Supplemental hydrogen is fast becoming essential in many people’s nutritional supplement regimens. Why? Because hydrogen offers significant health benefits, including excellent antioxidant protection, increased energy, faster recovery, and improved well-being. Who doesn’t want those benefits?
My favorite way to take hydrogen is to make hydrogen-infused water, or what I call a hydrogen “fizzy” drink. Two products I like best are Active H2 Ultra tablets and Megahydrate (available in powder and capsules). Active H2 Ultra provides molecular hydrogen (H2) and Megahydrate provides hydride (H-). Both are great standalone formulas, yet work well together as each provides unique means to quench free radicals effectively.
MAKE “FIZZY” HYDROGEN-INFUSED WATER WITH ACTIVE H2 ULTRA
Drinking H2-rich water is an easy and effective method for obtaining hydrogen, according to the Molecular Hydrogen Foundation. Making hydrogen-infused water is simple and convenient, as you can drink it at home or while traveling. Effective hydrogen products HPDI carries include Active H2 Ultra tablets, Megahydrate powder, and Megahydrate capsules.
My favorite hydrogen drink contains both Active H2 Ultra and Megahydrate. I take these products separately at times, but find it easier to take them together—and gain the benefits of both immediately.
Active H2 Ultra tablets and Megahydrate powder work together for major antioxidant power.
DIRECTIONS: Put one scoop of Megahydrate powder (or open one capsule) into your container of water. Let sit for about 30–60 seconds. Drop in one Active H2 Ultra tablet. Allow it to effervesce for one minute or until fully dissolved. Drink immediately. For best assimilation, preferably take on an empty stomach at least 10–15 minutes before food. Wait one hour after eating to drink hydrogen-infused water.
Note: Do not wait long after effervesce stops to drink the water because hydrogen will escape into the air. Alternatively you can cap the container with a lid, and this will allow the hydrogen to last a while longer.
Molecular hydrogen is sufficiently small to pass through glass, so use a metal container if you plan to cap it. If you drink immediately, then the type container you use won’t matter. I personally prefer a glass mason jar. This allows me to see the tablet dissolve, but also means drinking it immediately.
I make 1–3 hydrogen fizzy drinks daily, first in the morning and then in the afternoon, but almost never in the evening as it can be energizing. I drink hydrogen water on an empty stomach. I gain a significant energy boost, but also other benefits, including improved athletic performance, faster recovery from exercise, and an overall greater sense of well-being.
I highly recommend you try hydrogen supplements for yourself, and then consider them for your clients or patients. Our experience is that most people are pleasantly surprised by the results they get from hydrogen supplements, especially if they have a need for exceptional free-radical defense, or stand to benefit from the proven effects of hydrogen (see list below).
You will want to continue taking hydrogen supplements regularly because the benefits are so significant, especially over time. Let the power of hydrogen starting working for you.
Active H2 Ultra is a fast-effervescing tablet.
MOLECULAR HYDROGEN BACKGROUND
More than 1,000 scientific studies indicate molecular hydrogen offers therapeutic potential in 170 disease models, and every organ of the body, according to the Molecular Hydrogen Institute.
Hydrogen is an antioxidant. It is also an extremely small molecule that can penetrate even the tiniest cellular compartments. This helps explain how hydrogen works to offer free-radical defense throughout the entire body.
The medical and scientific literature is clear. Hydrogen’s modes of action:
• H2 reduces oxidative stress as a selective antioxidant and by maintaining homeostatic levels of glutathione, superoxide dismutase, catalase, etc.
• H2, like other gaseous signaling molecules (i.e. NO, CO, H2S), appears to have cell signal-modulating activity affording it with anti-inflammatory, anti-obesity, and anti-allergy benefits.
The scientific literature discusses the use of molecular hydrogen for many clinical applications, including:
• Metabolic Syndrome including diabetes, hyperlipidemia, arteriosclerosis, hypertension, and obesity
• Ischemia/reperfusion injuries, including cerebral and myocardial infarctions, organ transplants, post-cardiac arrest
• Neuroprotection, including applications for dementia, Parkinson’s disease, depression, and anesthesia
• Inflammation, including applications for polymicrobial sepsis, rheumatoid arthritis, wound healing, and bowel diseases
• Mitochondrial diseases
• Hemodialysis and ventilation
• Aging, including cognitive decline
• Exercise, including applications for fatigue, lactic acid, recovery, and oxidative stress related to heavy exercise
• Side effects of cancer therapies, including radiotherapy and chemotherapy
• Many other benefits
(Source: Molecular Hydrogen Foundation)
HOW HYDROGEN WORKS
According to the Molecular Hydrogen Foundation, there are three ways molecular hydrogen exerts positive health effects:
1. Molecular hydrogen easily diffuses into subcellular compartments where it scavengescytotoxic oxygen radicals, thereby protecting DNA, RNA, and proteins against oxidative stress.
2. Molecular hydrogen triggers activation or upregulation of additional antioxidant enzymes (e.g., glutathione, superoxide dismutase, catalase, and others) and/or cytoprotective proteins of the body.
3. Molecular hydrogen may be a novel signaling molecule that alters cell signaling, cell metabolism, and gene expression. This may explain its apparent anti-inflammatory, anti-allergic, and anti-apoptotic (or anti-cell death) effects.
Notably, two of these three mechanisms of action involve antioxidant activity. Hydrogen is one of the best antioxidants for all the reasons discussed, and we believe it acts synergistically with other antioxidants, including Vitamin C, glutathione, and Nrf2 activators (like those in HPDI’s Ultimate Protector).
MEGAHYDRATE MAKES MOLECULAR HYDROGEN BETTER
Why add Megahydrate to your hydrogen-infused water? Because Megahydrate provides hydride, the negative anion of hydrogen, or H-. Thus, a tiny scoop of Megahydrate provides vast quantities of electrons available to quench free radicals. Unlike molecular hydrogen, which dissipates quickly into the air, and therefore must be consumed immediately, hydride rich water (about -700 ORP!) may last for three weeks in an active state. That is a good reason to take Megahydrate by itself whether or not you already use it with molecular hydrogen in your hydrogen “fizzy” drink (see recipe above).
Megahydrate (powder or capsule) provides hydride (H-) for free radical defense.
The interesting thing about H- is that after it gives up its electron, it becomes simply “H” or atomic hydrogen. It then looks to pair up with another “H” to become H2, which is molecular hydrogen. In this way, Megahydrate not only gives you large quantities of stable H- and potent antioxidant capabilities, but also then creates molecular hydrogen in your body. This means it becomes a different kind of antioxidant, H2, which is therapeutic in itself.
By adding Megahydrate to your hydrogen-infused water (as described above), you create a unique “double whammy” drink in which you maximize the powers of hydrogen (H2 and H-) to create and maintain good health.
Note:Megahydrate powder is more cost effective than Megahydrate capsules, which must be opened into the fizzy drink. However, Megahydrate capsules are convenient for traveling and are easy to take by themselves. I keep both available, so I can use either one depending on my daily needs.
DRINKING HYDROGEN-INFUSED WATER
Drinking H2-rich water is an easy, effective method for obtaining hydrogen according to the Molecular Hydrogen Foundation. Drinking hydrogen-infused water is convenient as you can drink it at home or while traveling. Effective hydrogen products HPDI carries include Active H2 Ultra tablets, Megahydrate capsules, and Megahydrate powder.
As noted, I make 1–3 hydrogen drinks daily using Megahydrate and Active H2 Ultra. I drink them on an empty stomach. I enjoy a significant energy boost, which helps power me through my day. I gain other benefits, including improved athletic performance, noticeably faster recovery from exercise, and an overall greater sense of well-being.
The nice thing about hydrogen supplements is how flexibly you can use them. While I typically prefer to make hydrogen-infused “fizzy” drinks in water, I will often sip Megahydrate-infused water by itself during the day or even in the evening (as it is less energizing than molecular hydrogen).
Megahydrate does not immediately lose its potency in water, so it can be casually sipped. Also, if you’re traveling or on-the-go, you can simply swallow a Megahydrate capsule by itself. Finally, you can carry Active H2 Ultra tablets with you wherever you go, and add them to water whenever convenient for you.
Megahydrate and Active H2 Ultra creates an ultra-healthy hydrogen fizzy drink.
Try hydrogen supplements for yourself. Then consider recommending them to client, patients, friends, and family. Most people welcome the results from hydrogen. This is especially true if they need exceptional free-radical defense — and who doesn’t? We can all stand to benefit from the proven health benefits hydrogen uniquely provides.
After you try hydrogen, you will want to continue taking it. Hydrogen-infused “fizzy” water can become your go-to drink. Remember, hydrogen works best when taken consistently and daily!
Looking for an advanced antioxidant formula? Already using or recommending vitamin C? Curious about cellular Nrf2 activation? Look no further than PRO-C™.
PRO-C™ is among the most effective antioxidant formulas available. It is an HPDI foundational supplement that works most effectively when used with multivitamins, essential fats, and superfoods. However, it is also an excellent standalone formula that can rapidly provide the body with extremely high protection from free radicals.
We ourselves have taken PRO-C daily for many years with excellent results. Our personal experience together with detailed feedback from health professionals and end-users affirms the effectiveness of PRO-C as a super-antioxidant–vitamin C-Nrf2 activator formula.
PRO-C provides 500 mg of buffered vitamin C per capsule (buffered with calcium, magnesium, and zinc) along with grape extract (seed, skin, pulp) and green tea extract (95% polyphenols). In addition, we include a special combination of the “network antioxidants” l-glutathione (reduced), n-acetyl-l-cysteine (NAC), r-lipoic acid, and selenium. Vitamin B2 and Vitamin B6 in coenzyme forms support the enzymatic effectiveness of the “network antioxidants”. The formula works so well because this combination of ingredients leverages the antioxidant power of vitamin C, grape extract, green tea extract, and the other nutrients to act synergistically in order to maximize effectiveness.
FORMULATION HISTORY AND THE SCIENCE BEHIND PRO-C™
What you may not know is the history of the development PRO-C and the scientific knowledge on which Dr. Hank Liers based his formulation of it.
Dr. Hank formulated his first product in 1989. It was a potent antioxidant formula he called PYC-C™ (sounds like “pixie”). PYC-C consisted of a combination of buffered Vitamin C (including magnesium, calcium, and zinc ascorbates) and pycnogenols from pine bark.
By 1997 Dr. Hank had gathered a great deal of new scientific information regarding green tea catechins and the nutrients termed “network antioxidants” by Dr. Lester Packer, director of Packer Lab at University of California, Berkeley. Beyond this information, Dr. Hank studied additional research regarding how various nutrients worked together synergistically. At that point, he was ready to formulate the new, improved PRO-C™ super antioxidant formula.
PRO-C combines the ingredients of PYC-C (now known as OPC-C™) and uses grape pulp, skin, and seed extract with green tea extract (with high polyphenols >95% and EpiGalloCatechinGalate (EGCG) >45%), n-acetyl-l-cysteine (NAC), reduced glutathione (GSH), R-lipoic acid, selenium, and coenzyme Vitamins B2 and B6.
HPDI launched PRO-C™ in late 1997. It rapidly became one of our best-selling products. Our customers raved about how effective it was for them if they felt like they were “coming down with something” (like a cold, flu, virus, infection, etc.). Greater skin elasticity greatly helped pregnant women avoid stretch marks and episiotomies. Today, we highly recommend its use together with our other Foundational Supplements to ensure optimal health and anti-aging effects.
THE PRO-C™ SUPER ANTIOXIDANT FORMULA
PRO-C™ super antioxidant formula is extremely synergistic, especially in so far as it increases the body’s ability to quench free radicals in its aqueous (i.e., water-based) compartments. Because antioxidants may become free radicals themselves after they have done their job, the body has developed an elaborate system for recovery of oxidized antioxidants.
Dr. Lester Packer was the primary researcher investigating the synergistic character of antioxidants. He made this statement in his interview with Dr. Richard Passwater after publication of Packer’s The Antioxidant Miracle (1999):
” [The major theme of] The Antioxidant Miracle is that antioxidants work in a coordinated manner. They interact with one another, and this interaction, which we like to call the antioxidant network, is very important to the overall antioxidant defense that we possess. The key members of the antioxidant network are vitamin E and vitamin C, but there are other participants in this network. These are thiol antioxidants, antioxidants that contain sulfur groups in the body. Glutathione perhaps is the best known of these, but there are other sulfur-containing antioxidants that also are very important.”
Dr. Packer continues:
“This whole antioxidant network works like an orchestra depending on individuals who have, of course, different complements of antioxidants depending upon their nutritional regimens and the individuality of their own body metabolisms. The idea behind having a network of antioxidants is that if one antioxidant happens to be deficient the others can compensate and still keep the antioxidant defense system strong.”
The following diagram shows some of the relationships in the antioxidant network and how they support each other.
Figure 1 – Dr. Packer’s Antioxidant Network
We see, for example, reduced glutathione (GSH) has the ability to reduce oxidized Vitamin C back to its unoxidized state. Vitamin C reduces oxidized Vitamin E back to its unoxidized state, and both reduces glutathione and spares it for other important functions, including detoxification and immune enhancement.
Many polyphenols (e.g., oligomeric proanthocyanidins (OPCs), anthocyanidins and catechins) found in red grape and green tea extracts spare Vitamin C and glutathione in the body, as well as operate as powerful antioxidants, anti-inflammatories, and connective tissue strengtheners.
Grapes provide antioxidant nutrients such as polyphenols, OPCs, anthocyans, and resveratrol.
R-Lipoic Acid (see abstracts below) operates as an antioxidant both in its oxidized and reduced states, reduces the oxidized forms of both Vitamin E and Vitamin C, and and has been shown to enhance glutathione levels. Because several of these substances are able to protect Vitamin E contained in cell membranes, this combination also has a significant beneficial effect on the fat soluble antioxidant status of the body!
The nutrients in PRO-C have been carefully selected and balanced to provide optimal effects, especially as related to free radical protection, detoxification, immune system enhancement, connective tissue strengthening, and reduction of inflammation. PRO-C therefore provides outstanding nutritional support in a wide variety of conditions of poor health, as well as acts to support and maintain a state of health and well-being.
It the last several years the research results on Nrf2 activators have become well known and products developed that take advantage of these nutrients. For details see our blog article Natural Phytochemical Nrf2 Activators for Chemoprevention. Researchers have been studying specifically how enzyme-activating substances such as OPCs and anthocyans activate a transcription factor known as Nrf2 that causes the body to endogenously produce higher levels of a wide variety of protective enzymes including superoxide dismutase (SOD), catalase, and glutathione peroxidase.
Although we did not know about Nrf2 activators in 1997 when we formulated PRO-C, we have subsequently learned that four of the ingredients in the formula have powerful Nrf2 activity. These include grape seed extract, green tea extract, NAC, and r-lipoic acid. With this knowledge, we now understand that PRO-C provides both powerful external antioxidants (with extremely high ORAC5.0 values) that support redox cycles within the body, but also provides ingredients that allow the body to endogenously produce powerful protective enzymes for even greater free-radical protection and health.
PRO-C™ ANTIOXIDANT FORMULA INGREDIENTS
PRO-C contains buffered vitamin C (in the form of powdered calcium, magnesium, and zinc ascorbates), high-potency grape extract (from grape pulp, skins, and seeds), green tea extract (with>95% polyphenols and >45% EGCG), reduced glutathione, N-Acetyl-L-Cysteine (NAC), R-lipoic acid, coenzyme forms of vitamin B2 (R5P) and vitamin B6 (P5P), and selenium.
Below we will discuss each ingredient and show some of the research that confirms its effectiveness.
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 dehydroascorbate and semidehydroascorbate.
Vitamin C is known to perform many critical functions within the body involving detoxification, tissue building, immune enhancement, pain control, and controlling or killing pathogenic organisms. It is also known to be helpful for wound and bone healing, healthy skin and eyes, fighting infections, stress control, toxic exposure, and repairing damaged tissue of all types. For much more information on the many benefits of Vitamin C see our blog article Vitamin C – An Amazing Nutrient.
Below are two abstracts that show some of the beneficial effects of Vitamin C when used with other network antioxidants:
ABSTRACT 1: Exhaustive physical exercise causes oxidation of glutathione status in blood: prevention by antioxidant administration.
Sastre J, Asensi M, Gasco E, Pallardo FV, Ferrero JA, Furukawa T, Vina J
In: Am J Physiol (1992 Nov) 263(5 Pt 2):R992-5
We have studied the effect of exhaustive concentric physical exercise on glutathione redox status and the possible relationship between blood glutathione oxidation and blood lactate and pyruvate levels. Levels of oxidized glutathione (GSSG) in blood increase after exhaustive concentric physical exercise in trained humans. GSSG levels were 72% higher immediately after exercise than at rest. They returned to normal values 1 h after exercise. Blood reduced glutathione (GSH) levels did not change significantly after the exercise. We have found a linear relationship between GSSG-to-GSH and lactate-to-pyruvate ratios in human blood before, during, and after exhaustive exercise. In rats, physical exercise also caused an increase in blood GSSG levels that were 200% higher after physical exercise than at rest. GSH levels did not change significantly. Thus, both in rats and humans, exhaustive physical exercise causes a change in glutathione redox status in blood. We have also found that antioxidant administration, i.e., oral vitamin C, N-acetyl-L- cysteine, or glutathione, is effective in preventing oxidation of the blood glutathione pool after physical exercise in rats.
The effect of glutathione and vitamins A, C, and E on acute skin flap survival.
Hayden RE, Paniello RC, Yeung CS, Bello SL, Dawson SM
In: Laryngoscope (1987 Oct) 97(10):1176-9
Vitamins A, C, and E act as antioxidants and as free radical scavengers in biological systems. Glutathione is involved in several reactions in vitamin metabolism and also plays an important role in cell membrane protection against lipid peroxidation by free radicals. We sought to use these natural defense mechanisms against oxygen free radicals formed during reperfusion of ischemic skin flaps. An acute axial random skin flap model was utilized in the rat. Vitamins or glutathione were administered by oral gastric tube or intravenously in the perioperative period, and survival of the flap was measured at 1 week. Glutathione, beta-carotene, ascorbic acid and alpha-D- tocopherol showed mean flap survival of 84% to 89%, each of which was significantly improved over saline controls (67% p less than .0005). The mechanisms and biochemistry of these vitamins, and their interactions with other vitamins and with glutathione, are discussed, along with clinical implications of free radical scavenging and skin flap survival.
Grape extract (seeds, skin, pulp) contain highly bioavailable bioflavonoid complexes that in research studies have been shown to have powerful antioxidant capability. The Oligomeric Proanthocyanidins (OPCs) in grape seed 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 anthocyans, which are found in extracts of grape 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 stems (but not those of grape seed extract) contain a material called trans-resveratrol that has been shown to have chemopreventive effects.
ABSTRACT 3: Protective effects of grape seed proanthocyanidins and selected antioxidants against TPA-induced hepatic and brain lipid peroxidation and DNA fragmentation, and peritoneal macrophage activation in mice. Bagchi D, Garg A, Krohn RL, Bagchi M, Bagchi DJ, Balmoori J, Stohs SJ
In: Gen Pharmacol (1998 May) 30(5):771-6
1. The comparative protective abilities of a grape seed proanthocyanidin extract (GSPE) (25-100 mg/kg), vitamin C (100 mg/kg), vitamin E succinate (VES) (100 mg/kg) and beta-carotene (50 mg/kg) on 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced lipid peroxidation and DNA fragmentation in the hepatic and brain tissues, as well as production of reactive oxygen species by peritoneal macrophages, were assessed. 2. Treatment of mice with GSPE (100 mg/kg), vitamin C, VES and beta-carotene decreased TPA-induced production of reactive oxygen species, as evidenced by decreases in the chemiluminescence response in peritoneal macrophages by approximately 70%, 18%, 47% and 16%, respectively, and cytochrome c reduction by approximately 65%, 15%, 37% and 19%, respectively, compared with controls. 3. GSPE, vitamin C, VES and beta-carotene decreased TPA-induced DNA fragmentation by approximately 47%, 10%, 30% and 11%, respectively, in the hepatic tissues, and 50%, 14%, 31% and 11%, respectively, in the brain tissues, at the doses that were used. Similar results were observed with respect to lipid peroxidation in hepatic mitochondria and microsomes and in brain homogenates. 4. GSPE exhibited a dose-dependent inhibition of TPA- induced lipid peroxidation and DNA fragmentation in liver and brain, as well as a dose-dependent inhibition of TPA-induced reactive oxygen species production in peritoneal macrophages. 5. GSPE and other antioxidants provided significant protection against TPA-induced oxidative damage, with GSPE providing better protection than did other antioxidants at the doses that were employed.
ABSTRACT 4: Clinical and capillaroscopic evaluation of chronic uncomplicated venous insufficiency with procyanidins extracted from vitis vinifera
Costantini A, De Bernardi T, Gotti A
In: Minerva Cardioangiol (1999 Jan-Feb) 47(1-2):39-46
BACKGROUND: The pharmacological treatment of non-complicated chronic venous insufficiency is a current and well-debated topic. The introduction of new products with action on the venous system, improved knowledge on the physiopathology of venous insufficiency and the possibility provided by new analytical instruments, have given new impulse to the consolidation of the clinical value of phlebotonics in this indication. METHODS: In light of this, 24 patients with non-complicated chronic venous insufficiency were treated with oral administration of Oligomeric Proanthocyanidins (Pycnogenols-OPC) 100 mg/day. To evaluate the therapeutic efficacy of the treatment, an instrumental evaluation by optical probe capillaroscope was employed in addition to the traditional subjective clinical parameters: swelling, itching, heaviness and pain. The videocapillaroscope examination was performed at the lower third of the leg and the first toe. Edema in the capillaroscopic field, the number of observable capillaries and the capillary dilatation were the parameter chosen to evaluate the efficacy of treatment. All patients completed the study with no reports of adverse events during the period of observation. RESULTS: The results obtained show a positive clinical response (improved or absent symptoms) in over 80% of patients, with significant improvement of symptoms already evident after the first 10 days of treatment. The mechanism of action of the OPCs explains the rapid reduction of the swelling of the lower limbs and correlated with this are the other evaluable symptoms: heaviness and itching. Particularly striking results were observed for itching and pain which completely disappeared during the course of therapy in 80% and 53% of the patients respectively. Noteworthy is the good correlation between the clinical and instrumental data, with improvement in a total of 70% of patients. CONCLUSIONS: The results obtained in the course of this clinical experience, with evident improvement already during the first weeks of treatment, the absence of adverse events added to the benefit of a once-a-day administration, justify the use of OPC in the treatment of non-complicated chronic venous insufficiency.
Nuclear factor erythroid 2-related factor 2 (Nrf2) is an important transcription factor that regulates antioxidant response element (ARE)-driven phase II detoxification enzymes. In this study, induction of phase II enzymes via Nrf2/ARE activation in the cytoprotective effect of crude polyphenol extract (CPE), oligomeric procyanidin fraction (OPF), and polymeric procyanidin fraction (PPF) from defatted grape seeds in HepG2 cells was evaluated. Among these treatments, the treatment with PPF significantly increased Nrf2 protein expression in the nuclear fraction. Treating the samples increased heme oxygenase-1 (HO-1) and NAD(P)H:quinone oxidoreductase 1 (NQO1) protein expression in a dose-dependent manner, and PPF significantly increased the levels of phase II enzymes. Cellular generation of reactive oxygen species (ROS) were effectively reduced by PPF. These results suggest that pretreatment with PPF shows a cytoprotective effect by inhibiting ROS production and inducing HO-1 and NQO1 expression via Nrf2 activation in HepG2 cells.
GREEN TEA EXTRACT
Green tea extract is obtained from the unfermented leaves of Camellia sinensis for which numerous biological activities have been reported including: antimutagenic, antibacterial, hypocholesterolemic, antioxidant, and protective against tumorigenesis. Below we have selected a few of the many abstracts we have on file showing the benefit of green tea extract.
Green tea leaves are high in antioxidant polyphenols and catechins.
ABSTRACT 6: Enhancement of antioxidant and phase II enzymes by oral feeding of green tea polyphenols in drinking water to SKH-1 hairless mice: possible role in cancer chemoprevention.
Khan SG, Katiyar SK, Agarwal R, Mukhtar H
In: Cancer Res (1992 Jul 15) 52(14):4050-2
Following the oral feeding of a polyphenolic fraction isolated from green tea (GTP) in drinking water, an increase in the activities of antioxidant and phase II enzymes in skin, small bowel, liver, and lung of female SKH-1 hairless mice was observed. GTP feeding (0.2%, w/v) to mice for 30 days significantly increased the activities of glutathione peroxidase, catalase, and quinone reductase in small bowel, liver, and lungs, and glutathione S-transferase in small bowel and liver. GTP feeding to mice also resulted in considerable enhancement of glutathione reductase activity in liver. In general, the increase in antioxidant and phase II enzyme activities was more pronounced in lung and small bowel as compared to liver and skin. The significance of these results can be implicated in relation to the cancer chemopreventive effects of GTP against the induction of tumors in various target organs.
ABSTRACT 7: INHIBITORY EFFECT OF SIX GREEN TEA CATECHINS AND CAFFEINE ON THE GROWTH OF FOUR SELECTED HUMAN TUMOR CELL LINES. In: Anticancer Drugs (1996 Jun) 7(4):461-8
Institutional address: Department of Pharmacology and Toxicology College of Pharmacy University of Arizona Tucson 85721 USA.
Green tea is an aqueous infusion of dried unfermented leaves of Camellia sinensis (family Theaceae) from which numerous biological activities have been reported including antimutagenic, antibacterial, hypocholesterolemic, antioxidant, antitumor and cancer preventive activities. From the aqueous-alcoholic extract of green tea leaves, six compounds (+)-gallocatechin (GC), (-)-epicatechin (EC), (-)- epigallocatechin (EGC), (-)-epicatechin gallate (ECG), (-)- epigallocatechin gallate (EGCG) and caffeine, were isolated and purified. Together with (+)-catechin, these compounds were tested against each of four human tumor cells lines (MCF-7 breast carcinoma, HT-29 colon carcinoma, A-427 lung carcinoma and UACC-375 melanoma). The three most potent green tea components against all four tumor cell lines were EGCG, GC and EGC. EGCG was the most potent of the seven green tea components against three out of the four cell lines (i.e. MCF-7 breast cancer, HT-29 colon cancer and UACC-375 melanoma). On the basis of these extensive in vitro studies, it would be of considerable interest to evaluate all three of these components in comparative preclinical in vivo animal tumor model systems before final decisions are made concerning which of these potential chemopreventive drugs should be taken into broad clinical trials.
GLUTATHIONE AND N-ACETYL-L-CYSTEINE (NAC)
Glutathione and NAC (a major precursor of glutathione) both provide important protection against toxins and free radicals, and can strengthen the immune system. Glutathione is considered to be one of the most important protective substances in the human body with almost 60% of liver detoxification accounted for by this key substance. In addition, glutathione is one of the most potent anti-viral substances known.
Some research has indicated that glutathione may not be able to enter easily into certain types of cells, but NAC is able to enter these cells and be converted into glutathione once inside the cell. Thus, the combination of glutathione and NAC appear to be more potent than either alone.
ABSTRACT 8 GSH rescue by N-acetylcysteine.
Ruffmann R Wendel A
In: Klin Wochenschr (1991 Nov 15) 69(18):857-62
Reduced glutathione (GSH) is the main intracellular low molecular weight thiol. GSH acts as a nucleophilic scavenger and as an enzyme-catalyzed antioxidant in the event of electrophilic/oxidative tissue injury. Therefore, GSH has a major role as a protector of biological structures and functions. GSH depletion has been recognized as a hazardous condition during paracetamol intoxication. Conversely, GSH rescue, meaning recovery of the protective potential of GSH by early administration of N-acetylcysteine (NAC), has been found to be life-saving. Lack of GSH and electrophilic/oxidative injury have been identified among the causes of the adult respiratory distress syndrome (ARDS), idiopathic pulmonary fibrosis (IPF), and the acquired immunodeficiency syndrome (AIDS). Experimental and early clinical data (in ARDS) point to the role of NAC in the treatment of these conditions. Recently, orally given NAC has been shown to enhance the levels of GSH in the liver, in plasma, and notably in the bronchoalveolar lavage fluid. Rescue of GSH through NAC needs to be appreciated as an independent treatment modality for an array of different disease, all of which have one feature in common: pathogenetically relevant loss of GSH.
ABSTRACT 9 Cysteine and glutathione concentrations in plasma and bronchoalveolar lavage fluid after treatment with N-acetylcysteine.
Bridgeman MM Marsden M MacNee W Flenley DC Ryle AP
In: Thorax (1991 Jan) 46(1):39-42
N-acetylcysteine (600 mg/day) was given to patients by mouth for five days before bronchoscopy and bronchoalveolar lavage to determine whether N-acetylcysteine could increase the concentrations of the antioxidant reduced glutathione in plasma and bronchoalveolar lavage fluid. Bronchoalveolar lavage was performed 1-3 hours (group 2, n = 9) and 16-20 hours (group 3, n = 10) after the last dose of N-acetylcysteine and the values were compared with those in a control group receiving no N-acetylcysteine (group 1, n = 8). N-Acetylcysteine was not detected in plasma or lavage fluid. Plasma concentrations of cysteine, the main metabolite of N-acetylcysteine and a precursor of reduced glutathione, were greater in the groups receiving treatment (groups 2 and 3) than in group 1. Cysteine concentrations in lavage fluid were similar in the three groups. Concentrations of reduced glutathione were greater in both plasma and lavage fluid in group 2 than in group 1. These data suggest that N-acetylcysteine given by mouth is rapidly deacetylated to cysteine, with resulting increases in the concentrations of cysteine in plasma and of reduced glutathione in plasma and the airways, which thus temporarily increase the antioxidant capacity of the lung.
R-LIPOIC ACID / ALPHA-LIPOIC ACID
R-Lipoic Acid is normally made at low levels in the human body, where it functions primarily as an important metabolic nutrient in the conversion of pyruvic acid into acetyl coenzyme A. As such, it plays a crucial role in the metabolism of both fats and carbohydrates into energy. In addition, r-lipoic acid functions as an extremely powerful antioxidant capable of trapping many different types of free radicals in the body.
Because it is both water and fat soluble, lipoic acid is able to operate in a broader range of body tissues than most other antioxidants. Its small size allows lipoic acid to enter areas of the body not easily accessible to many other substances; this allows lipoic acid, for example, to enter the cell nucleus and prevent free-radical damage to DNA.
Because it is such a powerful antioxidant and can easily function as such in both a reduced and oxidized state, lipoic acid is able to protect other important antioxidants such as glutathione, Vitamin E, and Vitamin C. R-lipoic acid is also able to chelate heavy metals such as lead, cadmium, mercury, free iron, and free copper out of the body.
Below we provide relevant scientific abstracts from our database regarding R-Lipoic acid.
ABSTRACT 10: Alpha-Lipoic acid as a biological antioxidant.
Packer L Witt EH Tritschler HJ
In: Free Radic Biol Med (1995 Aug) 19(2):227-50
alpha-Lipoic acid, which plays an essential role in mitochondrial dehydrogenase reactions, has recently gained considerable attention as an antioxidant. Lipoate, or its reduced form, dihydrolipoate, reacts with reactive oxygen species such as superoxide radicals, hydroxyl radicals, hypochlorous acid, peroxyl radicals, and singlet oxygen. It also protects membranes by interacting with vitamin C and glutathione, which may in turn recycle vitamin E. In addition to its antioxidant activities, dihydrolipoate may exert prooxidant actions through reduction of iron. alpha-Lipoic acid administration has been shown to be beneficial in a number of oxidative stress models such as ischemia-reperfusion injury, diabetes (both alpha-lipoic acid and dihydrolipoic acid exhibit hydrophobic binding to proteins such as albumin, which can prevent glycation reactions), cataract formation, HIV activation, neurodegeneration, and radiation injury. Furthermore, lipoate can function as a redox regulator of proteins such as myoglobin, prolactin, thioredoxin and NF-kappa B transcription factor. We review the properties of lipoate in terms of (1) reactions with reactive oxygen species; (2) interactions with other antioxidants; (3) beneficial effects in oxidative stress models or clinical conditions.
Alpha-lipoic acid (α-LA) is an important antioxidant that is capable of regenerating other antioxidants, such as glutathione (GSH). However, the underlying molecular mechanism by which α-LA regenerates GSH remains poorly understood. The current study aimed to investigate whether α-LA regenerates GSH by activation of Nrf2 to alleviate cadmium-induced cytotoxicity in HepG2 cells. In the present study, we found that cadmium induced cell death by depletion of GSH through inactivation of Nrf2. Addition of α-LA to cadmium-treated cells reactivated Nrf2 and regenerated GSH through elevating the Nrf2-downstream genes γ-glutamate-cysteine ligase (γ-GCL) and GR, both of which are key enzymes for GSH synthesis. However, blocking Nrf2 with brusatol in the cells co-treated with α-LA and cadmium reduced the mRNA and the protein levels of γ-GCL and GR, thus suppressed GSH regeneration by α-LA. Our results indicated that α-LA activated Nrf2 signaling pathway, which upregulated the transcription of the enzymes for GSH synthesis and therefore GSH contents to alleviate cadmium-induced cytotoxicity in HepG2 cells.
Selenium has been shown by clinical research to be a key mineral in the body’s defenses against free radicals and has been shown to be a major factor in reducing the symptoms of HIV infections and in the prevention of tumors. Selenium is used in conjunction with glutathione to form the powerful enzyme glutathione peroxidase that is responsible for detoxification of peroxides formed during the process of aerobic metabolism in humans and other animals.
ABSTRACT 12 Serum selenium concentrations in rheumatoid arthritis.
In: Ann Rheum Dis (1991 Jun) 50(6):376-8
O’Dell JR, Lemley-Gillespie S, Palmer WR, Weaver AL, Moore GF, Klassen LW
Selenium is a trace element and an essential part of the enzyme glutathione peroxidase, which protects cells from oxidative damage. Selenium has been shown to have antiproliferative, anti-inflammatory, antiviral, and immune altering effects. Serum selenium concentrations in 101 patients with seropositive rheumatoid arthritis were found to be significantly lower than those in 29 normal, healthy controls (mean (SD) 148 (42) v 160 (25) micrograms/l) and also lower than those in eight patients with fibrositis (148 (42) v 166 (25) micrograms/l). It is speculated that serum selenium concentrations may modulate the effect of viral or other infections in subjects with the appropriate genetic background and in this way enhance the development or progression of rheumatoid arthritis.
ABSTRACT 13 Studies on selenium in top athletes.
Dragan I, Ploesteanu E, Cristea E, Mohora M, Dinu V, Troescu VS
In: Physiologie (1988 Oct-Dec) 25(4):187-90
The authors performed a controlled trial in 18 top athletes (9 weight lifters and 9 rowers, girls) in order to make evident some chronic and acute effects (antioxidant) of selenium. Nonprotein–SH (essential glutathione), lipid peroxides (MDA-malondialdehyde), glucose-6-phosphate dehydrogenases (G-6-PDH) and fructose-1,6- diphosphate aldolase in serum, have been recorded initially on basal conditions, after 3 weeks of treatment (100 micrograms/day selenium or placebo) and again after 3 weeks of treatment, also on basal conditions, when crossing over the groups (between a free interval of 10 days). In another trial we registered these parameters on basal conditions and after two hours of hard training accompanied by a per oral administration of 150 micrograms selenium (respectively placebo). The results show significant changes under selenium treatment of the peroxides, G-6-PDH and light changes, not significant of the nonprotein–SH, changes which could suggest an antioxidant effect of this element.
VITAMINS B2 and B6 IN COENZYME FORMS
Vitamin B2 as coenzyme riboflavin-5-phosphate is a key vitamin that supports the regeneration of glutathione (via glutathione reductase). Vitamin B6 as coenzyme pyridoxal-5-phosphate is a key vitamin that supports the ability of glutathione to combine with toxic substances (via glutathione transferase) in the process of eliminating them from the body. They are especially effective in their coenzyme forms which allows them to be directly utilized by the body starting in the intestinal tract.
MAGNESIUM, CALCIUM, AND ZINC
Magnesium, zinc, and calcium synergistically work with (and enhance the effects of) the other ingredients in PRO-C. Minerals are especially needed as active components of enzymes that drive metabolic activity. For example, magnesium is required in the functioning of more than 325 types of enzymes.
PRO-C™ SUPER ANTIOXIDANT FORMULA BENEFITS
HIGHLY EFFECTIVE VITAMIN C FORMULA PLUS ANTIOXIDANTS. A complete vitamin C formula, a powerful antioxidant Formula, and Nrf2 activator combined in a single advanced supplement!
POWERFUL, SYNERGISTIC FREE-RADICAL QUENCHING FORMULA. PRO-C™ components work together to quench free radicals in your body. Vitamin C enables grape seed extract to function more effectively, and conversely grape seed extract potentiates vitamin C. Green tea extract boosts ORAC (Oxygen Radical Absorbance Capacity) value.
PROVIDES SIGNIFICANT AMOUNTS OF POWERFUL NRF2 ACTIVATORS (from Grape Extract, Green Tea Extract, NAC, and R-Lipoic Acid) that stimulate the production of the body’s own protective antioxidants including superoxide dismutase, catalase, glutathione peroxidase, and heme oxygenase.
SUPERIOR, BUFFERED (NON-ACIDIC) FORM OF VITAMIN C. Mineral Ascorbates never acidify your body, keeping you pH balanced. Staying alkaline is an important element in maintaining a healthy body.
RAPID ASSIMILATION. Capsule form ensures rapid uptake and assimilation in the body. You may also empty capsule contents into water, food, or directly Into mouth, if desired. Good, mildly tart taste!
COMPOSITION OF PRO-C™ SUPER ANTIOXIDANT FORMULA
One (1) vegetarian capsule of PRO-C provides the following percentages of the Daily Value:
% Daily Value
Vitamin C (from mineral ascorbates)
BioVin® Grape Extract
Green Tea Extract
Calcium (from calcium ascorbate)
Magnesium (from magnesium ascorbate)
Zinc (from zinc ascorbate)
Vitamin B2 (from riboflavin-5′-phosphate)
Vitamin B6 (from pyridoxal-5′-phosphate)
Selenium (from l-selenomethionine)
* No established Daily Value
DIRECTIONS: As a dietary supplement take 1–3 capsules or more daily in divided doses (i.e., spread out over the day), or as recommended by a health care professional. It initially may be useful to take up to 6 capsules per day in divided doses for one week. The contents of the capsule may be emptied into juice or food, as needed.
INGREDIENTS: PRO-C™ SUPER ANTIOXIDANT FORMULA contains only the highest-quality USP grade magnesium ascorbate, USP grade calcium ascorbate, BioVin® grape extract (greater than 75% polyphenols, 93% OPC, greater than 3.5% anthocyanidins from grape pulp, skins, and seeds, and a small amount of trans resveratrol), green tea extract (95% min. polyphenols and 45% min. EGCG), l-glutathione (reduced), USP grade n-acetyl-l-cysteine, USP grade zinc ascorbate, r-(+)-lipoic acid, riboflavin-5′-phosphate, pyridoxal-5′-phosphate, l-selenomethionine, the smallest amounts of microcrystalline cellulose and silica in a vegetarian capsule.
PRO-C™ does not contain wheat, rye, oats, corn antigen, barley, gluten, soy, egg, dairy, yeast, sugar, sulfates, phosphates (other than coenzyme forms), fats, chlorides, GMOs, wax, preservatives, colorings, or artificial flavorings.
One of the most significant developments for nutrient uptake and assimilation is the advent of liposomal delivery systems. Once in the range of 300–5,000 nanometers, the latest liposomes are now just 20–100 nanometers (nm)!
The significance of these small liposomes—tiny bilayer lipid structures—is that there is a major increase in the amount of nutrient delivery to cells. That is, small liposomes show significantly greater efficiency at intracellular delivery of encapsulated compounds.
Liposomal delivery systems have evolved rapidly and now offer major advantages over nutritional supplements delivered by standard means—like capsules, tablets, powders, and liquids (e.g., tinctures).
Liposomal delivery systems first utilized multi-lamellar vesicles (MLV) ranging ins size from 300–5,000 nanometers. Later, “large” unilamellar vesicles (LUV) (100–300 nanometers) were developed. Products containing LUVs are more effectively assimilated than MLVs.
As noted, lipsomal technologies have shrunk liposome sizes to 20–100 nanometers (nm), the category size for small unilamellar vesicles (SUV). This means the body can far more easily assimilate nutrients delivered liposomally when the particle sizes are up to 10 times smaller than already effective liposome sizes.
Small liposomes (SUV) have a long circulation half-life and better cellular accumulation. Small lipid particles have the fastest uptake kinetics and can participate in paracellular (between cells) transport. The nutritional liposome industry is rapidly moving toward the use of small liposomes.
Key Point: Small liposomes (SUV) are significantly more efficient at intracellular delivery of encapsulated compounds. In a recent study with carefully sized liposomes, cellular uptake increased nine-fold as liposome size was decreased from 236 nm to 97 nm and was 34 fold higher at 64 nm.
Nutrients that can be delivered liposomally range from vitamin C and glutathione to many types of adaptogenic and medicinal herbs.
Benefits of Liposomal Delivery
Rapid update, assimilation, and movement into cells
Oral intake bypasses digestive system—nutrients go directly into body
High levels of nutrients assimilated
Reduced dosages and less “wasted” product
Nutrients penetrate smallest compartments in the body
Nutrients circulate widely
Precise intra-oral delivery
Simple manual pump from glass bottle
Easy water dispersability when desired
Liposomal delivery systems are the future of nutritional supplements given all the advantages they confer. HPDI recognizes the value of liposomal products, and now offers the best formulas available—from Quicksilver Scientific, Inc.—to our customers.
QUICKSILVER LIPOSOMAL FORMULAS
HPDI offers four liposomal formulas from Quicksilver Scientific, the leader in nanoliposomal delivery systems. Each formula offers unparalleled uptake and assimilation—and good taste!—via inta-oral delivery. These products include:
HPDI offers four liposomal formulas from Quicksilver Scientific.
Liposomal Vitamin C with R-Lipoic Acid (mean size 50–100nm): Quicksilver Scientific’s Etheric Delivery™ system for Liposomal Vitamin C (with R-Lipoic Acid) is the most absorbable form of professional-grade Vitamin C. Vitamin C is essential to any detoxification program because it feeds the system that eliminates toxins. It is also very effective in removing lead and other heavy metals from our system and fighting off the free radicals that form in the liver during the first phase of detoxification.
R-Lipoic Acid (as sodium R-Lipoate) has an exceptionally well-documented ability to upregulate the glutathione system via the Nrf2 nuclear transcription pathway. This combination of liposomal vitamin C and R-Lipoate in a nanoliposomal delivery system potently harnesses the potential of Vitamin C to the power of a fully functioning glutathione system.
The absorption of conventional oral Vitamin C diminishes rapidly as the dose increases (e.g., about 19% for 1000 mg oral vitamin C). Nanosphere delivery greatly increases absorption and for some compounds can provide higher intracellular delivery than an IV administration.
Quicksilver Liposomal Vitamin C with R-Lipoic Acid
Suggested Usage: General use for antioxidant and detoxification function, take eight pumps per day (1,000 mg of Vitamin C and 50 mg of R-Lipoate). For advanced intermittent use, use up to 50 pumps per day (6,250 mg Vitamin C and 312.5 mg R-Lipoate) or more, in divided doses throughout the day. For detoxification protocols, especially with metal toxicities, build dosage gradually, starting from low doses, as they are tolerated. If strong detoxification reactions are observed, back off dosage. Children should start at approximately 1/4 of adult (two pumps per day) dosage and work up. For topical application, one pump can cover the face for a daily treatment, or use several pumps as a mask and leave on for 10–15 minutes; skin can be re-wetted and left for another 10 minutes before rinsing off excess.
Liposomal Glutathione: Quicksilver’s Phospholipid Encapsulation Etheric Delivery system protects glutathione from digestive enzymes that otherwise inhibit absorption of oral glutathione supplementation. In cell cultures, liposomal products have demonstrated over 100 times more efficiency for intracellular delivery than IV-based liposomal glutathione.
Quicksilver’s Liposomal Glutathione comes with a precision pump to accurately deliver 50 mg of reduced glutathione and 68 mg of injectable-grade essential phospholipids (derived from sunflower oil) per pump. The patent-pending process, plus a natural lemon flavoring, allows this product to be taken intra-orally for maximum absorption without the foul sulfur taste typical of liposomal glutathione products. The formula can be taken every 3–4 hours for even delivery throughout the day. One bottle delivers 100, 0.5 ml doses.
Quicksilver Liposomal Glutathione with Lemon Mint
Suggested Usage: For general antioxidant and detoxification protection, use eight pumps per day (400 mg glutathione). For advanced protection, use up to 20 per day (1,000 mg glutathione) or more, in divided doses throughout the day. For large doses, take two pumps at a time to allow for maximum oral absorption, and hold at least 30 seconds before swallowing. Children should start at approximately 1/4 of adult (two pumps per day) dosage and work up.
Liposomal Colorado Hemp Oil: This product uses non-THC (<0.3%) cannabidiol (CBD) from all-natural Colorado Hemp Oil. CBD is the non-psychoactive part of the industrial hemp plant. Quicksilver Scientific’s liposomal delivery of Nanoemulsified Colorado Hemp Oil far outpaces tinctures and is faster, stronger and more effective. Cannabidiol interacts with our body’s naturally occurring cannabinoid receptors to aid with pain relief and enhanced feelings of well being. The advanced technology behind this groundbreaking liquid delivery method makes for precise dosing and immediate effect.
Because of the known interaction of CBD with these cannabidiol receptors, much new research has focused on CBD’s receptor-mediated neuro-protective, antiemetic, and analgesic properties, and of its effect on mood and other aspects of mental health.
New research on gene transcription modulation offers an even deeper look into the biochemical mechanisms at work when ingesting CBD. Research in this vein has shown more than 1,000 genes that are differentially upregulated by CBD (a more than ten-fold increase than those affected by THC). In general, the effects increased cell stress responses—including antioxidant-defense and detoxification genes (mainly via EhRE/ARE-Nrf2 induction)—and downregulated many inflammation-mediating genes. These effects combined with CBDs NMDA-receptor-stabilizing effects, show great promise for its use in calming the neuro-inflammatory responses accompanying neurotoxic and chronic illness states.
Nanoemulsified Colorado Hemp Oil
Suggested Use: Take 1–4 pumps by mouth, holding for 30 seconds before swallowing. Repeat if needed. Four pumps contain 30 mg of Hemp Extract (aerial parts) and 12 mg of Phytocannabinoid Diols. There are 25 four-pump servings per container. Best taken on an empty stomach 10 minutes before meals. May be stirred into a small amount of water. Once opened, use within 60 days. Store at room temperature and away from light.
Liposomal NanoMojo (adaptogenic blend): Dr. Christopher Shade, PhD of Quicksilver Scientific, collaborated with master herbalist Dan Moriarty of Sun Horse Energy to create NanoMojo, a groundbreaking functional medicine product. By combining Moriarty’s unique adaptogenic formulation with Dr. Shade’s state-of-the-art liposomal encapsulation, they’ve overcome the limitations of poor oral adsorption and made the phytochemicals quickly available at the cellular level. This new innovative blend of adaptogens from around the world is maximized for effectiveness.
Adaptogens are non-toxic phytochemicals that help the body achieve homeostatic balance under adverse conditions that would typically be associated with sympathetic (fight or flight) reactions. They help regulate natural harmony, adrenal balance, and stress accommodation (resistance to stress). In fact, adaptogenic herbs have been used in Ayurvedic medicine for more than 4,000 years and Chinese medicine for nearly 3,000 years to increase energy (chi) and concentration.
Scientific literature reports that adaptogenic herbs play significant roles in decreasing markers of stress-activated protein kinases, cortisol, and nitric oxide. These markers indicate a lowered level of systemic stress and inflammation and decreased symptoms of an over-taxed adrenal system.
NanoMojo helps your body adapt to the various conditions that cause stress, something most of us experience daily. This liposomal formulation is the culmination of more than eight years of research and development. Not only is it effective, but it also tastes very good.
NanoMojo Liposomal Adaptogenic Blend
Directions: Take two pumps twice daily, or more. May be mixed into a small amount of water. Best taken on an empty stomach. Once opened, use within 60 days.
The advent of small liposomes means significantly greater uptake and assimilation of nutrients than ever before. This means you stand to benefit greatly from advanced intra-orally delivered nanoliposomal formulas like those developed by Quicksilver Scientific, Inc.
Health Products Distributors, Inc. recently decided to augment the variety of liposomal products we carry based upon the significant advancements of the technology during the last few years.
Among the benefits of using liposomes are that significantly higher levels of certain nutrients can be delivered directly to the cells where they are needed. In this article, I will discuss some of the recent scientific advances and new products associated with these advances.
Figure 1 – liposomal types
SMALLER IS SIGNIFICANTLY BETTER
In December 2015, I wrote a blog article on liposomes to introduce the liposomal products we began selling at that time. Unfortunately, the particle size of these original products are on the order of 500 nanometers (nm), and as such are not nearly as well absorbed as the much smaller liposomes that have recently been developed by Quicksilver Scientific.
Figure 1 gives an overview of current liposome types. These include multi-lamellar vesicles (MLV) that range in size from 300–5,000 nm and have more than one bilayer.
Large unilamellar vesicles (LUV) range in size from 100–300 nm. They have a single bilayer and a high trapped volume, but have lower thermodynamic stability and decreased uptake.
Small unilamellar vesicles (SUV) range in size from 20–100 nm. SUV have a long circulation half-life and better cellular accumulation. Small lipid particles have the fastest uptake kinetics and can participate in paracellular (between cells) transport. The nutritional liposome industry is moving toward the use of SUV.
Small liposomes (SUV) are drastically more efficient at intracellular delivery of encapsulated compounds. In a recent study with carefully sized liposomes, cellular uptake increased nine-fold as liposome size was decreased from 236 nm to 97 nm and was 34 fold higher at 64 nm (see Figure 2). This figure shows flow cytometry results (a measure of cellular uptake) for Caco-2 cells incubated with liposomes containing Dil-C18 at 15 min and 60 min intervals.
Figure 2 – Chart showing greatly enhanced absorption of liposomes as size decreases
HPDI CARRIES NEW LIPOSOMAL PRODUCTS
Our new liposomal product supplier currently is providing a wide range of products that have stable liposomes of about 50 nm. These products are bottled in such a way that they are taken by pumping (or squirting) the contents directly into your mouth (i.e., oral administration). This is an extremely clean method of dosing in which a few pumps of liposomal liquid can be rapidly taken or administered with no need for placing the product into separate glass of water or squeezing packets.
Because of the very small size much of the ingredients are absorbed through mucus membranes and into the system and cells extremely quickly (within seconds/minutes). In addition to the ingredients within the liposome, one gets significant amounts of phosphytidal choline into the cell membranes with a very beneficial effect on membrane function.
We are currently carrying the following Quicksilver Scientific liposomal products:
Ultimate Protector™ contains freeze dried cranberry, as well as components from 29 different fruits, vegetables, and herbs. Each of these ingredients contain substances that may be considered to be polyphenols, antioxidants, and Nrf2 activators. In this article I explore the ingredient strawberries, which is a component of VitaBerry Plus® from Futureceuticals.
VitaBerry® (N1023) is the trade name for a line of high ORAC blends of fruit powders and fruit extracts, exclusively available through FutureCeuticals.
VitaBerry® is a proprietary formula that combines wild bilberry and wild blueberry, cranberry, raspberry, strawberry, prune, cherry, and grape whole powders and extracts into lines of custom blends. High in fruit polyphenols, anthocyanins, proanthocyanins, ellagic acid, chlorogenic acid, resveratrol, and quinic acid, VitaBerry offers 6,000 ORAC units in a single gram.
VitaBerry® Plus (N81.3) combines the standard blend of VitaBerry® with resveratrol and quercetin to deliver a minimum of 12,000 ORAC units per gram.
HEALTH BENEFITS OF CRANBERRIES
Cranberries (Vaccinium macrocarpon) are native to the boggy regions of temperate and subalpine North America and Europe. Although Native Americans used them extensively, they were first cultivated in the U.S. in the early 19th century. Cranberries grow on viney plants belonging to the heath family Ericaceae that also includes blueberries, bilberries, huckleberries, and bearberries (Arctostaphylos uva ursi). Cranberries contain tannins, fiber, anthocyanins (and other flavonoids), and Vitamin C. Their tannins prevent bacteria from attaching to cells. Consequently, cranberries have been used against infections, including urinary tract infections. In addition, cranberries may be helpful in protecting against heart disease and stroke.
Cranberries are 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 cranberries.
Type of PhytonutrientSpecific Molecules
Phenolic Acids hydroxybenzoic acids including vanillic acids;
—Phenolic Acids (cont.) hydroxycinnamic acids inculding caffeic,
—Phenolic Acids (cont.) coumaric, cinnamic, and ferulic acid
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 against cancer, aging and neurological diseases, inflammation, diabetes, and bacterial infections.
Antioxidant compounds in cranberries including OPC’s, anthocyanidin flavonoids, cyanidin, peonidin and quercetin may prevent cardiovascular disease 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.
In 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.
Cranberry fruit has been reported to have high antioxidant effectiveness that is potentially linked to its richness in diversified polyphenolic content. The aim of the present study was to determine the role of cranberry polyphenolic fractions in oxidative stress (OxS), inflammation and mitochondrial functions using intestinal Caco-2/15 cells. The combination of HPLC and UltraPerformance LC®-tandem quadrupole (UPLC-TQD) techniques allowed us to characterize the profile of low, medium and high molecular mass polyphenolic compounds in cranberry extracts. The medium molecular mass fraction was enriched with flavonoids and procyanidin dimers whereas procyanidin oligomers (DP > 4) were the dominant class of polyphenols in the high molecular mass fraction. Pre-incubation of Caco-2/15 cells with these cranberry extracts prevented iron/ascorbate-mediated lipid peroxidation and counteracted lipopolysaccharide-mediated inflammation as evidenced by the decrease in pro-inflammatory cytokines (TNF-α and interleukin-6), cyclo-oxygenase-2 and prostaglandin E2. Cranberry polyphenols (CP) fractions limited both nuclear factor κB activation and Nrf2 down-regulation. Consistently, cranberry procyanidins alleviated OxS-dependent mitochondrial dysfunctions as shown by the rise in ATP production and the up-regulation of Bcl-2, as well as the decline of protein expression of cytochrome c and apoptotic-inducing factor. These mitochondrial effects were associated with a significant stimulation of peroxisome-proliferator-activated receptor γ co-activator-1-α, a central inducing factor of mitochondrial biogenesis and transcriptional co-activator of numerous downstream mediators. Finally, cranberry procyanidins forestalled the effect of iron/ascorbate on the protein expression of mitochondrial transcription factors (mtTFA, mtTFB1, mtTFB2). Our findings provide evidence for the capacity of CP to reduce intestinal OxS and inflammation while improving mitochondrial dysfunction.
Chemical characterization and chemo-protective activity of cranberry phenolic powders in a model cell culture. Response of the antioxidant defenses and regulation of signaling pathways
Oxidative stress and reactive oxygen species (ROS)-mediated cell damage are implicated in various chronic pathologies. Emerging studies show that polyphenols may act by increasing endogenous antioxidant defense potential. Cranberry has one of the highest polyphenol content among commonly consumed fruits. In this study, the hepato-protective activity of a cranberry juice (CJ) and cranberry extract (CE) powders against oxidative stress was screened using HepG2 cells, looking at ROS production, intracellular non-enzymatic and enzymatic antioxidant defenses by reduced glutathione concentration (GSH), glutathione peroxidase (GPx) and glutathione reductase (GR) activity and lipid peroxidation biomarker malondialdehyde (MDA). Involvement of major protein kinase signaling pathways was also evaluated. Both powders in basal conditions did not affect cell viability but decreased ROS production and increased GPx activity, conditions that may place the cells in favorable conditions against oxidative stress. Powder pre-treatment of HepG2 cells for 20 h significantly reduced cell damage induced by 400 μM tert-butylhydroperoxide (t-BOOH) for 2 h. Both powders (5–50 μg/ml) reduced t-BOOH-induced increase of MDA by 20% (CJ) and 25% (CE), and significantly reduced over-activated GPx and GR. CE, with a significantly higher amount of polyphenols than CJ, prevented a reduction in GSH and significantly reduced ROS production. CJ reversed the t-BOOH-induced increase in phospho-c-Jun N-terminal kinase. This study demonstrates that cranberry polyphenols may help protect liver cells against oxidative insult by modulating GSH concentration, ROS and MDA generation, antioxidant enzyme activity and cell signaling pathways.
Cranberry extract suppresses interleukin-8 secretion from stomach cells stimulated by Helicobacter pylori in every clinically separated strain but inhibits growth in part of the strains
It is known that cranberry inhibits the growth of Helicobacter pylori (HP). In human stomach, HP basically induces chronic inflammation by stimulating stomach cells to secrete interleukin (IL)-8 and other inflammatory cytokines, and causes stomach cancer, etc. The aim of this study was to investigate the inhibiting effects of cranberry on HP growth and IL-8 secretion from stomach cells induced by HP, using clinically separated HP strains. HP growth in liquid culture and on-plate culture was evaluated by titration after 2-day incubation and by agar dilution technique, respectively. For IL-8 experiments, MKN-45, a stomach cancer cell line, was incubated with HP for 24 h and IL-8 in the medium was assayed by ELISA. Cranberry suppressed growth of the bacteria only in six of the 27 strains. Meanwhile, it suppressed IL-8 secretion in all the strains. The results may suggest a possible role of cranberry in prevention of stomach cancer by reducing gastric inflammation.
Effects of cranberry powder on biomarkers of oxidative stress and glucose control in db/db mice
Increased oxidative stress in obese diabetes may have causal effects on diabetic complications, including dyslipidemia. Lipopolysccharides (LPS) along with an atherogenic diet have been found to increase oxidative stress and insulin resistance. Cranberry has been recognized as having beneficial effects on diseases related to oxidative stress. Therefore, we employed obese diabetic animals treated with an atherogenic diet and LPS, with the aim of examining the effects of cranberry powder (CP) on diabetic related metabolic conditions, including lipid profiles, serum insulin and glucose, and biomarkers of oxidative stress. Forty C57BL/KsJ-db/db mice were divided into the following five groups: normal diet + saline, atherogenic diet + saline, atherogenic diet + LPS, atherogenic diet + 5% CP + LPS, and atherogenic diet + 10% CP + LPS. Consumption of an atherogenic diet resulted in elevation of serum total cholesterol and atherogenic index (AI) and reduction of high density lipoprotein (HDL)-cholesterol. However, with 10% CP, the increase in mean HDL-cholesterol level was close to that of the group with a normal diet, whereas AI was maintained at a higher level than that of the group with a normal diet. LPS induced elevated serum insulin level was lowered by greater than 60% with CP (P < 0.05), and mean serum glucose level was reduced by approximately 19% with 5% CP (P > 0.05). Mean activity of liver cytosolic glutathione peroxidase was significantly increased by LPS injection, however it was reduced back to the value without LPS when the diet was fortified with 10% CP (P < 0.05). In groups with CP, a reduction in mean levels of serum protein carbonyl tended to occur in a dose dependent manner. Particularly with 10% CP, a reduction of approximately 89% was observed (P > 0.05). Overall results suggest that fortification of the atherogenic diet with CP may have potential health benefits for obese diabetes with high oxidative stress, by modulation of physical conditions, including some biomarkers of oxidative stress.
Cranberries are an important fruit full of polyphenols, anthocyanins, antioxidants, and Nrf2 activators that help to make Ultimate Protector such an outstanding nutritional supplement.