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ULTIMATE PROTECTOR+ INGREDIENTS – GREEN TEA EXTRACT

Dr. Hank Liers, PhD biography about us HPDI integratedhealth formulator founder CEO scientist physicist wild bilberry and wild blueberry Ultimate Protector+ includes green tea extract, as well as extracts 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 explore the ingredient green tea extract. Green tea extract is added as a separate ingredient in Ultimate Protector+.

Ultimate Protector+ Includes Green Tea Extract

Ultimate Protector+ Includes Green Tea Extract

Green tea extract (high in EGCG) 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.

The green tea extract in Ultimate Protector+ has been extracted with non-GMO food grade ethanol and distilled water. Testing has indicated the product over 93% polyphenols, over 50% EGCG, and about 4% caffeine.

Bioactive Compounds in Tea
Tea contains over 2,000 components, including polyphenols (flavonoids), pigments (carotenoids and chlorophyll), alkaloids (caffeine, theophylline, theobromine), lignans, carbohydrates, lipids, proteins, amino acids (including L-theanine), vitamins (vitamin C, vitamin E, riboflavin), and various minerals and trace elements.

Flavonoids in Green Tea
Dietary flavonoids are divided in six subclasses: flavan-3-ols, anthocyanidins, flavanones, flavonols, flavones, and isoflavones. Total flavonoid content in green tea is about 138 mg a per 100 mL. A major subclass of flavonoids in green tea is that of flavan-3-ols. Flavan-3-ol monomers, also known as catechins, constitute 30%-42% of the solid weight of brewed green tea. The principal catechins found in tea are (-)-epicatechin (EC), (-)-epigallocatechin (EGC), (-)-epicatechin gallate (ECG), and (-)-epigallocatechin gallate (EGCG).

EGCG (Epigallocatechin Gallate) is one of the most powerful compounds in green tea. It has been studied to treat various diseases and may be one of the main reasons green tea has such powerful medicinal properties

Vitamins and Minerals Found in Green Tea

Green Tea Plant

GREEN TEA STUDIES

Below we provide information from several research articles that highlight some of the potential health effects of green tea extracts.

1. EGCG upregulates phase-2 detoxifying and antioxidant enzymes via the Nrf2 signaling pathway in human breast epithelial cells

Hye-Kyung Na and Young-Joon Surh
Proc Amer Assoc Cancer Res, Volume 46, 2005
From: http://cancerres.aacrjournals.org/content/65/9_Supplement/367.1

Abstract

There are multiple lines of compelling evidence from epidemiologic and laboratory studies supporting that frequent consumption of green tea is inversely associated with the risk of several types of human cancer and other chronic diseases. The chemopreventive and chemoprotective activity of green tea have been attributed to the polyphenolic ingredient (-)epigallocatechin-3-gallate (EGCG). Oxidative DNA damage has been implicated in initiation of carcinogenesis. The induction of phase-2 detoxifying or antioxidant defense enzymes contributes to the cancer chemopreventive and cytoprotective effects of many phytochemicals against oxidative stress. Here, we report that treatment of human breast epithelial (MCF10A) cells with EGCG induces the mRNA expression of both modulatory and catalytic subunits of γ-glutamate-cystein ligase (GCL), which is the rate-limiting enzyme in the synthesis of GSH. In addition, EGCG upregulated the expression of other antioxidant enzymes, including manganese superoxide dismutase and glutathione S-transferase π in a concentration- and time-dependent manner. NF-E2-related factor (Nrf2), a basic-leucine zipper transcription factor, has been reported to regulate the antioxidant/electrophile responsive elements (ARE/EpRE)-mediated expression of various phase-2 detoxifying or antioxidant enzymes. The nuclear accumulation and ARE/EpRE binding of Nrf2 were increased in EGCG-treated MCF10A cells. Moreover, MCF10A cells transfected with the luciferase reporter gene under the control of ARE/EpRE-driven promoter exhibited a strong transcriptional activity following exposure to EGCG. In contrast, mutation of the GC core box in the ARE/EpRE-driven promoter abolished the EGCG-induced transcriptional activity. MCF10A cells transiently transfected with dominant negative Nrf-2 were less responsive to EGCG-induced expression of GCLC mRNA compared to the vector-transfected control cells. Furthermore, EGCG treatment activated the extracellular signal-regulated protein kinase1/2 and Akt through phosphorylation. These findings, taken together, suggest that induction of antioxidant enzymes by EGCG can be mediated by activation of Nrf2 and possibly upstream signaling kinases, which may provide the cells with acquired antioxidant defense capacity against oxidative insult.

2. Neurological mechanisms of green tea polyphenols in Alzheimer’s and Parkinson’s diseases

The Journal of Nutritional Biochemistry, Volume 15, Issue 9, September 2004, Pages 506-516
OrlyWeinreba, SilviaMandela, TamarAmitaMoussa, B.H.Youdima
From: https://doi.org/10.1016/j.jnutbio.2004.05.002

Abstract
Tea consumption is varying its status from a mere ancient beverage and a lifestyle habit, to a nutrient endowed with possible prospective neurobiological–pharmacological actions beneficial to human health. Accumulating evidence suggest that oxidative stress resulting in reactive oxygen species generation and inflammation play a pivotal role in neurodegenerative diseases, supporting the implementation of radical scavengers, transition metal (e.g., iron and copper) chelators, and nonvitamin natural antioxidant polyphenols in the clinic. These observations are in line with the current view that polyphenolic dietary supplementation may have an impact on cognitive deficits in individuals of advanced age. As a consequence, green tea polyphenols are now being considered as therapeutic agents in well controlled epidemiological studies, aimed to alter brain aging processes and to serve as possible neuroprotective agents in progressive neurodegenerative disorders such as Parkinson’s and Alzheimer’s diseases. In particular, literature on the putative novel neuroprotective mechanism of the major green tea polyphenol, (−)-epigallocatechin-3-gallate (EGCG), are examined and discussed in this review.

3. Renoprotective effects of (+)-catechin in streptozotocin-induced diabetic rat model

Abstract
Diabetic nephropathy is a complication of diabetes mellitus leading to end-stage renal disease. Oxidative stress and inflammation play a major role in the pathogenesis of diabetic nephropathy. Green tea, known for its antioxidant and anti-inflammatory properties, has been shown to be renoprotective. We hypothesized that (+)-catechin (CTN), a component of green tea, is responsible for the renoprotection. Our investigation of the therapeutic potential of CTN in streptozotocin-induced diabetic rats demonstrated for the first time that the effects of CTN treatment were comparable with the effects of an angiotensin-converting enzyme inhibitor (ACEi) enalapril for the treatment of albumin excretion. After 12 weeks of CTN treatment with 35 mg/d in the drinking water, urinary albumin excretion and plasma creatinine concentrations in all the diabetic treatment groups were reduced, compared with the diabetic group with no treatment. Urine creatinine and creatinine clearance were higher in diabetic groups treated with CTN and ACEi compared with the diabetic group with no treatment. Endothelin 1, lipid peroxidation, concentration of alanine transferase enzyme, and expression of fibronectin were lower in all the treatment groups compared with the diabetic group with no treatment. Concentrations of free thiols were higher in the CTN-treated group compared with the diabetic rats with no treatment. Our findings suggest that CTN has renoprotective properties comparable with ACEi, and coadministration of CTN and enalapril might be useful in reducing albumin excretion as well as improving endothelial function. (+)-Catechin might be successfully used in the future for clinical situations where ACEi is poorly tolerated or contraindicated.

4. Green Tea Polyphenol (−)-Epigallocatechin-3-Gallate Restores Nrf2 Activity and Ameliorates Crescentic Glomerulonephritis

published: March 18, 2015https://doi.org/10.1371/journal.pone.0119543
Ting Ye , Junhui Zhen , Yong Du , Jason K. Zhou, Ai Peng, Nosratola D. Vaziri, Chandra Mohan , Yan Xu , Xin J. Zhou
From: https://journals.plos.org/plosone/article?id=10.1371/journal.pone.0119543

Abstract
Crescentic glomerulonephritis (GN) is the most severe form of GN and is associated with significant morbidity and mortality despite aggressive immunotherapy with steroids, cytotoxic drugs, and plasmapheresis. We examined the therapeutic efficacy of the green tea polyphenol (−)-epigallocatechin-3-gallate (EGCG, 50 mg/kg BW/day x3weeks), a potent anti-inflammatory and anti-oxidant agent, on experimental crescentic GN induced in 129/svJ mice by administration of rabbit anti-mouse glomerular basement membrane sera. Routine histology and key molecules involved in inflammatory and redox signaling were studied. EGCG treatment significantly reduced mortality, decreased proteinuria and serum creatinine, and markedly improved renal histology when compared with vehicle-treated mice. The improvements in renal function and histology were accompanied by the restoration of Nrf2 signaling (which was impaired in vehicle-treated mice) as shown by increased nuclear translocation of Nrf2 and cytoplasmic glutamate cysteine ligase catalytic subunit, glutamate cysteine ligase modifier subunit, and glutathione peroxidase. EGCG-treated mice also showed reduction in p-Akt, p-JNK, p-ERK1/2 and p-P38 as well as restoration of PPARγ and SIRT1 levels. Lower dose of EGCG (25 mg/kg BW/day x2 weeks) treatment also significantly decreased proteinuria and serum creatinine, and markedly improved renal histology when compared with vehicle-treated mice. Thus, our data illustrate the efficacy of EGCG in reversing the progression of crescentic GN in mice by targeting multiple signaling and inflammatory pathways as well as countering oxidative stress.

SUMMARY

Green Tea Extract is an exciting natural ingredient full of important polyphenols, catechins, antioxidants, and Nrf2 activators that help to make Ultimate Protector such an outstanding nutritional supplement. Continued research shows an amazing list of health benefits for this substance including its ability to function as a powerful stimulator of Nrf2 activity. It truly belongs in the Ultimate Protector+™ formula.

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ULTIMATE PROTECTOR+ INGREDIENTS – CRANBERRY

Dr. Hank Liers, PhD biography about us HPDI integratedhealth formulator founder CEO scientist physicist wild bilberry and wild blueberryUltimate Protector+ contains cranberry extract, 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 ingredient cranberry, which is a component of SFB® – Standardized Fruit Blend from Ethical Naturals, Inc.

Ultimate Protector+ Includes Cranberry

Ultimate Protector+ Includes Cranberry Extract

SFB® – Standardized Fruit Blend

SFB® is a proprietary formula that combines extracts from Grape, Cranberry, Pomegranate, Blueberry, Apple, Mangosteen, Bilberry, Chokeberry, and Goji Berry. It is high in fruit polyphenols, flavonoids, anthocyanins, catechins, proanthocyanins, ellagic acid, xanthines, chlorogenic acid, pterostilbenes, resveratrol, phloridzin, quercetin, zeaxanthin, carotenoids, polysaccharides, quinic acid, and more. 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 elements 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 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.

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

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

Type of Phytonutrient             Specific Molecules
Phenolic Acids                             hydroxybenzoic acids including vanillic acids;
—Phenolic Acids (cont.)             hydroxycinnamic acids inculding caffeic,
—Phenolic Acids (cont.)             coumaric, cinnamic, and ferulic acid
Proanthocyanidins                     epicatechins
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 cranberry extract 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.
    • It is known that cranberries turns urine acidic. This, together with the inhibition of bacterial adhesion helps prevent the formation of alkaline (calcium ammonium phosphate) stones in the urinary tract by working against proteus bacterial-infections.
    • In addition, the berries prevent plaque formation on the tooth enamel by interfering with the ability of the gram-negative bacterium, Streptococcus mutans, to stick to the surface. In this way cranberries helps prevent the development of cavities.
    • The berries are also good source of many vitamins like vitamin C, vitamin A, ß-carotene, lutein, zea-xanthin, and folate and minerals like potassium, and manganese.
  • Oxygen Radical Absorbance Capacity (ORAC) demonstrates cranberry at an ORAC score of 9584 µmol TE units per 100 g, one of the highest in the category of edible berries.

For more information on cranberries visit: http://www.whfoods.com/genpage.php?tname=foodspice&dbid=145

SCIENTIFIC STUDIES ON THE ANTIOXIDANT EFFECTS OF CRANBERRIES

Below, I provide relevant scientific studies on the antioxidant effects and potential health benefits of cranberries.

PREVENTION OF OXIDATIVE STRESS, INFLAMMATION AND MITOCHONDRIAL DYSFUNCTION IN THE INTESTINE BY DIFFERENT CRANBERRY PHENOLIC FRACTIONS.

ABSTRACT

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

ABSTRACT

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

From: http://www.sciencedirect.com/science/article/pii/S1756464613000364

ABSTRACT

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

From: http://www.ncbi.nlm.nih.gov/pubmed/24353827

ABSTRACT

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.

SUMMARY

Cranberry extract is full of polyphenols, anthocyanins, antioxidants, and Nrf2 activators that help to make Ultimate Protector+ such an outstanding nutritional supplement.

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ULTIMATE PROTECTOR+ INGREDIENTS – APPLE

Dr. Hank Liers, PhD biography about us HPDI integratedhealth formulator founder CEO scientist physicist wild bilberry and wild blueberry Ultimate Protector+ includes apple extract, as well as extracts from 12 different fruits, vegetables, and herbs. Each of these ingredients contain substances considered to be polyphenols, antioxidants, and Nrf2 activators. In this article, I explore the ingredient apple (Malus pumila mill.) extract, which is a component of SFB® – Standardized Fruit Blend from Ethical Naturals, Inc.

apple extract

Ultimate Protector+ Includes Apple

SFB® is a proprietary formula that combines extracts from Grape, Cranberry, Pomegranate, Blueberry, Apple, Mangosteen, Bilberry, Chokeberry, and Goji Berry. It is high in fruit polyphenols, flavonoids, anthocyanins, catechins, proanthocyanins, ellagic acid, xanthines, chlorogenic acid, pterostilbenes, resveratrol, phloridzin, quercetin, zeaxanthin, 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 elements 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 APPLE

The Apple extract in Ultimate Protector+ has been extracted with non-GMO food grade ethanol and distilled water. Testing has indicated the product contains over 40% polyphenols. In numerous epidemiological studies, apples have been associated with a decreased risk of chronic diseases such as cardiovascular disease, cancer, and asthma.

When compared to many other commonly consumed fruits in the United States, apples had the second highest level of antioxidant activity. Apples also ranked the second for total concentration of phenolic compounds, and perhaps more importantly, apples had the highest portion of free phenolics when compared to other fruits.

APPLE PHYTOCHEMICALS

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

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

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

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

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

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

SCIENTIFIC STUDIES ON THE ANTIOXIDANT EFFECTS OF APPLE

Below, I provide relevant scientific studies on the antioxidant effects and potential health benefits of apple.

Apple phytochemicals and their health benefits

Jeanelle Boyer1 and Rui Hai Liu1

Abstract

Evidence suggests that a diet high in fruits and vegetables may decrease the risk of chronic diseases, such as cardiovascular disease and cancer, and phytochemicals including phenolics, flavonoids and carotenoids from fruits and vegetables may play a key role in reducing chronic disease risk. Apples are a widely consumed, rich source of phytochemicals, and epidemiological studies have linked the consumption of apples with reduced risk of some cancers, cardiovascular disease, asthma, and diabetes. In the laboratory, apples have been found to have very strong antioxidant activity, inhibit cancer cell proliferation, decrease lipid oxidation, and lower cholesterol. Apples contain a variety of phytochemicals, including quercetin, catechin, phloridzin and chlorogenic acid, all of which are strong antioxidants. The phytochemical composition of apples varies greatly between different varieties of apples, and there are also small changes in phytochemicals during the maturation and ripening of the fruit. Storage has little to no effect on apple phytochemicals, but processing can greatly affect apple phytochemicals. While extensive research exists, a literature review of the health benefits of apples and their phytochemicals has not been compiled to summarize this work. The purpose of this paper is to review the most recent literature regarding the health benefits of apples and their phytochemicals, phytochemical bioavailability and antioxidant behavior, and the effects of variety, ripening, storage and processing on apple phytochemicals..

Cancer chemopreventive potential of apples, apple juice, and apple components.

 Gerhauser C1.

From: https://www.ncbi.nlm.nih.gov/pubmed/18855307

Abstract

Apples ( MALUS sp., Rosaceae) are a rich source of nutrient as well as non-nutrient components and contain high levels of polyphenols and other phytochemicals. Main structural classes of apple constituents include hydroxycinnamic acids, dihydrochalcones, flavonols (quercetin glycosides), catechins and oligomeric procyanidins, as well as triterpenoids in apple peel and anthocyanins in red apples. Several lines of evidence suggest that apples and apple products possess a wide range of biological activities which may contribute to health beneficial effects against cardiovascular disease, asthma and pulmonary dysfunction, diabetes, obesity, and cancer (reviewed by Boyer and Liu, Nutr J 2004). The present review will summarize the current knowledge on potential cancer preventive effects of apples, apple juice and apple extracts (jointly designated as apple products). In brief, apple extracts and components, especially oligomeric procyanidins, have been shown to influence multiple mechanisms relevant for cancer prevention in IN VITRO studies. These include antimutagenic activity, modulation of carcinogen metabolism, antioxidant activity, anti-inflammatory mechanisms, modulation of signal transduction pathways, antiproliferative and apoptosis-inducing activity, as well as novel mechanisms on epigenetic events and innate immunity. Apple products have been shown to prevent skin, mammary and colon carcinogenesis in animal models. Epidemiological observations indicate that regular consumption of one or more apples a day may reduce the risk for lung and colon cancer.

Apple Peel Polyphenols and Their Beneficial Actions on Oxidative Stress and Inflammation

. 2013; 8(1): e53725.
Marie Claude Denis, Alexandra Furtos, Stéphanie Dudonné, Alain Montoudis, Carole Garofalo, Yves Desjardins, Edgard Delvin, and Emile Levy
From: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3553108/#

Abstract

Since gastrointestinal mucosa is constantly exposed to reactive oxygen species from various sources, the presence of antioxidants may contribute to the body’s natural defenses against inflammatory diseases.

Hypothesis

To define the polyphenols extracted from dried apple peels (DAPP) and determine their antioxidant and anti-inflammatory potential in the intestine. Caco-2/15 cells were used to study the role of DAPP preventive actions against oxidative stress (OxS) and inflammation induced by iron-ascorbate (Fe/Asc) and lipopolysaccharide (LPS), respectively.

Results

The combination of HPLC with fluorescence detection, HPLC-ESI-MS TOF and UPLC-ESI-MS/MS QQQ allowed us to characterize the phenolic compounds present in the DAPP (phenolic acids, flavonol glycosides, flavan-3-ols, procyanidins). The addition of Fe/Asc to Caco-2/15 cells induced OxS as demonstrated by the rise in malondialdehyde, depletion of n-3 polyunsaturated fatty acids, and alterations in the activity of endogenous antioxidants (SOD, GPx, G-Red). However, preincubation with DAPP prevented Fe/Asc-mediated lipid peroxidation and counteracted LPS-mediated inflammation as evidenced by the down-regulation of cytokines (TNF-α and IL-6), and prostaglandin E2. The mechanisms of action triggered by DAPP induced also a down-regulation of cyclooxygenase-2 and nuclear factor-κB, respectively. These actions were accompanied by the induction of Nrf2 (orchestrating cellular antioxidant defenses and maintaining redox homeostasis), and PGC-1α (the “master controller” of mitochondrial biogenesis).

Conclusion

Our findings provide evidence of the capacity of DAPP to reduce OxS and inflammation, two pivotal processes involved in inflammatory bowel diseases.

APPLE SUMMARY

Apple is an important fruit full of polyphenols, anthocyanins, antioxidants, and Nrf2 activators that help to make Ultimate Protector+ such an outstanding nutritional supplement.

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ULTIMATE PROTECTOR+ INGREDIENTS – MANGOSTEEN

Dr. Hank Liers, PhD biography about us HPDI integratedhealth formulator founder CEO scientist physicist wild bilberry and wild blueberry Ultimate Protector+ includes mangosteen extract, as well as extracts 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 explore the ingredient mangosteen (Garcinia mangostana) extract which is a component of SFB® – Standardized Fruit Blend from Ethical Naturals, Inc.

Ultimate Protector+ Includes Mangosteen

Ultimate Protector+ Includes Mangosteen

SFB® is a proprietary formula that combines extracts from Grape, Cranberry, Pomegranate, Blueberry, Apple, Mangosteen, Bilberry, Chokeberry, and Goji Berry. It is high in fruit polyphenols, flavonoids, anthocyanins, catechins, proanthocyanins, ellagic acid, xanthines, chlorogenic acid, pterostilbenes, resveratrol, phloridzin, zeaxanthin, 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 elements 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 MANGOSTEEN

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

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

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

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

Metabolite Composition of Mangosteen

Xanthone is one of the compound classes that are prevalent in mangosteen. These metabolites have been extracted and characterized in various studies as reviewed by several publications. So far, there are more than 68 xanthones isolated from the mangosteen fruit with the majority of them are a- and c-mangostin. The molecular structure of these compounds have been elucidated and more recently, novel xanthones have been discovered such as 1,3,6-trihydroxy-2-(3-methylbut-2-enyl)-8-(3-formyloxy-3-methylbutyl)–xanthone, 7-O-demethyl mangostin, garmoxanthone, as well as mangostanaxanthone III, IV, and VII. These xanthones were also implicated in various pharmaceutical properties but more studies are needed to verify their effectiveness in human applications.It is interesting that using subcritical water extraction to extract xanthones from mangosteen fruit, eliminated the need for the chemical solvents.

A study showed that the aqueous micellar biphasic system they developed could also efficiently extract xanthones from mangosteen pericarp. This suggests that xanthones could be viable for human application but bioavailability studies need to be performed in the future to ascertain their delivery and efficacy. Interestingly, solubilizing a-mangostin in soybean oil (containing traces of linoleate, linolenic acid, palmitate, oleic acid, and stearate) improved the xanthone bioavailability in rats, such that the compound was found in brain, pancreas, and liver organs after 1 h treatment. This signifies the potential of using oil-based formulation for increasing the bioavailability of xanthones.

Other than xanthones, mangosteen pericarp is also known to contain one of the highest procyanidin content, compared to other fruit such as cranberry, Fuji apple, jujube, and litchi. These procyanidins including monomer (47.7%), dimer (24.1%), and trimer (26%) may also contribute to the antioxidant capability of mangosteen extract as shown in 1,1-diphenyl-2-picrylhydrazyl (DPPH) and Ferric Reducing Antioxidant Power (FRAP) assays. Other phenolics such as benzoic acid derivatives (vanilic acid and protocatechuic acid), flavonoids (rutin, quercetin, cactechin, epicatechin) and anthocyanins (cyanidin 3-sophoroside) were also highly present in mangosteen pericarp.

Furthermore, mangosteen compounds have also been profiled using metabolomics approach. Using GC-MS analysis, a study reported that mangosteen pericarp contains mainly sugars (nearly 50% of total metabolites) followed by traces of other metabolite classes such as sugar acids, alcohols, organic acids, and aromatic compounds. This study also found several phenolics such as benzoic acid, tyrosol, and protocatechuic acid which are known to possess anti-oxidative and anti-inflammatory activities.

SCIENTIFIC STUDIES ON THE ANTIOXIDANT EFFECTS OF MANGOSTEEN

Below, I provide relevant scientific studies on the antioxidant effects and potential health benefits of mangosteen.

Recent updates on metabolite composition and medicinal benefits of mangosteen plant

Wan Mohd Aizat, Ili Nadhirah Jamil, Faridda Hannim Ahmad-Hashim and Normah Mohd Noor
Institute of Systems Biology (INBIOSIS), Universiti Kebangsaan Malaysia (UKM), Bangi, Selangor, Malaysia

From: https://peerj.com/articles/6324.pdf

ABSTRACT

Background: Mangosteen (Garcinia mangostana L.) fruit has a unique sweet-sour taste and is rich in beneficial compounds such as xanthones. Mangosteen originally been used in various folk medicines to treat diarrhea, wounds, and fever. More recently, it had been used as a major component in health supplement products for weight loss and for promoting general health. This is perhaps due to its known medicinal benefits, including as anti-oxidant and anti-inflammation. Interestingly, publications related to mangosteen have surged in recent years, suggesting its popularity and usefulness in research laboratories. However, there are still no updated reviews (up to 2018) in this booming research area, particularly on its metabolite composition and medicinal benefits.

Method: In this review, we have covered recent articles within the years of 2016 to 2018 which focus on several aspects including the latest findings on the compound composition of mangosteen fruit as well as its medicinal usages.
Result: Mangosteen has been vastly used in medicinal areas including in anti-cancer, anti-microbial, and anti-diabetes treatments. Furthermore, we have also described the benefits of mangosteen extract in protecting various human organs such as liver, skin, joint, eye, neuron, bowel, and cardiovascular tissues against disorders and diseases.

Conclusion: All in all, this review describes the numerous manipulations of mangosteen extracted compounds in medicinal areas and highlights the current trend of its research. This will be important for future directed research and may allow researchers to tackle the next big challenge in mangosteen study: drug development and human applications.

α-Mangostin induces apoptosis in human chondrosarcoma cells through downregulation of ERK/JNK and Akt signaling pathway.

2011 May 25;59(10):5746-54. doi: 10.1021/jf200620n. Epub 2011 Apr 11.
Krajarng A1, Nakamura Y, Suksamrarn S, Watanapokasin R.
From: https://www.ncbi.nlm.nih.gov/pubmed/21446759

Abstract

Chondrosarcoma is a malignant primary bone tumor that is resistant to chemotherapy and radiation therapy. α-Mangostin, a component of Garcinia mangostana Linn, is a xanthone derivative shown to have antioxidant and antitumor properties. This study is the first to investigate anticancer effects of α-mangostin in the human chondrosarcoma cell line SW1353. We showed that α-mangostin inhibited cell proliferation of SW1353 cells in a time- and dose-dependent manner by using the trypan blue exclusion method. Hoechst 33342 nuclear staining and nucleosomal DNA-gel electrophoresis revealed that α-mangostin could induce nuclear condensation and fragmentation, typically seen in apoptosis. Flow cytometry using Annexin V/PI double staining assessed apoptosis, necrosis and viability. α-Mangostin activated caspase-3, -8, -9 expression, decreased Bcl-2 and increased Bax. This promotes mitochondrial dysfunction, leading to the release of cytochrome c from the mitochondria to the cytoplasm. In addition, total and phosphorylated ERK and JNK were downregulated in α-mangostin-treated SW1353 cells but no changes in p38. α-Mangostin also decreased phosphorylated Akt without altering total Akt. These results suggest that α-mangostin inhinbited cell proliferation and induced apoptosis through downregulation of ERK, JNK and Akt signaling pathway in human chondrosarcoma SW1353 cells.

Characterized mechanism of alpha-mangostin-induced cell death: caspase-independent apoptosis with release of endonuclease-G from mitochondria and increased miR-143 expression in human colorectal cancer DLD-1 cells.

2007 Aug 15;15(16):5620-8. Epub 2007 May 18.
Nakagawa Y, Iinuma M, Naoe T, Nozawa Y, Akao Y.

From: https://www.ncbi.nlm.nih.gov/pubmed/17553685

Abstract

alpha-Mangostin, a xanthone from the pericarps of mangosteen (Garcinia mangostana Linn.), was evaluated for in vitro cytotoxicity against human colon cancer DLD-1 cells. The number of viable cells was consistently decreased by the treatment with alpha-mangostin at more than 20 microM. The cytotoxic effect of 20 microM alpha-mangostin was found to be mainly due to apoptosis, as indicated by morphological findings. Western blotting, the results of an apoptosis inhibition assay using caspase inhibitors, and the examination of caspase activity did not demonstrate the activation of any of the caspases tested. However, endonuclease-G released from mitochondria with the decreased mitochondrial membrane potential was shown. The levels of phospho-Erk1/2 were increased in the early phase until 1h after the start of treatment and thereafter decreased, and increased again in the late phase. On the other hand, the level of phospho-Akt was sharply reduced with the process of apoptosis after 6h of treatment. Interestingly, the level of microRNA-143, which negatively regulates Erk5 at translation, gradually increased until 24h following the start of treatment. We also examined the synergistic growth suppression in DLD-1 cells by the combined treatment of the cells with alpha-mangostin and 5-FU which is one of the most effective chemotherapeutic agents for colorectal adenocarcinoma. The co-treatment with alpha-mangostin and 5-FU, both at 2.5 microM, augmented growth inhibition compared with the treatment with 5 microM of alpha-mangostin or 5 microM 5-FU alone. These findings indicate unique mechanisms of alpha-mangostin-induced apoptosis and its action as an effective chemosensitizer.

 

γ-Mangostin, a xanthone from mangosteen, attenuates oxidative injury in liver via NRF2 and SIRT1 induction

Abstract

γ-Mangostin (γ-man), an active compound from Garcinia mangostana L., has been discovered as a hepatoprotective agent against oxidative injury. However, the underlying mechanisms remained unclear. The current study showed that γ-man stimulated the nuclear translocation of nuclear factor erythroid 2-related factor 2 (NRF2) to enhance antioxidant capacity under oxidative stress, which was partially reversed by treatment of the NRF2 inhibitor, all-trans-retinoic acid. Moreover, γ-man increased the expression and activity of SIRT1 (silent mating type information regulation 2 homolog 1), which facilitated the deacetylation of peroxisome proliferator-activated receptor γ coactivator 1α to improve the mitochondrial function in L02 cells. The protective effect of γ-man was partially blocked by treatment of the SIRT1 inhibitor tenovin-1 or SIRT1 knockdown. In vivo studies showed γ-man protected mice from carbon tetrachloride-induced acute liver injury, through up-regulation of NRF2 and SIRT1. Thus, γ-man might be a candidate to protect liver from acute oxidative injury.

SUMMARY

Mangosteen is an important fruit full of polyphenols, anthocyanins, antioxidants, xanthones, and Nrf2 activators that help to make Ultimate Protector+ such an outstanding nutritional supplement.

Mangosteen
MANGOSTEEN, Garcinia mangostana—Painted by Dr. M.J. Dijkman

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ULTIMATE PROTECTOR+ INGREDIENTS – CHOKEBERRY (ARONIA)

Dr. Hank Liers, PhD aronia (chokeberry) nrf2 ultimate protectorUltimate Protector+ contains chokeberry (aronia), 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 explore the ingredient chokeberry (aronia) which is a component of SFB® Standardized Fruit Blend from Ethical Naturals, Inc.

Ultimate Protector+ Includes Chokeberry

Ultimate Protector+ Includes Chokeberry

SFB® is a proprietary formula that combines extracts from Grape, Cranberry, Pomegranate, Blueberry, Apple, Mangosteen, Bilberry, Chokeberry, and Goji Berry. It is high in fruit polyphenols, flavonoids, anthocyanins, catechins, proanthocyanins, ellagic acid, xanthines, chlorogenic acid, pterostilbenes, resveratrol, phloridzin, quercetin, zeaxanthin, carotinoids, polysaccharides, quinic acid, and more. 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 elements 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 CHOKEBERRY (ARONIA)

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

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

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

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

Below we provide information from several research articles that highlight some of the potential health effects of Aronia (Chokeberry)

CHOKEBERRY STUDIES

Chokeberry (Aronia melanocarpa)
A Review on the Characteristic Components and Potential Health Effects

From: https://www.thieme-connect.com/products/ejournals/html/10.1055/s-0028-1088306

Abstract

The intention of this review is to contribute to a better understanding of the potentials of the nutritional contribution of Aronia berries (Aronia melanocarpa). The paper gives a short background to their botanical classification and cultivation practice, going in detail to describe the chemical composition of the berries. The emphasis is laid thereby upon the phenolic constituents. The paper finally gives a short resume of their beneficial effects in biological systems in vitro, in animals, and in humans, thus underlining their medicinal potential.

Antioxidant Effect

Aronia (Chokeberry)

Black Aronia (Chokeberry)

A few reports also describe an antioxidant effect in an animal model, where chokeberry anthocyanins decrease lipid peroxidation and enhance the activity of enzymes which are involved in the antioxidant defense system. One further study noted that the red pigment fraction of chokeberry fruits composed of cyanidin derivatives is a potent scavenger of DPPH radicals in both in vitro and in vivo systems and is able to prevent in a dose-dependent manner gastric mucosal damage that was induced by the subsequent application of ethanol. The authors suggested that one of the mechanisms by which the extract suppresses the development of the gastric mucosal damage is the scavenging of active oxygen by its cyanidin derivatives since the suppression of gastric acid secretion was not observed. An antioxidant effect was also found in humans, where a dietary supplementation with chokeberry juice limits the exercise-induced oxidative damage to red blood cells in rowers.

Inhibition of cancer cell proliferation

Many reports suggest anti-proliferative or protective effects of chokeberries and/or chokeberry extracts against colon cancer on the basis of in vitro studies and in one animal study. An anthocyanin-rich extract from Aronia melanocarpa was shown to inhibit the growth as well as to stimulate apoptosis of human HT-29 colon cancer cells but exerted only little effect on the growth of non-transformed NCM460 colonic cells. Interestingly, the chokeberry extract inhibited the growth to a greater extent than grape and bilberry anthocyanin-rich extracts when inhibition was compared at similar concentrations of monomeric anthocyanin. Another study demonstrated that the exposure to chokeberry juice inhibited Caco-2 cell proliferation by causing G2/M cell cycle arrest. Gene expression analysis revealed that the tumour suppressor carcinoembryonic antigen-related cell adhesion molecule 1 (CEACAM1), whose expression is known to be reduced in the majority of early adenomas and carcinomas, was up-regulated in the Caco-2 cells following repetitive exposure to dietary levels of chokeberry juice. The anticarcinogenic potential was further supported by data from an animal study using male rats treated with the colon carcinogen azoxymethane. An anthocyanin-rich extract from chokeberry inhibited the formation of the azoxymethane-induced aberrant crypt foci, a tentative marker of dysplasia and malignant transformation, and decreased the colonic epithelial cell proliferation rate as well as the faecal bile acid concentration. The data go in line with recent studies reporting that isolated cyanidin 3-O-glucoside exhibits chemopreventive activities.

Antimutagenic effects

Phenolic compounds isolated from berries of Aronia melanocarpa also exert an antimutagenic activity. Anthocyanins isolated from aronia (chokeberry) markedly inhibited the mutagenic activity of benzo[a]pyrene and 2-aminofluorene in the Ames test as well as in the sister chromatid exchange assay with cultured human lymphocytes. Furthermore, aronia juice intake was shown to inhibit the endogenous generation of N-nitrosamines in rats treated with aminopyrin plus sodium nitrite. In consequence, histopathological changes observed in livers of rats fed with nitrosamine precursors were prevented by co-treatment with aronia juice.

Hepatoprotective effects

In an animal study, anthocyanins from aronia (chokeberry) decreased the toxicity and accumulation of cadmium in the liver and kidney of rats receiving both these components in their diet. It may testify to the possibility of anthocyanins chelating metal ions which in consequence may decrease the damages caused by cadmium. Interestingly, a hepatoprotective effect of aronia juice was also observed in rats after acute exposure to carbon tetrachloride (CCl4). The liver cytotoxicity from CCl4 is dependent upon its metabolism by cytochrome P450 to highly reactive trichloromethyl free radicals. The reaction of the CCl3 radical with oxygen initiates lipid peroxidation which results ultimately in the cell death. Aronia (chokeberry) juice prevented the CCl4-induced increase of lipid peroxidation as measured by the malonodialdehyde content in rat liver and plasma. One might conclude that the ability of anthocyanins and/or other phenolic constituents to scavenge free radicals is mainly responsible for the observed effect.

Cardioprotective effects

Aronia (chokeberry) can positively influence several risk factors for cardiovascular disease. In vitroexperiments demonstrate that the phenolic constituents contribute to the protection and restoration of endothelial cells and consequently to their function. Furthermore anti-platelet effects, as well as vasoactive and vasoprotective properties in porcine coronary arteries were observed. In an experimental model of hyperlipidaemia in rats aronia fruit juice hindered the dietary-induced elevation of plasma total cholesterol, LDL cholesterol and plasma lipids. In men with a mild hypercholesterolaemia regular aronia (chokeberry) juice drinking (250 mL per day) for six weeks resulted in a significant decrease in serum total cholesterol, LDL cholesterol and trigylceride level whereas the HDL2 cholesterol level was increased. Furthermore a moderate but significant decrease in serum glucose, homocysteine and fibrinogen concentration was noted. The metabolic changes were associated with a reduction in systolic and diastolic blood pressure by a mean of 13 and 7 mm Hg, respectively. A similar hypotensive effect of a flavonoid-rich extract from chokeberry fruits was lately observed in patients after myocardial infarction, treated simultaneously with statins and in patients with diabetes mellitus type II. Other effects studied include enhanced reduction in cardiovascular risk markers in patients after myocardial infarction suggesting a possible clinical use for secondary prevention of isachaemic heart diesease.

Antidiabetes effects

Research of other authors has demonstrated that Aronia melanocarpa anthocyanins might be useful in the prevention and control of diabetes mellitus type II and diabetes-associated complications. In an animal model the administration of aronia (chokeberry) fruit juice to diabetic rats appeared to attenuate hyperglycaemia and hypertriglyceridaemia. In a human intervention study the daily intake of 200 mL aronia (chokeberry) juice over a period of 3 months was effective in lowering fasting glucose levels in patients with non-insulin dependent diabetes. Furthermore aronia (chokeberry) juice showed a beneficial effect on HbA1c-glycosylated haemoglobin, total cholesterol and lipid levels. These findings go in line with reports showing an effect of other procyanidin-rich foods on diabetes. Recent human studies also document that aronia (chokeberry) juice may be useful in in the treatment of obesity disorders.

Conclusions

In conclusion, aronia (chokeberry) (Aronia melanocarpa), a lesser known berry fruit, is one of the richest plant sources of highly interesting phenolic phytochemicals including procyanidins and anthocyanins. The high content as well as the pattern of the phenolic constituents seems to be responsible for the wide range of its potential medicinal and therapeutic effects. Further studies are needed to understand the beneficial effects reported so far also from the mechanistic point of view. However, it seems desirable that the spread and popularity of aronia (chokeberry) food products in the future will increase and expand consumers’ choice for healthy berry fruits.

Protective effect of chokeberry on chemical-induced oxidative stress in rat.

From: http://www.ncbi.nlm.nih.gov/pubmed/20488852

Hum Exp Toxicol. 2011 Mar;30(3):199-208. doi: 10.1177/0960327110371697. Epub 2010 May 20. Kujawska M1, Ignatowicz E, Ewertowska M, Oszmiański J, Jodynis-Liebert J.

Abstract

Male Wistar rats were treated with chokeberry juice per os, 10 mL/kg/day, for 28 days and a single intraperitoneal (i.p.) dose of N-nitrosodiethylamine (NDEA), 150 mg/kg, or carbon tetrachloride (CCl(4)), 2 ml/kg. The level of hepatic microsomal lipid peroxidation, expressed as thiobarbituric acid reactive substances (TBARS), was increased in animals dosed with NDEA and CCl(4). Juice pretreatment resulted in a significant decrease in TBARS by 53% and 92%, respectively. In rats administered juice alone, 50% decrease in TBARS was noted. The activities of all antioxidant enzymes were decreased in the liver of rats administered either toxicant by 29%-52% as compared to controls. Juice pretreatment resulted in an increase in the activity of catalase, glutathione peroxidase and glutathione reductase by 117%, 56% and 44%, respectively, only in rats challenged with NDEA. Although no response of plasma protein carbonyls to both toxicants was observed, the pretreatment with juice caused a 55% decrease of this parameter in CCl(4)-dosed rats. DNA damage in blood leukocytes induced by either toxicant was slightly reduced, by 24%, in the rats pretreated with juice and administered NDEA. The results of the study showed that pretreatment with chokeberry juice confers some protection against chemical-induced oxidative stress.

Evidence-Based Complementary and Alternative Medicine Volume 2013 (2013), Article ID 912769, 8 pages http://dx.doi.org/10.1155/2013/912769

The Involvement of a Polyphenol-Rich Extract of Black Chokeberry in Oxidative Stress on Experimental Arterial Hypertension

From: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3600185/

Manuela Ciocoiu, Laurentiu Badescu, Anca Miron, and Magda Badescu

Abstract

The aim of this study is to characterize the content of Aronia melanocarpa Elliott (black chokeberry) extract and also to estimate the influence of polyphenolic compounds contained in chokeberries on oxidative stress, on an L-NAME-induced experimental model of arterial hypertension. The rat blood pressure values were recorded using a CODA Noninvasive Blood Pressure System. HPLC/DAD coupled with ElectroSpray Ionization-Mass Spectrometry allowed identification of five phenolic compounds in berries ethanolic extract as follows: chlorogenic acid, kuromanin, rutin, hyperoside, and quercetin. The serous activity of glutathione-peroxidase (GSH-Px) has significantly lower values in the hypertensive (AHT) group as compared to the group protected by polyphenols (AHT + P). The total antioxidant capacity (TAC) values are lower in the AHT group and they are significantly higher in the AHT + P group. All the measured blood pressure components revealed a biostatistically significant blood pressure drop between the AHT group and the AHT + P group. The results reveal the normalization of the reduced glutathion (GSH) concentration as well as a considerable reduction in the malondialdehyde (MDA) serum concentration in the AHT + P group. Ethanolic extract of black chokeberry fruits not only has a potential value as a prophylactic agent but also may function as a nutritional supplement in the management of arterial hypertension.

Evidence-Based Complementary and Alternative Medicine Volume 2013 (2013), Article ID 912769, 8 pages http://dx.doi.org/10.1155/2013/912769

Extracts, anthocyanins and procyanidins from Aronia melanocarpa as radical scavengers and enzyme inhibitors.

From: http://www.ncbi.nlm.nih.gov/pubmed/23459328

Bräunlich M1, Slimestad R, Wangensteen H, Brede C, Malterud KE, Barsett H.

Abstract

Extracts, subfractions, isolated anthocyanins and isolated procyanidins B2, B5 and C1 from the berries and bark of Aronia melanocarpa were investigated for their antioxidant and enzyme inhibitory activities. Four different bioassays were used, namely scavenging of the diphenylpicrylhydrazyl (DPPH) radical, inhibition of 15-lipoxygenase (15-LO), inhibition of xanthine oxidase (XO) and inhibition of α-glucosidase. Among the anthocyanins, cyanidin 3-arabinoside possessed the strongest and cyanidin 3-xyloside the weakest radical scavenging and enzyme inhibitory activity. These effects seem to be influenced by the sugar units linked to the anthocyanidin. Subfractions enriched in procyanidins were found to be potent α-glucosidase inhibitors; they possessed high radical scavenging properties, strong inhibitory activity towards 15-LO and moderate inhibitory activity towards XO. Trimeric procyanidin C1 showed higher activity in the biological assays compared to the dimeric procyanidins B2 and B5. This study suggests that different polyphenolic compounds of A. melanocarpa can have beneficial effects in reducing blood glucose levels due to inhibition of α-glucosidase and may have a potential to alleviate oxidative stress.

Nutrients. 2013 Mar 4;5(3):663-78. doi: 10.3390/nu5030663.

Aronia (Chokeberry) Tea

Aronia (Chokeberry) makes a nice tea.

CHOKEBERRY SUMMARY

Chokeberry (Aronia) is an exciting fruit full of important polyphenols, antioxidants and Nrf2 activators that help to make Ultimate Protector+ such an outstanding nutritional supplement. This ingredient is becoming much more well known as research studies identify its many benefits. Recently, I was happy to find that the Knudsen “Just Fruit” brand has introduced “Just Aronia”. Try it!!!