Bilberry (Vaccinium myrtillus)


Modern

Studies
Bilberry Traditional

use


Review

Legend has it that during WWII British pilots have noticed an improvement in their nighttime vision after including Bilberry jam in the diet. The jam was a popular dessert, apparently due to the lack of alternatives. Because of the story or not, Bilberry (Vaccinum myrtillus, fam. Ericaceae) has become one of the 10 most popular herbal supplements in the United States. While Bilberry effects on night vision remain to be confirmed, it is well known and widely used in Europe traditional and modern herbal medicine. Even more popular are fresh berries offering the combination of delicious taste and rich array of nutrients.

Bilberry herbal medicnes

The use of the dried Bilberry berries to combat diarrhea, especially in children, is wide spread throughout European continent. For example, German government approves Bilberry for diarrhea and inflammation of the mouth or throat and Russian government approves Bilberry for diarrhea and as astringent and anti-inflammatory oral treatment. A tea is made of 3 tablespoons of dried berries boiled in a quart of water for 10 min or steeped in a warm water for several hours. The same tea is used as a mouthwash to help treat gum inflammations and sores. Bilberry berry tea is considered a safe and efficient remedy against hemorrhoids. To this end the tea is taken during 3 - 4 weeks at a dose of 2 cups a day. The tea made of Bilberry leaf (usually about two tea spoons per cup of boiling water) was used for similar purposes (mostly in adults), and also to help combat upset stomach, cough, skin inflammatory conditions. Another traditional application of leaf tea is to help improve sugar metabolism - it is believed to contain ingredients helpful for the treatment of type II diabetes. Considering side effects, there is no reason to be afraid of the overdose of the berries or berry tea. Bilberry leaf tea, when used continuously at excessively high doses may cause symptoms of poisoning due to high content of hydrohynons. Symptoms are reversible with discontinuation of the treatment.

Ingredients

Health beneficial ingredients of Bilberry include flavonoids and glycosides(1,2) The main known group of Bilberry berry flavonoids are anthocyanidins, also called anthocyanosides or anthocyanins (5). Dried berries contain about 360 mg per 100 g of total anthocyanidins, that is 3 times higher than in Black Currant and more than 10 times higher than in red wine (2). More than a dozen of anthocianidins has been identified so far in the Bilberry berries, including delphinidin, cyanidin, petunidin, pelargonidin, peonidin, and malvidin and corresponding 3-glucosides. Other group of flavonoids found in Bilberry are flavones and flavonols. In fresh berries the total content of flavonols was determined as 41 mg/kg (1) and the level of quercetin and miricetin as 30 and 20 mg/kg respectively (3). Several iridoid glucosides were identified in the Bilberry, the major representative was monotropein (4).

The Bilberry leaf offers different menu of flavonoids where flavones and flavonols represent the main group(6). Total flavonoid content in dry leaf was determined to be in the range of 2 - 3 %, with major constituents quercetin 3-glucuronide (0.8 - 1 %) and hyperoside (0.15 - 0.2%). Anthocyandins level in the leaf was negligible. The content of chlorogenic acid in dry Bilberry leaf was in the range of 1.5 - 3%. Bilberry leaf ingredients with potential health beneficial properties include large number of polyphenol compounds with total content up to 9 % and tannins (7 - 7.8 %).

 

Research

It is tempting to speculate that significant differences between the berry and the leaf of Bilberry in the spectrum of health beneficial ingredient have found their reflection in the prescriptions of traditional medicine. Preclinical and clinical investigations so far have been focused on the anthocyanidins, the main known health beneficial ingredients of the berries.

Alleged health beneficial effects of Bilberry include effects on visual system, prevention and restriction of tumor development, improvement of sugar metabolism in patients with type 2 diabetes.
A majority of clinical trials were trailing the notorious legend and focused on the action of Bilberry on visual system (7,8). French studies from the mid-1960s found improved light sensitivity in pilots, air traffic controllers, and truck drivers who had taken bilberry. A 1987 Italian report on 34 patients suggested that bilberry might improve conditions of blood vessels in the retina. A 1997 Israeli study on 18 people found no effect of bilberries (apparently used as an extract) on night vision. A 2000 American study reported no improvement in night vision, although the subjects swallowed the maximum recommended dose of bilberry extract for three weeks. It appears that data of more recent studies may question the vision beneficial effect of Bilberry. However, negative results may be attributed to a) depletion of the Bilberry extract used in these trials in certain nutrients, b) low degree of assimilation of anthocianiding from the formulation of the extract used in the trials, 3) nutritional and/or general health background of the trial participants. It should be mentioned that no chemical analysis of the extracts and no control of the level of assimilation of anthocianidins were implemented in any trial. At the same time, the possibility of beneficial effects of Bilberry on visual functions is supported by in vitro observations. Thus, Bilberry extract reduces the epoxidation of fluorophore A2E, a autofluorescent pigments that accumulate in retinal pigment epithelial cells with aging and also in some retinal disorders (9). Fluorophore A2E-epoxidation involve light induced generation of singlet oxygen, followed by autooxidation and formation of epoxides with reactivity towards DNA, and have been implicated in the etiology of macular degeneration (9). Accordingly, the additional trials involving both whole berries and anthoicianidin enriched extracts seem well justified to evaluate the beneficial action of Bilberry on visual system.

A number of preclinical studies were focused on evaluation of anticarcinogenic action of Bilberry extract. Anthocyanins anticancer action may be mediated by several molecular mechanisms including antioxidation, anticarcinogenesis and targeted elimination of tumor cells. As a potent antioxidants Bilberry anthocyaniding may play significant role in protections against mutagens and carcinogens with oxidative and peroxidative activities - antioxidation (12). Anticarcinogenesis includes the molecular mechanisms of action leading to tumor growth inhibition. The examples of anticarcinogenesis action include the ability of Bilberry extracts to cause the induction of xenobiotic detoxification enzyme quinone reductase and to inhibit the induction of the tumor associated enzyme ornithine decarboxylase by the tumor promoter phorbol 12-myristate 13-acetate in vitro (10). Authors conclude that fractions of Bilberry extract exhibit potential anticarcinogenic activity. In another study Bilberry extract was shown to significantly inhibit the expression of vascular endothelial growth factor (VEGF) which plays critical role for the vascularization of tumors and has been implicated as a promoter of tumor growth (11). Elimination of tumor cells may be mediated by anthocyanins through the induction of apoptosis (12). Bilberry extract and the anthocyanins, bearing delphinidin or malvidin as the aglycon, were shown to inhibit the growth of HL60 tumor cells through the induction of apoptosis (13). Therefore, Billberry appear to demonstrate promising in vitro effects in several areas of anticancer treatment and, assuming the lack of undesirable side effects, may offer at least well tolerated supplemental therapy.

In spite of numerous traditional references to the use of Bilberry leaf and berry for the improvement of sugar metabolism, the extend of modern investigations in that direction remains very limited. The encouraging results were obtained in the study on 82 patients with Diabetes mellitus of the 2nd type who received a herbal tea made of Bilberry leaf and two other plants three times daily during two months (14). The study revealed significant, nearly 25% decrease in the average glycemia values in 90% of patients after the treatment. While study lacks the control group and was conducted not in a blind fashion, it clearly suggest that traditional application of Bilberry for the treatment of Diabetes is worth further consideration.

In conclusion, Bilberry offers two sources of potential health beneficial supplements and medicines: leaf and berry. Major interest of current research is focused on one group of berry flavonoids with antioxidant peorperties - anthocianidins. Overall high safety and promising, but sometimes contradictory results obtained in clinical and preclinical studies, calls for further research and clinical trials of this exciting plant.

Bibliography

1. Hakkinen SH, Karenlampi SO, Mykkanen HM, Torronen AR J Agric Food Chem 2000, 48, 2960-5 Influence of domestic processing and storage on flavonol contents in berries
2. Nyman NA, Kumpulainen JT. J Agric Food Chem 2001, 49, 4183-7. Determination of anthocyanidins in berries and red wine by high-performance liquid chromatography
3. Hakkinen SH, Karenlampi SO, Heinonen M, Mykkanen HM, Torronen AR. J. Agric Food Chem 1999, 47, 2274-9. Content of flavonols quercetin, myricetin and Kaempferol in 25 eadible berries.
4. Jensen HD, Krogfelt KA, Cornett C, Hansen SH, Christensen SB. J Agric Food Chem 2002, 50, 6871- 4. Hydrophilic carboxylic acids and iridoid glycosides in the juice of American and European cranberries (Vaccinium macrocarpon and V. oxycoccos), lingonberries (V. vitis-idaea), and blueberries (V. myrtillus).
5. Jaakola L, Maatta K, Pirttila AM, Torronen R, Karenlampi S, Hohtola A. Plant Physiol 2002, 130, 729-39. Expression of genes involved in anthocyanin biosynthesis in relation to anthocyanin, proanthocyanidin, and flavonol levels during bilberry fruit development.
6. Fraisse D, Carnat A, Lamaison JL. Ann Pharm Fr 1996, 54, 280-3. Polyphenolic composition of the leaf of bilberry.
7. Muth ER, Laurent JM, Jasper P. The effect of bilberry nutritional supplementation on night visual acuity and contrast sensitivity. Altern Med Rev 2000, 5, 164-73
8. Head KA. Altern Med Rev 2001, 6, 141-66. Natural therapies for ocular disorders, part two: cataracts and glaucoma.
9. Sparrow JR, Vollmer-Snarr HR , Zhou J, Jang YP, Jockusch S, Itagaki Y, Nakanishi K. A2E-epoxides damage DNA in retinal pigment epithelial cells. Vitamin E and other antioxidants inhibit A2E-epoxide formation. J Biol Chem 2003, 19
10. Bomser J, Madhavi DL, Singletary K, Smith MA. Planta Med 1996, 62, 212-6. In vitro anticancer activity of fruit extracts from Vaccinium species.
11. Roy S, Khanna S, Alessio HM, Vider J, Bagchi D, Bagchi M, Sen CK. Free Radic Res 2002, 36, 1023-31 Anti-angiogenic property of edible berries
12. Hou DX. Curr Mol Med 2003, 3, 149-159. Potential mechanisms of cancer chemoprevention by anthocyanins.
13. Katsube N, Iwashita K, Tsushida T, Yamaki K, Kobori M J Agric Food Chem 2003, 51, 68-75. Induction of apoptosis in cancer cells by Bilberry (Vaccinium myrtillus) and the anthocyanins.
14. Ionescu-Tirgoviste C, Popa E, Mirodon Z, Simionescu M, Mincu I. Rev Med Interna Neurol Psihiatr Neurochir Dermatovenerol Med Interna 1989, 41, 185-92. The effect of a plant mixture on the metabolic equilibrium in patients with type-2 diabetes mellitus


Modern Studies

In vitro anticancer activity of fruit extracts from Vaccinium species.
Bomser J, Madhavi DL, Singletary K, Smith MA. Planta Med 1996, 62, 212-6
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.

Polyphenolic composition of the leaf of bilberry.
Fraisse D, Carnat A, Lamaison JL. Ann Pharm Fr 1996; 54(6):280-3
Dried leaves of 14 harvested batches and one batch from commercial origine of Vaccinium myrtillus L present a similar polyphenolic pattern. The mean levels of the harvested batches and the levels of the commercial batch were respectively: total polyphenol compounds 12.98 and 10.62%, tannins 7.84 and 7.43%, total flavonoid compounds 2.98 and 2.20% (spectrophotometry), 1.41 and 1.16% (HPLC), quercetin 3-glucuronide 1.02 and 0.83%, hyperoside 0.22 and 0.16%, chlorogenic acid 3.66 and 1.58%. The levels were higher in young leaves and lower in old leaves. A specific chromatographic profile of the flavonoid compounds and a determination method of the tannin or the total polyphenol content were proposed in a standardization purpose.

Content of the flavonols quercetin, myricetin, and kaempferol in 25 edible berries.
Hakkinen SH, Karenlampi SO, Heinonen IM, Mykkanen HM, Torronen AR. J Agric Food Chem 1999 Jun;47(6):2274-9
The amounts of quercetin, myricetin, and kaempferol aglycons in 25 edible berries were analyzed by an optimized RP-HPLC method with UV detection and identified with diode array and electrospray ionization mass spectrometry detection. Sixteen species of cultivated berries and nine species of wild berries were collected in Finland in 1997. Quercetin was found in all berries, the contents being highest in bog whortleberry (158 mg/kg, fresh weight), lingonberry (74 and 146 mg/kg), cranberry (83 and 121 mg/kg), chokeberry (89 mg/kg), sweet rowan (85 mg/kg), rowanberry (63 mg/kg), sea buckthorn berry (62 mg/kg), and crowberry (53 and 56 mg/kg). Amounts between 14 and 142 mg/kg of myricetin were detected in cranberry, black currant, crowberry, bog whortleberry, blueberries, and bilberry. Kaempferol was detected only in gooseberries (16 and 19 mg/kg) and strawberries (5 and 8 mg/kg). Total contents of these flavonols (100-263 mg/kg) in cranberry, bog whortleberry, lingonberry, black currant, and crowberry were higher than those in the commonly consumed fruits or vegetables, except for onion, kale, and broccoli.

The effect of a plant mixture on the metabolic equilibrium in patients with type-2 diabetes mellitus
Ionescu-Tirgoviste C, Popa E, Mirodon Z, Simionescu M, Mincu I. Rev Med Interna Neurol Psihiatr Neurochir Dermatovenerol Med Interna 1989 Mar-Apr;41(2):185-92
The present paper analyses the results obtained in 82 patients with diabetes mellitus of the 2nd type: 59 women and 23 men, between 41 and 74 years old (average +/- DS, 58 +/- 9 years), of which 58 had an index of the body weight higher than 26. The diabetes duration ranged between newly discovered and 11 years. Each patient was given, 3 times a day, a 150 ml cup containing an infusion of the following mixture of plants previously cut into small pieces: Phaseolus vulgaris (pod), Morus alba (leaf), and Vaccinum myrtillus (leaves). The approximate dose used was of about 15 g/day. The treatment lasted for two months. Before and after treatment, the following parameters were determined: Hb Al (Bio-Rex method) in 31 cases; the average of 3 consequent glycemias; the value of glycemia and insulinemia recorded after a standard lunch, consisting of about 40 g glucides, 14 g proteins and 6 g lipids (50 g bread, a boiled egg and a boiled apple of 100 g). Analysis of the results obtained enabled the following temporary conclusions (1). In 74 out of the 82 cases studied, the average values of glycemia, after the treatment with plants, were lower than those recorded before the treatment (the average values of the whole lot: 219 +/- 82 mg/dl before treatment and 166 +/- 76 mg/dl after treatment (2). The overall decrease recorded, of 53 mg/dl, represents 24.3% of the initial value

Berry phenolics and their antioxidant activity.
Kahkonen MP, Hopia AI, Heinonen M. J Agric Food Chem 2001 Aug;49(8):4076-82
Phenolic profiles of a total of 26 berry samples, together with 2 apple samples, were analyzed without hydrolysis of glycosides with HPLC. The phenolic contents among different berry genera varied considerably. Anthocyanins were the main phenolic constituents in bilberry, bog-whortleberry, and cranberry, but in cowberries, belonging also to the family Ericaceae genus Vaccinium, flavanols and procyanidins predominated. In the family Rosaceae genus Rubus (cloudberry and red raspberry), the main phenolics found were ellagitannins, and in genus Fragaria (strawberry), ellagitannins were the second largest group after anthocyanins. However, phenolic acids were dominant in rowanberries (genus Sorbus) and anthocyanins in chokeberry (genus Aronia). In the family Grossulariaceae genus Ribes (currants and gooseberry), anthocyanins predominated, as well as in crowberries (family Empetraceae genus Empetrum). In apples, hydroxycinnamic acids were the main phenolic subgroup. Extraction methods for berries and apples were studied to produce phenolic extracts with high antioxidant activity. Evaluation of antioxidant activity was performed by autoxidazing methyl linoleate (40 degrees C, in the dark). The extraction method affected remarkably both the phenolic composition and the antioxidant activity, but with statistical analysis the observed activity could not be well explained with the contents of individual phenolic subgroups.

Induction of apoptosis in cancer cells by Bilberry (Vaccinium myrtillus) and the anthocyanins.
Katsube N, Iwashita K, Tsushida T, Yamaki K, Kobori M. J Agric Food Chem 2003 Jan 1;51(1):68-75
Among ethanol extracts of 10 edible berries, bilberry extract was found to be the most effective at inhibiting the growth of HL60 human leukemia cells and HCT116 human colon carcinoma cells in vitro. Bilberry extract induced apoptotic cell bodies and nucleosomal DNA fragmentation in HL60 cells. The proportion of apoptotic cells induced by bilberry extract in HCT116 was much lower than that in HL60 cells, and DNA fragmentation was not induced in the former. Of the extracts tested, that from bilberry contained the largest amounts of phenolic compounds, including anthocyanins, and showed the greatest 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity. Pure delphinidin and malvidin, like the glycosides isolated from the bilberry extract, induced apoptosis in HL60 cells. These results indicate that the bilberry extract and the anthocyanins, bearing delphinidin or malvidin as the aglycon, inhibit the growth of HL60 cells through the induction of apoptosis. Only pure delphinidin and the glycoside isolated from the bilberry extract, but not malvidin and the glycoside, inhibited the growth of HCT116 cells.

The effect of bilberry nutritional supplementation on night visual acuity and contrast sensitivity.
Muth ER, Laurent JM, Jasper P. Altern Med Rev 2000 Apr;5(2):164-73
PURPOSE: The purpose of this study was to investigate the effect of bilberry on night visual acuity (VA) and night contrast sensitivity (CS). METHODS: This study utilized a double-blind, placebo-controlled, crossover design. The subjects were young males with good vision; eight received placebo and seven received active capsules for three weeks. Active capsules contained 160 mg of bilberry extract (25-percent anthocyanosides), and the placebo capsules contained only inactive ingredients. Subjects ingested one active or placebo capsule three times daily for 21 days. After the three-week treatment period, a one-month washout period was employed to allow any effect of bilberry on night vision to dissipate. In the second three-week treatment period, the eight subjects who first received placebo were given active capsules, and the seven who first received active capsules were given placebo. Night VA and night CS was tested throughout the three-month experiment. RESULTS: There was no difference in night VA during any of the measurement periods when examining the average night VA or the last night VA measurement during active and placebo treatments. In addition, there was no difference in night CS during any of the measurement periods when examining the average night CS or the last night CS measurement during active and placebo treatments. CONCLUSION: The current study failed to find an effect of bilberry on night VA or night CS for a high dose of bilberry taken for a significant duration. Hence, the current study casts doubt on the proposition that bilberry supplementation, in the forms currently available and in the doses recommended, is an effective treatment for the improvement of night vision in this population.

Determination of anthocyanidins in berries and red wine by high-performance liquid chromatography.
Nyman NA, Kumpulainen JT. J Agric Food Chem 2001 Sep;49(9):4183-7
A high-performance liquid chromatographic (HPLC) method for the determination of anthocyanidins from berries and red wine is described. Delphinidin, cyanidin, petunidin, pelargonidin, peonidin, and malvidin contents of bilberry (Vaccinium myrtillus), black currant (Ribes nigrum), strawberry (Fragaria ananassa cv. Jonsok), and a Cabernet sauvignon (Vitis vinifera) red wine were determined. The aglycon forms of the anthocyanins present in the samples were revealed by acid hydrolysis. A reversed phase analytical column was employed to separate the anthocyanidins before identification by diode array detection. The suitability of the method was tested by determining the recovery (95-102% as aglycons and 69-104% from glycosides) for each anthocyanidin. Method repeatability was tested by charting the total aglycon content of two samples over a period of 14 analyses and determining the coefficients of variation (1.41% for bilberry and 2.56% for in-house reference material). The method developed proved thus to be effective for reliable determination of anthocyanidins from freeze-dried berry samples and red wine.
The total anthocyanidin content of the tested samples was as follows:
Reference material 447 +/- 8 mg/100 g
Strawberry 23.8 +/- 0.4 mg/100 g
Black currant 135 +/- 3 mg/100 g
Bilberry 360 +/- 3 mg/100 g
Cabernet sauvignon red wine 26.1 +/- 0.1 mg/100 ml

Anti-angiogenic property of edible berries
Roy S, Khanna S, Alessio HM, Vider J, Bagchi D, Bagchi M, Sen CK. Free Radic Res 2002 Sep;36(9):1023-31
Recent studies show that edible berries may have potent chemopreventive properties. Anti-angiogenic approaches to prevent and treat cancer represent a priority area in investigative tumor biology. Vascular endothelial growth factor (VEGF) plays a crucial role for the vascularization of tumors. The vasculature in adult skin remains normally quiescent. However, skin retains the capacity for brisk initiation of angiogenesis during inflammatory skin diseases such as psoriasis and skin cancers. We sought to test the effects of multiple berry extracts on inducible VEGF expression by human HaCaT keratinocytes. Six berry extracts (wild blueberry, bilberry, cranberry, elderberry, raspberry seed, and strawberry) and a grape seed proanthocyanidin extract (GSPE) were studied. The extracts and uptake of their constituents by HaCaT were studied using a multi-channel HPLC-CoulArray approach. Antioxidant activity of the extracts was determined by ORAC. Cranberry, elderberry and raspberry seed samples were observed to possess comparable ORAC values. The antioxidant capacity of these samples was significantly lower than that of the other samples studied. The ORAC values of strawberry powder and GSPE were higher than cranberry, elderberry or raspberry seed but significantly lower than the other samples studied. Wild bilberry and blueberry extracts possessed the highest ORAC values. Each of the berry samples studied significantly inhibited both H2O2 as well as TNF alpha induced VEGF expression by the human keratinocytes. This effect was not shared by other antioxidants such as alpha-tocopherol or GSPE but was commonly shared by pure flavonoids. Matrigel assay using human dermal microvascular endothelial cells showed that edible berries impair angiogenesis.

Cyclooxygenase inhibitory and antioxidant cyanidin glycosides in cherries and berries.
Seeram NP, Momin RA, Nair MG, Bourquin LD. Phytomedicine 2001 Sep;8(5):362-9
Anthocyanins from tart cherries, Prunus cerasus L. (Rosaceae) cv. Balaton and Montmorency; sweet cherries, Prunus avium L. (Rosaceae); bilberries, Vaccinum myrtillus L. (Ericaceae); blackberries, Rubus sp. (Rosaceae); blueberries var. Jersey, Vaccinium corymbosum L. (Ericaceae); cranberries var. Early Black, Vaccinium macrocarpon Ait. (Ericaceae); elderberries, Sambucus canadensis (Caprifoliaceae); raspberries, Rubus idaeus (Rosaceae); and strawberries var. Honeoye, Fragaria x ananassa Duch. (Rosaceae), were investigated for cyclooxygenase inhibitory and antioxidant activities. The presence and levels of cyanidin-3-glucosylrutinoside 1 and cyanidin-3-rutinoside 2 were determined in the fruits using HPLC. The antioxidant activity of anthocyanins from cherries was comparable to the commercial antioxidants, tert-butylhydroquinone, butylated hydroxytoluene and butylated hydroxyanisole, and superior to vitamin E, at a test concentration of 125 microg/ml. Anthocyanins from raspberries and sweet cherries demonstrated 45% and 47% cyclooxygenase-I and cyclooxygenase-II inhibitory activities, respectively, when assayed at 125 microg/ml. The cyclooxygenase inhibitory activities of anthocyanins from these fruits were comparable to those of ibuprofen and naproxen at 10 microM concentrations. Anthocyanins 1 and 2 are present in both cherries and raspberry. The yields of pure anthocyanins 1 and 2 in 100 g Balaton and Montmorency tart cherries, sweet cherries and raspberries were 21, 16.5; 11, 5; 4.95, 21; and 4.65, 13.5 mg, respectively. Fresh blackberries and strawberries contained only anthocyanin 2 in yields of 24 and 22.5 mg/100 g, respectively. Anthocyanins 1 and 2 were not found in bilberries, blueberries, cranberries or elderberries.

A2E-epoxides damage DNA in retinal pigment epithelial cells. Antioxidants inhibit A2E-epoxide formation.
Sparrow JR, Vollmer-Snarr HR, Zhou J, Jang YP, Jockusch S, Itagaki Y, Nakanishi K J Biol Chem 2003, 19
The autofluorescent pigments that accumulate in retinal pigment epithelial cells with aging and in some retinal disorders, have been implicated in the etiology of macular degeneration. The major constituent is the fluorophore A2E, a pyridinium bisretinoid. Light-exposed A2E-laden RPE exhibit a propensity for apoptosis with light in the blue region of the spectrum being most damaging. Efforts to understand the events precipitating the death of the cells have revealed that during irradiation (430 nm), A2E self-generates singlet oxygen with the latter in turn reacting with A2E to generate epoxides at carbon-carbon double bonds. Here we demonstrate that A2E-epoxides, independent of singlet oxygen, exhibit reactivity towards DNA, with oxidative base changes being at least one of these lesions. Mass spectrometry revealed that the antioxidants vitamins E and C, butylated hydroxytoluene, resveratrol, a trolox analogue (PNU-83836-E) and bilberry extract, reduce A2E-epoxidation while single cell gel electrophoresis and cell viability studies revealed a corresponding reduction in the incidence of DNA damage and cell death. Vitamin E, a lipophilic antioxidant, produced a more pronounced decrease in A2E-epoxidation than vitamin C and treatment with both vitamins simultaneously did not confer additional benefit. Studies in which singlet oxygen was generated by endoperoxide in the presence of A2E, revealed that vitamin E, butylated hydroxytoluene, resveratrol, the trolox analogue and bilberry, reduced A2E-epoxidation by quenching singlet oxygen. Conversely, vitamin C and ginkgolide B were not efficient quenchers of singlet oxygen under these conditions.

 

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Traditional Use

As a dietary supplement and source of anthocyanins take 2 - 3 tablespoons a day. To increase bioavailability of nutrients place berries in a cup, add warm drinking water or milk, let steep for 1 - 2 h. Alternatively add water or milk and microwave for 30 - 60 sec. Mix with cereals, ice cream, yogurt etc.

To help combat diarrhea in children and adults and as astringent and anti-inflammatory oral treatment. A tea is made of 3 tablespoons of dried berries boiled in a quart of water for 10 min or steeped in a warm water for several hours. Take a cup every 3 - 4 hours until symptoms will improve. The same tea is used as a mouthwash to help treat gum inflammations and sores.

Bilberry berry tea is also considered a safe and efficient remedy against hemorrhoids. To this end the tea is taken during 3 - 4 weeks at a dose of 2 cups a day.

There are unconfirmed reports of positive effect of Bilberry berries in the treatment of Type 2 diabetes, however we were not able to find any documented evidences or clinical trials conducted to this end. Assuming high safety of this supplement hopefully the funds will become available to conduct a reliable clinical trial.

Considering side effects, there is no known reason to be afraid of the overdose of the berries or berry tea. If fact, in places where Bilberry grows, it is considered quite healthy to eat 2 - 3 LB of fresh berries a day during the harvesting season. In the Northern Europe in old times doctors used to prescribe Bilberry diet to patients with circulatory or visual conditions, the diet included 2 LB of fresh Bilberry per day during a month.

The tea made of Bilberry leaf (usually about two tea spoons per cup of boiling water) was used for similar purposes (mostly in adults), and also to help combat upset stomach, cough, skin inflammatory conditions. Another traditional application of leaf tea is to help improve sugar metabolism - it is believed to contain ingredients helpful for the treatment of type II diabetes. Bilberry leaf tea, when used continuously at excessively high doses may cause symptoms of poisoning due to high content of hydrohynons. Symptoms are reversible with discontinuation of the treatment. Floraleads Gr offers two herbal teas with Bilberry leaf: tea Rousseau and Propancra. Please review at the Tea section of retail web site.

Traditional Bilberry Supplements

Bilberry for tea - Bilberry berry tea is rich natural source of anthocyanosides, antioxidant flavonoids with beneficial effects on circulatory system. Bilberry tea is a delicious refreshing healthy drink and may be used both hot or cold.

Sustainol
- Traditional herbal supplement used ages ago, in particular to prevent nutrients deficiencies during cold winter time. Sustainol contains wide variety of active antioxidants in natural highly bioavailable form. It comprises herbs proven to be among richest natural sources of antioxidants, vitamins and other essential nutrients: Rose hips, Bilberry and Sea Buckthorn.


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