Every now and then I get a break in putting together a newsletter. I get to steal the entire newsletter from myself. In this case, I was able to take most of the material for this newsletter from the formulation information for the new Ultimate Antioxidant™ that I just put together for Baseline Nutritionals®. However, don’t think of this as a pitch for a particular formula — more as a guide for the range of antioxidants you need for full spectrum protection. If you’re so inclined, you can assemble your own version of the formula by buying separate bottles of each ingredient from your favorite manufacturer.
Designing an Antioxidant Formula
Over the years, I have formulated a number of antioxidant formulas for various companies. In fact, this is my specialty — the design of cutting edge nutritionals using standardized herbs and isolates. On the other hand, I have also become known as a strong advocate for the use of whole herbs and food complexes in all formulations. Why the apparent contradiction?
There is no question but that nature packages nutrients in “food complexes;” and that, in general, it is best to design supplements using only whole food complexes. Antioxidants, however, provide one of the few exceptions to that rule — as long as a few provisos are followed.
The reason for the exception is that because no one antioxidant works on all free radicals and in every area of the body, you need to combine a number of antioxidants in one supplement to offer an effective defense. (In fact, many antioxidants reinforce and/or recycle each other.) For this reason, it is impossible to fit the variety you need (at adequate levels) into one supplement unless you use some standardized herbs and isolates.
The trick is (1) to use only natural isolates — no synthetics, (2) to offer as complete a complex as you can even when using isolates, and (3) to make sure you TAKE ADVANTAGE OF THE SYNERGISTIC EFFECT that a number of the antioxidants share with each other.
The Ultimate Antioxidant™
Here now is the latest version of my ultimate antioxidant formula based on years of expertise in the field — even including the amounts required for each antioxidant. (Note: as ways to incorporate whole-food complexes while still maintaining potency are developed, or new phytochemicals are discovered, this formula will change.)
Vitamin A as Alpha and Beta carotene — 5,250 IU
Carotenoids are phytonutrients that protect plants from damage caused by UV radiation and other environmental factors. In humans, they have been shown to inhibit the proliferation of various types of cancer cells such as those affecting the lungs, stomach, cervix, breast, bladder, and mouth. They also have been proven to protect against atherosclerosis, cataracts, macular degeneration and other major degenerative disorders. The key carotenoids are: beta carotene, alpha carotene, lycopene, and zeaxanthin.
Probably the best known of the carotenoids, beta carotene is converted by the body into vitamin A as needed to strengthen the immune system and promote healthy cell growth. In addition, beta carotene is a potent antioxidant, offering particular benefits to the immune system and the lungs. (Note: synthetic beta carotene, made from acetylene gas is to be avoided. As a side note, synthetic beta carotene was used in the studies that produced negative results when beta carotene was tested.)
But also, it is important to understand that beta carotene is not the most important of the carotenoids. It’s just the only one that is a recommended daily requirement. Once again, the FDA and the USDA are several decades behind the times.
For example, recent studies have shown that alpha carotene is one of the most powerful carotenoids and has a strong inhibitory effect on the proliferation of various types of cancer cells such as those affecting the lungs, stomach, cervix, breast, bladder and mouth. It works by allowing normal cells to send growth-regulating signals to premalignant cells.
Bottom line. You want a carotenoid complex, not pure synthetic beta carotene.
Lutein — 10 mg
In addition to being a specific for the prevention of macular degeneration (lowering the risk by over 50%), lutein has also been shown to have strong anti-cancer properties. Its antioxidant effect is significantly enhanced by the presence of zeaxanthin, and bilberry. When combined with vitamin C, these three antioxidants have been shown to significantly decrease the risk of cataracts. In this version of the formula, I upped lutein levels by 25%.
Zeaxanthin — 500 mcg
To match the increase in lutein, I increased zeaxanthin levels by 66%. Lutein and zeaxanthin are both part of a group of carotenoids known as xanthophylls, which are extremely beneficial to the eyes and help significantly in the prevention of macular degeneration
Lycopene — 6 mg
Derived primarily from tomatoes (cooked, not raw), lycopene appears to be one of the best defenses against prostate cancer and bladder cancer. When used in conjunction with vitamin E and green tea extract, studies indicate that it inhibits prostate cancer proliferation by some 90%.1Mariella Pastoria, Hanspeter Pfandera, Daniel Boscoboinikb, Angelo Azzib. Lycopene in Association with a-Tocopherol Inhibits at Physiological Concentrations Proliferation of Prostate Carcinoma Cells.” Biochem Biophys Res Commun. 1998 Sep 29;250(3):582-5. <http://www.ncbi.nlm.nih.gov/pubmed/9784387>
Selenium (as methylselenocysteine) — 140 mcg
Food sources provide selenium in either an inorganic form (selenite or selenate) or in an organic form where it displaces sulfur in methionine or cysteine. By switching from the inorganic form to the organic, readily useable methylselenocysteine form, I was able to virtually double selenium levels with no concerns about toxicity and improve absorbability at the same time.
Selenium is a component of glutathione peroxidases which are primarily responsible for reducing peroxide free radicals that include lipid peroxide formation in cell membranes. Reduction of peroxides breaks the auto-oxidative chain reaction that damages cell membranes. Selenium is synergistic with glutathione and catalase in helping to protect the integrity of cell membranes. It stops the growth of tumors, and it protects the liver.
Specifically, low levels of selenium have been connected to death from heart disease, breast cancer, prostate cancer, colon cancer, and in fact cancer of all kinds. Some studies have shown that selenium may be 50-100 times more powerful than any other anti-carcinogen known.
Sodium Citrate — 0 mg
If you keep increasing levels of some ingredients, you have to remove others. I dropped sodium citrate from the formula to make room.
N-Acetyl-Cysteine (NAC) — 225 mg
One of the keys to a healthy immune system is maintaining high levels of glutathione in the body. Unfortunately, supplementing with glutathione doesn’t really help. Fortunately, there are alternatives. Supplementation with N-acetyl-cysteine (NAC) has been proven to substantially raise the body’s glutathione levels. In addition, NAC supplementation is mandatory for all smokers and big-city dwellers as it protects against toxic aldehydes that enter the body through cigarette smoke and pollution.
L-Methionine — 225 mg
An essential sulfur amino acid, methionine is a powerful antioxidant and liver detoxifier — where it assists in the normal detoxification processes. As an antioxidant, it provides powerful protection in the colon. And finally, methionine is involved in the synthesis of choline, adrenaline, lecithin, and B12, and it works as a powerful SAMe precursor.
Quercetin — 180 mg
Quercetin is one of the class of antioxidants known as bioflavonoids. A prime role of quercetin is to protect the integrity of cell walls from free radical damage. In addition, quercetin prevents the release of histamines into the bloodstream, thereby helping to control food and pollen allergies.
Gingko biloba– 180 mg (24/6%)
Known as the brain antioxidant, gingko has been shown to increase brain functionality, which makes it useful in helping to improve concentration and memory. This makes it a specific for Alzheimer’s, where it has the added benefit of helping to significantly reduce depression.
In addition, gingko oxygenates the blood, increases circulation, and strengthens blood vessels. And finally, its anti-inflammatory, lung-relaxant properties have proven useful in the treatment of asthma, where it eases coughing and reduces tissue inflammation.
Curcumin — 120 mg
Curcumin is what gives turmeric its yellow color. Studies have shown that it can inhibit colon cancer cells by some 96% in a matter of hours. It also appears to have great potential in countering the effects of prostate cancer and breast cancer. In a sense, curcumin can be thought of as natural chemotherapy — with the ability to selectively kill cancer cells, while at the same time leaving normal cells alone. Note: Curcumin and green tea strongly reinforce each other.
Green tea extract — 120 mg (95%)
By moving up from an 83% extract to a 95% extract, I was effectively able to increase the activity level of the green tea by 14% while keeping the amount the same. Green tea antioxidants are of the same family as grape seed and pine bark extracts. They are polyphenols, chief of which are the flavonoids called proanthocyanidins. In green tea, the main proanthocyanidins are the catechins, and the most powerful of the catechins is Epigallocatechin Gallate (EGCG), found in the highest concentration in green tea.
Green tea works to prevent tumors from developing the blood vessels they need to survive. It has been shown to inhibit metastasis. And it is the first known natural telomerase inhibitor. That is to say, it eliminates the “immortality” of cancer cells which is their trademark and which makes them so deadly. Green tea is particularly effective in destroying the causes of leukemia, prostate cancer, and breast cancer.
And the benefits of green tea don’t stop there. It has also been shown to be effective in regulating blood sugar, reducing triglycerides and in reversing the ravages of heart disease. (Incidentally, the Japanese, who drink large amounts of green tea, have some of the lowest rates of cardiovascular disease in the world.)
Green tea seems to be able to almost totally prevent cancer causing DNA damage in smokers — a possible explanation as to why the Japanese, who are among the world’s heaviest smokers, have such a low incidence of lung cancer.
And finally, green tea has great benefits for the brain as well, serving as an effective MAO inhibitor, protecting against brain-cell death from glucose oxidase, over-production of nitric oxide, and lowering the amount of free iron reaching the brain (a bad thing). The net result is that there are strong indications that green tea extract may play a major role in protecting against both Parkinson’s and Alzheimer’s disease.
Note: if you drink green tea, adding cream or milk to the tea seems to destroy the antioxidant benefits.
Bilberry — 120 mg (25%)
The anthocyanosides found in bilberry are known for their ability to help nourish and repair the tiny capillaries within the eye. In addition, the bilberry bioflavonoids are beneficial to the connective tissue that lines blood vessels and binds ligaments throughout the body.
Alpha lipoic acid — 100 mg
Sometimes called the “Mother” antioxidant, alpha lipoic acid (ALA) plays a major role in helping recycle vitamins E and C so that they can be used over and over again by your body. In its own right, ALA is one of the main boosters of glutathione levels in body cells, and is one of the key co-factors involved in generating energy in the cells mitochondria. And ALA has also been shown to significantly rejuvenate the cognitive skills of people as they age.
Alpha-lipoic acid exists in three different forms: alpha R-lipoic acid, alpha S-lipoic acid, and alpha RS-lipoic acid. Alpha S-lipoic acid and alpha RS-lipoic acid are synthetics; these are the forms commonly known and sold as alpha-lipoic acid supplements. On the other hand, alpha R-lipoic acid (better known as R-lipoic acid) is the only version of lipoic acid that exists in nature. It is synthesized by both plants and animals. Supplements sold as R-lipoic acid contain only the natural (cis) form of lipoic acid. They are twice as effective as the synthetic (trans) form supplements sold as alpha lipoic acid. Thus, formulas that use R-lipoic acid require only about 50 mg per serving.
SOD — 75 mg
Superoxide dismutase (SOD) works along with glutathione to neutralize reactive oxygen molecules in the body. SOD specifically targets the superoxide radical, which, as we discussed in the last newsletter, attacks cell mitochondria. When mitochondria are destroyed, the cell loses its ability to convert food to energy. It dies. SOD also works in the cytoplasm of the cell to prevent the hydroxyl radical from attacking enzymes, proteins, and the unsaturated fats in cell membranes.
Tocotrienols — 100 mg
In this version of the formula, I increased tocotrienol levels by 33%. Derived from rice bran or palm oil, tocotrienols are a unique vitamin E fraction that is 40 times more powerful than standard vitamin E. Tocotrienols are rich in the gamma tocopherol fraction of vitamin E that strongly inhibits both the estrogen-responsive and the non-estrogen responsive breast cancer cells.
OPCs 95-97% 100 mg
By moving up to a 95-97% extract and increasing the amount from 60 mg to 100 mg, I was able to more than double the activity level of the grape seed extract I had previously used.
Similar to green tea, the active ingredients in grape seed extract are the proanthocyanidins (but in a different combination and ratio). The importance of the proanthocyanidins in grape seed extract is that they are water soluble and highly bio-available.
Above all else, grape seed extract is known as a defender of the circulatory system. It improves peripheral circulation, revives declining capillary activity by up to 140%, and increases vascular response by some 82%. It repairs varicose veins and aids in the prevention of bruising.
In addition, grape seed extract is synergistic with vitamin C, vastly increasing vitamin C activity and strengthening collagen activity — including in the connective tissue of the arterial wall and the skin.
Resveratrol — 30 mg
For several years, grape seed extract was all the rage. As it turns out, grape SKIN contains its own powerful phytoalexin antioxidant called resveratrol. In controlled studies, resveratrol has been shown to reduce skin-cancer tumors by up to 98% and to stop production of leukemia cells. In addition, it works as a Cox inhibitor, thus halting the spread of cancer throughout the body. Resveratrol is a naturally occurring antioxidant that decreases the “stickiness” of blood platelets and helps blood vessels to remain open.
In addition, resveratrol appears to have estrogen-like properties, and may be helpful in the treatment of breast diseases. Also, studies indicate that resveratrol can profoundly inhibit glucose uptake in HL-60 and U937 cells. Thus, resveratrol may prevent or abate metabolic disorders such as obesity and non-insulin dependent diabetes mellitus type 2.
And finally, on August 25, 2003, the results of a study were released that showed resveratrol extended the life span of yeast cells by 70% by activating a “longevity gene” expressed during caloric restriction. Since mammals have the same “longevity gene” and since caloric restriction is known to extend the lifespan of mammals, scientists speculated humans might be able to receive the longevity benefits of caloric restriction simply by supplementing with resveratrol.
I previously used 60 mg of a general grape skin extract, high in polyphenols, but not necessarily high in resveratrol. By switching to 30 mg of a concentrated resveratrol extract I was able to significantly boost its impact in the formula.
Chaparral Extract — 100 mg (4:1)
I moved this puppy way up from 375 mcg to 100 mg of 4:1 extract. The active antioxidant in Chaparral, a lignan called Nordihydroguaiaretic Acid (NDGA), has been shown to specifically target virtually all forms of herpes virus — and has been shown to be up to 97.5% effective. It also is an effective counter to radiation induced free radical damage. And there are strong indications it is an effective aid in the prevention of Alzheimer’s and rheumatoid arthritis.
Catalase — 300 mcg
Glutathione peroxidase, superoxide dismutase, and catalase are the primary three enzymes produced in the body as an antioxidant defense. Catalase is a specific for protection against tumors. A little catalase can go a long way: one catalase enzyme molecule can catalyze the breakdown of five million molecules of peroxide radicals into water and oxygen in just one minute.
Biotin — 1.8 mg
When taking high doses of alpha lipoic acid, it is important to also take biotin because alpha lipoic acid can compete with biotin and interfere with its activity in the body.
Bioperine — 4500 mcg
Bioperine serves the same purpose in this formula that cayenne serves in my liquid tinctures. It drives the other ingredients into the blood and significantly improves their efficacy. In human studies, for example, the bioavailability of curcumin was increased twentyfold when used with bioperine. Bioperine improves the absorption of many vitamins and biochemicals in the intestine, promotes their retention in cells, and prevents their being metabolized in the liver. Effectively, it increases the efficacy of virtually all of the ingredients in this formula.
There are other antioxidants that are well worth taking, but because of the quantity needed to be effective, make no sense to include as part of an overall formula. These include:
- Vitamin E
In addition to protecting the cardio-vascular system, a complete Vitamin E complex (4 tocopherols and 4 tocotrienols), is particularly effective in reducing the incidence and mortality of prostate cancer. When combined with lycopene, the synergistic effect is even more pronounced. 800 IU a day is recommended.
- Vitamin C
The antioxidant benefits of vitamin C are invaluable. The trick is that almost all of the vitamin C sold today is marginal. You need 500-1,000 mg of vitamin C a day — but ideally it should be a complete complex, bound to food, so your body can use it properly. In fact, there is some evidence that although it is “chemically” identical, the synthetic form of vitamin C (ascorbic acid) may actually thicken the arterial walls of the heart by as much as 2.5 times!
Although technically not a free radical problem, the results of methylation (the exchange of methyl groups in the body) has similar effects. As we age, our body’s ability to provide methyl donor groups declines. The bottom line is that everyone should be on a supplement to prevent homocysteine damage to the cardiovascular system, cancer, DNA damage, and deterioration of the brain. S-adenosylmethionine, also known as SAMe is a popular alternative. But a less expensive choice is to purchase at any discount health store a formula that contains, approximately: 500 mg of trimethylglycine, 50 mg of B-6, 800 mcg of folic acid, 500 mcg of B-12 (best in the form of methyl-cobalamine, if you can find it).
Certain foods are high in antioxidants and should be a regular part of the diet. In fact, the US Department of Agriculture recently rated a large number of foods according to their Oxygen Radical Absorbence Capacity. The higher the number, the more powerful the antioxidant value. All ratings were based on 3 1/2 oz of the tested food. As a reference, carrots (high in the carotenoids) had a 207 rating.
- Broccoli florets, Brussels sprouts, Raw spinach, and Kale
Broccoli carries a rating of 890, brussels sprouts 980, spinach 1,260, and kale 1,770. Be aware that these foods contain other phytonutrients that go well beyond their antioxidant value.
- Strawberries, Raspberries, Pomegranates
The key polyphenol found in these fruits is ellagic acid. Studies have shown that men who eat the most strawberries have the lowest rates of prostate cancer. Strawberries were rated at 1,540.
The antioxidants found in blueberries are called anthocyanins, which are particularly effective in increasing dopamine levels in the brain. This alone makes regular consumption of blueberries beneficial. Blueberries were rated at 2,400.
Surprise! Raisins carry a value of 2,830.
Whoa! The lowly prune is top rated at 5,770. Eat prunes daily!
- Broccoli florets, Brussels sprouts, Raw spinach, and Kale
Well, there you have it: my version of the ultimate antioxidant. Over the years, I have watched people use earlier versions of this formula with remarkable effect. Enjoy.
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|↑1||Mariella Pastoria, Hanspeter Pfandera, Daniel Boscoboinikb, Angelo Azzib. Lycopene in Association with a-Tocopherol Inhibits at Physiological Concentrations Proliferation of Prostate Carcinoma Cells.” Biochem Biophys Res Commun. 1998 Sep 29;250(3):582-5. <http://www.ncbi.nlm.nih.gov/pubmed/9784387>|