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PREVENTING FREE RADICAL DAMAGE WITH ULTIMATE PROTECTOR+

Back in 2012, I learned about Nrf2 activators and was excited about pursuing the development of a supplement that would incorporate the new knowledge we were learning into a effective product for preventing free radical damage. At that time, I published two articles: New Directions for Preventing Free Fadical Damage and Natural Phytochemical Nrf2 Activators for Chemoprevention. I started working on a new Nrf2-activator formula I called Ultimate Protector that incorporated many of the ideas contained in these articles. The product was introduced November 2012.

More recently, in early 2019, I decided to upgrade the product using new information and ingredients. The upgraded product is called Ultimate Protector+. In this article, I provide new details of our design logic and product ingredients. I expect the new formula to be released in July 2019.

Ultimate Protector+

Ultimate Protector+ is new and improved!

PREVENTING FREE RADICAL DAMAGE WITH ULTIMATE PROTECTOR+

Ultimate Protector+™ is a unique cell protection formula that simultaneously meets the needs for high levels of non-GMO Vitamin C, full spectrum antioxidants (high ORAC values), and protective enzyme activators (Nrf2 activators) in a single product. This potent combination of characteristics distinguishes the formula because no other single product available today offers such complete protection. This is the single best formula for preventing free radical damage that is available.

Ultimate Protector+™ provides extremely high levels of natural antioxidants, including high levels of ingredients such as polyphenols, flavonoids, anthocyanidins, oligomeric proanthocyanidins, catechins, curcuminoids, pterostilbene, resveratrol, chlorogenic acid, punicalagins, zeaxanthin and other carotenoids that act powerfully as antioxidants. These antioxidants come from more than 12 plant-based ingredients with demonstrated free-radical quenching capacity. These “exogenous” food-based antioxidants (supplied from outside the body) provide you with immense oxidative defenses that can be used to defend against free-radical assault.

Ultimate Protector+™ contains USP-grade non-GMO Vitamin C , SFB® standardized fruit blend (~50% polyphenols, high-ORAC powder: 9,000 µmole TE/g) from Grape, Cranberry, Pomegranate, Blueberry, Apple, Mangosteen, Bilberry, Chokeberry, and Goji Berry), Curcumin (standardized extract with 95% curcuminoids), Trans-Resveratrol (98% from Giant Knotweed), Green Tea Extract (90% polyphenols, 50% EGCG), VinCare® Whole Grape Extract (>80% polyphenols, ORAC>19,000 µmole TE/g), Calcium Malate, Magnesium Malate, and Bioperine® (a patented black pepper extract that enhances absorption of all ingredients and is a known Nrf2 activator).

Ultimate Protector+™ is contained in a capsule suitable for vegetarians (i.e., a veggie cap) and contains no magnesium stearate.

NUTRITIONAL CONSIDERATIONS AND APPLICATIONS

Ultimate Protector+™ satisfies three distinct needs:

1) The need for a non-GMO Vitamin C product. That is, a Vitamin C formula that avoids protein from genetically modified sources such as corn, potatoes, or beets.

2) The need for a single, powerful antioxidant formula for preventing free radical damage. That is, a single, easy-to-take antioxidant formula offering a broad range of extremely high-ORAC plant source antioxidants. These antioxidants should protect against the full range of free radicals found in the human body including: superoxide anion (O2·-), peroxyl radicals (ROO·), hydroxyl radicals (HO·), singlet oxygen (1O2), and peroxynitrite (ONOO-).

3) The need for a supplement providing a full spectrum of Nrf2 activators. That is, a supplement providing a wide range of natural Nrf2 transcription factor activators that allow the body to make its own antioxidant enzymes (e.g., superoxide dismutase (SOD), catalase, hemeoxygenase, and glutathione peroxidase). Scientific research has shown that these are found naturally in many fruits, vegetable, and herbs. These ingredients provide a wide range of Nrf2 activators that result in significantly high levels of the endogenously produced antioxidant enzymes.

The ways Ultimate Protector+™ satisfies these three needs are discussed below:

1) NON-GMO VITAMIN C / ASCORBIC ACID

High-quality, USP grade Vitamin C has been obtained historically from corn, potatoes, and/or beets. Unfortunately, many of these sources have to a large extent gone to genetically modified (GMO) variants. However, with highly refined production methods and the use of PCR testing, we have been able to obtain final products that are free from GMOs.

In nature, Vitamin C is found generally in plant sources containing polyphenols. Vitamin C and polyphenols work together to provide a high level of antioxidant protection and they support the function of each other in the process. For example, Vitamin C is needed by the body to produce collagen and certain polyphenols (especially oligomeric proanthocyanidins) (OPCs) crosslink the collagen and make it stronger.

2) EXTREMELY HIGH ORAC SOURCES

Free radicals are reactive species that can have adverse effects on normal physiological functions. Studies associate the five major types of free radicals (i.e., hydroxyl, peroxyl, peroxynitrite, singlet oxygen, and superoxide anion) with health conditions such as cardiovascular disease, hypertension, breakdown of vital proteins, chronic inflammation, Alzheimer’s disease, and certain cancers. Avoiding free radical damage is the goal.

Antioxidants function as a vital line of defense against free radicals by blocking their attack on DNA, vital proteins, lipids, and amino acids. Until now, efforts to identify the effect of antioxidants on all five types of free radicals were constrained by limited testing procedures. However, new technological developments have resulted in a comprehensive testing method called the Total ORAC5.0™ assay. Because of the development of the Total ORAC5.0™ test, it is now possible to target and measure the effects of antioxidants on the five major types of free radicals found in the body.

We are currently in the process of testing Ultimate Protector+™ using this new ORAC5.0™ assay. We are confident that our formula offers protection against these five major types of free-radicals because we combine a wide range of extremely high-ORAC fruit, vegetable, and herbal blends. As soon as the results are available (in July 2019), we will update this article with the findings.

3) NRF2 TRANSCRIPTION FACTOR ACTIVATORS

In order to survive under a variety of environmental or intracellular stresses, our cells have developed highly efficient protective mechanisms to protect themselves from oxidative or electrophilic challenges. Proteins that comprise phase II detoxification and antioxidant enzymes provide an enzymatic line of defense against reactive oxygen species (ROS). These enzymes include superoxide dismutase (SOD), catalase, glutathione peroxidase, glutathione S-transferase (GST), and glutamate cysteine ligase.

Induction of phase II and antioxidant enzymes are regulated at the DNA/gene level by an antioxidant responsive element (ARE). ARE-mediated gene expression plays a central role in the cellular defense against cellular oxidative damage. Experimental evidence supports the view that induction of ARE-mediated cytoprotective enzymes is a critical and sufficient mechanism to enable protection against disease provoked by environmental and endogenous insults.

One of the key ARE-binding transcription factors is Nrf2. Induction of cytoprotective enzymes in response to ROS, electrophiles, and phytochemicals is a cellular event that is highly dependent on Nrf2 protein. By activating Nrf2 signaling, phytochemicals can increase cellular detoxification and antioxidant enzymes, thereby enhancing removal of ROS and toxic chemicals and preventing disease. Numerous research studies carried out over the last 15 years have demonstrated the effectiveness of a very wide range of Nrf2 activators extracted from fruits, vegetables, and herbs.

For example, a study with sulforaphane (an isothiocyanate present abundantly in cruciferous vegetables) shows that oral administration of this phytochemical can effectively block benzo[a]pyrene-induced forestomach tumors in mice. This protective effect was abrogated in mice that could not produce Nrf2. This supports the critical role of phase II detoxification and antioxidant enzymes in the prevention of carcinogenesis by chemopreventive agents.

Nrf2 is normally bound in the cytoplasm of cells to a protein called KEAP1. However, when an appropriate phytochemical agent attaches to a kinase receptor on the cell wall a phosphate group is released that causes the Nrf2 to be released. Also, there are other mechanisms that allow Nrf2 to be released from KEAP1. The released Nrf2 then migrates into the cell nucleus and causes an antioxidant enzyme (e.g., superoxide dismutase (SOD)) to be fabricated and released. This endogenously produced enzyme then can protect against ROS, electrophiles, and other toxic agents.

In practical experience, it has been found that a combination of multiple polyphenols works significantly better than single ingredients. In fact, in one experiment it was found that a combination of five ingredients all known to be Nrf2 activators was 18 times more effective than any single ingredient. Furthermore, it was found that this combination of five ingredients was able to increase levels of SOD by 30% and catalase by 56% after 120 days of taking the combination.

In view of the considerations above, we include a wide range of Nrf2 activators in Ultimate Protector+™. These include a large variety of freeze-dried and concentrated fruits, vegetables, and herbs. These include Grape, Cranberry, Pomegranate, Blueberry, Apple, Mangosteen, Bilberry, Chokeberry, Goji Berry), Curcumin (standardized extract with 95% curcuminoids), Trans-Resveratrol (98% from Giant Knotweed), Green Tea Extract (93% polyphenols, 50% EGCG), VinCare® Whole Grape Extract (>80% polyphenols, ORAC>19,000 µmole TE/g)

Ultimate Protector+™ includes the following phytonutrients in its array of freeze-dried and concentrated fruits, vegetables, and herbs: polyphenols, flavonoids, anthocyanins, catechins, proanthocyanins, ellagic acid, xanthines, chlorogenic acid, pterostilbenes, resveratrol, phloridzin, quercetin, zeaxanthin, carotinoids, polysaccharides, quinic acid, and more.

The phytochemical ingredients in Ultimate Protector+™ are discussed below:

1. SFB® – (Standardized Fruit Blend)

SFB® is a nutritious, non-GMO blend that provides a broad spectrum of polyphenols, anthocyanins, and other antioxidants derived from water and/or ethanol extracts of grape (Vitis vinifera), cranberry (Vaccinium macrocarpon), pomegranate (Punica granatum) with >75% polyphenols, blueberry (Vaccinium uliginosum), apple (Malus pumilla Mill), mangosteen (Garcinia mangostana), bilberry (Vaccinium myrtillis), chokeberry (Aronia arbutifolia), and goji berry (Lycium barbarum). This powder has an ORAC value in excess of 9,000 µmole TE/g and contains 50% polyphenols.

Polyphenols and anthocyanins are not all created equal. Every fruit, vegetable and herb provides its own set of unique polyphenols and anthocyanins that reside in the body for different lengths of time and in different locations, providing a range of benefits. SFB® has been designed to provide a wide range of plant polyphenols, flavonoids, anthocyanins, catechins, OPCs, zeaxanthin and other carotinoids, etc. Published research associates these plant ingredients with healthy aging, inflammation management, improved blood sugar metabolism, and cardiovascular disease management.

SFB® provides the following benefits: Superior source of natural antioxidants and Nrf2 activators, helps ameliorate the effects of premature aging, promotes cardiovascular health, promotes healthy brain function and mental acuity, promotes healthy vision, promotes healthy blood sugar levels, and is an excellent source of flavonoids and organic acids.

I have prepared detailed blog articles for the ingredients in SFB®. Below some of these are summarized and links to the articles are provided.

a) Cranberry Extract

Ultimate Protector+ Includes Cranberry

Ultimate Protector+ Includes Cranberry Extract

Cranberry extract is an especially good source of antioxidant polyphenols. In animal studies, the polyphenols in cranberries have been found to decrease levels of total cholesterol and so-called “bad” cholesterol. Cranberries may also inhibit the growth of tumors in human breast tissue and lower the risk of both stomach ulcers and gum disease.

Here is a list of the antioxidant and anti-inflammatory phytonutrients in found in cranberry extract.

Type of Phytonutrient Specific Molecules
Phenolic Acids hydroxybenzoic acids including vanillic acids;
—Phenolic Acids (cont.) hydroxycinnamic acids inculding caffeic,
—Phenolic Acids (cont.) coumaric, cinnamic, and ferulic acid
Proanthocyanidins epicatechin oligomers
Anthocyanins cyanidins, malvidins, and peonidins
Flavonoids quercetin, myricetin, kaempferol
Triterpenoids ursolic acid

OTHER CRANBERRY INFORMATION

    • Cranberries hold significantly high amounts of phenolic flavonoid phytochemicals called oligomeric proanthocyanidins (OPC’s). Scientific studies have shown that consumption of the berries have potential health benefits regarding cancer, aging and neurological diseases, inflammation, diabetes, and bacterial infections.
    • Antioxidant compounds in cranberry extract including OPC’s, anthocyanidin flavonoids, cyanidin, peonidin and quercetin may support cardiovascular health by counteracting against cholesterol plaque formation in the heart and blood vessels. Further, these compounds help the human body lower LDL cholesterol levels and increase HDL-good cholesterol levels in the blood.
    • Scientific studies show that cranberry juice consumption offers protection against gram-negative bacterial infections such as E.coli in the urinary system by inhibiting bacterial-attachment to the bladder and urethra.
    • It is known that cranberries turns urine acidic. This, together with the inhibition of bacterial adhesion helps prevent the formation of alkaline (calcium ammonium phosphate) stones in the urinary tract by working against proteus bacterial-infections.
    • In addition, the berries prevent plaque formation on the tooth enamel by interfering with the ability of the gram-negative bacterium, Streptococcus mutans, to stick to the surface. In this way cranberries helps prevent the development of cavities.
    • The berries are also good source of many vitamins like vitamin C, vitamin A, ß-carotene, lutein, zea-xanthin, and folate and minerals like potassium, and manganese.
  • Oxygen Radical Absorbance Capacity (ORAC) demonstrates cranberry at an ORAC score of 9584 µmol TE units per 100 g, one of the highest in the category of edible berries.

b) Pomegranate Extract

Ultimate Protector+ Includes Pomegranate

Ultimate Protector+ Includes Pomegranate

For thousands of years, the pomegranate has been extensively used as a source of food and medicine. Full of antioxidants, vitamin C and potassium, pomegranate has been used to control body weight, reduce cholesterol, fight against cell damage, and inhibit viral infections. Pomegranate extracts have anti-bacterial effects.

Pomegranates are rich in ellagic acid, gallic acid, lignans, polyphenols and other bioactive compounds, and have been shown to lower blood pressure and enhance vascular function. Furthermore, it can offset some of the negative effects of medications and chemicals. These compounds occur naturally in its peel, seeds, leaf and juice. The seeds are high in p-coumaric acid, plant sterols, tannins and fatty acids. In addition to their antihypertensive effects, they may help reduce blood sugar levels.

Pomegranate fruit is a rounded berry with a thick reddish skin covering approximately 200–1400 white to deep red or purple seeds. Pomegranate seeds are edible and hold strong antioxidant and anti-inflammatory properties due to their high content of hydrolysable tannins and anthocyanins. As compared to the antioxidant activity of vitamin E, β-carotene, and ascorbic acid, the pomegranate antioxidants appear unique due to combinations of a wide array of polyphenols, having a broader range of action against several types of free radicals. As compared to the recognized antioxidants in red wine and green tea, anthocyanins from pomegranate fruit possess significantly higher antioxidant activity.

Pomegranate has been used in various medicinal systems of medicine for the treatment and therapy of a multitude of diseases and ailments. In the ancient Indian medicinal system, i.e., in Ayurvedic medicine, the pomegranate was considered to be a whole pharmacy unto itself. It was recommended to be used as an antiparasitic agent and to treat diarrhea and ulcers. The medicinal properties of pomegranate have sparked significant interest in today’s scientific community as evidenced by the scientific research relating to health benefits of pomegranate that have been published in last few decades.

Studies have shown that pomegranate and its constituents can efficiently affect multiple signaling pathways involved in inflammation, cellular transformation, hyperproliferation, angiogenesis, initiation of tumorigenesis, and eventually suppressing the final steps of tumorigenesis and metastasis. The pomegranate constituents are shown to modulate transcription factors, pro-apoptotic proteins, anti-apoptotic proteins, cell cycle regulator molecules, protein kinases, cell adhesion molecules, pro-inflammatory mediators, and growth factors.

c) Chokeberry (Aronia)

Ultimate Protector+ Includes Chokeberry

Ultimate Protector+ Includes Chokeberry

HEALTH BENEFITS OF CHOKEBERRY (ARONIA)

Aronia melanocarpa (black chokeberry) has attracted scientific interest due to its deep purple, almost black pigmentation that arises from dense contents of polyphenols, especially anthocyanins. Total polyphenol content is 1752 mg per 100 g in fresh berries, anthocyanin content is 1480 mg per 100 g, and proanthocyanidin concentration is 664 mg per 100 g. These values are among the highest measured in plants to date.

The plant produces these pigments mainly in the leaves and skin of the berries to protect the pulp and seeds from constant exposure to ultraviolet radiation and production of free radicals. By absorbing UV rays in the blue-purple spectrum, leaf and skin pigments filter intense sunlight, serve antioxidant functions and thereby have a role assuring regeneration of the species.

Analysis of polyphenols in chokeberries has identified the following individual chemicals (among hundreds known to exist in the plant kingdom): cyanidin-3-galactoside, cyanidin-3-arabinoside, quercetin-3-glycoside, epicatechin, caffeic acid, delphinidin, petunidin, pelargonidin, peonidin, and malvidin.All these except caffeic acid are members of the flavonoid category of phenolics.

In a standard measurement of antioxidant strength, the oxygen radical absorbance capacity or ORAC, demonstrates aronia to have one of the highest values yet recorded for a fruit — 16,062 micro moles of Trolox Eq. per 100 g. The components contributing to this high measurement were both anthocyanins and proanthocyanidins, with the proanthocyanidin level “among the highest in foods”, which may explain their potent astringent taste.

d) Goji Berry

Ultimate Protector+ Includes Goji Berry

Ultimate Protector+ Includes Goji Berry

Goji Berries contain abundant polysaccharides (LBPs, comprising 5%–8% of the dried fruits), scopoletin (6-methoxy-7-hydroxycoumarin, also named chrysatropic acid, ecopoletin, gelseminic acid, and scopoletol), the glucosylated precursor, and stable vitamin C analog 2-O-β-D-glucopyranosyl-L-ascorbic acid, carotenoids (zeaxanthin and β-carotene), betaine, cerebroside, β-sitosterol, flavonoids, amino acids, minerals, and vitamins (in particular, riboflavin, thiamin, and ascorbic acid).

The predominant carotenoid is zeaxanthin, which exists mainly as dipalmitate (also called physalien or physalin). The content of vitamin C (up to 42 mg/100 g) in goji berry (also known as wolfberry) is comparable to that of fresh lemon fruits. As to the seeds, they contain zeaxanthin (83%), β-cryptoxanthin (7%), β-carotene (0.9%), and mutatoxanthin (1.4%), as well as some minor carotenoids.

In fact, increasing lines of experimental studies have revealed that L. barbarum berries have a wide array of pharmacological activities, which is thought to be mainly due to its high LBPs content. Water-soluble LBPs are obtained using an extraction process that removes the lipid soluble components such as zeaxanthin and other carotenoids with alcohol. LBPs are estimated to comprise 5%–8% of LBFs and have a molecular weight ranging from 24 kDa to 241 kDa. LBPs consist of a complex mixture of highly branched and only partly characterized polysaccharides and proteoglycans.

The glycosidic part accounts, in most cases, for about 90%–95% of the mass and consists of arabinose, glucose, galactose, mannose, rhamnose, xylose, and galacturonic acid. LBPs are considered the most important functional constituents in LBFs. Different fractions of LBPs have different activities and the galacturonic acid content is an imperative factor for activities of LBP. The bioactivities of polysaccharides are often in reverse proportion with their molecular weights. Increasing lines of evidence from both preclinical and clinical studies support the medicinal, therapeutic, and health-promoting effects of LBPs.

e) Mangosteen

Ultimate Protector+ Includes Mangosteen

Ultimate Protector+ Includes Mangosteen

The Mangosteen extract in Ultimate Protector+ has been extracted with non-GMO food grade ethanol and distilled water. Testing has indicated the product contains over 10% polyphenols.

Mangosteen extract in obtained from the skin and whole fruit for which numerous biological activities have been reported including: antimutagenic, antibacterial, hypocholesterolemic, antioxidant, and protective against tumorigenesis.

Mangosteen contains nutrients with antioxidant capacity, such as vitamin C and folate. Plus, it provides xanthones — a unique type of plant compound known to have strong antioxidant properties. In several test-tube and animal studies, the antioxidant activity of xanthones has resulted in anti-inflammatory, anticancer, anti-aging, heart protective, and antidiabetic effects.

Additionally, some research suggests that certain plant compounds in mangosteen may have antibacterial properties — which could benefit your immune health by combating potentially harmful bacteria. In a 30-day study in 59 people, those taking a mangosteen-containing supplement experienced reduced markers of inflammation and significantly greater increases in healthy immune cell numbers compared to those taking a placebo.

f) Apple Extract

Ultimate Protector+ Includes Apple

Apples contain a large concentration of flavonoids, as well as a variety of other phytochemicals, and the concentration of these phytochemicals may depend on many factors, such as cultivar of the apple, harvest and storage of the apples, and processing of the apples. The concentration of phytochemicals also varies greatly between the apple peels and the apple flesh.

Some of the most well studied antioxidant compounds in apples include quercetin-3-galactoside, quercetin-3-glucoside, quercetin-3-rhamnoside, catechin, epicatechin, procyanidin, cyanidin-3-galactoside, coumaric acid, chlorogenic acid, gallic acid, and phloridzin. Recently researchers have examined the average concentrations of the major phenolic compounds in six cultivars of apples. They found that the average phenolic concentrations among the six cultivars were: quercetin glycosides, 13.2 mg/100 g fruit; vitamin C, 12.8 mg/100 g fruit; procyanidin B, 9.35 mg/100 g fruit; chlorogenic acid, 9.02 mg/100 g fruit; epicatechin, 8.65 mg/100 g fruit; and phloretin glycosides, 5.59 mg/100 g fruit.

The compounds most commonly found in apple peels consist of the procyanidins, catechin, epicatechin, chlorogenic acid, phloridzin, and the quercetin conjugates. In the apple flesh, there is some catechin, procyanidin, epicatechin, and phloridzin, but these compounds are found in much lower concentrations than in the peels. Quercetin conjugates are found exclusively in the peel of the apples. Chlorogenic acid tends to be higher in the flesh than in the peel.

Because the apple peels contain more antioxidant compounds, especially quercetin, apple peels may have higher antioxidant activity and higher bioactivity than the apple flesh. Research showed that apples without the peels had less antioxidant activity than apples with the peels. Apples with the peels were also better able to inhibit cancer cell proliferation when compared to apples without the peels. More recent work has shown that apple peels contain anywhere from two to six times (depending on the variety) more phenolic compounds than in the flesh, and two to three times more flavonoids in the peels when compared to the flesh. The antioxidant activity of these peels was also much greater, ranging from two to six times greater in the peels when compared to the flesh, depending on the variety of the apple. This work is supported a study which found that rats consuming apple peels showed greater inhibition of lipid peroxidation and greater plasma antioxidant capacity when compared to rats fed apple flesh.

Many of these phytochemicals from apples have been widely studied, and many potential health benefits have been attributed to these specific phytochemicals. The procyanidins, epicatechin and catechin, have strong antioxidant activity and have been found to inhibit low density lipoprotein (LDL) oxidation in vitro. In mice, catechin inhibits intestinal tumor formation and delays tumors onset. One study found that chlorogenic acid has very high alkyl peroxyl radical (ROO•) scavenging activity. Compared to about 18 other antioxidant compounds (including quercetin, gallic acid, α-tocopherol), chlorogenic was second only to rutin. Since ROO• may enhance tumor promotion and carcinogenesis, chlorogenic acid may add to the protective effect of apples against cancer. Chlorogenic acid has been found to inhibit 8-dehydroxy-deoxyguanosine formation in cellular DNA in a rat model following treatment with 4-nitroquinoline-1-oxide.

Quercetin is also a strong antioxidant, and is thought to have potential protective effects against both cancer and heart disease. Briefly, quercetin has been found to down regulate expression of mutant p53 in breast cancer cells, arrest human leukemic T-cells in G1, inhibit tyrosine kinase, and inhibit heat shock proteins. Quercetin has protected Caco-2 cells from lipid peroxidation induced by hydrogen peroxide and Fe2+. In mice liver treated with ethanol, quercetin decreased lipid oxidation and increased glutathione, protecting the liver from oxidative damage. Recently, it has been found that high doses of quercetin inhibit cell proliferation in colon carcinoma cell lines and in mammary adenocarcinoma cell lines, but at low doses quercetin increased cell proliferation (20% in colon cancer cells and 100% in breast cancer cells). However, low doses of quercetin (10 uM) inhibited cell proliferation in Mol-4 Human Leukemia cells and also induced apoptosis. Quercetin inhibited intestinal tumor growth in mice, but not in rats. Low levels of quercetin inhibited platelet aggregation, calcium mobilization, and tyrosine protein phosphorylation in platelets. Modulation of platelet activity may help prevent cardiovascular disease.

g) Blueberry and Bilberry Extract

wild bilberry and wild blueberry
Wild bilberry and wild blueberry provide Nrf2 activators.

The key compounds in bilberry fruit are called anthocyanins and anthocyanosides. These compounds help build strong blood vessels and improve circulation to all areas of the body. They also prevent blood platelets from clumping together (helping to reduce the risk of blood clots), and they have antioxidant properties (preventing or reducing damage to cells from free radicals). Anthocyanins boost the production of rhodopsin, a pigment that improves night vision and helps the eye adapt to light changes.

Bilberry fruit is also rich in tannins, a substance that acts as an astringent. The tannins have anti-inflammatory properties and may help control diarrhea.

Bilberries have been shown to have the highest Oxygen Radical Absorbance Capacity (ORAC) rating of more than 20 fresh fruits and berries. The antioxidant properties of bilberries were shown to be even stronger than those of cranberries, raspberries, strawberries, plums, or cultivated blueberries.

The antioxidant powers and health benefits of bilberries and blueberries can be attributed to a number of remarkable compounds contained in them, including the following:

  • Anthocyanins
    • malvidins
    • delphinidins
    • pelargonidins
    • cyanidins
    • peonidins
  • Hydroxycinnamic acids
    • caffeic acids
    • ferulic acids
    • coumaric acids
  • Hydroxybenzoic acids
    • gallic acids
    • procatchuic acids
  • Flavonols
    • kaempferol
    • quercetin
    • myricetin
  • Other phenol-related phytonutrients
    • pterostilbene
    • resveratrol
  • Other nutrients
    • lutein
    • zeaxanthin
    • Vitamin K
    • Vitamin C
    • manganese

2) Curcumin

Ultimate Protector+ Includes Curcumin

Ultimate Protector+ Includes Curcumin

We have included Curcumin (95% curcuminoids in ULTIMATE PROTECTOR™. This ingredient contains three main chemical compounds – Curcumin, Demethoxycurcumin and Bisdemethoxycurcumin – collectively known as Curcuminoids and all derived from Turmeric. Curcumin has been shown to be one of the most potent Nrf2 transcription factor activators. Studies have reported that curcumin and turmeric protect the liver against several toxicants both in vitro and in vivo. A number of reports showed the curative action of turmeric and curcuminoids. Curcumin is a potent scavenger of free radicals such as superoxide anion radicals, hydroxyl radicals, and nitrogen dioxide radicals. It exerts powerful antioxidant and anti-inflammatory properties.


3) Trans-Resveratrol (98% from Polygonum cuspidatum – giant knotweed)

giant knotweed resveratrol

Knotweed (Polygonum cuspidatum) is a major source for resveratrol.

Trans-resveratrol provides antioxidant protection, boosts cellular energy, and balances the immune system. It has been proven in studies to activate the SIRT1 longevity gene and enhance cellular productivity. Several research studies have shown that trans-resveratrol activates Nrf2 transcription factor, significantly modulates biomarkers of bone metabolism, inhibits pro-inflammatory enzymes such as COX-1 and COX-2, and exhibits cardioprotective effects, neuroprotective properties, and caloric restrictive behavior. Trans-resveratrol has shown the ability to increase the number of mitochondria thereby increasing total daily energy. Studies have shown that trans-resveratrol promotes an increase in mitochondrial function. Increased mitochondrial function translates into an increase in energy availability, improved aerobic capacity, and enhanced sensorimotor function. Trans-resveratrol has an ORAC value of 31,000 µmole TE/g.


4) Green Tea Extract

Ultimate Protector+ Includes Green Tea Extract

Ultimate Protector+ Includes Green Tea Extract

Green Tea Extract contains highly bioavailable bioflavonoid complexes that in research studies have been shown to have powerful antioxidant capability. Green tea extract is obtained from the unfermented leaves of Camellia sinensis for which numerous biological activities have been reported including: cell protective, antimicrobial, and antioxidant. The green tea extract in Ultimate Protector is extracted is extracted by non-GMO ethanol and distilled water and contains ~ 90% polyphenols and 50% epigallocatechingallate (EGCG).

Epigallocatechin gallate (EGCG) is the most abundant catechin compound in green tea. It is well established that EGCG is a potent antioxidant and anti-inflammatory agent. Epidemiological studies show that consumption of 100 or more mg of EGCG per day is beneficial, as it is the most potent Nrf2 activator among all green tea catechins. EGCG exhibits robust diffusion through bodily tissues, including the endothelium of the blood brain barrier.

EGCG has the capacity to activate Nrf2/ARE and induce Heme oxygenase-1 (HO-1) expression. Several studies have shown that EGCG can also interact with kinases, causing the disassociation of Nrf2/Keap1 complex.

Protective effects of EGCG have been reported against ischemia/reperfusion injury. Administration of EGCG showed improved neurologic scores, reduced infarct volume, and ameliorated neuronal apoptosis due to increased GSH biosynthesis (via Nrf2 activation) and decreased ROS content. By inducing the expression of Nrf2 and HO-1, EGCG increases important endogenous antioxidants in microglial cells.

5) VinCare® whole grape extract (seed, pulp, and skin)

Ultimate Protector+ Includes Whole Grape Extract

Ultimate Protector+ Includes Whole Grape Extract

Whole Grape Extract contains highly bioavailable bioflavonoid complexes that in research studies have been shown to have powerful antioxidant capability. The Oligomeric Proanthocyanidins (OPCs) in grape extract are able to strengthen collagen fibers in aging or damaged connective tissue and can act as a preventative against connective tissue degradation. Some research indicates that anthocyanidins, which are found in extracts of grape seed, skin, and stems (but not in grape seed extract), can reduce oxidized glutathione while at the same time become reduced themselves. In addition, extracts of grape skin and pulp (but not those of grape seed extract) contain trans-resveratrol that has been shown to have cell protective effects.

Grape seed extract has been reported to demonstrate a remarkable spectrum of biological, pharmacological and therapeutic properties against oxidative stress. The antioxidative activities of grape seed extract have been found to be much stronger than those of vitamins C and E. Studies have indicated that grape seed extract showed a protective effect on cardiovascular disease, nephropathy, atherosclerosis, and neuropathy, among other conditions.

Vincare® contains ~80% polypnenols and has an ORAC value of about 19,000 µmole TE/g. ORAC 5.0 testing of grape seed extract exhibits one of the highest values of any tested material at about 100,000 µmole TE/g.

It has been shown that grape seed OPCs activate nuclear erythroid2-related factor2 (Nrf2), which is a key antioxidative transcription factor, with the concomitant elevation of downstream hemeoxygenase-1 (HO-1). Click here to view an excellent article entitled Proanthocyanidins [OPCs] against Oxidative Stress: From Molecular Mechanisms to Clinical Applications.

7) Bioperine®:

Bioperine® is a black pepper extract that has been shown to enhance the absorption of nutrients by 30–60 percent and makes all of the nutrients in this product more effective.

Ultimate Protector+™ will be most effective when used in conjunction with other foundational nutritional supplements that support the body’s metabolism, including Multi Two or Mighty Multi-Vite!™ (therapeutic multivitamin formulas), Omega Plus (essential fatty acids with Vitamin E), PRO-C™ (antioxidant formula), and one of our high-RNA Rejuvenate!™ superfoods.

COMPOSITION: six veggie capsules provides the following percentages of the Daily Value:

Serving Size: 6 Veggie Capsules Servings per Container: 30
Amount Per Serving Amounts % Daily Value
Vitamin C (as 100% USP-grade, non-GMO ascorbic acid) 1,500 mg 1667%
Calcium (from calcium malate) 60 mg 6
Magnesium (from magnesium malate) 60 mg 15
SFB®† (50% polyphenols, Orac: 9,000 units/gm) 180 mg *
Curcumin (95% min. curcuminoids from Curcuma longa) (root) 135 mg *
Green Tea extract (92% polyphenols, 50% EGCG) 135 mg *
Trans-Resveratrol 98% 135 mg *
Vincare®† whole grape extract (80% polyphenols, Orac: 19,000 units/gm) 135 mg *
Bioperine®†† 7.5 mg *
*
* Daily Value not established

Other ingredients: vegetarian capsule (veggie cap), microcrystalline cellulose, silica, and ascorbyl palmitate.

Directions for Use: As a dietary supplement take two capsules three times daily with food, or as directed by a health care professional.

ULTIMATE PROTECTOR Does Not Contain: wheat, rye, oats, barley, corn, gluten, soy, egg, dairy, yeast, sugar, shellfish, GMOs, wax, preservatives, colorings, or artificial flavorings.

ULTIMATE PROTECTOR+™ will be most effective when used in conjunction with other foundational nutritional supplements that support the body’s metabolism, including Multi Two or Mighty Multi-Vite!™ (therapeutic multivitamin formulas), Essential Fats plus E (essential fatty acids with Vitamin E), PRO-C™ (antioxidant formula), and one of our high-RNA Rejuvenate!™ superfoods.

†SFB® and VinCare® are registered trademark of Ethical Naturals, Inc.

†† Bioperine® is a registered trademark of Sabinsa Corporation.

ADDITIONAL RESOURCES

New Directions for Preventing Free-Radical Damage

Natural Phytochemical Nrf2 Activators for Chemoprevention

0

BONE FRACTURES SUPPORT

Dr. Hank Liers, PhD bone fracturesSeveral years ago a customer asked me for a program that could be helpful to those suffering with bone fractures. A relative had been diagnosed with multiple bone fractures in his ankle.

Since I have been counseling individuals regarding natural treatments for supporting those with bone fractures and injury for many years, I was able to provide a comprehensive program that could be helpful in recovery. More recently, we have introduced products and tools that can be even more supportive. Therefore, in this article we are providing an update to the bone fractures program.

Clearly, the need for such a program is great. According to the American Academy of Orthopaedic Surgeons (AAOS), about six million individuals suffer fractures each year in North America. In about 5–10 percent of cases, patients suffer either delayed healing or fractures that do not heal.

The problem of bone fractures is especially troubling for the elderly, many of whom suffer from osteoporosis, a condition in which bones become weak and break more easily. For an older person, a fracture affects quality of life because it significantly reduces function and mobility, and requires an extended period of recuperation.

The bone fracture program set forth below also works well to support the healing of other types of bone problems, including broken bones, bone surgery, osteoporosis, and wisdom tooth removal.

THE BONE FRACTURE PROGRAM

IMPORTANCE OF FOUNDATIONAL SUPPLEMENTS

The first element of the program consists of Foundational Supplements. This group of supplements ensures the body is being supplied with all of the basic elements needed for optimal function. The primary foundational supplements consists of 1) a therapeutic multivitamin and mineral formula, 2) a complete buffered Vitamin C with antioxidants formula, 3) an essential fatty acids supplement, and 4) a high-RNA superfoods formula.

Our Foundational Supplements are described in great detail on the HPDI website where we provide a free downloadable e-book “The Need for Foundational Supplements” (.pdf). Suffice it to say that the foundational supplements are a essential part of the program that ensure healing will take place quickly and effectively. I encourage everyone to become familiar with this information as foundational supplements are basic to any wellness or healing program.

bone fractures

ENHANCEMENT FORMULAS ARE CRITICAL FOR HEALING BONE FRACTURES

The second element of the program for healing bone fractures consists of Enhancement Formulas that strengthen the body as it relates to dealing with the damaging effects of bone fractures. These include a Vitamin D3 formula with the synergistic nutrients of Vitamin A and Vitamin K2 that are required for the rebuilding of bone as well as strengthening the body in many other ways. The HPDI Vitamin D3 Plus formula to designed to specifically address this need.

A second Enhancement Formula in this program is our comprehensive Bone Guardian formula that is based upon micronized veal bone that provides hydroxyapatite (Ca10(PO4)6(OH)2). Hydroxyapatite is the basic component of human bone that is 50% by volume and 70% by weight. Whereas the Vitamin D3 Plus formula builds the bone matrix, the Bone Guardian fills in the matrix with materials such as calcium, phosphorus, magnesium, boron, zinc, manganese, copper, silica, and strontium. HPDI sells Bone Guardian in both the tablet and capsule forms. The capsule form may be better for older people who are able to absorb capsules better than tablets.

A third Enhancement Formula to the program is additional amounts of Vitamin C. Vitamin C is known to participate in every step of the process of building collagen, which is a key component of bone. Vitamin C has been shown to increase bone mass density. We recommend slowly increasing your intake of buffered Vitamin C until you reach your bowel tolerance. This can be accomplished by increasing your intake of HPDI’s foundational supplement PRO-C™ formula. The PRO-C has the added value of containing oligomeric proanthocyanidins (OPCs) from grape seed, skin, & pulp. OPCs in the body are able to strongly crosslink and strengthen new and damaged collagen fibers needed needed to repair bones, ligaments, tendons, and cartilage.

SPECIFIC CONDITION FORMULAS TARGET BONE FRACTURES

The third element in the program are Specific Condition Formulas that directly address issues related to bone fractures. The first of these is the addition of a joint formula that allows the body to build and repair connective tissue and to significantly reduce inflammation in the area of bone fractures. In most cases of fractures there will be damaged ligaments and tendons as well as inflammation in the area.

HPDI’s Joint Health Formula includes the ingredients glucosamine hydrochloride, MSM, and sea cucumber (a significant source of chondroiten sulfate) in addition to anti-inflammatory substances such as turmeric extract, rutin, and grape extract (seed, pulp, and skin) that have been extremely helpful in both repairing connective tissue and reducing pain and inflammation.

A second strongly recommended condition-specific formula is proteolytic enzymes. Because it is highly likely in the case of bone fractures and injury that there is significant tissue damage, a formula with pancreatic and plant enzymes as well as anti-inflammatories can be extremely helpful is clearing out the damaged tissue. This gives the body the opportunity to begin the rebuilding process much sooner.

Our recommended PROLYT formula contains the proteolytic enzymes bromelain, trypsin (pancreatic enzyme), and chymotrypsin (pancreatic enzyme), and the polyphenols/bioflavonoids turmeric extract (95% curcuminoids), quercetin and oligomeric proanthocyanidins (OPCs) from grape extract. This formula when taken on an empty stomach between meals is quickly absorbed into the bloodstream and goes to work cleaning up any damaged tissues in the area surrounding a fracture and assists in reducing pain and inflammation.

TOPICAL MAGNESIUM CHLORIDE FOR PAIN AND RAPID HEALING

A final Specific Condition Formula that I highly recommend for healing bone fractures is to rub Ancient Minerals Magnesium Oil on and surrounding the fracture area. Bones cannot heal without having adequate amounts of magnesium available. Unfortunately, many people are deficient in magnesium and even taking oral magnesium cannot easily provide sufficient amounts to an area with a bone fracture. Magnesium oil (mostly magnesium chloride) is quickly absorbed transdermally (via skin) and often can provide rapid healing and pain relief!

BODY pH COULD BE A FACTOR IN HEALING BONE FRACTURES

The processed food diets with a high protein and low vegetable content consumed by many people in the U.S. and elsewhere often produce conditions in the body of acidity. This in turn leads to decreased oxygenation of cells and encourages a greater amount of anaerobic processes in metabolism. In addition, when the body is acidic calcium can be taken from bones in order to balance the acidity. This can lead to poor healing of bone fractures.

In order to counter acidic conditions in the body we recommend the use of HPDI’s pH ADJUST formula. As a dietary supplement, take 1 gm (about a rounded ¼ tsp) in 4-8 ounces of purified water preferably away from food, or as directed by a health care professional.  For extremely acidic conditions, try 4–10 doses per day, depending on acidity level. Use pH paper to ensure pH levels remain balanced, and do not become too alkaline (alkalosis may occur above pH 8.2).

TESTING pH LEVELS: The best way to test pH levels is to use litmus paper, which HPDI offers in rolls (Hydrion brand) for this purpose. You can test salivary or urinary pH. In order to test salivary pH, simply use a small strip of pH paper to dip into a small amount of saliva. Advantages of pH paper include rapid results, ease of use, and cost effectiveness.

pH Paper bone fractures protocol

The color of the litmus paper indicates the pH level of the body fluid tested. Most litmus paper comes with an indicator chart showing colors corresponding to various pH levels. Alkaline states will generally produce a dark green, blue or purple color (most basic). Acidic states will range from yellow (most acidic) to light green.

Salivary pH and urinary pH are significantly affected by recent food consumption and other factors, so it it best to test pH hours after meals or in the morning when you awake. We prefer to measure urinary pH since results are more consistent. Measuring urinary pH is a simple as placing a few drops of urine on the paper or dipping the paper into a sample cup of fresh urine.

A consistent pH measurement of less than 7.0 indicates that you are too acidic (values less than 6.2 show extreme acidity). This indicates that you should consume more alkaline forming foods (usually vegetables) and/or take pH ADJUST. A single dose of pH ADJUST can change conditions in the body from acidic to alkaline within a few hours.

GENETIC VARIATIONS IN YOUR VITAMIN D RECEPTOR GENE (VDR) MAY BE AN IMPORTANT FACTOR

The VDR gene (contained in every cell of the body) provides instructions for making a protein called vitamin D receptor (VDR), which allows the body to respond appropriately to vitamin D. This vitamin can be acquired from foods in the diet or made in the body by exposure to from sunlight. Vitamin D is involved in maintaining the proper balance of several minerals in the body, including calcium and phosphate, which are essential for the normal formation of bones and teeth. One of vitamin D’s major roles is to control the absorption of calcium and phosphate from the intestines into the bloodstream. Vitamin D is also involved in several process unrelated to bone formation.

VDR attaches (binds) to the active form of vitamin D, known as calcitriol. Calcitrol is produced in the body from Vitamin D3 (cholecalciferol) in the liver and kidneys. The interaction with calcitriol allows VDR to partner with another protein called retinoid X receptor (RXR). The resulting complex of proteins then binds to particular regions of DNA, known as vitamin D response elements, and regulates the activity of vitamin D-responsive genes. By turning these genes on or off, VDR helps control calcium and phosphate absorption and other processes.

In recent years, genetic tests have become available that show VDR variations can cause serious conditions related to low bone density and other important body functions such a higher blood glucose levels or lower immune system function. If a person is having little success in healing bone fractures, it is possible that VDR variations are a key factor of causation.

In such cases, we recommend having genetic testing done to determine if VDR variations are present. Recently, HPDI has teamed with a genetic testing company (BodySync, Inc.) and sells the BodySync test kits on our Reseller site. Please click here to see our blog article regarding the BodySync genetic test. Among the genes tested for in the test are three variations of the VDR gene. Resellers can purchase the test kits directly from HPDI and retail customers can call us  (800-228-4265) to find out how we can help them get a test kit and support them with any associated counseling regarding the results.

SUGGESTED SUPPLEMENT SCHEDULE – BONE FRACTURES

I have included all of the above supplements including recommended dosages plus more related to having an excellent diet in the table provided below.

Description AM Noon PM Night Comments
PRO-C 2 caps 2 caps 2 caps Take with meals or with snack.
Bone Guardian 

Bone Guardian Caps (easier to absorb)

3 tabs

3 caps

 

3 caps

3 tabs

3 caps

Take with meals.

Take with meals.

Mighty Multi-Vite! or
Multi Two — Multivitamins
2 caps or
1 tab
2 caps or
1 tab
Take with meals.
Essential Fats plus E 2 softgel 2 softgel 2 softgel Take with meals.
PROLYT – Proteolytic Enzyme Formula 2 caps 2 caps 2 caps 2 caps Take between meals.
Buffered Vitamin C, Tablets — 1,000 mg (1 gm) or Powder (1/4 tsp = 1 gm) 2 tabs or
1/2 tsp
2 tabs or
1/2 tsp
2 tabs or 1/2 tsp 2 tabs or 1/2 tsp Best with meals, but other times are okay. Start with 2 tabs or 1/2 tsp twice per day and add another 2 tabs or 1/2 tsp every few days until you are taking 8 tabs or 2 tsp per day.
Vitamin D3 Plus 5,000 IU 1 softgel 1 softgel Take with meals. Reduce to 1 softgel after 2 months.
Joint Health Formula 2 caps 2 caps 2 caps Take between meals and away from Bone Guardian.
Magnesium Oil 10 pumps 10 pumps 10 pumps 10 pumps Spray on affected area – or nearby area.
Rejuvenate! Plus or
Rejuvenate! (original)
1 scoop 1 scoop Take as a meal by itself or with fruit/berries.

ADDITIONAL NUTRIENTS FOR BONE FRACTURES

Additional nutrients that may be helpful include pH ADJUST (to balance excess acidity in the body),  Warrior Mist™ for pain relief (rub on adjacent area several times daily), Echinacea (as drops or capsules), N-Acetyl-L-Cysteine – NAC (2 gms per day), Progesterone Cream – for women (1/4–1/2 tsp twice daily), and Prescript-Assist™ probiotics (2 capsules daily) if on antibiotics.

PROPER DIET IS ESSENTIAL

Consume a diet that provides good amounts of protein which is needed by the body to support the healing of bone fractures. Eat meats, poultry and fish (e.g., sardines, salmon, mackerel) in the amount of a 5–10 ounces per day. Ensure a good intake of organic vegetables, including high levels of dietary fiber. Drink 16 oz per day of fresh vegetable juices from carrot, celery, beets, cabbage, etc.

Other healthy foods (preferably organic) include fruits, whole grains (e.g., brown rice, millet, and quinoa), beans, nuts and seeds (sunflower, chia, flax, pumpkin, almond, walnut and sesame in small amounts — 2 or 4 ounces — are good). Try eating Hank’s Vegetable Soup several times a week. Avoid all sweets (sugar), processed/refined foods (white bread and pasta), preservatives, and artificial flavors and colors. Vary your diet.

HYDROTHERAPY (WATER THERAPY) FOR BONE FRACTURES

An additional treatment that can be useful is hydrotherapy. In particular, hot and cold showers are a very effective way to move the blood and create circulation. This can speed up both detoxification and delivery of healing nutrients to the area of a bone fracture. Here’s how to do this. Once daily, take a complete hot and cold shower. You will start with hot water for one minute, then cold for one minute. Repeat this seven (7) times so the shower should last about 15 minutes.

Another time, daily, you can perform a complete hot and cold shower routine again or a partial one just applying the water directly to or near the area where there is a bone fracture. While you are doing both hot and cold showers, pay special attention to any affected area and massage it as vigorously as is safe and comfortable. If a shower is impossible, then alternate hot packs and ice packs on the area of the bone fracture.

BONE FRACTURES – CONCLUSION

By following the recommendations and suggested supplement schedule, healing time for bone fractures can be significantly reduced and fractures may heal more completely with fewer complications. By ensuring your body receives the proper nutrients it needs to heal itself, and by engaging in other relevant practices (e.g., hydrotherapy), you and/or your loved ones may be able to deal with bone fractures successfully, and continue a healthy, vibrant lifestyle.

ADDITIONAL RESOURCES

HPDI REJUVENATION PROGRAM

REJUVENATION PROGRAM PART 6 (INCLUDES HYDROTHERAPY)

REJUVENATE!™ SUPERFOODS

ULTIMATE PROTECTOR™

“FRED’S FAVORITE VEGETABLE JUICE RECIPE: ‘THE DOCTOR'”

1

VITAMIN C – AN AMAZING NUTRIENT

Doctor Hank Liers PhD vitamin c ascorbic acid antioxidant collagen support immunityPeriodically, it is beneficial for me to present a review of accumulated scientific knowledge regarding key nutrients and remind readers of their importance.

In this article, I will review some of the research and clinical findings on vitamin C that have been gathered over the past 70 years. As you will see, vitamin C is an amazing nutrient!

GENERAL FACTS REGARDING VITAMIN C

Vitamin C typically is called l-ascorbic acid or ascorbate and is an essential nutrient for humans and other animal species. The term “vitamin C” refers to a number of vitamins that have vitamin C activity in animals, including ascorbic acid and its salts (e.g., magnesium ascorbate, calcium ascorbate, sodium ascorbate, etc.), and some oxidized forms such as dehydroascorbic acid.

Vitamin C is a cofactor in at least eight enzymatic reactions, including several collagen syntheses reactions that when dysfunctional (usually because of lack of Vitamin C) cause the most severe symptoms of scurvy.  In animals, these reactions are especially important in wound healing and in preventing bleeding from capillaries.

Ascorbate acts as an electron donor and/or hydrogen donor, and this ability makes it a potent antioxidant. It rapidly reduces superoxide and nitroxide radicals and scavenges hydroxyl, alkoxyl, and peroxyl radicals. It also reacts with non-radical species such as singlet oxygen and hypochlorous acid. It has been observed in in vitro experiments that Vitamin C acts as the first line of defense in the plasma.

vitamin c fruits citrus

Fruits high in vitamin C include citrus, strawberries, and kiwi

Vitamin C can “recycle” other antioxidants (i.e., due to its function as an electron donor) and thereby allow these antioxidants to quench more free radicals. Also, the one- and two- electron forms of vitamin C, semidehydroascorbic acid and dehydroascorbic acid, respectively, can be reduced in the body by glutathione and NADPH-dependent enzymatic mechanisms. The presence of glutathione in cells and extracellular fluids helps maintain ascorbate in a reduced state.

The vast majority of animals and plants are able to synthesize vitamin C, through a sequence of enzyme-driven steps. However, some animals, including guinea pigs and humans, lack the enzyme that is required in the last step of vitamin C synthesis. These species are able to survive with the lower levels available from their diets by recycling oxidized vitamin C. Animals that have the enzyme needed to synthesize of vitamin C do not have the ability to recycle oxidized vitamin C.

Ascorbic acid is absorbed in the body by both active transport and simple diffusion. Sodium-Dependent Active Transport—Sodium-Ascorbate Co-Transporters (SVCTs) and Hexose transporters (GLUTs)—are the two transporters required for absorption. SVCT1 and SVCT2 import the reduced form of ascorbate across plasma membrane. GLUT1 and GLUT3 are the two glucose transporters, and transfer only the dehydroascorbic acid form of Vitamin C.

Although dehydroascorbic acid is absorbed at a higher rate than ascorbate, the amount of dehydroascorbic acid found in plasma and tissues under normal conditions is low, as cells rapidly reduce dehydroascorbic acid to ascorbate. I have used this fact to advantage by incorporating dehydroascorbic acid in several of the products I have previously formulated (Ultimate Protector™ and Synergy C). This approach allows for greater absorption and retention of vitamin C in the body.

Vitamin C Products at integratedhealth.com

Ascorbate concentrations in the blood above the kidney (renal) re-absorption threshold pass freely into the urine and are excreted. At high dietary doses, ascorbate is accumulated in the body until the plasma levels reach the renal resorption threshold, which is about 1.5 mg/dL in men and 1.3 mg/dL in women. Concentrations in the plasma larger than this value are excreted in the urine with a half-life of about two hours.

Although the body’s maximal stores of vitamin C are to some extent determined by the renal threshold for blood, there are many tissues that maintain vitamin C concentrations far higher than in blood. Biological tissues that accumulate over 100 times the level in blood plasma of vitamin C are the adrenal glands, pituitary, thymus, corpus leuteum, and retina. Tissues with 10–50 times the concentration present in blood plasma include the brain, spleen, lung, testicle, lymph nodes, liver, thyroid, small intestinal mucosa, leukocytes, pancreas, kidney, and salivary glands.

Historically, the discovery of vitamin C was related to the findings that a substance in citrus fruits (and other fresh foods) was able to prevent scurvy. In the early 1930s research teams in Hungary (led by Albert Szent-Georgi) and Pittsburgh, Pennsylvania USA (led by Charles Glen King) first identified the anti-ascorbutic factor. Szent-Georgi initially called it l-hexuronic acid, but later proposed that the substance L-hexuronic acid be called “a-scorbic acid,” and chemically “L-ascorbic acid,” in honor of its activity against scurvy.

Shortly thereafter (around 1934), the Polish chemist Tadeus Reichstein succeeded in synthesizing the vitamin in bulk. The process made possible the cheap mass-production of vitamin C, which was quickly marketed by the Hoffman-La Roche company. Even today, all industrial methods for the production of ascorbic acid are based on the Reichstein process.

The Reichstein process involves using microbial fermentation of sugar derived mainly from corn, potatoes, or beets. When the final product is highly purified to over 99.9% purity in accordance with USP standards, none of the protein from the original source remains. The product is bio-identical to vitamin C found in plants and animals. This is an important fact in the current issues relating to genetically modified organisms (GMOs) in corn, potatoes, and beets. Polymerase chain reaction (PCR) testing is currently used to verify and certify that most of the vitamin C being produced is GMO free. To learn more about testing for GMOs, visit: http://www.gmotesting.com/Testing-Options/Genetic-analysis.aspx.

pro-c-180-f pro-c vitamin c bioflavonoids

PRO-C™

BENEFITS OF VITAMIN C 

Bone and its connecting ligaments and tendons obtain strength from a long, chain-like protein molecule called collagen. Collagen is a structural protein that is the main component of connective tissue, and is the most abundant protein in mammals, making up about 25% to 35% of the whole-body protein content.

Vitamin C is vital to the body’s production of collagen. Absence of vitamin C causes scurvy, leading to spongy gums, loosened teeth, bruising, and bleeding into the mucous membranes. Several of these symptoms are caused by loss of collagen and connective tissue from blood vessels, which then become fragile and unable to respond to blood pressure and other stresses.

Studies have shown that vitamin C concentrations in the plasma and leukocytes rapidly decline during infections and stress. Supplementation of vitamin C has been found to improve components of the human immune system such as antimicrobial and natural killer cell activities, lymphocyte proliferation, chemotaxis, and delayed-type hypersensitivity.

Vitamin C contributes to maintaining the redox integrity of cells, and thereby protects them against reactive oxygen species generated during the respiratory burst and in the inflammatory response. It is therefore clear that vitamin C plays an important role in immune function and the modulation of host resistance to infectious agents, reducing the risk, severity, and duration of infectious diseases.

Vitamin C plays a role in protecting the brain and nervous system from detrimental effects of stress. Synthesis and maintenance of the chemical messengers (neurotransmitters) adrenaline (epinephrine) and noradrenaline (norepinephrine) depends on an adequate supply of vitamin C. These neurotransmitters are vital to brain functioning and affect people’s mood. They function as stress-signaling hormones and are produced in the adrenal glands, from which they derive their name. The adrenal glands and central nervous system maintain high levels of vitamin C by means of special cellular pumps, which absorb the vitamin when the body is deficient.

Vitamin C is also needed for synthesis of carnitine, a small molecule involved in transporting fat (lipids) to mitochondria, the “furnaces” of the body’s cells that burn nutrients to produce energy. The energy provided is used either to power the cells’ activities or to provide antioxidant electrons that prevent harmful oxidation.

Vitamin C is involved in breaking down cholesterol to form bile acids. This may have implications for people needing to lower their cholesterol levels. While the role of cholesterol in causing cardiovascular disease is generally overstated, the action of vitamin C on cholesterol levels suggests that higher levels may lower the risk of gallstones.

Vitamin C has been shown to lower lipoprotein a (LPa) levels in the body. High LPa levels correlate strongly with cardiovascular disease. Dr. Linus Pauling and others have suggested that the body uses plaques containing LPa to “patch” weak blood vessels that are caused by insufficient levels of vitamin C to build strong vessels with adequate collagen.

Vitamin C is widely known as an antioxidant, a substance that fights free radicals that can damage tissues and cause illness. As the principal water-soluble antioxidant in the diet, vitamin C is essential to health.

A shortage of vitamin C results in free radical damage to essential molecules in the body. The molecules affected include DNA (deoxyribonucleic acid) and RNA (ribonucleic acid), proteins, lipids (fats), and carbohydrates. Examples of sources of damaging free radicals and oxidation include mitochondrial by-products, chemical toxins from smoking, exposure to pesticides, as well as x-rays and other types of radiation.

The importance of vitamin C in preventing free radical damage, aging, and oxidation is frequently understated by those who are unaware of the volumes of research and clinical studies that have been conducted since the 1930s. An adequate supply of vitamin C enables the regeneration of vitamin E and other antioxidants in the body. The main water-soluble antioxidant generated within our cells is called glutathione, a small protein molecule (tripeptide of the amino acids glutamic acid, cysteine, and glycine) that plays a central role in protecting our cells from oxidation damage.

Because glutathione is typically present in ten times the concentration of vitamin C, it has often been considered to play a more important role. However, the functions of vitamin C and glutathione are linked with vitamin C being required for the antioxidant functioning of glutathione, even when glutathione is present in a significantly greater concentrations.

In nature vitamin C is often found in combination with plant substances called polyphenols and bioflavonoids. These plant substances are often powerful antioxidants and Nrf2 activators that stimulate the body’s endogenous production of protective enzymes. In fact, oligomeric proanthocyanidins (OPCs) from grape seeds and pine bark have been shown to cross link and strengthen collagen that requires vitamin C for synthesis. For these reasons, it makes sense to combine vitamin C with these plant substances.

I have formulated powerful products such as PRO-C™ and Ultimate Protector+™ that contain vitamin C with plant substances such as grape seed extract, green tea extract, and fruit and vegetable extracts high in Nrf2 activators.

Ultimate Protector+

VITAMIN C DOSING

Single-digit, gram-level doses of vitamin C may prevent many diseases, but much higher doses are required for treatment of illness. The massive doses needed for therapy are often in the range of 50–100 grams (50,000–100,000 mg) of vitamin C per day. Most clinical studies have considered doses of a single gram. A dose 100 times larger has very different properties.

An optimal intake of vitamin C is the amount that prevents or cures disease while minimizing the potential risk. It is a ridiculous assumption to think that intakes sufficient to prevent acute scurvy are adequate to prevent or treat other diseases. Furthermore, there is plenty of evidence that the intake of vitamin C needed to prevent chronic illness is much greater than the RDA.

A person starting to take vitamin C supplements is starting from a level of relative deficiency. By taking repeated doses, the levels in the tissues and blood plasma increase and more can be tolerated. Human requirements for vitamin C appear to be more variable than previously realized.

The key point is that people need more vitamin C — and in many cases far more — than previously assumed. Using the criteria used to set the RDA, and removing the errors, leads to a suggestion that the intake for a healthy adult should be in the range of about 500 mg to 20 grams (20,000 mg), or even more. Some individuals would require low doses and would not tolerate higher intakes. Other individuals need higher levels, above 10 grams.

A person who wishes to estimate his or her own requirement needs to determine their bowel tolerance level. To do this, start with a low dose and repeat it each hour until bowel effects (gas, distension, and loose stools) are observed. This level of intake is your bowel tolerance level and the optimal intake is 50% to 90% of this maximum.

Keep in mind that a high carbohydrate intake can interfere with the bowel tolerance test and falsely indicate a lower limit. In addition, during times of illness your bowel tolerance level can be many times higher than when you are in a state of good health. Furthermore, the level that a person can tolerate increases with time, as dynamic flow is maintained.

People vary in their requirements and it is not possible to provide a definitive statement about intakes that applies to all. Furthermore, a person’s requirement will vary, increasing with even a slight illness. The minimum intake required to raise a typical adult’s blood plasma levels consistently is two to three grams (2,000–3,000 mg) per day, in divided doses of about 500–1,000 mg. For some, this will be too high and they may need to lower the dose slightly. For many, this intake will be far too low to provide resistance to infections and chronic disease.

Vitamin C is remarkably safe, which is not surprising considering it is essential to human life and is actively retained in the body. Vitamin C is a simple molecule, used by both animals and plants, often at high concentrations. Organisms have had hundreds of millions of years to evolve mechanisms for prevention of damage by vitamin C. But even allowing for such tolerance, the safety of vitamin C is outstanding. It is unusual in that it can be taken in massive doses, for long periods, without apparent harm.

Therapeutic levels of vitamin C required for dealing with serious illnesses are much higher than the levels described above. Under these conditions, Dr. William Klenner, one of the pioneers of vitamin C usage, recommended the amount of 350 mg per kilogram of body weight per day.

In most cases, Dr. Klenner recommended that the doses be divided into amounts taken hourly during waking hours. For example, a 50 kg (110 lb) person should take a total of 18,000 mg daily in hourly 1,000 mg doses for 18 hours. A 100 kg (220 lb) person should take 36,000 mg daily in hourly 2,000 mg doses for 18 hours. When dealing with conditions of illness these (and even higher) doses do not usually cause diarrhea. However, you can adjust these starting doses up or down according to your bowel tolerance level.

 CONCLUSION

Vitamin C is considered to be a vitamin because in relatively small amounts (less than 60 mg) it prevents and cures scurvy. However, vitamin C is so important that virtually every plant and animal on this planet requires it to be healthy. In conditions of good health the body needs between three and twenty (3–20) grams of vitamin C daily to maintain good health and prevent a wide range of serious health problems. In many conditions of poor health and illness the body can require amounts of vitamin C as high as 100 grams (and in some cases more) in order to recover.

The best way to determine your personal need for vitamin C is to check your bowel tolerance level and supplement in divided daily doses with about 70% of this level. My personal recommendation is that most people should take the buffered forms of vitamin C that are combined with other antioxidants and plant polyphenols such as are in PRO-C™ and Ultimate Protector+™. In cases where higher levels of vitamin C are called for (greater than 20 grams daily) I suggest adding buffered C powder and or ascorbic acid crystals to the PRO-C™ and Ultimate Protector™.

In my personal experience, vitamin C is an amazing nutrient especially in combination with other antioxidants. For this reason it is one of the foundational supplements in the HPDI Master Rejuvenation Program.

ADDITIONAL RESOURCES

SOURCES

  1. The Vitamin C Cure for Heart Disease. Hilary Roberts and Steve Hickey, 2011.
  2. Vitamin C: The Real Story. Steve Hickey and Andrew Saul, 2009.
  3. Curing the Uncurable: Vitamin C, Infectious Diseases, and Toxins, 3rd Ed. Thomas E. Levy, 2009.
  4. Cancer and Vitamin C: A Discussion of the Nature, Causes, Prevention, and Treatment of Cancer With Special Reference to the Value of Vitamin C. Ewan Cameron and Linus Pauling, 1993.
  5. How to Live Longer and Feel Better.  Linus Pauling, 1986.
  6. Vitamin C, the Common Cold and the Flu. Linus Pauling, 1977.
  7. The Healing Factor: Vitamin C Against Disease.  Irwin Stone, 1972.
  8. Bowel tolerance as an indicator of vitamin C saturation is discussed by Dr. RF Cathcart at http://www.doctoryourself.com/titration.html and http://www.doctoryourself.com/cathcart_thirdface.html
  9. For more about Dr. Klenner’s life and work: http://www.doctoryourself.com/klennerbio.html
  10. The complete text of Irwin Stone’s book The Healing Factor is posted for free reading at http://vitamincfoundation.org/stone/
  11. The full text of Dr. Frederick R. Klenner’s Clinical Guide to the Use of Vitamin C is posted for free reading at: http://www.seanet.com/~alexs/ascorbate/198x/smith-lh-clinical_guide_1988.htm