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ULTIMATE PROTECTOR+ INGREDIENTS – BLUEBERRY AND BILBERRY

Dr. Hank Liers, PhDUltimate Protector+ contains blueberry and bilberry extracts, as well as components from 12 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 will explore the ingredients blueberry and bilberry, which are components of SFB® – Standardized Fruit Blend from Ethical Naturals, Inc.

Ultimate Protector+ Includes Blueberry and Bilberry

Ultimate Protector+ Includes Bilberry and Blueberry

SFB® – Standardized Fruit Blend

SFB® is a proprietary formula that combines extracts from Grape, Cranberry, Pomegranate, Blueberry, Apple, Mangosteen, Bilberry, Chokeberry, and Goji Berry. High in fruit polyphenols, anthocyanins, proanthocyanins, catechins, ellagic acid, chlorogenic acid, resveratrol, and quinic acid. With its diverse blend, SFB® offers over 40–50% polyphenols as well as >9,000 ORAC units in a single gram.

Polyphenols, anthocyanins, and other plant components are powerful ingredients associated with a variety of areas of human health, including healthy aging, healthy glucose metabolism, cardiovascular health, and inflammation management.

HEALTH BENEFITS OF
BILBERRY AND BLUEBERRY

Bilberry is any of several Eurasian  species of low-growing shrubs in the genus Vaccinium, bearing edible, nearly black berries. The species most often referred to is Vaccinium myrtillus L., but there are several other closely related species. Bilberries are distinct from blueberries but closely related. Whereas the bilberry is native to Europe, the blueberry is native to North America.

The bilberry fruit is smaller than that of the blueberry, but with a fuller taste. Bilberries are darker in color, and usually appear near black with a slight shade of purple. While blueberry fruit pulp is light green in color, bilberry is red or purple, heavily staining the fingers, lips, and tongue of consumers eating the raw fruit. The color comes from diverse anthocyanins.

So-called wild (lowbush) blueberries, smaller than cultivated highbush ones, are prized for their intense color. “Wild” has been adopted as a marketing term for harvests of managed native stands of lowbush blueberries. The bushes are not planted or genetically manipulated, but they are pruned or burned every two years, and pests are “managed.” The content of polyphenols and anthocyanins in lowbush (wild) blueberries (V. angustifolium) exceeds values found in highbush cultivars.

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

Scientific Studies on the Antioxidant Effects of Bilberry and Blueberry

Databases of scientific studies (like the National Institutes of Health (NIH) PubMed database) contain thousands of up-to-date studies and abstracts about various Vaccinium species, including wild bilberry and wild blueberry (V. myrtillis and V. angustfolium, respectively).

We provide a few relevant scientific studies on the antioxidant effects of wild bilberry and wild blueberry.

In vitro anticancer activity of fruit extracts from Vaccinium species.

From: http://www.ncbi.nlm.nih.gov/pubmed/8693031

Abstract

Fruit extracts of four Vaccinium species (lowbush blueberry, bilberry, cranberry, and lingonberry) were screened for anticarcinogenic compounds by a combination of fractionation and in vitro testing of their ability to induce the Phase II xenobiotic detoxification enzyme quinone reductase (QR) and to inhibit the induction of ornithine decarboxylase (ODC), the rate-limiting enzyme in polyamine synthesis, by the tumor promoter phorbol 12-myristate 13-acetate (TPA). The crude extracts, anthocyanin and proanthocyanidin fractions were not highly active in QR induction whereas the ethyl acetate extracts were active QR inducers. The concentrations required to double QR activity (designated CDqr) for the ethyl acetate extracts of lowbush blueberry, cranberry, lingonberry, and bilberry were 4.2, 3.7, 1.3, and 1.0 microgram tannic acid equivalents (TAE), respectively, Further fractionation of the bilberry ethyl acetate extract revealed that the majority of inducer potency was contained in a hexane/chloroform subfraction (CDqr = 0.07 microgram TAE). In contrast to their effects on QR, crude extracts of lowbush blueberry, cranberry, and lingonberry were active inhibitors of ODC activity. The concentrations of these crude extracts needed to inhibit ODC activity by 50% (designated IC50) were 8.0, 7.0, and 9.0 micrograms TAE, respectively. The greatest activity in these extracts appeared to be contained in the polymeric proanthocyanidin fractions of the lowbush blueberry, cranberry, and lingonberry fruits (IC50 = 3.0, 6.0, and 5.0 micrograms TAE, respectively). The anthocyanidin and ethyl acetate extracts of the four Vaccinium species were either inactive or relatively weak inhibitors of ODC activity. Thus, components of the hexane/chloroform fraction of bilberry and of the proanthocyanidin fraction of lowbush blueberry, cranberry, and lingonberry exhibit potential anticarcinogenic activity as evaluated by in vitro screening tests.

Bilberry (Vaccinium myrtillus) anthocyanins modulate heme oxygenase-1 and glutathione S-transferase-pi expression in ARPE-19 cells.

From: http://www.ncbi.nlm.nih.gov/pubmed/17460300

Abstract

PURPOSE: To determine whether anthocyanin-enriched bilberry extracts modulate pre- or posttranslational levels of oxidative stress defense enzymes heme-oxygenase (HO)-1 and glutathione S-transferase-pi (GST-pi) in cultured human retinal pigment epithelial (RPE) cells.

METHODS: Confluent ARPE-19 cells were preincubated with anthocyanin and nonanthocyanin phenolic fractions of a 25% enriched extract of bilberry (10(-6)-1.0 mg/mL) and, after phenolic removal, cells were oxidatively challenged with H(2)O(2). The concentration of intracellular glutathione was measured by HPLC and free radical production determined by the dichlorofluorescin diacetate assay. HO-1 and GST-pi protein and mRNA levels were determined by Western blot and RT-PCR, respectively.

RESULTS: Preincubation with bilberry extract ameliorated the intracellular increase of H(2)O(2)-induced free radicals in RPE, though H(2)O(2) cytotoxicity was not affected. By 4 hours, the extract had upregulated HO-1 and GST-pi protein by 2.8- and 2.5-fold, respectively, and mRNA by 5.5- and 7.1-fold, respectively, in a dose-dependent manner. Anthocyanin and nonanthocyanin phenolic fractions contributed similarly to mRNA upregulation.

CONCLUSIONS: Anthocyanins and other phenolics from bilberry upregulate the oxidative stress defense enzymes HO-1 and GST-pi in RPE, suggesting that they stimulate signal transduction pathways influencing genes controlled by the antioxidant response element.

Berry anthocyanins suppress the expression and secretion of proinflammatory mediators in macrophages by inhibiting nuclear translocation of NF-κB independent of NRF2-mediated mechanism.

From: http://www.ncbi.nlm.nih.gov/pubmed/24565673

Abstract

The objectives of this study were to compare the anti-inflammatory effects of anthocyanins from blueberry (BBA), blackberry (BKA), and blackcurrant (BCA) and to determine the relationship between their antioxidant capacity and anti-inflammatory effect in macrophages. Major anthocyanins in BBA, BKA and BCA were malvidin-3-glucoside (16%), cyanidin-3-glucoside (98%) and delphinidin-3-rutinoside (44%), respectively. BKA showed higher total antioxidant capacity than BBA and BCA. RAW 264.7 macrophages were incubated with 0-20 μg/ml of BBA, BKA and BCA, and subsequently activated by lipopolysaccharide (LPS) to measure proinflammatory cytokine production. Interleukin 1β (IL-1β) messenger RNA (mRNA) levels were significantly decreased by all berry anthocyanins at 10 μg/ml or higher. Tumor necrosis factor α (TNFα) mRNA levels and secretion were also significantly decreased in LPS-treated macrophages. The levels of the repression were comparable for all berry anthocyanins. LPS-induced nuclear factor κB (NF-κB) p65 translocation to the nucleus was markedly attenuated by all of the berry anthocyanins. In bone marrow-derived macrophages (BMMs) from nuclear factor E2-related factor 2 wild-type (Nrf2(+/+)) mice, BBA, BKA and BCA significantly decreased cellular reactive oxygen species (ROS) levels with a concomitant decrease in IL-1β mRNA levels upon LPS stimulation. However, in the BMM from Nrf2(-/-) mice, the anthocyanin fractions were able to significantly decrease IL-1β mRNA despite the fact that ROS levels were not significantly affected. In conclusion, BBA, BKA and BCA exert their anti-inflammatory effects in macrophages, at least in part, by inhibiting nuclear translocation of NF-κB independent of the NRF2-mediated pathways.

Purified Anthocyanins from Bilberry and Black Currant Attenuate Hepatic Mitochondrial Dysfunction and Steatohepatitis in Mice with Methionine and Choline Deficiency

From: http://pubs.acs.org/doi/abs/10.1021/jf504926n

Abstract

The berries of bilberry and black currant are rich source of anthocyanins, which are thought to have favorable effects on non-alcoholic steatohepatitis (NASH). This study was designed to examine whether purified anthocyanins from bilberry and black currant are able to limit the disorders related to NASH induced by a methionine-choline-deficient (MCD) diet in mice. The results showed that treatment with anthocyanins not only alleviated inflammation, oxidative stress, steatosis and even fibrosis, but also improved the depletion of mitochondrial content and damage of mitochondrial biogenesis and electron transfer chain developed concomitantly in the liver of mice fed the MCD diet. Furthermore, anthocyanins treatment promoted activation of AMP-activated protein kinase (AMPK) and expression of peroxisome proliferator-activated receptor-gamma coactivator-1α (PGC-1α). These data provide evidence that anthocyanins possess significant protective effects against NASH and mitochondrial defects in response to a MCD diet, with mechanism maybe through affecting the AMPK/PGC-1α signaling pathways.

Effect of blueberry on hepatic and immunological functions in mice.

From: http://www.ncbi.nlm.nih.gov/pubmed/20382588

Abstract

Background: Conventional drugs used in the treatment and prevention of liver diseases often have side effects, therefore research into natural substances are of significance. This study examined the effects of blueberry on liver protection and cellular immune functions.

METHODS: To determine the effects of blueberry on liver protective function, male mice were orally administered blueberry (0.6 g/10 g) or normal saline for 21 days. Hepatic RNA was extracted by Trizol reagent, and the expression of Nrf2, HO-1, and Nqo1 was determined by real-time RT-PCR. Superoxide dismutase (SOD) and malondialdehyde (MDA) in liver homogenate were determined, and liver index was measured. To assess the effects of blueberry on cellular immune function, male mice received blueberry (0.4, 0.6, or 0.8 g/10 g) for 35 days, and the percentages of CD3+, CD4+, and CD8+ T lymphocyte subgroups in peripheral blood were detected by flow cytometry, the index of the thymus and spleen was measured, and lymphocyte proliferation in the spleen was determined by MTT assay.

RESULTS: Blueberry treatment significantly increased the expression of Nrf2, HO-1, and Nqo1, the important antioxidant components in the liver. Hepatic SOD in the blueberry group was higher and MDA was lower than that in the control group (P<0.05). Blueberry also increased the index of the spleen and enhanced the proliferation of lymphocytes of the spleen (P<0.05). The percentages of the CD3+ and CD4+ T lymphocyte subsets and the CD4+/CD8+ ratio were also increased by blueberry (P<0.05).

CONCLUSIONS: Blueberry induces expression of Nrf2, HO-1, and Nqo1, which can protect hepatocytes from oxidative stress. In addition, blueberry can modulate T-cell function in mice.

Anthocyanins: Janus Nutraceuticals Displaying Chemotherapeutic and Neuroprotective Properties

From: http://link.springer.com/chapter/10.1007/978-94-007-4575-9_21

Abstract

Anthocyanins are natural polyphenolic compounds widely distributed as pigments in many fruits and vegetables. In addition to displaying antioxidant properties, these nutraceuticals exhibit anti-inflammatory, anti-proliferative, and pro-apoptotic activities suggesting their potential as novel chemotherapeutic agents. Through cell cycle down-regulation, and context-specific pro-oxidant activity, anthocyanins induce cytotoxicity in cancer cells in vitro and in vivo. Specifically, via regulation of the Bcl-2 protein family and induction of caspase-dependent or caspase-independent apoptotic pathways, anthocyanins inhibit the growth of cancers by inducing cell death. Moreover, by modulating the activities of specific kinases and proteases, including (but not limited to) cyclin-dependent kinases, mitogen-activated protein kinases, matrix metalloproteases, and urokinase-type plasminogen activators, anthocyanins induce apoptosis, inhibit motility, and suppress invasion of cancer cells. In marked contrast to their effects in cancer cells, we have found that anthocyanins display significant anti-apoptotic activity in neurons. Antioxidant properties of these nutraceuticals, particularly at the level of the mitochondria, appear to underlie their neuroprotective effects. The opposing effects of anthocyanins on cancer cells and neurons suggest that these nutraceuticals are promising candidates for development as either chemotherapeutic agents or novel neuroprotective compounds for the treatment of cancers or neurodegenerative diseases, respectively.

Recent Research on Polyphenolics in Vision and Eye Health

From: http://pubs.acs.org/doi/abs/10.1021/jf903038r#end-1

Abstract

A long-standing yet controversial bioactivity attributed to polyphenols is their beneficial effects in vision. Although anecdotal case reports and in vitro research studies provide evidence for the visual benefits of anthocyanin-rich berries, rigorous clinical evidence of their benefits is still lacking. Recent in vitro studies demonstrate that anthocyanins and other flavonoids interact directly with rhodopsin and modulate visual pigment function. Additional in vitro studies show flavonoids protect a variety of retinal cell types from oxidative stress-induced cell death, a neuroprotective property of significance because the retina has the highest metabolic rate of any tissue and is particularly vulnerable to oxidative injury. However, more information is needed on the bioactivity of in vivo conjugates and the accumulation of flavonoids in ocular tissues. The direct and indirect costs of age-related vision impairment provide a powerful incentive to explore the potential for improved vision health through the intake of dietary polyphenolics.

Bilberry Extracts Induce Gene Expression Through the Electrophile Response Element

From: http://www.tandfonline.com/doi/abs/10.1207/s15327914nc5401_11#.VLK6LVqBO24

Abstract

A number of genes important for detoxification and antioxidant defense induced by mild stress generated by, for example, physical activity/exercise, caloric restriction, or alcohol may provide health benefits by causing the organism to mount such a defense response. More recently, induction of these defenses has also been attributed to phytochemicals or secondary metabolites from dietary plants. Many polyphenols, which constitute a large fraction of these phytochemicals, increase cellular levels of antioxidants, such as glutathione and other components of the detoxification systems, via the transactivation of genes containing electrophile response elements (EpREs) within their promoters. One such gene, γ-glutamylcysteine synthetase, has previously been shown to be positively regulated by quercetin, a flavonoid found in high concentrations in onions, apples, and bilberries through EpRE transactivation. As a further step, we have investigated whether bilberries and quercetin have the ability to induce transcription of Fos-related antigen 1 (Fra-1), which contains two EpREs in its promoter. Fra-1 is a member of the activator protein 1 (AP-1) family of transcription factors and, due to the lack of transactivation domain Fra-1, can suppress activation of AP-1. We present results demonstrating that extracts from bilberries, and the flavonoid quercetin, abundant in bilberries, induce the fra-1 promoter and the cellular content of Fra-1 mRNA. We further provide evidence that this induction is mediated through EpREs.

Bilberry (Vaccinium myrtillus)

From: http://www.sigmaaldrich.com/life-science/nutrition-research/learning-center/plant-profiler/vaccinium-myrtillus.html

Synonyms / Common Names / Related Terms
Airelle, anthocyanins, Bickbeere (German), bilberry leaf, black whortle, Blaubeere (Dutch), blaubessen, bleaberry, blueberry, blueberry leaf, bogberry, bog bilberry, burren myrtle, cranberry, dwarf bilberry, dyeberry, Ericaceae (family), European blueberry, Heidelbeere (Dutch), Heidelbeereblatter, heidelberry, huckleberry, hurtleberry, lingonberry, lowbush blueberry, Mirtillo nero (Italian), Myrtilli folium, Myrtilli fructus, Myrtilus niger Gilib., Optiberry, resveratrol, sambubiosides, trackleberry, Vaccinium angulosum Dulac, Vaccinium montanum Salibs., Vaccinium myrtillus anthocyanoside extract, VMA extract, VME, whortleberry, wineberry
Mechanism of Action

Pharmacology:

  • Constituents: Bilberry contains several compounds that have demonstrated biological activity. The main chemicals contained in bilberry extract have been shown to be: anthocyanins30,31, flavonoids, hydroquinone, oleanolic acid, neomyrtillin, sodium, tannins, and ursolic acid17,20,32,33,34. Bilberry also contains resveratrol.28,29 The anthocyanosides, tannins, and flavonoids have been of particular scientific interest. Flavonoids have been shown in vitro to possess a number of biological properties, including inhibition of prostacyclin synthesis, reduction of capillary permeability and fragility, free radical scavenging, inhibition of a wide range of enzymes, impairment of coagulation and platelet aggregation, and anticarcinogenicity.33,5
  • Mechanism of action: Anthocyanins and other phenolics from bilberry upregulate the oxidative stress defense enzymes heme-oxygenase-1 and glutathione S-transferase-pin cultured human retinal pigment epithelial cells, suggesting that they stimulate signal transduction pathways, influencing genes controlled by the antioxidant response element.30
  • Antibacterial effects: In an in vitro study using Staphylococcus aureus, Staphylococcus aureus Oxford, Enterococcus faecalisBacillus subtilis, and Escherichia coli, an aqueous extract of bilberry leaves had a MIC of 12.7-17.8mg/mL and an aqueous extract of bilberry fruit had a MIC of 15.4-30.7mg/mL.24
  • Anticarcinogenic effects: In an in vitro study, anthocyanin-rich extracts from bilberry (Vaccinium myrtillus L.) inhibited the growth of a colon cancer cell line.6
  • Bomser et al. screened fruit extracts of bilberry for potential anticarcinogenic compounds by a combination of fractionation and in vitro testing of their ability to induce the Phase 2 xenobiotic detoxification enzyme quinone reductase (QR) and to inhibit the induction of ornithine decarboxylase (ODC), the rate-limiting enzyme in polyamine synthesis, by the tumor promoter phorbol 12-myristate 13-acetate (TPA).5 The crude extracts, anthocyanin, and proanthocyanidin fractions were not found to be highly active in Phase 2 xenobiotic detoxification enzyme quinone reductase (QR) induction, whereas the ethyl acetate extracts were active QR inducers. The concentrations required to double QR activity (designated CDqr) for the ethyl acetate extracts of bilberry were 1.0mcg tannic acid equivalents (TAE). Further fractionation of the bilberry ethyl acetate extract revealed that the majority of inducer potency was contained in a hexane/chloroform subfraction (CDqr = 0.07mcg TAE). The anthocyanidin and ethyl acetate extracts of bilberry were either inactive or relatively weak inhibitors of ornithine decarboxylase (ODC) activity. The authors concluded that components of the hexane/chloroform fraction of bilberry exhibit potential anticarcinogenic activity, as evaluated by in vitro screening tests.
  • Antihyperglycemic effects: In normal and depancreatized dogs, oral administration of bilberry leaves reduced hyperglycemia, even when the glucose was injected intravenously concurrently.15,16
  • Antioxidant effects: Bilberry contains anthocyanosides that are flavonoid derivatives of anthocyanins (the blue, red, or violet pigments found in many berry varieties), which are closely related in structure and activity to flavonoids17 and possess free radical scavenging/antioxidant properties. Antioxidant properties have been attributed to bilberry based on in vitro studies.1,2,34
  • Antiplatelet activity: In a clinical study of 30 subjects with normal platelet aggregation, 480mg of Myrtocyan® (Vaccinium myrtillus anthocyanins) daily, 3g of ascorbic acid daily, or both treatments all reduced platelet aggregation after 30 and 60 days.11 Bilberry anthocyanins reduced platelet aggregation more than ascorbic acid alone, but bilberry anthocyanins and ascorbic acid together were the most effective. Also, in in vitro studies, anthocyanins extracted from bilberry have inhibited platelet aggregation.13,14,10,12
  • Flavonoids have been shown in vitro to inhibit prostacyclin synthesis. In one animal model, Vaccinium myrtillus anthocyanosides were studied for their effects on prostacyclin-like activity in rat arterial issue.7
  • Antiproliferative effects: According to one laboratory study, anthocyanins were the predominant phenolic compounds in bilberry extracts.31 Compared to other plants with anthocyanins, such as black currant or lingonberry, cell growth inhibition was greater for bilberry than other plants studied. The pro-apoptosis marker, Bax, was increased 1.3-fold in bilberry-treated cells, whereas the pro-survival marker, Bcl-2, was detected only in control cells. The results demonstrated that bilberry and other berry extracts containing anthocyanins inhibited cancer cell proliferation, mainly via the p21WAF1 pathway.
  • Antiulcer effects: In an animal study, large doses of cyanidin chloride from bilberry significantly increased gastric mucosal release of prostaglandin E2.19 In animal models of gastric ulcers, cyanidin chloride showed antiulcer activity.26,8
  • Astringent effects: Bilberry contains tannins that have been used medicinally as astringents and to treat diarrhea.
  • Connective tissue stabilizing effects: An in vitro study has suggested that anthocyanosides appear to stabilize connective tissue by enhancing collagen synthesis, inhibiting collagen degradation, and enhancing collagen cross linking.35 In contrast, Boniface et al. found a significant decrease in connective tissue synthesis (collagen and glycoproteins) in gingival tissue samples of 12 adult diabetics treated with 600mg of anthocyanosides daily for two months.36
  • Hepatoprotective activity: In an animal study, anthocyans exerted a protective effect on liver cells.27
  • Hyperglycemic effects: In an oral glucose tolerance test in healthy rats, an alcoholic extract of Vaccinium myrtillus leaves increased serum glucose levels compared to controls.25
  • Hypotensive effects: Bilberry has been theorized to potentially drop blood pressure, based on pre-clinical evidence of vascular smooth muscle-relaxing properties.21,22,23
  • Anthocyanoside extracts have been shown to have smooth muscle-relaxing activity, which may account for their purported effects in one series of women with dysmenorrhea.18 Bioflavonoids and extracts of anthocyanosides (such as those present in bilberry) have been shown to relax vascular smooth muscles in experimental models, possibly via stimulation of prostaglandins.21,22,23
  • Intracellular signaling effects: Anthocyanosides have been shown to inhibit cAMP phosphodiesterase, which is involved in intracellular signal transduction pathways.8
  • Ocular effects: Anthocyanosides have been shown to exert direct effects on the retina, including the alteration of local enzymatic reactions and enhancement of the recovery of rhodopsin.9 The multi-ingredient product Mirtogenol (Pycnogenol® – French maritime pine bark extract and Mirtoselect® – standardized bilberry extract) has been reported to lower intraocular pressure and improve ocular blood flow.37
  • Smooth muscle relaxant effects: Anthocyanoside extracts have been shown to have smooth muscle-relaxing activity, which may account for their purported effects in one series of women with dysmenorrhea.18 Bioflavonoids and extracts of anthocyanosides (such as those present in bilberry) have been shown to relax vascular smooth muscles in experimental models, possibly via stimulation of prostaglandins.21,22,23
  • Vasoprotective effects: Flavonoids have been shown in vitro to reduce capillary permeability and fragility. Anthocyanosides have been studied for their potential protective effect in disorders due to abnormal capillary fragility.33

Pharmacodynamics/Kinetics:

  • There are limited data regarding the pharmacodynamics and kinetics of Vaccinium myrtillus (bilberry) anthocyanosides (VMA). In one animal study, bilberry anthocyanosides were rapidly distributed after intra-peritoneal injection and intravenous administration.38 In another animal study, bilberry anthocyanosides were found to be eliminated via the bile and urine with a modest level of liver extraction.32
  • Bioavailability in animals is low. Following oral doses in rats, plasma levels of VMA reached a peak at 15 minutes and declined rapidly within two hours, and the absolute bioavailability was 1.2% of the administered dose.38 The gastrointestinal absorption of VMA was 5% of the administered dose. Another study found a differential affinity of VMA for certain tissues (especially skin and kidney).20 This suggests that different tissues may have more persistent local concentrations.
References:

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  5. Bomser, J., Madhavi, D. L., Singletary, K., and Smith, M. A. In vitro anticancer activity of fruit extracts from Vaccinium species. Planta Med 1996;62(3):212-216.
  6. Zhao, C., Giusti, M. M., Malik, M., Moyer, M. P., and Magnuson, B. A. Effects of commercial anthocyanin-rich extracts on colonic cancer and nontumorigenic colonic cell growth. J Agric Food Chem  10-6-2004;52(20):6122-6128. 15453676
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  24. Brantner, A. and Grein, E. Antibacterial activity of plant extracts used externally in traditional medicine. J Ethnopharmacol 1994;44(1):35-40. 7990502
  25. Neef H, Declercq P, and Laekeman G. Hypoglycaemic activity of selected European plants. Phytotherapy Research 1995;9:45-48.
  26. Cristoni, A. and Magistretti, M. J. Antiulcer and healing activity of Vaccinium myrtillus anthocyanosides. Farmaco [Prat] 1987;42(2):29-43. 3582621
  27. Mitcheva, M., Astroug, H., Drenska, D., Popov, A., and Kassarova, M. Biochemical and morphological studies on the effects of anthocyans and vitamin E on carbon tetrachloride induced liver injury. Cell Microbiol 1993;39(4):443-448. 8329983
  28. Lyons, M. M., Yu, C., Toma, R. B., Cho, S. Y., Reiboldt, W., Lee, J., and van Breemen, R. B. Resveratrol in raw and baked blueberries and bilberries. J Agric Food Chem  9-24-2003;51(20):5867-5870. 13129286
  29. Rimando, A. M., Kalt, W., Magee, J. B., Dewey, J., and Ballington, J. R. Resveratrol, pterostilbene, and piceatannol in vaccinium berries. J Agric Food Chem 7-28-2004;52(15):4713-4719. 15264904
  30. Milbury, P. E., Graf, B., Curran-Celentano, J. M., and Blumberg, J. B. Bilberry (Vaccinium myrtillus) anthocyanins modulate heme oxygenase-1 and glutathione S-transferase-pi expression in ARPE-19 cells. Invest Ophthalmol Vis Sci 2007;48(5):2343-2349. 17460300
  31. Wu, Q. K., Koponen, J. M., Mykkanen, H. M., and Torronen, A. R. Berry phenolic extracts modulate the expression of p21(WAF1) and Bax but not Bcl-2 in HT-29 colon cancer cells. J Agric Food Chem 2-21-2007;55(4):1156-1163. 17243699
  32. Lietti, A. and Forni, G. Studies on Vaccinium myrtillus anthocyanosides. II. Aspects of anthocyanins pharmacokinetics in the rat. Arzneimittelforschung  1976;26(5):832-835. 989354
  33. Mian E. Anthocyanosides and microvessel walls: new findings on the mechanism of action of their protective effect in syndromes due to abnormal capillary fragility. Minerva Med 1977;68(52):3565-3581.
  34. Marcollet M, Bastide P, and Tronche P. Effet angio-protecteur des anthocyanosides de Vaccinium myrtillus odjective vis a vis de la liberation de la lactate deshydrogenase (LDH) et de ses isoenzymes cardiaques chez le rat soumis a une epreuve de nage. C R Soc Biol  1970;163:1786.
  35. Jonadet, M., Meunier, M. T., Bastide, J., and Bastide, P. [Anthocyanosides extracted from Vitis vinifera, Vaccinium myrtillus and Pinus maritimus. I. Elastase-inhibiting activities in vitro. II. Compared angioprotective activities in vivo]. J Pharm Belg 1983;38(1):41-46. 6553084
  36. Boniface, R. and Robert, A. M. [Effect of anthocyanins on human connective tissue metabolism in the human]. Klin Monatsbl Augenheilkd  1996;209(6):368-372. 9091714
  37. Steigerwalt, R. D., Gianni, B., Paolo, M., Bombardelli, E., Burki, C., and Schonlau, F. Effects of Mirtogenol on ocular blood flow and intraocular hypertension in asymptomatic subjects. Mol Vis  2008;14:1288-1292. 18618008
  38. Morazzoni, P., Livio, S., Scilingo, A., and Malandrino, S. Vaccinium myrtillus anthocyanosides pharmacokinetics in rats. Arzneimittelforschung  1991;41(2):128-131. 2043174

BLUEBERRY & BILBERRY SUMMARY

Wild bilberries and wild blueberries are important fruits full of polyphenols, anthocyanins, antioxidants, and Nrf2 activators that help to make Ultimate Protector+ such an outstanding nutritional supplement.

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IRENA OSSOLA UPDATE – ROLE OF SUPPLEMENTS IN PROFESSIONAL CYCLING

Irena Ossola pro cyclist nutritional supplementsHPDI’s sponsored athlete Irena Ossola has been a bike tour leader in Italy this summer and fall. During that time, she scaled back her nutritional supplement regimen. This is partly because the summer and fall period is one of rest from high-intensity competitive bike training—and because her training for the new racing season has not yet begun. However, she recorded her observations regarding nutritional supplements. She concludes they are important whether or not she is actively training for races. – editor

Irena Ossola

I have been working like a maniac and nonstop since I arrived in Italy for my bike touring job at the end of August. However, I am feeling good and recovering well and happy to move forward for next year in training. I am starting to really look forward to getting in some hard solid winter training now and especially being in Tucson will be amazing!! I can’t wait to get back into my regular training regime. On another note, I’ve recorded some observations during my time in Italy about my nutrition and vitamins.

Beginning August:

“As I am now at the beginning of my touring/working season, I like to use this time as my sort of “off time” for supplements. Regarding vitamins and other nutritional supplements, I have found in the past that I have trouble staying on schedule and taking them while working. I feel that my nutrition is still adequate as I eat vegetables and meat and other necessary things for the amount of effort and activity I am putting my body through. Yet, I also know I will feel the difference without a constant flow of vitamins and supplements from Health Products Distributors, Inc.”

Beginning September:

“Now that I am in my moment of break and I’ve been working constantly for about a month, I must stay that I have also not been taking vitamins for a couple weeks and I can definitely feel the difference. Especially in my diet when I am not eating as healthy (as I do when training) or being as consistent with consuming vegetables.

I notice a lack of energy when I am working and lack of intensity on the bike when I’m riding. This is fine for now, and a good test for me as during this time I do not need a high-intensity effort while riding and it is a good test of my energy levels to see the contrast while I’m working compared to training.

I will begin taking some supplements again regularly which I think will help and will also demonstrate the necessity to have a regular schedule of nutritional supplements even when my work and travel schedule is so busy.”

Beginning October:

“Boy do I feel the difference! Since I have been regularly taking supplements again I can feel my energy going up and my willingness to push more and have more intensity on the bike. I feel the difference in my regular diet as well as I feel more motivated to eat healthy. This is a big contrast and difference I can see from the period when I was taking supplements to when I stopped and now again to taking them. This shows how big the influence of nutritional supplementation is for my body.

I will continue taking my vitamins and being active while working and also eating a healthy diet to maintain my energy levels and physical ability. I am so busy while working that supplements are often hard to take while changing hotels or setting things up for the day. But if I have my vitamin bag and make sure to keep it somewhere easily accessible, then I am more willing to take them and can easily.

It is great to be working so closely with an amazing company like Health Products Distributors, Inc. where I can do this sort of test to see the differences. It shows a huge difference in their products compared to just food and how they affect my body. I have been taking Mighty Multi-Vite!, Ultimate Protector, Essential Fats Plus E, and Myo-Mag.

The supplements are amazing and I LOVE them and again I cannot wait to return to my competitive training this winter in Tucson.” ~

==

Editor’s notes: Irena primarily takes HPDI Foundational Supplements which are the base or core of a nutritional supplement program. Foundational supplements include a high-potency multivitamin (Hank & Brian’s Mighty Multi-Vite!™), vitamin C/antioxidant formulas (Ultimate Protector Nrf2 activator formula), essential fats (Essential Fats Plus E), and Rejuvenate! high-RNA superfoods (Rejuvenate! Original Greens, Rejuvenate! PLUS, and Rejuvenate! Berries & Herbs). She also takes other HPDI formulas like Myo-Mag (magnesium formula), pH Adjust alkalinizing formula, Warrior Mist (topical pain reliever), and other formulas depending on her needs.

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OMEGA-3 ESSENTIAL FATS REMAIN “ESSENTIAL” – A REBUTTAL FROM OMNS

Fred Liers PhD omega-3 essential fats plus e EFA formulaOmega-3 essential fatty acids (EFA) are critically important for health. That is the reason we at HPDI include them in our foundational supplements system in the form of our Essential Fats Plus E formula. Essential Fats Plus E provides a balanced ratio of 4:1 omega-3 EPA to omega-6 GLA fatty acids proven to optimally support health.

As important as Omega-3 fats are in good health, various studies conclude they are of little value. In order to help clarity the fallacies found in such studies, this month we re-print the recent article “Omega 3 Fatty Acids and Cardiovascular Disease” from the Orthomolecular News Service (OMNS).

BACKGROUND

Essential fats including Omega-3 and Omega-6 are so important to health that we consider them as foundational or “core” to basic nutrition as multivitamins, antioxidants/vitamin C formulas, and high-RNA superfoods, like Rejuvenate! Plus.

Many of today’s health problems relate to deficiencies in Omega-3 essential fatty acids rather than overabundance of it. It makes sense for everyone to supplement their diets with at least a minimum amount of essential fats. This is addition to consuming foods high in Omega-3 (and Omega-6) essential fats, including leafy greens, nuts, seeds, and seed oils. Also, small amounts of wild-caught fish from clean waters. Preferably these fish would come from low on the food chain, such as sardines, herring, or young mackerel, for example.

In December 2107, my father Hank Liers, PhD, wrote “The Truth about Essential Fatty Acids.” In his article, he delves into detail about why essential fatty acids are critical for health.

The diagram below from Dr. Hank’s article shows in detail the pathways for the production and use of fatty acids in the body. In the figure the metabolic pathways (running left to right) for four fatty acids types are shown (top – Omega-3, second – Omega-6, third – Omega-9, bottom – Omega-7). Notice that only the omega-3 and omega-6 oils are considered to be essential fatty acids because they cannot be made in the body. This means they must come from food.

omega-3 fats omega-6 fats

Furthermore, an additional diagram from Dr. Hank’s article shown below provides details of the omega-6 and omega-3 pathways. Pathway specifics indicate key eicosanoids (series 1 prostaglandins [anti-inflammatory], series 2 prostaglandins [pro-inflammatory], and series 3 prostaglandins [anti-inflammatory]), oil sources, and important nutrient cofactors that are needed for the reactions to take place.

omega-3 fats omega-6 fats

In particular, Dr. Hank discusses how superior benefits to health result from a balanced 4:1 ratio between Omega-3 eicosapentanoic acid (EPA) fatty acids and Omega-6 gamma linoleic acid (GLA).

Below we list some of the functions and benefits obtained when by diet or supplementation the correct ratios and amounts of essential fatty acids are consumed.

• Regulate steroid production and hormone synthesis
• Regulate pressure in the eyes, joints, and blood vessels
• Regulate response to pain, inflammation, and swelling
• Mediate Immune Response
• Regulate bodily secretions and their viscosity
• Dilate or constrict blood vessels
• Regulate smooth muscle and autonomic reflexes
• Are primary constituents of cellular membranes
• Regulate the rate at which cells divide
• Necessary for the transport of oxygen from the red blood cells to tissues
• Necessary for proper kidney function and fluid balance
• Prevent red blood cells from clumping together
• Regulate nerve transmission

Dr. Hank also discusses the fallacy of thinking that supplemental Omega-3 fats alone are sufficient to produce health. That is, despite the relative lack of Omega-3 essential fats and the prevalence of Omega-6 fats in modern diets, it is nevertheless the forms (EPA and GLA)—and the critical 4:1 ratio between them—that makes the difference in how they act synergistically for health. The result of Hank’s scientific understanding of essential fatty acids has resulted in his formulation of a balanced EFA product, Essential Fats Plus E.

Orthomolecular Medicine News Service Article “Omega 3 Fatty Acids and Cardiovascular Disease”

Regarding the Orthomolecular Medicine News Service article “Omega 3 Fatty Acids and Cardiovascular Disease” (republished below) rebutting the “Cochrane Database of Systematic Reviews” which relies on so-called “Evidence Based Medicine” (EBM) to distort truth on Omega-3 essential fatty acids, the fact that Omega-3 fats are under such false attack represents a huge disservice to the public.

While essential fatty acids may not generate profits for corporations—and in fact may lead to improved health outcomes that threaten the use of chemicals and drugs—essential fats nevertheless remain foundational for health.

Above we have shown the important reasons Omega-3 fats and other essential fatty acids are scientifically termed “essential.” And why people continue taking essential fats, and giving them to their families and children, for supporting health and well-being. Primary among these reasons is that you cannot be healthy without them. Hence, they are essential. Why believe anyone who says otherwise?

The bottom line: Omega-3 essential fatty acids are critical for health. Supplementing the diet with them is a good idea for nearly everyone. This is especially true because typical diets are proven to be most deficient in Omega-3 among essential fats.

Below we re-print in full the recent article “Omega 3 Fatty Acids and Cardiovascular Disease” from the Orthomolecular News Service (OMNS) for the benefit of our HPDI blog readers. ~

===

FOR IMMEDIATE RELEASE
Orthomolecular Medicine News Service, Aug 6, 2018

Omega-3 Fatty Acids and Cardiovascular Disease

Commentary by Damien Downing, MBBS, MSB and Robert G. Smith, PhD

The Cochrane Database of Systematic Reviews has just updated its own review: Omega-3 fatty acids for the primary and secondary prevention of cardiovascular disease [1]. Here’s our take on it.

Michael Pollan, the brilliant food writer, reckoned you could sum up what to do about nutrition and diets in 7 words; “Eat food, not too much, mostly plants.” That sums up both what’s best for humans and what’s best for the planet.

We reckon you can sum up what’s wrong with evidence-based medicine (EBM) in 10 words; “Evidence is a waste of data; systematic reviews are palimpsests.” You can use that as a knife to quickly dissect this study.

There are many things wrong with this review. Somebody’s PR department has spun the review’s “no clear evidence of benefit” into “evidence of no benefit” – absence of evidence becoming evidence of absence. And clearly the media were entirely happy to take that one and run with it.

Systematic reviews are palimpsests

What’s a palimpsest? Back when things got written on vellum, an animal skin, not on paper, you didn’t throw it away; you recycled it and wrote over the original. It was called a palimpsest.

A systematic review gives an opportunity to write over the conclusions of a whole list of papers with your new version of the truth. You do that by the way that you select and exclude them.

For instance there was a meta-analysis (that’s a systematic review with more numbers) in 2005 that concluded that vitamin E supplements significantly increased the risk of death [2]. The way they did that was to rule out any study with less than 10 deaths – when fewer deaths was exactly the outcome they were supposed to be looking for.

The reason they gave for doing that was “because we anticipated that many small trials did not collect mortality data.” We’re not buying it; they used it as a trick to enable them to get the negative result they wanted – to over-write the findings of a long list of original studies.

And here we have authors doing the very same thing in this omega-3 study – and upping the ante slightly. Now the threshold is 50 deaths. Fewer than that and your study is ruled out of the final, supposedly least biased, analysis . . on the grounds that it’s more biased.

We don’t know how they could keep a straight face while saying (our interpretation); “The studies with fewer deaths showed more benefit from omega-3s, so we excluded them.” At least that’s what happened back in 2004 when the first version of this came out.[3]

But this is the 8th update (we think) and they no longer bother to tell you about what they included or excluded in detail, so we can only assume that if they had changed that exclusion they would have told us.

The weird thing is that they are allowed to do it. Nutrition researcher Dr. Steve Hickey has shown that in systematic reviews there is generally control for bias in the included studies, but none for bias in the actual review and its authors.[4,5]

They found not one example of adequate blinding among 100 Cochrane reviews (like this one); they could all be palimpsests. Do we know that they are fake? No, but it doesn’t matter: what we do know is that we can’t trust them. Nor can we trust this Cochrane review. Things haven’t changed since 2004.

Evidence is a waste of data

Evidence is what lawyers and courts use to find someone Guilty or Not Guilty, and we all know how that can go wrong. It’s a binary system: you’re either one or the other. But at least if you’re on trial all the evidence should be about you and whether you did the crime.

In EBM the evidence is all about populations, not about individuals. When a doctor tells you “There’s a 1 in 3 chance this treatment will work” he is required to base that on big studies, or even systematic reviews. You don’t, and you can’t, know what that means for you because very likely you don’t fit the population profile.

As Steve Hickey (again) said, the statistical fallacy underlying all this states that you have one testicle and one ovary – because that’s the population average! The authors of this study update started off with about 2100 papers that looked relevant. They then excluded 90 per cent of them for various reasons – some of them good reasons, some not.

A smarter way to work would be to data-mine them and look for useful information about sub-groups and sub-effects in all the papers. Is there a particular reason omega-3s might work for you and not for others? Perhaps you can’t stand fish, or are allergic to them, and so are deficient in omega-3s.

But the review system doesn’t allow it, it insists on overall conclusions (about populations), and that’s a colossal waste of data. It also confounds the overall finding of the review – it biases it in fact.

Here’s an example: while most subgroups that made it to the final analysis showed a small reduction in risk from taking omega-3s in one form or another (pills, food, whatever), those who got it from supplemented foods, which we understand means stuff like margarine with added omega-3, showed a 4.3-fold death risk increase!

The problem here is that the effects of omega-3 fatty acids cannot be studied alone as if they were a drug. What counts are all the other components of the diet that affect a person’s health.

Processed foods and drinks that contain many unhealthy ingredients can’t be made healthy by adding small doses of vitamins, minerals, and omega-3 fatty acids. In fact, many processed foods that contain small doses of vitamins and other essential nutrients are unhealthy because they contain large doses of sugar, salt, and harmful ingredients such as preservatives, dyes, and other non-food items.

Why lipids are so important

Part of the problem is that lipids are truly complicated, and not many people, patients, doctors or even scientists, understand them well. You need a good understanding of lipid metabolism to appreciate the difference in metabolism and impact between alpha-linolenic acid (ALA, in food such as oily fish) and extracted oils such as EPA and DHA that are only found at high levels in omega-3 supplements.

At these levels they are effectively new to nature; nobody, indeed no mammal, was exposed to really high doses of DHA until we invented fish oil supplements [6]. Miss that fact and you miss the difference between having people eat fresh oily fish or just using omega-3 margarine!

We know from a variety of studies that a diet containing generous portions of green leafy and colorful vegetables and fruits, moderate portions of eggs, fish, and meat, and supplements of adequate doses of essential nutrients (vitamins and minerals) is effective at lowering the risk for cardiovascular disease.

Adequate doses of both omega-3 (in flax oil, walnuts, fish) and omega-6 (in seed oils such as canola, soybean, peanut) fatty acids are essential for health. Although essential, omega-6 fatty acids are thought to contribute to inflammation throughout the body whereas omega-3 fatty acids are anti-inflammatory.

Omega-3 fatty acids are essential for most body organs including the brain but are found in lower levels than omega-6 fatty acids in most vegetables. Risk for cardiovascular disease can be lowered by adequate doses of vitamins C (3,000-10,000mg/d), D (2,000-10,000 IU/d), E (400-1,200 IU/d), and magnesium (300-600 mg/d) in addition to an excellent diet that includes an adequate dose of omega-3 fatty acids.[7]

(Dr. Damien Downing is a specialist physician practicing in London, and President of the British Society for Ecological Medicine. Robert G. Smith is a physiologist and Research Associate Professor at the University of Pennsylvania Perelman School Of Medicine.)

 

References:

1. Abdelhamid, A, Brown TJ, Brainard JS, et al., (2018) Omega 3 fatty acids for the primary and secondary prevention of cardiovascular disease. Cochrane Database of Syst Rev. 7:CD003177. https://www.ncbi.nlm.nih.gov/pubmed/30019766
http://cochranelibrary-wiley.com/doi/10.1002/14651858.CD003177.pub3/abstract

2. Miller ER, Pastor-Barriuso R, Dalal D, et al., (2005) Review Meta-Analysis?: High-Dosage Vitamin E Supplementation May Increase. Annals of Internal Medicine, 142(1), pp.37-46. Available at: http://annals.org/article.aspx?articleid=718049.

3. Hooper L, Thompson RL, Harrison RA, et al.. (2004) Omega 3 fatty acids for prevention and treatment of cardiovascular disease. Cochrane Database Syst Rev. (4):CD003177. http://cochranelibrary-wiley.com/doi/10.1002/14651858.CD003177.pub2/abstract

4. Hickey S, Noriega LA. Implications and insights for human adaptive mechatronics from developments in algebraic probability theory, IEEE, UK Workshop on Human Adaptive Mechatronics (HAM), Staffs, 15-16 Jan 2009.

5. Hickey S, Hickey A, Noriega LA, (2013) The failure of evidence-based medicine? Eur J Pers Centered Healthcare 1: 69-79. http://ubplj.org/index.php/ejpch/article/view/636

6. Cortie CH, Else, PL, (2012) Dietary docosahexaenoic acid (22:6) incorporates into cardiolipin at the expense of linoleic acid (18:2): Analysis and potential implications. International Journal of Molecular Sciences, 13(11): 15447-15463. http://www.mdpi.com/1422-0067/13/11/15447

7. Case HS (2017) Orthomolecular Nutrition for Everyone. Turner Publication Co., Nashville, TN. ISBN-13: 978-1681626574

Nutritional Medicine is Orthomolecular Medicine

Orthomolecular medicine uses safe, effective nutritional therapy to fight illness. For more information: http://www.orthomolecular.org

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The peer-reviewed Orthomolecular Medicine News Service is a non-profit and non-commercial informational resource.

Editorial Review Board:

Ilyès Baghli, M.D. (Algeria)
Ian Brighthope, M.D. (Australia)
Prof. Gilbert Henri Crussol (Spain)
Carolyn Dean, M.D., N.D. (USA)
Damien Downing, M.D. (United Kingdom)
Michael Ellis, M.D. (Australia)
Martin P. Gallagher, M.D., D.C. (USA)
Michael J. Gonzalez, N.M.D., D.Sc., Ph.D. (Puerto Rico)
William B. Grant, Ph.D. (USA)
Tonya S. Heyman, M.D. (USA)
Suzanne Humphries, M.D. (USA)
Ron Hunninghake, M.D. (USA)
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Robert E. Jenkins, D.C. (USA)
Bo H. Jonsson, M.D., Ph.D. (Sweden)
Jeffrey J. Kotulski, D.O. (USA)
Peter H. Lauda, M.D. (Austria)
Thomas Levy, M.D., J.D. (USA)
Homer Lim, M.D. (Philippines)
Stuart Lindsey, Pharm.D. (USA)
Victor A. Marcial-Vega, M.D. (Puerto Rico)
Charles C. Mary, Jr., M.D. (USA)
Mignonne Mary, M.D. (USA)
Jun Matsuyama, M.D., Ph.D. (Japan)
Dave McCarthy, M.D. (USA)
Joseph Mercola, D.O. (USA)
Jorge R. Miranda-Massari, Pharm.D. (Puerto Rico)
Karin Munsterhjelm-Ahumada, M.D. (Finland)
Tahar Naili, M.D. (Algeria)
W. Todd Penberthy, Ph.D. (USA)
Dag Viljen Poleszynski, Ph.D. (Norway)
Jeffrey A. Ruterbusch, D.O. (USA)
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Jagan Nathan Vamanan, M.D. (India)
Garry Vickar, MD (USA)
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Andrew W. Saul, Ph.D. (USA), Editor-In-Chief
Editor, Japanese Edition: Atsuo Yanagisawa, M.D., Ph.D. (Japan)
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HYDROGEN SUPPLEMENTS – ACTIVE H2 ULTRA and MEGAHYDRATE

Fred Liers PhD hydrogen supplements Active H2 Ultra MegahydrateSupplemental 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 Megahydrate

Active H2 Ultra tablets and Megahydrate powder work together for major antioxidant power.

INGREDIENTS – HYDROGEN-INFUSED WATER

• 1 Scoop Megahydrate powder (500 mg) or 1 Megahydrate capsule (600 mg)

• 1 Tablet of Active H2 Ultra

• 8–16 Ounces of Purified Water

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.

We include hydrogen supplements in HPDI’s system of Foundational Supplements. In fact, hydrogen formulas as just one of six foundational supplements. We consider hydrogen a “secondary” foundational supplement usually to be added to a supplement regimen after the four primary ones: multivitamins, antioxidant & vitamin C formulas, essential fatty acids, and superfoods high in dietary nucleic acids (i.e., Rejuvenate! superfoods).

THERAPEUTIC USES OF HYDROGEN

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 scavenges cytotoxic 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 Active H2 Ultra

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.

hydrogen supplements active h2 ultra

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 tabletsMegahydrate 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.

http://www.integratedhealth.com/supplements/hydrogen-products.html

Megahydrate and Active H2 Ultra creates an ultra-healthy hydrogen fizzy drink.

TRY HYDROGEN!

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!

 

HYDROGEN RESOURCES

Hydrogen Articles

Hydrogen Supplements – Make Hydrogen Drinks

Hydrogen for Optimal Health

Wonders of Molecular Hydrogen

Molecular Hydrogen (H2) at the Forefront of Health Research

The Science Behind MegaHydrate by Hank Liers, PhD

Hydrogen Supplements

Active H2 Ultra tablets

Megahydrate capsules

Megahydrate powder

HPDI hydrogen products

Other Hydrogen Resources

Molecular Hydrogen Foundation

hydrogen supplements megahydrate active H2

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RESTORE GUT HEALTH FORMULA + VIDEO

Fred Liers PhD restore liquid mineral supplement ion gut healthHeard of RESTORE (ION* GUT HEALTH) liquid mineral supplement? If not, you’re about to discover something important for gut health.

ION* GUT HEALTH (formerly RESTORE) is formulated to help restore gut health. It works by strengthening the integrity of tight junctions in your intestinal wall.

Maintaining tight junctions is important because they protect your body from substances entering the blood stream. ION* GUT HEALTH (formerly Restore) also supports the communications systems of the bacteria in your microbiome.

Tight junctions are natural barriers protecting the lining of your gut barrier, organs such as kidneys and heart, and the blood-brain barrier thereby keeping out unwanted substances. Even as we take in nutrients from the GI tract, the function of tight junctions is maintaining the integrity of the gut wall and other barriers that protect the body.

These days, our gut membrane has a tough job keeping out unwanted substances. Because tight junctions are weakened by many things, including highly processed foods, especially those containing gluten and gliadin, the herbicide glyphosate (the primary ingredient in RoundUp weedkiller), and other exposures like electromagnetic fields (EMF) from digital devices and Wi-Fi networks.

As a result of weakened tight junctions, undesirable substances from food proteins, harmful chemicals and other toxins can slip though into our bloodstream. This can lead to a powerful immune response that can weaken immunity and cause significant inflammation. Foreign substances in the bloodstream can also result in extreme food allergies and food sensitivities to various toxins entering the body.

We live in an age in which our microbiome health is under assault. Studies show our ancient ancestors had 20,000–30,000 different strains of beneficial bacteria in their GI tracts. Many people today have just 5,000 or less. Why is that?

There are many reasons for low microbiome diversity. These reasons include antiobiotic use (both from pharmaceuticals and foods), glyphosate (which essentially acts like an antibiotic), processed foods (especially those containing gluten and gliadin), and systemic degradation of the gut environment rendering it less hospitable for maintaining health populations of gut flora.

These impacts are significant because diversity in your microbiome not only supports gut health, but also appropriate brain health, immune system health, and overall vitality. ION* Gut Health (Restore) acts as a “microbiome fertilizer” helping establish and maintain healthy microbiota.

In fact, ION* Gut Health (Restore) contains important “redox” molecules produced millions of years ago by existing soil bacteria. These molecules are an important part of communications systems within the body between gut bacteria and with the body’s mitochondria. These communication systems play an important role in establishing proper homeostasis throughout the body.

REASONS TO USE ION* GUT HEALTH (RESTORE)

There are important reasons to try ION* GUT HEALTH (Restore)—whether or not you experience significant gut health issues. These reasons include:

• Maintaining strong tight junctions for mega membrane health, and helping the body restore tight junction integrity

• Creating an environment in which beneficial bacteria can thrive

• Boosting microbiome diversity

• Healing the gut

• Mitigating the adverse effects substances like antibiotics, gluten/gliadin, glyphosate, and GMOs on microbiome health

• Supporting immune system function

• Protecting integrity of blood-brain barrier

Other benefits include support for respiratory wellness, enhancing mental clarity, and promoting proper homeostasis throughout the body.

For all these reasons and more, you should consider taking ION* GUT HEALTH (formerly Restore). You can start by taking one teaspoon or less daily, and gradually increasing your dose to one tablespoon or more.Restore Ion gut health liquid supplement

I have taken ION* GUT HEALTH (formerly Restore) daily for more than two years, and benefit greatly from it. The most noticeable effects are a complete cessation of spring allergies (after two decades of worsening symptoms), greater clarity of thinking, and improved overall well being. I have seen other people get good results with a variety of conditions from dysbiosis to gluten/gliadin sensitivity.

MORE ABOUT ION* GUT HEALTH

You can learn more about ION* Gut Health (Restore) on our website. Also, the Restore website offers in-depth information and videos. Here is how the Restore website and Dr. Zach Bush describe the formula:

ION* Gut Health (Restore) is a dietary supplement supplying first line defense against daily exposure to environmental and food-borne factors. It helps create an optimal environment or ecology in the gut membrane for beneficial or “good” bacteria to flourish. Beneficial gut flora protect your immune system and maintain health. Restore is a scientifically proven soil-derived mineral supplement designed to support protection of the intestinal walls.

ION* Gut Health (Restore) protects the entire gastrointestinal (GI) tract against agricultural herbicides, antibiotics, GMOs, gluten, and food-borne toxins. It helps create an environment in which 20,000–30,000 different strains of beneficial gut bacteria can thrive. This is a far different mode of action from probiotics, most of which contain just 3–30 strains of beneficial bacteria.

ION* Gut Health (Restore) helps create a strong immune system along with proper gut function. Microbiome balance and tight junction integrity are known to constitute a significant part of the immune system. They directly affect DNA transcription of cells to promote optimal health and prevent a leaky gut syndrome, thereby improving gut intelligence.

Seventy percent (70%) of our immune system is found in our gut. We need tens of thousands different strains of good gut bacteria to support a healthy immune system. Clinical experience, in addition to cell culture studies, support the theory that Restore’s proprietary formula creates the optimal environment in the gut to create a tight junction barrier and maintain our health and wellness.

ION* Gut Health (Restore) is a daily liquid supplement designed to support the protection of the entire gastrointestinal (GI) tract against agricultural herbicides, antibiotics, GMOs, gluten and food-borne toxins by helping to create an environment where between 20,000-30,000 different strains of good gut bacteria thrive. Most probiotics on the market contain fewer than 24 different strains of good gut bacteria.

TRY ION* GUT HEALTH

ION* Gut Health is ideal for individuals suffering from gut health issues. Yet, it is also excellent for supporting and maintaining gut health generally. That is the reason we at HPDI consider Restore important enough to designate as a foundational supplement, one of the top six supplements you need for good health.

Given the safety and effectiveness of ION* Gut Health (Restore), there is broad applicability for its use. This is especially true because gut and microbiome health are under constant assault. These assaults range from multiple environmental and lifestyle factors—including poor diets high in processed foods, antibiotics in pharmaceuticals and animal foods—to massive glyphosate (herbicide) contamination of foods, soils, air, and water.

Let ION* Gut Health be your first line of defense against assaults on your gut health, tight junctions, microbiome diversity, and immune function. As it says on the bottle, “Complete well-being begins in the gut.”

ION* GUT HEALTH (RESTORE) RESOURCES

Gut Health – Effects of Glyphosate and Antibiotics
by Hank Liers, PhD and Fred Liers, PhD

ION* Gut Health (formerly Restore) – 32 oz

ION* Gut Health (formerly Restore) – 8 oz

HPDI Gut Health Formulas

HPDI Foundational Supplements

Restore blog (Restore4Life)

ION* Biome site