended for therapeutic purposes.

Green Tea

The plant Camellia sinensis has been the subject of many investigations on the positive health benefits of tea. It has been shown that the daily consumption of tea may be involved in the prevention of coronary heart disease, artherosclerosis, and some cancers. These health benefits of tea are presumed to be related to the antioxidant effects of its components, namely, its polyphenolic tannins and catechins. These phytochemicals are in highest concentrations in green tea as opposed to other types. Although black tea contains a number of polyphenols as well (i.e. theaflavine gallate, digallate, etc.), the effects of these compounds are not well researched. The phytochemicals in green tea appear to stabilize cell membranes in the presence of carcinogen related free radicals.

Although green tea is not recognized as medicinal within the medical community, there are anecdotal reports of its benefits in the relief of headache, diarrhea, and stomach upset. Some recent research has shown green tea to be thermogenic to a greater extent than would be expected from its caffeine content alone. Usually, for the antioxidant benefits, 3 cups or more per day are recommended.

Milk Thistle

This herb, otherwise known as Silybum marianum, contains the active flavonolignans, which include the compounds silybin, silydianin, and silychristine. These compounds are collectively known as silymarins. Silymarins are known primarily for their liver protective effects. This liver protection involves the defense against drugs and toxins (including acetaminophen, ethanol, carbon tetra-chloride, and D-galactosamine); protection against liver injury (induced by poor blood delivery); and defense against radiation, iron toxicity, and viral hepatitis. These benefits are thought to be due to antioxidant action, cell membrane protection, enhanced detoxification, and protection of the cell's natural antioxidants. Milk thistle appears to prevent some toxins from entering the liver cells while it also promotes the formation of new liver cells to repair those with damage. With milk thistle supplementation, the improved antioxidant status displayed by certain liver cells (cells that detoxify the blood as it bathes the liver) can actually result in improved clinical outcomes in hepatitis, cirrhosis, and inflammatory liver disease. The typical dosage is 200-400 mg per of silymarin per day.

Pine Bark (Pycnogenol)

Pine bark, or Pinus maritima, has been examined for its principal extract, pycnogenol. This extract has been shown to contain a variety of bioavailable phenolic derivatives (proathrocynadins, catechins and flavonoids). Like grape seed extracts (which are also high in proathrocynadins), pine bark extracts have been shown to have strong antioxidant activity through their free radical-scavenging activities. In addition, this antioxidant is especially interesting because it appears to interact with and to regenerate the other cellular antioxidants including Vitamins C and E as well as the endogenous antioxidants glutathione, SOG, and CAT. This enables the natural antioxidant defenses to better do their respective jobs. Typically, 30-50mg of pine bark extract (85-95% proanthroxynadins) is recommended for its antioxidant benefits.

A Sensible Plan

As you can see, the new generation of antioxidants is showing real promise in the future as both preventative and therapeutic medicine. Not only do the phytochemicals discussed have antioxidant benefits associated with disease prevention, but also possess very real treatment options for numerous ailments. From the current research, ginkgo may assist in brain and vascular diseases, grape seed extract is useful for heart and vascular ailments, green tea may assist in digestive discomfort and in cancer prevention, milk thistle may protect the liver, and pine bark extract may upregulate the other antioxidant defense mechanisms.

As more research is conducted examining these compounds, a much clearer picture of the exact benefits and mechanisms of phytochemicals will be made available. For the present however, after consulting with a physician and learning about the potential benefits of each group of nutrients, an informed decision can be made as to how to most effectively incorporate the different nutrients into your holistic health regimen.

Although each of the discussed substances has unique properties, there is considerable overlap in function. This is especially the case with their antioxidant functions. Remember, indiscriminant combinations of the different phytochemicals may cause nutrient interactions that may render the supplements ineffective or worse yet, harmful. With sound medical advice and cautious experimentation, the use of phytochemicals may provide individuals with some of the tools necessary to reap the rewards of the aging process without falling victim to excessive decline in function that the passage of time can bring with it.