FWD 2 Expanded Commission E: Bilberry fruit

Herbal Medicine Expanded Commission E

Bilberry fruit

Latin Name: Vaccinium myrtillus
Pharmacopeial Name: Myrtilli fructus
Other Names: dwarf bilberry, European blueberry, huckleberry, whortleberry

Overview

Bilberry is a small deciduous shrublet found in underbrush and barren fields throughout central and northern Europe, northern Asia, and North America (Wichtl, 1996). In North America, it is found in montane and subalpine regions from British Columbia to Alberta, south to Arizona and New Mexico (Leung and Foster, 1996). The material of commerce is obtained from Albania, Poland, the former Yugoslavia, and the former U.S.S.R. (Wichtl and Bisset, 1994). The common name bilberry is derived from the Danish word bollebar, which means dark berry (Grieve, 1979).

Bilberry fruit has been used in traditional European medicine for nearly one thousand years (Morazzoni and Bombardelli, 1996), reported by twelfth century German herbalist Hildegarde von Bingen (1098-1179 C.E.) and later by sixteenth century herbalist Hieronymos Bock. Traditionally, strong decoctions of the dried fruit have been used as an astringent for treatment of diarrhea and dysentery (Bone and Morgan, 1997; Foster, 1996). Bilberry preparations were also administered to help stop the flow of breast milk, as well as to relieve scurvy and dysuria (Grieve, 1979). For these purposes, fruits were dried in the sun and eventually prepared as teas or syrups (Tyler, 1994).

In Germany, bilberry fruit is approved in the Commission E monographs (BAnz, 1998), listed in the German Drug Codex (DAC, 1986), and the tea form is official in the German Standard Licenses (Braun et al., 1997). Due to its tannin content, it is used internally to treat acute diarrhea, particularly in children, and externally to treat mild inflammation of oral mucous membranes. Bilberry is used as a component in a few astringent tea preparations (e.g., Stopftee Fides) (Wichtl and Bisset, 1994). A mother tincture (1:10) of the fresh, ripe fruit is also official in the German Homeopathic Pharmacopoeia (GHP, 1993). However, in other parts of Europe, particularly in Italy, fruit preparations are used to treat microcirculatory disorders, which include varicose veins, atherosclerosis, venous insufficiency, and degenerative retinal conditions, such as macular degeneration, glaucoma, and cataracts (Leung and Foster, 1996; Morazzoni and Bombardelli, 1996; Tyler, 1994). Possible mechanisms of action for its effects on ophthalmic conditions include its ability to protect against the breakdown of rhodopsin (retinal purple), a light sensitive pigment located in the rods of the retina, and its ability to regenerate rhodopsin. It may also provide vasoprotection by decreasing capillary fragility and permeability (Bone and Morgan, 1997; Regtop, 1998).

Bilberry anthocyanidins have demonstrated a variety of physiological effects. They may prevent angina episodes as exhibited by the prevention of lactate dehydrogenase liberation from cardiac isoenzymes in in vitro experiments (Leung and Foster, 1996). Retinal protection may be aided by anthocyanidinic retinal phosphoglucomutase and glucose-6-phosphatase inhibition (Cluzel et al., 1969). The anthocyanidins also stimulate prolonged capillary resistance, and are vasoprotective, antiedematous, and vasodilative (Lietti et al., 1976). They inhibit platelet aggregation and thrombus formation, interacting with vascular prostaglandins (Leung and Foster, 1996). In one study, an injected proprietary bilberry preparation altered the rhythmic changes in the diameter of mouse cheek pouch and terminal arterioles, which was beneficial to microvascular blood flow and interstitial fluid formation (Colantuoni et al., 1991). These findings, however, have largely employed animal or in vitro conditions, and have not been replicated with well-designed human trials (Tyler, 1994).

Several human clinical studies have been found in the literature investigating possible new uses for bilberry not mentioned in the Commission E monograph, particularly visual dysfunctions, including those caused by impaired microcirculation and diabetes mellitus. Bilberry fruit preparations have been investigated for their effects on vision acuity in dim light (Jayle and Aubert, 1964), on patients with pigmentary retinitis when taken with beta-carotene (Fiorini et al., 1965), on night vision in normal subjects (Jayle et al., 1965), on patients with diabetic retinopathy when taken in combination with beta-carotene (Sevin and Cuendet, 1966), on patients with significant hemeralopia (diminished vision in bright light) (Zavarise, 1968), on patients with macular degeneration, diabetic retinopathy, retinal inflammation, or retinitis pigmentosa (Neumann, 1971), and on patients with progressive myopia (Politzer, 1977). Later research investigated bilberry's capillarotropic activity in patients with venous diseases (Ghiringhelli et al., 1978) and in diabetic patients with microangiopathy (Lagrue et al., 1979) and microcirculatory function in patients with various retinopathies (Scharrer and Ober, 1981), myopia, glaucoma, or retinitis pigmentosa (Caselli, 1985), diabetic and/or hypertensive retinopathy (Perossini et al., 1987), and polyneuritis due to vascular insufficiency (Pennarola et al., 1980). Additional studies also investigated bilberry's effects on the progression of cataract formation in patients with senile cortical cataracts when taken in combination with vitamin E (Bravetti, 1989).

German pharmacopeial grade bilberry fruit consists of the whole, dried, ripe fruit of Vaccinium myrtillus L. An identity test is described wherein the fruit is first extracted with water, in order to extract the invert sugars. Subsequently, the anthocyanin glycosides are extracted with methanol. The anthocyanidins are then obtained by hydrolysis with hydrochloric acid (DAC, 1986; Wichtl, 1996). Macroscopic and microscopic examinations are carried out as well as a thin-layer chromatography (TLC) test for detection of anthocyan pigments. A test for adulteration with the fruit of bog bilberry (V. uliginosum L.) is carried out (DAC, 1986; Wichtl and Bisset, 1994; Wichtl, 1996). As bilberry is typically used in its whole form, macroscopic verification is the most essential requirement (Wichtl and Bisset, 1994). The Austrian Pharmacopoeia requires that it contain not less than 50% water-soluble extractive ( AB, 1983; Wichtl and Bisset, 1994). Additionally, the Swiss Pharmacopoeia requires that it contain not less than 1.5% tannins (Ph.Helv.VII, 1987; Wichtl and Bisset, 1994).

Description

Bilberry consists of the dried, ripe fruit of V. myrtillus L. [Fam. Ericaceae], and its preparations in effective dosage. The fruit contains tannins, anthocyanins, and flavonoid glycosides.

Chemistry and Pharmacology

Bilberry fruit contains 5-10% catechin tannins; approximately 30% invert sugar; over 1% fruit acids (Wichtl, 1996); flavonol glycosides including astragalin, hyperoside, isoquercitrin, and quercitrin; phenolic acids (e.g., caffeic and chlorogenic acids) (Azar et al., 1987; Friedrich and Schönert, 1973); pectins; triterpenes (0.25% ursol acid); polyphenols (0.5% anthocyans) (Hänsel et al., 1992-1994; Meyer-Buchtela, 1999), such as the procyanidins B1-B4 (Leung and Foster, 1996; Morazzoni and Bombardelli, 1996), and particularly the anthocyanidins malvidin, cyanidin, and delphinidin (Wichtl, 1996) bonded to one of three carbohydrates (e.g., glucose, galactose, arabinose) (Barrette, 1999), for example, delphinidine-3-O-arabinoside, delphinidine-3-O-galactoside, and delphinidine-3-O-glucoside. The anthocyanosides (anthocyanins) are aglycones bound to one of three glycosides (Cunio, 1993). The anthocyanoside content increases as the fruit ripens whereas the catechin tannins and dimeric proanthocyanidins (B1-B4) decrease with the progression of ripeness (Morazzoni and Bombardelli, 1996).

The Commission E reported astringent activity.

Bilberry has shown vasoprotective, antiedematous, antioxidant, anti-inflammatory, and astringent actions (Bone and Morgan, 1997). It has demonstrated free radical scavenging and inhibition of cAMP phosphodiesterase actions (Bruneton, 1995; Ferretti et al., 1988). In vitro and in vivo clinical studies show platelet aggregation and stimulation of vascular prostacyclin. Preliminary human trials indicate vasoprotective properties. Bilberry anthocyanins regenerate rhodopsin and are indicated in treatment of poor night vision, macular degeneration, glaucoma, and cataracts (Bruneton, 1995).

Uses

The Commission E approved the internal use of bilberry to treat non-specific, acute diarrhea, and local therapy for mild inflammation of the mucous membranes of mouth and throat.

The German Standard License indicates the use of bilberry fruit tea as a supportive therapy in the treatment of acute, non-specific diarrhea in children and adults (Braun et al., 1997; Wichtl and Bisset, 1994). Bilberry fruit extracts may offer symptomatic relief for vascular disorders including capillary weakness, venous insufficiency, and hemorrhoids. It is also used as a secondary treatment for spasmodic colitis (Bruneton, 1995).

Contraindications

None known.

Side Effects

None known.

Use During Pregnancy and Lactation

No restrictions known.

Interactions with Other Drugs

None known.

Dosage and Administration

Unless otherwise prescribed: 20-60 g of dried ripe fruit per day for infusions or decoctions, as well as other galenical preparations for internal use.

External: 10% decoction or equivalent preparations for local application.

Internal:

[Note: According to the Austrian Pharmacopeia, the average single dose for bilberry fruit is 5 g (Meyer-Buchtela, 1999; ÖAB, 1991).]

Dried fruit: 4-8 g taken with water, several times daily (Braun et al., 1997; Meyer-Buchtela, 1999; Wichtl and Bisset, 1994).

Decoction: Place 5-10 g crushed dried fruit in 150 ml cold water, bring to a boil for approximately 10 minutes, then strain while hot. Drink cold several times daily until the diarrhea is gone (Braun et al., 1997; Meyer-Buchtela, 1999; Wichtl and Bisset, 1994).

Cold macerate: Soak 5-10 g crushed dried fruit in 150 ml cold water for two hours, allowing the fruit to swell. Drink cold several times daily (Braun et al., 1997; Meyer-Buchtela, 1999; Wichtl and Bisset, 1994).

Fluidextract 1:1 (g/ml): 2-4 ml, three times daily (Anderhuber, 1991; Cunio, 1993).

Dry extract (25% anthocyanosides): 80-160 mg, three times daily (Foster, 1996; Pizzorno and Murray, 1992).

External:

Decoction: Place 5-10 g crushed dried fruit in 150 ml cold water, bring to a boil for approximately 10 minutes, then strain while hot (Meyer-Buchtela, 1999; Wichtl and Bisset, 1994).

Gargle mouthwash: Containing 10% decoction.

Duration of administration: If diarrhea persists for more than 3 to 4 days, consult a physician.

References

Anderhuber, R. 1991. Vaccinium myrtillus. Aust J Med Herbalism 3:13-14.

Azar, M., E. Verette, S. Brun. 1987. Identification of some phenolic compounds in bilberry juice Vaccinium myrtillus.J Food Sci 52(5):1255-1257.

BAnz. See Bundesanzeiger.

Barrette, E.P. 1999. Bilberry fruit extract for night vision. Alternative Medicine Alert 2(2):20-21.

Bone, K. and M. Morgan. 1997. BilberryThe Vision Herb. MediHerb Professional Review 59:14.

Braun, R. et al. 1997. Standardzulassungen für Fertigarzneimittel—Text and Kommentar. Stuttgart: Deutscher Apotheker Verlag.

Bravetti, G. 1989. Preventive medical treatment of senile cataract with vitamin E and anthocyanosides: clinical evaluation. Ann Ottalmol Clin Ocul 115:109.

Bruneton, J. 1995. Pharmacognosy, Phytochemistry, Medicinal Plants. Paris: Lavoisier Publishing.

Bundesanzeiger (BAnz). 1998. Monographien der Kommission E (Zulassungs- und Aufbereitungskommission am BGA für den humanmed. Bereich, phytotherapeutische Therapierichtung und Stoffgruppe). Köln: Bundesgesundheitsamt (BGA).

Caselli, L. 1985. Studio clinico ed elettroretinografico sull'attivita degli antocianosidi [Clinical and electroretinographic study on activity of anthocyanosides]. Arch Med Int (Parma) 37:29-35.

Cluzel, C., P. Bastide, P. Tronche. 1969. [Phosphoglucomutase and glucose-6-phosphatase activities of the retina and anthocyanoside extracts from Vaccinium myrtillus (study in vitro and in vivo)] [In French]. C R Seances Soc Biol Fil 163(1):147-150.

Colantuoni, A., S. Bertuglia, M.J. Magistretti, L. Donato. 1991. Effects of Vaccinium myrtillus anthocyanosides on arterial vasomation. Arzneimforsch 41(9):905-909.

Cunio, L. 1993. Vaccinium myrtillus. Aust J Med Herbalism 5(4):81-85.

Deutscher Arzneimittel-Codex (DAC). 1986. Stuttgart: Deutscher Apotheker Verlag.

Ferretti, C., M.J. Magistretti, A. Robotti, P. Ghi, E. Genazzani. 1988. Vaccinium myrtillus anthocyanosides are inhibitors of cAMP and cGMP phosphodiesterases. Pharm Res Comm 20(11):150.

Fiorini, G., A. Biancacci, F.M. Graziano. 1965. Modificazioni perimetriche ed adattometriche dopo ingestione di mirtillina associata a beta-carotene [Perimetric and adaptometric modifications after ingestion of myrtillin associated with beta-carotene]. Ann Ottalmol Clin Ocul 91(6):371-386.

Foster, S. 1996. Bilberry: A Long History. Health Food Business. August 1996: 40.

Friedrich, V.H. and J. Schnert. 1973. Untersuchungen über einige Inhaltsstoffe der Blätter und Früchte von Vaccinium myrtillus [Phytochemical investigation of leaves and fruits of Vaccinium myrtillus]. Planta Med 24(1):90100.

German Homeopathic Pharmacopoeia (GHP). 1993. Translation of the Deutsches Homopathisches Arzneibuch (HAB 1), 1st ed., 5th suppl. 1991. Stuttgart: Deutscher Apotheker Verlag. 383384.

Ghiringhelli, C., F. Gregoratti, F. Marastoni. 1978. Attivita capillarotrop di antocianosidi and alto dosaggio nella stasi da flebopatia [Capillarotropic activity of anthocyanosides in high doses in phlebopathic statis]. Minerva Cardioangiol 26(4):255-276.

Grieve, M. 1979. A Modern Herbal. New York: Dover Publications, Inc.

Hänsel, R., K. Keller, H. Rimpler, G. Schneider (eds.). 19921994. Hagers Handbuch der Pharmazeutischen Praxis, 5th ed. Vol. 46. Berlin-Heidelberg: Springer Verlag.

Jayle, G.E. and L. Aubert. 1964. [Action des glucosides d'anthocyanes sur la vision scotopique et mesopique du sujet normal] [In French]. Therapie 19:171.

Jayle, G.E. et al. 1965. [Study concerning the action of anthocyanoside extracts of Vaccinium Myrtillus on night vision] [In French]. Ann Ocul (Paris) 198(6):556-562.

Lagrue, G. et al. 1979. Pathology of the microcirculation in diabetes and alterations of the biosynthesis of intracellular matrix molecules. Front Matrix Biol S Karger 7:324-325.

Leung, A.Y. and S. Foster. 1996. Encyclopedia of Common Natural Ingredients Used in Food, Drugs, and Cosmetics, 2nd ed. New York: John Wiley & Sons, Inc. 84-85.

Lietti, A., A. Cristoni, M. Picci. 1976. Studies on Vaccinium myrtillus anthocyanosides. I. Vasoprotective and antiinflammatory activity. Arzneimforsch 26(5):829-832.

Meyer-Buchtela, E. 1999. Tee-Rezepturen—Ein Handbuch für Apotheker und Ärzte. Stuttgart: Deutscher Apotheker Verlag.

Morazzoni, P. and E. Bombardelli. 1996. Vaccinium myrtillus L. Fitoterapia 67(1):329.

Neumann, L. 1971. Therapeutische Versuche mit Anthozyanosiden bei Langzeitbehandlungen in der Augenheilkunde [In German]. Klin Monatsbl Augenheilkd 158:592-597.

Österreichisches Arzneibuch, 1st suppl. (ÖAB). 1983. Wien: Verlag der Österreichischen Staatsdruckerei.


Österreichisches Arzneibuch (ÖAB). 1991. Wien: Verlag der Österreichischen Staatsdruckerei.

Pennarola, R. et al. 1980. The therapeutic action of the anthocyanosides in microcirculatory changes due to adhesive-induced polyneuritis. Gazz Med Ital 139:485-491.

Perossini, M. et al. 1987. Diabetic and hypertensive retinopathy therapy with Vaccinium myrtillus anthocyanosides (Tegens): Double blind placebo controlled clinical trial. Ann Ottalmol Clin Ocul 113:1173.

Pharmacopoeia Helvetica, 7th ed. Vol. 1-4.(Ph.Helv.VII). 1987. Bern: Office Central Fédéral des Imprimés et du Matériel.

Pizzorno, J.E. and M.T. Murray. 1992. A Textbook of Natural Medicine. Seattle, WA: Bastyr University Publications.

Politzer, M. 1977. [Experiences in the medical treatment of progressive myopia] [In German]. Klin Monatsbl Augenheilkd 171(4):616-619.

Regtop, H. 1998. Age related macular degeneration. Aust J Med Herbalism 10(2):38-45.

Scharrer, A. and M. Ober. 1981. Anthocyanoside in der Behandlung von Retinopathien [Anthocyanosides in the treatment of retinopathies] [In German]. Klin Monatsbl Augenheilkd 178(5):368-389.

Sevin, R. and J.F. Cuendet. 1966. Effets d'une association d'anthocyanosides de myrtille et de beta-carotene sur la resistance capillaire des diabetiques [In French]. Ophthalmologica 152:109-117.

Tyler, V.E. 1994. Herbs of Choice: The Therapeutic Use of Phytomedicinals. New York: Pharmaceutical Products Press.

Wichtl, M. and N.G. Bisset (eds.). 1994. Herbal Drugs and Phytopharmaceuticals. Stuttgart: Medpharm Scientific Publishers. 351-352.

Wichtl, M. 1996. Monographien—Kommentar. In: Braun, R. et al. 1997. Standardzulassungen für Fertigarzneimittel—Text and Kommentar. Stuttgart: Deutscher Apotheker Verlag.

Zavarise, G. 1968. Sull'effetto del trattamento prolungato con antocianosidi sul senso luminoso [Effect of prolonged treatment with anthocyanosides on light senstivity]. Ann Ottalmol Clin Ocul 94(2):209-214.

Additional Resources

Alexeeff, T. 1998. Circulatory insufficiency: a historical and modern review of three classic herbs. Aust J Med Herbalism 10(4):135-140.

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

Benninger, J. 1997. Understanding Bilberry. Health Supplement Retailer. March 1997: 54.

Bettini, V. et al. 1984. Interactions between Vaccinium myrtillus anthocyanosides and serotonin on splenic artery smooth muscle. Fitoterapia 55(4):201-208.

———. 1984. Interactions between Vaccinium myrtillus anthocyanosides on vascular smooth muscle. Fitoterapia 55(5):265-272.

Bomser, J., D.L. Madhavi, K. Singletary, M.A. Smith. 1996. In vitro anti-cancer activity of fruit extracts from Vaccinium species. Planta Med 62(3):212-216.

Der Marderosian, A. (ed.). 1999. The Review of Natural Products. St. Louis: Facts and Comparisons.

Detre, Z., H. Jellinek, R. Miskulin. 1986. Studies on vascular permeability in hypertension: action of anthocyanosides. Clin Physiol Biochem 4(2):143-149.

Mian, E. et al. 1977. Anthocyanosides and microvessel walls: new findings on the mechanism of action of their protective effect in syndromes due to abnormal capillary fragility. Min Med 68:35-65.

Morazzoni, P. and M.J. Magistretti. 1990. Activity of bilberry, an anthocyanoside complex from Vaccinium myrtillus (VMA), on platelet aggregation and adhesiveness. Fitoterapia 61(1):13-21.

Orsucci, P.L. et al. 1983. Treatment of diabetic retinopathy with anthocyanosides: a preliminary report. Clin Oc 5:377.

Repossi, P., R. Malagola, C. De Cadilhac. 1987. The role of anthocyanosides on vascular permeability in diabetic retinopathy. Ann Ottalmol Clin Ocul 357.

Wichtl, M. (ed.). 1989. Teedrogen, 2nd ed. Stuttgart: Wissenschaftliche Verlagsgesellschaft.

This material was adapted from The Complete German Commission E Monographs—Therapeutic Guide to Herbal Medicines. M. Blumenthal, W.R. Busse, A. Goldberg, J. Gruenwald, T. Hall, C.W. Riggins, R.S. Rister (eds.) S. Klein and R.S. Rister (trans.). 1998. Austin: American Botanical Council; Boston: Integrative Medicine Communications.

1) The Overview section is new information.

2) Description, Chemistry and Pharmacology, Uses, Contraindications, Side Effects, Interactions with Other Drugs, and Dosage sections have been drawn from the original work. Additional information has been added in some or all of these sections, as noted with references.

3) The dosage for equivalent preparations (tea infusion, fluidextract, and tincture) have been provided based on the following example:

  • Unless otherwise prescribed: 2 g per day of [powdered, crushed, cut or whole] [plant part]
  • Infusion: 2 g in 150 ml of water
  • Fluidextract 1:1 (g/ml): 2 ml
  • Tincture 1:5 (g/ml): 10 ml

4) The References and Additional Resources sections are new sections. Additional Resources are not cited in the monograph but are included for research purposes.

This monograph, published by the Commission E in 1994, was modified based on new scientific research. It contains more extensive pharmacological and therapeutic information taken directly from the Commission E.

Excerpt from Herbal Medicine: Expanded Commission E Monographs
Copyright 2000 American Botanical Council
Published by Integrative Medicine Communications
Available from the American Botanical Council.