16 Herbal Medicine

BILBERRY FRUIT Latin Name: Vaccinium myrtil/us

Pharmacopeial Name: Myrtilli fructus

Other Names: dwarf bilberry, European blueberry, huckleberry, whortleberry

Overview Bilberry is a small deciduous shrublet fo und in underbrush and barren fi elds th roughout central and northern Europe, northern Asia, and North America (Wichtl , 1996). In North America, it is fo und in montane and subalpine regions from British Columbia to Alberta, south to Arizona and New M exico (Leung and Foster, 1996). The material of commerce is obtained from Albania, Poland, the for­mer Yugoslavia, and th e former U. S.S.R. (Wicht! and Bisset, 1994) . The common name bil berry is derived from the Danish word bollebar, which means dark berry (Grieve, 1979).

Bilberry fruit has been used in traditional European medicine fo r nearl y one thousand years (Morazzoni and Bombardelli, 1996), reported by twelfth century Germ an herbalist Hildegarde von Bingen (1098-11 79 C.E.) and later by sixteenth century herbalist Hieronymos Bock. Traditionally, strong decoctions of the dried fruit have been used as an astringent fo r treatment of diarrhea and dysentery (Bone and M organ, 1997; Foster, 1996). Bilberry preparations were also admini stered 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 th e 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 fo rm is official in the German Standard Licenses (Braun et aI. , 1997). Due to its tannin content, it is used internall y to treat acute di arrhea, particul arly in children, and externally to treat mild inflammation of oral muco us membra nes. Bilberry is used as a compo­nent in a few astringent tea preparati ons (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). H owever, in other parts of Europe, particularly in Italy, fr uit preparati ons are used to treat microcirculatory disord ers, which include varicose ve ins, ath erosclerosis, venous insufficiency, and degenerative retinal conditions, such as macular degenerati on, glaucoma, and cataracts (Leung and Foster, 1996; M orazzoni 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 th e rods of the retina, and its ability to regenerate rhodopsin . It may also provide vaso protection by decreasing capillary fragility and perm eability (Bone and M organ, 1997; Regtop, 1998 ).

Bilberry anthocyanidins have demonstrated a variety of physiological effects. They may prevent angina ep isodes as exhibited by the prevention of lactate dehy­drogenase liberation from cardiac isoenzy mes in in vitro experiments (Leung and Foster, 1996). Retin al protecti on may be aided by anthocyanidini c retinal phospho­glucomutase and glucose-6-phosphatase inhibiti on (Cluzel et aI. , 1969). The antho-

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Bilberry fruit 17

cyanidins also stimulate prolonged capillary resistance, and are vasoprotective, antiedematous, and vasodilative (Lietti et a!., 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 aI., 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 Gayle and Aubert, 1964), on patients with pigmentary retinitis when taken with beta-carotene (Fiorini et aI., 1965), on night vision in normal subjects Gayle et aI., 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 aI., 1978), diabetic patients with microangiopathy (Lagrue et aI., 1979), microcirculatory function in patients with polyneuritis due to vascular insufficiency (Pennarola et aI., 1980), patients with various retinopathies (Scharrer and Ober, 1981), patients with myopia, glaucoma, or retinitis pigmentosa (Caselli, 1985), patients with diabetic and/or hypertensive retinopathy (Perossini et aI., 1987), and its effects on the progression of cataract formation in patients with sen il e 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; Wicht! and Bisset, 1994; Wicht!, 1996). As bilberry is typically used in its whole form, macroscopic verification is the most essential requirement (Wicht! and Bisset, 1994). The Austrian Pharmacopoeia requires that it contain not less than 500/0 water-soluble extractive (OAB, 1983; Wicht! and Bisset, 1994). Additionall y, the Swiss Pharmacopoeia requires that it contain not less than 1.50/0 tannins (Ph.Helv.VII, 1987; Wicht! 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, anthocyan ins, and flavonoid glycosides.

Chemistry and Pharmacology Bilberry fruit contains 5-100/0 catechin tannins; approximately 300/0 invert sugar; over 1 % fruit acids (Wicht!, 1996); flavonol glycosides including astragalin , hyperoside, isoquercitrin, and quercitrin; phenolic acids (e.g., caf­feic and chlorogenic acids) (Azar et aI., 1987; Friedrich and Schonert, 1973);

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18 Herbal Medicine

pectins; tri te rpenes (0 .250/0 ursol acid) ; polyphenols (0 .5% anthocyans) (Hansel et aI. , 1992-1994 ; M eyer-Buchtela, 1999), such as the procyanidins BI-B4 (Leung and Foster, 1996; Morazzoni and Bombard elli, 1996), and parti cu­larly the anthocyanidins malvidin, cyanidin, and delphinidin (Wicht! , 1996) bonded to one of three carbohy­drates (e.g., glucose, ga lactose, arabi­nose) (Barre tte, 1999), for example, delphinidine-3-0-arabinoside, delphini ­dine-3-0 -ga lactoside, and delphinidine-3-0-glucoside. The anthocyanosides (a nthocyan ins) are aglycones boun d to one of three glycosides (Cuni o, 1993 ). The anth ocyanoside content increases as the fruit ripens whereas the catechin tannins and dimeric proanthocyanidins (BI-B4) decrease with the progression of ripeness (Morazzoni and Bom­bardelli , 1996).

The Commission E reported ast rin ­gent activity.

Bilberry has shown vasoprotective, antiedematous, antioxidant, anti­in fl ammatory, and astringent actions (Bone and Mo rgan, 1997). It has demonstrated free radica l scavenging and inhibition of cAMP phosphodi­esterase actions (Brun eton, 1995 ; Fer­retti et aI. , 1988). In vitro and in vivo clinical studies show platelet aggrega­ti on and stimulation of vascular prosta­cycl in . Preliminary human trials indicate vasoprotective properti es. Bil­berry anthocyan ins regenerate rhodopsin and are indicated in treat­ment of poor night vision, macular degenerati on, glaucoma, and catarac ts (Bruneton, 1995).

Uses The Comm ission E approved the inter­nal use of bilberry to treat non-specific, acute di arrhea, and local therapy for mild in flammati on of the mu cous 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 adul ts (Braun et aI. , 1997; Wicht! an d Bisset, 1994). Bilberry fruit extracts

may offer symptomati c reli ef for vascu­lar disord ers including capillary weak­ness, venous insufficiency, and hemorrh oids. It is also used as a second­ary treatm ent for spasmodic co liti s (Bruneton, 1995).

Contraindications No ne known.

Side Effects No ne known.

Use During Pregnancy and Lactation No restric tions known.

Interactions with Other Drugs None known.

Dosage and Administration Unless oth erw ise prescribed: 20-60 g of dried ripe fruit per day fo r infusions o r decoctions, as well as other galenical preparations fo r internal use. External: 10% decocti on or equ ivalent preparations fo r local appli cati on. Internal: [Note: According to the Aus­trian Pharmacopeia, the average single dose fo r bilberry fruit is 5 g (Meyer­Buchtela, 1999; OAB, 199 1) .] Dried fruit: 4-8 g taken with water, seve ral times daily (Braun et aI. , 1997; Meyer-Buchtela, 1999; Wicht! and Bis­set, 1994). Decoction: Place 5-1 0 g crushed dri ed fruit in 150 ml co ld water, bring to a boil fo r approximately 10 minutes, th en strain while hot. Drink cold several times daily unti l the diarrhea is go ne (Braun et aI. , 1997; M eyer-Buchtela, 1999; Wicht! and Bisset, 1994). Co ld mace rate: Soak 5-1 0 g crushed dried fruit in 150 ml cold water for two hours, allowing the fr uit to swell. Drink cold several tim es dail y (Braun et aI. , 1997; M eyer-Buchtela, 1999; Wicht! and Bisset, 1994).

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Fluidextract 1:1 (glml): 2--4 ml, three times daily (Anderhuber, 1991; Cunio, 1993). Dry extract (25% anthocyanosides): 80-160 mg, three tim es daily (Foster, 1996; Pizzo rno and Murray, 1992). External: Decoction: Place 5-10 g crushed dried fruit in 150 ml cold water, bring to a bo il for approximately 10 minutes, then strain while hot (Meyer-Buchtela, 1999 ; Wicht! and Bis­set, 1994). Gargle mouthwash: Containing 10% decoction. Duration of admini stration: If diarrh ea persists for more than 3 to 4 days, con­sult a physician.

References Anderhuber, R. 199 1. Vaccinium myrtillus. AusIJ

Med Herbalislll 3: 13- '14. Azar, M ., E. Verette, S. Brun. 198 7. Identification

of some pheno lic compounds in bilberry ju ice Vaccinium myrtilllls. } Food Sci 52(5): 1255-125 7.

BAnz. See Uundesanzeiger. Barrette, E.I~ 1999. Bilberry fruit extract for night

vision. Alternative Medicine Alert '" 2(2):20-21. Bone, K. an d M. M organ . 1997. Bilberry-The

Vision Herb. MediHerb Pro(essional Review 59:1-4.

Brau n, R. et al. 1997. Standardzulassungen (Iir Fer­tigarzneil'l1ittel-Text and Kommentar. Stuttgart: Deutscher Apoth eker Verlag.

Bravetti, C. 1989 . Preventive medical trcatment of senile cataract with vita min E and anthocyano­sides: clin ical evaluation . Ann Ottalmol Clin Owl 11 5: 109.

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

Blllldesanzeiger (BAnz). 1998. Monographi cn der Kommission E (Z ulassungs- und Aufbere irungs­kommi ss ion am BGA fUr den humanmed. Bere­ich, ph ytotherapeutische Th erapie richtung und Stoffgruppe). Kiiln : Bundesgesundh eitsa mt (BGA).

Caselli, L. 1985 . Studio ciinico ed elerrroretino­grafico su ll'artiyitJ degli antocianosidi IClinica l and electroretinographic study o n acti vity of anthocyan osides). Arch Med Int (Parma) 37:29-35 .

Cluzel, c., P. Bastide, I~ Tronche. 1969. IPh ospho­glucomutase and glucose-6-phosphatase activi ­ties of th e retina and anrhocyanoside extractS from Vacc inium myrtiflus (study in vitro and ill vivo)] [In French]. C R Seances Soc Bioi Fi! 163(1): 147-150.

Bilberry fruit 19

Colantuoni, A., S. Bertuglia, M.J . Magistretti, L. Donato. 199 1. Effects of Vaccil1iu l'I1 m yrtil/us anthocyanosides on arte rial vasomation. Arzneim(orsch 41 (9):905-909.

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

Deutscher ArZl1eimiltel-Codex (DAC). ] 986. Stuttgart: Deutsche r Apotheker Verlag.

Ferrerti, c., M.]. M agistretti, A. Roborti, I' Ghi, E. Genazzani. 1988. Vaccinium myrtillus antho­cyanosidcs are inhibitors of cAMP and cG MP phosph odiesrerases. Pharm Res Comm 20( 11): 15 0.

Fiorini, G. , A. Biancacc i, EM. Graziano. ] 965. Modificazioni perimetriche ed adarromerriche dopo ingestione di mirtillina associata a beta­ca rotene I Peri metric an d adaprometric modifica­tions after in gestion of myrr illin assoc iated with beta-carotene]. Anll Ottalmol Clin Ocul 9 1(6):37 1-38 6.

Foster, S. 1996. Bilberry: A Long History. /-I ealth Food Business. August 1996: 40 .

Friedr ich, VH . and J. Schiinerr. j 973 . Unter­suchungen Liber ein ige Inhaltsstoffe der BUtter und Fruchte von Va cciniulil Inyrtiffus (Ph yto­chemica l investigation of leaves and fruits of Vacciniull1 myrtiffusl . Planla Med 24(1 ):90-1 00.

German HOll'l eopathic Pharmaco/Joeia (GHP) . 1993 . Translation of th e Deutsches H Oll1oopathisches ArZlleibuch (HAB I ), 1st ed. , 5 th ,uppl. 199 1. Stuttgart: Deutsche r Apoth eke r Verlag. 383-384.

Ghiringhelli, c., F. Gregoratti, F. Marastoni. j 978 . Artivira capil larotrop di antocianosi di and alto d osaggio nella stas i da flebopatia (Ca pil­larorropic activity of anrhocyanosid es in high doses in phlebopathic sratis] . Minerva Cardioall­gioI26(4):255-276.

Griev e, M . 1979. A Model'll Herbal. New York: Dover Publications, In c.

H ansel, R., K. Kel ler, H . Rimpler, G. Schneid er (eds.). 1992- 1994. Hagel'S Harrdbuch der Phar­mazeutischen IJraxis, 5th ed. Vol. 4- 6. Berlin ­Heid elberg: Sp ringer Verlag.

Jayle, G.E. and L. Aubert. 1964. [Action des gluco­sides d 'anthocyanes sur 1a vision scotopiqu e et mesopique du suj et norm al] [in French]. Thera­pie 19: 17 1.

Jayle, G .E. et al. 1965. [5rudy concerning rhe action of anthocyanosidc extracts of Vaccinium Myrtiffus on 11Ight vision I l in French] . AIIII Owl (Paris) 198(6):556-562.

Lagrue, G. er al. 1979. Pathology of the microci r­cuLuion in di abetes and a lterations of the biosynthesis of intracellular matrix molecu les. Frollt Matrix Bioi S Karger 7 :324-325.

Leung, A.Y. and S. Foster. 1996. Ellcyclopedia of COII/mon Natural ingredients Used in Food, Drugs, and Cosmetics, 2nd ed. New York: John Wiley & So ns, Inc. 84-85 .

Lietti, A., A. Cristoni, M . Picci. 1976. Studies o n Vaccillium myrtiffus anthocyanos id es. I. Vaso­protective and antiinflammatory activity. Arzneim(orsch 26(5):829-832.

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20 Herbal Medicine

Meyer-Buchtela, E. ] 999 . Tee-Rezepturell-Ein Handbuch f"r Apotheker und Arzte. Stuttgart : Deutscher Apotheker Verlag.

Morazzoni, P. and E. Bombardell i. 1996. Vacciniulll myrtillus L. Fitoterapia 67(1):3-29.

Neumann, L. 197 1. Therapeutische Ve rsuche mit Anthozyanosiden bei Langzeitbehandlungen in der Augenheilkunde lin German]. Klin MOllatsbl Augellheilkd 158:592-597 .

Osterreichisches Arzneibuch, 1st suppl. (bAB). 1983. Wien: Verlag der bsterre ichischen Staats­druckerei.

Osterreichisches ArZlleibuch (bAB) . ]99 ] . Wien: Verlag der b sterreichischen Staatsdruckerei.

Penn arola, R. et al. 1980. The therapeutic actio n of the anthocyanosides in microcirculatory changes due to adhesive- induced polyneuritis. Gazz Med ItaI139:485-49 1.

Perossin i, M. et al. 1987. Diabeti c and hypertensive retinopathy therapy with VaccilliulIl myrtillus anthocya nosides (Tegens): Doub le blind placebo control led cli nical trial. Alln Oltalmol Clin Ocul 11 3:1 173.

Pharmacopoeia Helvetica, 7th ed. Vol. 1-4. (Ph.Helv.VII ). 1987. Bern: Office Central Federal des Imprimes et du M aterie l.

Pizzo rn o, J.E. and M.T. Murray. 1992. A Textbook of Natural Medicine. Seattle, WA : Bastyr Univer­sity Publicarions.

Politzer, M. ] 977. [Experiences in the med ical treatment of progressive myopia] [In German]. Klill Monatsbl Augellheilkd ] 71(4):6 16-619.

Regtop, H . 1998 . Age related macular degenera­ti on. Aust J Med H erbalism 10(2):38-45.

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

Sevin, R. and J.F. Cuendet. 1966. EHets d 'un e asso­ciation d 'anthocyanosides de myrtill e et de beta­carotene sur la resistance capill aire des diabetiques [In Frenchl. Ophthalmologica ] 52: 109- 11 7.

Tyler, Y.E. 1994. Herbs of Choice: The Therapeutic Use of Phytomedicillals. New York: Pharmaceuti ­ca l Products Press.

Wichtl, M. and N.G. Bisset (eds.). 1994 . Herbal Drugs and Phytopharmaceuticals. Stuttgart: M edpharm Scientific Publi shers. 35 1-352.

Wichtl, M. ]996. Monographien-Kommentar. In: Braun, R. et a l. 1997. Stalldardzulassullgell fiir FertigarZileimiltel-Text mId Kommmtar. Stuttgart: Deutscher Apoth eker Verlag.

Zava rise, G. 1968 . Sull'effetto del trattamento pro­lungaro con antocianosid i sui se nsa iumin oso [Effect of prolonged treatment with anthocyano­sides on li ght se nstivity] . AIIII Oltalmol Clin OcuI 94(2):209-2 14.

Additional Resources Alexeeff, T. 1998. C irculatory insufficiency: a his­

torical and modern review of three classic herbs. Aust J Med Herbalisml 0(4) :135-"140.

Alfier i, R. and P. Sole. 1964. Influence des antho­cyanosides administres par voie parenera le sur I'adaptoelectro retinogramme du lapin. C R Soc Bioi 158:2338 .

Benninger, j . '1997. Understanding Bilberry. Health Supplement Retaile r. March 1997: 54.

Bettini , Y. et a l. 1984. Interactions between Vac­cin ium myrtillus anrhocyanosides and serotonin on splenic artery smooth muscle. Fitoterapia 55(4):201-208 .

---, 1984. Interactions between Vaccillium myrtillus anrhocya nosides on vascular smooth muscle. Fitoterapia 55(5):265-272 .

Bomser, j ., D.L. Madhavi, K. Si ngletary, M .A. Smith. 1996. In vitro anti-cancer ac ti vity of fruit extracts from Vaccin ium species. Planta Med 62(3):2 12-216.

Der Mard erosian, A. (ed .). ] 999. The Review of Natural Products. Sr. Louis: Facts and Compar­isons.

Detre, Z., H . jellinek, R. Miskulin . 1986. Stud ies on vascu lar permeab ility in hypertension: action of anthocyanosides. Clill Physiol Biochem 4(2):143-149.

This materi al was adapted from The Complete Germall Comlllissioll E MOllographs-Therapeutic Guide to Herbal Medicilles. M . Blumenthal, WR. Busse, A. Goldberg, j. Gruenwald, T. Hall , C.W Riggins, R.S. Ris­ter (eds.) S. Klein and R.S. Riste r (trans.). 1998. Austin: Ameri can Botanical Cou ncil; Boston : Integrative Medicine Communications. 1) The Overview section is new in format ion . 2) Description, Chemistry and Pharmacology, Uses, Contraind ications, Side Effects, In teracti ons ;vith

Othe r Drugs, and Dosage sections have been drawn from the original work . Additional information has been added in some or a ll of these sections, as noted with references.

3) The dosage for eq ui va lent preparations (tea infusion, fluidextract, and tincture) have been provided based on the fo llowing exa mpl e: Un less othetwise prescribed: 2 g per day of [powdered, crushed, cut or whole] [p lant parr] Infusion: 2 g in 150 ml of water Fluidextract 1: 1 (g/ml): 2 ml Tincture 1:5 (g/mI): JO ml

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

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Mia n, E. et al. 1977. Anthocyanosides and mi crovessel wa lls: new find ings on the mecha­nism of action of the ir protecti ve effect in sy n­dromes du e to abnormal capillary fragility. Min Med 68:35 65 .

Morazzoni, P. and M .J. Magistretti. 1990. Activ ity of bilberry, an anthocya noside co mplex from Va ccinium myrtillus (VMA), on platelet aggrega­tion and adh esiveness. Fitoterapia 61 (1): 13-2 1.

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Orsucci, P. L. et al. 1983. Treatment of di abetic re tin opathy with anthocyanos ides : a prel iminary report. Clin Oc 5 :377.

Repossi, P. , R. M alagola, C. De Cadilhac. 1987. The rol e of anthocyanosides on vascu lar perme­abili ty in diabetic re tinopath y. Ann Ottalmol CIi" Owl 357.

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

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