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Bilberry

Botanical Description & Habitat

Vaccinium myrtillus

Family
Ericaceae

Habitat
Europe

Medicinal Parts
The berry

Historical Properties & Uses

Bilberry fruit has been a popular source of fresh jam for hundreds of years. The berry is a native of northern Europe and Asia. The nearest American counterpart is the huckleberry. Both the leaves and berries of the bilberry bush have been used medicinally, but it is the berry in particular that has yielded the most promising therapeutic data.

One of the most startling folk/clinical uses for bilberry fruit occurred during World War II when RAF pilots swore that the intake of bilberry jam prior to night missions significantly improved dark adaptation and visual acuity. Following the war such reports stimulated considerable research interest in bilberry both in Europe and in South America.

Over the course of several years, studies were published implicating bilberry fruit extract in the effective treatment of a variety of visual problems including night blindness (nyctalopia), visual fatigue from prolonged reading and working under dimly lit conditions, severe nearsightedness (myopia) and various vascular disturbances of the retina.

In Europe standardized bilberry extracts are listed as the primary ingredient in a wide range of proprietary over-the-counter preparations. Many of these are designed specifically for the treatment or relief of the various eye problems discussed. Others are recommended for disturbances of the central nervous system, and others for varicose veins, and so on. The medicine as become firmly established in European pharmacology.

European products usually contain secondary active ingredients such as: lecithin, citric acid, vitamin E, vitamin C, Vitamin A, aspartic acid, vitamin B-6, vitamin B-12, L-glutamine, and beta-carotene. Bilberry is often found in standardized anti-diabetic preparations, but not often as the primary ingredient.

This herb has not achieved approval status by the German Commission E. Either there was insufficient evidence in favor, or a contraindication.

References:

Blumenthal, M (Ed.): The Complete German Commission E Monographs: Therapeutic Guide to Herbal Medicines. American Botanical Council. Austin, TX. 1998.

Method of Action

Bilberry contains anthocyanosides (cyanidine, malvidine, delphynidine, petunidine and peonidiene, among others). Whole bilberry fruit extract in which the level of anthocyanosides has been standardized is preferable to isolated anthocyanosides. The standardized level of active principle should be no less than 15%. Compared to traditional dry bilberry extract with a maximum anthocyaniden content of 1-2 percent, the concentrate is appreciably more cost effective. This highly concentrated extract (with an extract/fresh fruit ratio of more than 1:100) allows precise manipulation of therapeutic dosages.

Only vaccinium myrtillus should be used. The North American blueberry (vaccinium myrtilloides) for example is unsuitable for standardized medicinal preparation or use.

Animal and laboratory studies have revealed much about how bilberry extract works. On the most basic level it increases the resistance of blood capillaries and reduces their permeability. On a more interesting level bilberry affects some major physiological processes. One of the most important of these is the visual apparatus. By accelerating the regeneration of retinal purple, bilberry anthocyanosides markedly affect the course of several visual disorders.

Anthocyanosides (pigmentary substances, as is rhodopsin) when administered intravenously to rabbits dramatically sped up the regeneration of rhodopsin and produced remarkably fast dark adaptation.

Other studies, some utilizing whole extract, others investigating isolated constituents, involving different species of animals, sometimes just isolated visual tissue, have found the same thing--considerable impact on visual purple.

Bilberry anthocyanosides also favorably affect the operation of crucial enzymes in the retinal cellular metabolism and function, such as glucose-6-phosphatase and phosphoglucomutase. Bilberry has shown important effects on blood capillary stability in tests utilizing the Ambrose and De Eds technique, which involves injecting a dyeing agent (normally blue) into a vein and rubbing the bare skin with chloroform. This produces a local irritation and subsequent spreading of the dye into tissues outside of the vein and capillaries.

The rapidity with which the skin turns blue is a measure of the permeability (or leakiness) of the vessels. Bioflavonoid which decrease the permeability of blood vessels are known collectively as vitamin P. In one test comparing bilberry anthocyanosides against the best known vitamin P factors, bilberry demonstrated greater intensity and duration of action than any of the others. In another experiment, bilberry extract was compared to Vitamin P in their respective effects on rhodopsin. Again, the bilberry was observed to be more effective.

In tests using a number of different species of animals, bilberry anthocyanosides significantly protected vassal walls against the application of vacuum suction, a technique that eventually leads to the total failure of surface vessels.

Likewise, in another measure of capillary protection--the inhibition of experimentally induced edema bilberry has been shown to be very effective.

Highly technical experiments in animals and isolated tissues have demonstrated the ability of bilberry anthocyanosides to protect the blood-brain barrier through a process similar to that exhibited by centella.

Further research is needed to explore the implications of these findings.

In other pre-clinical trials bilberry anthocyanosides have been shown to possess the following kinds of activity:

1. Protection of the heart against the stress of prolonged exposure to swimming as measured by activation of the crucial enzyme lactic dehydrogenase as well as other cardiac enzymes. Other cardio-protective actions of bilberry have been reported.

2. Possession of good anti-inflammatory activity.

3. Inhibition of cholesterol-induced atherosclerosis.

4. Modest inhibition of serum platelet aggregation, thus possessing some anti-thrombotic potential.

Ophthalmology
Bilberry fruit extract has been used successfully to treat some specific and rather esoteric ophthalmic conditions such as night blindness, severe myopia, retinal disturbances of various kinds and chronic visual fatigue.

People whose jobs make heavy demands on the visual apparatus have responded well to bilberry treatment. These include airline pilots, air-traffic controllers, car and truck drivers, students, computer terminal operators, navigators, watch makers (and similar professions) and sportsmen of various kinds.

Results of the first controlled clinical study confirmed the anecdotes in every particular: dark adaptation was significantly accelerated following prolonged exposure to bright light, and some improvement in visual acuity in dim light was observed in experimental subjects. The most obvious effects were observed during the first fours following ingestion of a single dose of the product; most all effects had worn-off after 24 hours.

Almost identical results were obtained in other early studies. Again normal healthy subjects were used, and a similar effect on retinal sensitivity to light was observed.

Much early clinical work used patients with various kinds of retinal disorders as subjects, mostly patients with pigmentary retinitis. Results similar to those observed in healthy subjects were obtained: enlargement of the range of vision as well as a more responsive adaptation.

It was the opinion of many investigators to observe such results in diseased patients was a truly remarkable phenomenon.

The opposite of nyctalopia is hemeralopia, or day blindness, a condition in which night vision is substantially normal, but day vision is greatly reduced, often to the point of total blindness. By the second day of treatment with bilberry, an improvement in retinal luminous sensitivity was observed in many of these patients.

Significant improvement remained constant throughout the following three months of treatment, and then gradually diminished during a subsequent period during which the product was withdrawn. Then, after treatment was reinstated, improved visual adaptation and acuity were once again observed. No side-effects of any kind were reported during the entire period of the study. The findings of this study have been replicated at least once.

Vascular disorders
As researchers gradually became aware of the true mechanism of action of bilberry anthocyanoside, they became more and more curious about how this substance would affect the course of other disorders involving faulty vascularity. A series of experiments and detailed studies followed.

In one study, patients with blood purpuras and various central nervous system circulation problems were successful treated, as were patients suffering from anti-coagulating problems and varicose veins.

On another occasion, as part of a doctoral dissertation, bilberry anthocyanosides (then still a very new product) were used to treat 124 cases of various arterial and venous problems and 10 cases of capillary fragility. The results were generally very satisfactory.

An in-depth investigation of the effects of bilberry in patients suffering from marked hyperpermeability of the capillaries found that the treatment effectively restored ionic balance to blood vessel walls and eliminated the leaks that were allowing plasmatic proteins to dangerously distribute on both sides of the membranes.

Further studies have found good results in the treatment of conditions ranging from phlebitis to hypertension as long as they involved breakdown of capillary walls (hyperpermeability or fragility). Even capillary fragility associated with advanced diabetes was susceptible to bilberry extract.

Interestingly, several of the referenced studies reported a synergistic action between bilberry anthocyanosides and beta-carotene. Bilberry anthocyanosides can have a beneficial effect in persons suffering from the rupture and breakdown of increasingly fragile capillaries in the glomerulus (filtering unit) of the kidneys. Many patients exhibiting hematuria experience a significant improvement while using bilberry. Others do not improve.

Researchers believe the chances for improvement are related to the seriousness and stage of the underlying disease. The more serious the disease and the more advanced the stage, the less likely bilberry extract will have an observable effect.

In obstetrics, pregnant women suffering from varices and various blood troubles have been treated with anthocyanosides. A combination of bilberry anthocyanosides and vitamin E has proven very effective and seems to be well tolerated; no side effects occur in either mother or infant.

Drug Interactions & Precautions

Possible Interactions
The anti-inflammatory activity of bilberry can be seriously inhibited by phenobarbital and certain other sedatives and hypnotics, such as chloral hydrate and meprobamate, as well as beta-adrenergic blocking agents (propranolol).

Colchicine may increase sensitivity or enhance the response to this herb.

The antiarrhythmic agent, quinidine, may increase the hypoprothrombinemic effect of bilberry.

Comments
Due to the presence of blood serum platelet aggregation inhibitors, such as linolenic acid, this herb may potentiate the effects of anticoagulant drugs such as heparin.

Safety Factors & Toxicity

Anthocyanosides have been shown to be completely non-toxic when administered in the normal manner, i.e., orally. In toxicity tests on mice and rats, no toxicity was observed when the anthocyanosides were administered orally.

Intraperitoneal and intravenous administration produced LD50s of very high values, again validating the low toxicity of the product. Since the preferred route of administration is oral, no toxicity should be expected.

The German Commission E notes the possibility for intoxication with a high, or chronic dose of the leaf.

This herb (specifically the fruit) has approval status by the German Commission E.

The German Commission E recommends a limited duration for the use of this herb of 3 - 4 days if diarrhea persists.

References:

Blumenthal, M (Ed.): The Complete German Commission E Monographs: Therapeutic Guide to Herbal Medicines. American Botanical Council. Austin, TX. 1998.


Preparation & Administration

Guaranteed potency bilberry is available in capsule form

Use 2-4 25mg capsules daily

This herb has approval status by the German Commission E regarding these specific pharmacological actions: for diarrhea and mild inflammation of the mouth and throat.

Daily dosages are as follows:

20 - 60 g

References:

Blumenthal, M (Ed.): The Complete German Commission E Monographs: Therapeutic Guide to Herbal Medicines. American Botanical Council. Austin, TX. 1998.

Note: This Herbal Preparation information is a summary of data from books and articles by various authors. It is not intended to replace the advice or attention of health care professionals.

References

Ala El Din Barradah, M., I. Shourkry & M. Hegazy. Difrarel 100 in the treatment of retinal vascular disorders and high myopia. Bull. Ophth. Soc. Egypt, 60, 251, 1967.

Alfieri, R & P. Sole. Influence des anthocyanosides administres par voie parenterale sur l'adaptoelectroretinogramme du lapin. C.R. Soc. Biol., 158, 2338, 1964.

Alfieri, R. & P. Sole. Influence des anthocyanosides administres par voie oroperilinguale sur l'adapto-electroretinogramme (AERG) en lumiere rouge chez l'homme. C.R. Soc. Biol. 160, 1590, 1966.

Alfieri, R., P. Sole & F. Rouher. Action et mecanisme des anthocyanosides dans la vision nocturne.Vie Medic., dic. 1969.

Bailliart, J. Tentative d'amelioration de la vision nocturne. Le Medicin de Reserve, 121, 1969.

Bastide, Rouher & Tronche. Rhodosine et anthocyanosides. A propos de quelques faits experimentaux. Bull.Soc. Ophtalm. Fran., 68, 801, 1968.

Bastide, Rouher & Tronche. Aspects pharmacologiques de quelques facteurs de protection vasculaire. Bull. Soc. Pharm. Marseille, 17, 209, 1968.

Baudon, Bruhat, Plane & Hermabessiere. Utilisation d'une association d'angio-protecteur et de vitamine E. Lyon Medit. Medical, 46, ott. 1969.

Belleoud, L., D. Leluan & Y. Boyer. Etude des effets des glucosides d'anthocyanes sur la vision nocturne des controleurs d'approche d'aerodrome. Rev. Med. Aero. Spat., 5, 45, 1966.

Belleoud, L, D. Leluan & Y. Boyer. Etude des effets des glucosides d'anthocyanes sur al vision nocturne du personnel navigant. Rev. Med. Aero. Spat., 6, 5, 1967.

Blumenthal, M (Ed.): The Complete German Commission E Monographs: Therapeutic Guide to Herbal Medicines. American Botanical Council. Austin, TX. 1998.

Bomser, J. et al: In vitro anticancer activity of fruit extracts from Vaccinium species. Planta Med. 1996, 62(3): 212 - 216.

Bonacina, F. & F. Pacchiano. Attivita complementare degli antocianosidi in un preparato ad azione antiedemigena e capillaro-protettiva. Boll, Chim. Farm., 113, 540, 1974.

Bonacina, F., G. Galliani & F. Pacciano. Attivita degli antocianosidi nei processi flogistici acuti. Farmaco, ed. pr., 28, 428, 1973.

Bottecchia, D., Bettini, V., Martino, R., Camerra, G. Preliminary report on the inhibitory effect of Vaccinium myrtillus anthocyanosides on platelet aggregation and clot retraction. Fitoterapia 58 (1987): 3-8.

Bravetti, G.O., Fraboni, E., Maccolini, E. Preventive medical treatment of senile cataract with vitamin E and Vaccinium myrtillus anthocyanosides. Clinical Evalu Ann Ottalmol Clin Ocul II 5 (1989): 109-116.

Chevaleraud, J. & G. Perdriel. Peut-on ameliorer la vision nocturne des aviateurs. Gaz. Med. de France, 18, 25 June 1968.

Cluzel, C., P. Bastide & P. Tronche. Activites phosphoglucomutasique et glucose-6-phosphatasique de la retine et anthocyanosides extraits de vaccinium myrtillus. C.R. Soc. Biol., 163, 147, 1969.

Cluzel, C., P. Bastide, R. Wegman & P. Tronche. Activites enzymatiques de la retine et anthocyanosides extraits de vaccinium myrtillus. Biochem. Pharm., 19, 2295, 1970.

Coget, J. & J.F. Merlen. Etude clinique d'un nouvel agent de protection vasculaire, le Difrarel 20, compose d'anthocyanosides isoles de vaccinium myrtillus. Phlebologie, 2, 221, 1968.

Criado, M.T, et al. I.R.C.S. Medical Sci. 11 (1983): 286. Cristoni, A., Magistretti, M. Antiulcer and healing activity of Vaccinium myrtillus anthocyanosides. Farmaco [Ed Prat] 42 (1987): 29-43.

Cuvelier, R., J. Terrasse, C. Derycke, G. Andraud & J. Aublet-Cuvelier. Essai d'appreciation par le test de landis de l'action sur les capillaires d'un complexe anthocianique. Clermont Med., 63, 61, 1966.

Demure, G. Etude experimentale et clinique d'un nouveau facteur vitaminique P: les anthocynosides. These Medicine Clermont, 1964.

Detre Z et al., Studies on vascular permeability in hypertension: action of anthocyanosides. Clin. Physiol. Biochem. 1986, 4(2):143.

Fiorini, G., A. Bianacci & F. Graziano. Modificazioni perimetriche ed adattometriche dopo ingestione di mirtillina associata a beta-carotene. Ann. Ottalm. Clin. Ocul., 91, 371,1965.

Gil Del Rio. Los antocianosidos del vaccinium myrtillus en oftalmologia. Arch. Soc. Oftal. Hisp.-Amer., 26, 969, 1966.

Gomez-Serranillos, F., F. Zaragoza & P. Alvarez. Efectos sobre la agregacion plaquetaria 'in vitro' de los antocianosidos del vaccinium myrtillus L. An. R. Acad. Farm., 49, 79, 1983.

Goria, E. & A. Peria. Effetto degli antocianosidi sulla soglia visiva assoluta. Ann. Ottalm. Clin. Ocul., 92, 595,1966.

Guermonprez, J.L. & M. Miltgen. Action des anthocyanosides de vaccinium myrtillus sure la resistance capillaire chez l'hypertendu et la diabetique (a propos de 40 observations). Vie Med., avril 1972/73.

Jayle, G.E., M. Aubry, M. Gavini, G. Braccini. Etude concernant l'action sur al vision nocturne des anthocyanosides extraits de vaccinum myrtillus. Ann. Ocul. (Paris), 198, 556,1965.

Jayle, G.E. & Aubert, L. Action des glucosides d'anthocyanes sur la vision scotopique et mesopique du sujet normal. Therapie, 19, 171, 1964.

Jonadet, M., M.T. Meumier & P. Bastide. Anthocyanosides extraits de vitis vinifera, de vaccinium myrtillus et de pinus maritimus. I. Activites inibitrices vis-a-vis de l'elastase in vitro. II. Activites angioprotectrice compares in vivo. J. Pharm. Belg., 38, 41, 1983.

Jueneman, G. Ueber die wirkung der anthozyanoside auf die hemeralopie nach chininintoxikation. Augenheilkunde, 151, 891, 1968.

Kadar, A., L. Robert, M. Miskulin, J. Tixier, D. Breachemier & A. Robert. Influence of anthocyanoside treatment on the cholesterol-induced atherosclerosis in the rabbit. Paroi Arter., 5, 18l, 1979.

Magnasco, A. & M. Zingirian. Influenza degli antocianosidi sulla soglia retinica differenziale mesopica. Ann. Ottal. Clin. Ocul., 92, 188, 1966.

Marcollet, M, P. Bastide, & P. Tronche. Effet angio- protecteur des anthocyanosides de vaccinium myrtillus objective vis-a-vis de la liberation de la lactate deshydrogenase (LDH) et de ses isoenzymers cardiaques chez le rat soumis a une epreuve de nage. C.R. Soc. Biol. 163, 1786, 1970.

Mercier, A., G. Perdriel & H. Carves. Note concernant l'activite des glucosides d'anthocyanes sure la vision scotopique et l'acuite visuelle mesopique des sujets normaux. Rev. Med. Aero., 13, 57, 1965.

Mercier, A., G. Perdriel, J. Rozier & J. Chevaleraud. Note concernant l'action des glucosides d'anthocyanes sur l'electroretinogramme humain. J. Bull. Soc. Ophtalm. Fr., 65, 1049, 1965.

Mowrey, Daniel B., Ph.D. Exper. Psych., Brigham Young University. Director of Nebo Institute of Herbal Sciences. Director of Behavior Change Agent Training Institute. Director of Research, Nova Corp.

Plazonnet, B., P. Bastide & P. Tronche. C.R. Soc. Biol., 162, 1490, 1968.

Pourrat, Bastide, Dorier, Pourrat & Tronche. Preparation et activite therapeutique de quelques glucosides d'anthocyanes. Chim. Therap., 2, 33, 1967.

Robert, A.M., G. Godeau, F. Moati & M. Miskulin. Action of anthocyanosides of vaccinium myrtillus on the permeability of the blood brain barrier. J. Med., 8, 321, 1977.

Romeuf, J.C. Essai clinique d'un facteur vitaminique P sur les hematuries microscopiques. These-Univ. Clermont-Fd., Faculte Mixte de Medicine et de Pharmacie, 1967.

Rouher, F. & P. Sole. Peut-on ameliorer la vision nocturnedes conducteurs automobiles. Ann. Med. Accidents Traffic, 3-4, 1965.

Scialdone, D. L'azione delle antocianine sul senso luminoso. Ann. Ottal. Clin. Ocul., 92, 43, 1966.

Sevin, R. & J.F. Cuendet. Effets d'une association d'anthocyanosides de myrtille et de beto-carotene sur la resistance capillaire des diabetiques. Opthalmologica, 152, 109, 1966.

Terrasse, J. & S. Moinade. Premiers resultats obtenus avec un nouveau facteur vitaminique P 'Les anthocyanosides' extraits du vaccinum myrtillus. Presse Med., 72, 397, 1964.

Thomas, C. & P. Barisain. L'action des anthocyanosides sur al fagilite des capillaires oculaire dans le diabete et l'hypertension arterielle. Bull. Soc. Ophtalm. Fran., 65, 212, 1965.

Tronche, P., P. Bastide, J. Komor. Effet des glucosides d'anthocyanes sur al cinetique de regeneration du pourpe retinien chez le lapin. C.R. Soc. Bul., 161, 2473, 1967.

Urso, G. Azione degli antocianosidi del vaccinium myrtillus associati a beta-carotene sulla sensibilita luminosa. Ann. Ottal. Clin. Ocul., 93, 931, 1968.

Volpi, U. & G. Bertoni. L'azione del 'pourpranyl' sulfa sinsibilita luminosa retinica del soggetto normale. Ann. Ottal. Clin. Ocul., 90, 492, 1964.

Zaragoza, G.F & P.A. De Llano. Estudio del efecto antiagregante de los antocianosidos del vaccinum myrtillus en conejos. An. Real. Acad. Farm. in press.

Zavarisse, G. Sull'effetto del trattamento prolungato con antocianosidi sul senso luminoso. Ann. Ottal. Clin. Ocul., 94, 209, 1968.

Multimedia

Vaccinium myrtillus

Bilberry 2.

Bilberry 3.

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