HERB5557 Pharmacognosy

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Botanic name Vaccinium myrtillus.

Other botanic name that have been historically used include Myrtillus niger Gilib (MYRTILUS sYLVITACUS Drejer), Myrtillus sylvaticus Drejer), Vaccinium oreophilum Rydb and Vitis-idaea mertillus L. Moench (Ritchie 1956).

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Botanical description Vaccinium Myrtillus is a member in the Ericaceae family. It is a shrub with a low growth rate.

It is also found in North America, Asia and other regions.

Along with other plants such as Vaccinium macrocarpon, blueberry, and Vaccinium corymbosum, the Plant is part of Vaccinum.

Vaccinium mertillus thrives in moist coniferous forests, meadows and heaths. This plant prefers moderately dry ground conditions and light shade.

American Herbal Products Association designated Vaccinium Myrtillus a Class I herb. This means the fruits can safely be consumed when used correctly.

It has also been shown to have no mutagenic or contraindications.

The bell-shaped, pink-coloured flowers of Vaccinium mertillus bear a reddish or pink color.

The alternating branches produce bright green leaves that are elliptical and bright green.

The fruit is small and purple in color, with blue-black flesh.

The plant flowers in April and June. The seeds mature between July and September.

Vaccinium hermaphrodite is pollinated with Lepidoptera, flies, and bees.

The plant is self-fertile.

The plant can grow in sandy or loamy soil.

Vaccinium myrtillus prefers acidic soils but can also thrive in alkaline soils.

It prefers moist soil, but it cannot tolerate maritime exposure (Koopphyto.org (2018)

Parts used Vaccinium myrtillus’s parts are the ripe fruit and leaves.

Sometimes, the root bark and root are also used (Pfaf.org 2018).

Relevant Constituents – The Following Constituents Can Be Found In Vaccinium Mirtillus

Anthocyanosides- Anthocyanosides is a group of compounds found in plants. They are known as glycosides or anthocyanins.

The cyaniding glycosides are the important anthocyanins. They are mainly present in fruits as a color.

While the anthocyanins of the Vaccinium species can be found in ripe fruits, most are found in Vaccinium mertillus fruit.

Anthocyanins are found in Vaccinium myrtillus fruits ranging from 300 to 700g.

Important to note is that the anthocyanins content can vary depending on where you live. It can vary from 19 to 38mg/g of fruit dry weight.

Concentrated extracts of bilberry extracts have a nearly 24 percent total amount of anthocyanin.

European Pharmacopoeia 8.0 estimates that a dry extract of Vaccinium mertillus contains between 32 and 39 percent anthocyanin. This is expressed in the form cyanide 3-Oglucoside, chloride (European Pharmacopoeia 2018).

Studies have shown that Vaccinium mertillus contains 14 to 15 different anthocyanins.

Canter & Ernst (2004) found that bilberry juice, extract and fruit contain 15 different anthocyanins.

Structure of 3-Oglucoside chloride cyanide

Polyphenols- The two main polyphenols in the bilberry include the Flavan-3 and the Proanthocyanidins.

The fruit’s ripening affects how much of these polyphenols are present.

Other identified polyphenols include cathechin dimer A-3 and Epicatechin dimerB-2 (Faria et. al., 2005).

Structure of Proanthocyanidins

Flavonoids – approximately 14 mg of flavonoid Glycosides are found within 100g.

The fruit’s concentration of flavonoids declines with age.

Kaemferol and chrysoroil are some of the flavonoids found in bilberry (Riihinen, et al. 2008).

Kaemferol structure

Alkaloids- Quinzolidine, an alkaloid, was found. However, it is not known where the alkaloids came from (Slosse, Hootele, 1981).

Structure of Quinzolidine

Tannins – These tannins are available in condensed and hydrolyzable forms.

Dry fruits have around 1% of the tannin. It is also known as pyrogallol (Moss & Parkinson 1995).

Structure of pyrogallol

Vitamins- Fresh fruits are rich in vitamin B1, nicotinamide, and pantothenic Acid (Prior, et al. 1998).

Structure of pantothenic acids

Preparation form

Commercial bilberry products are made by standardizing the anthocyanidin to 25 percentages, which is equivalent of the 36 percent.

The percentages can vary widely.

The medicines are available in a pharmaceutical form that contains 100 mg of anthocyanosidic as well as 5 mg beta-carotene.

The soft capsules contain approximately 70 mg of Vaccinium Myrtillus. It contains 70 percent methanol V/V and 36% anthocyanosides.

Historical Information

Culpeper stated that Vaccinium mertillus has the properties of being sour and drying, cold, and astringent.

Culpeper, 2006: Vaccinium Myrtillus has a slightly binding action on the stomach. This prevents nausea and vomiting.

The medicinal properties of Vaccinium mertillus’ leaves have been found to be similar to that of Urva ursi. These medicinal properties can be found both in the roots and the leaves.

The treatment for ulceration of the throat and mouth can be done using Vaccinium Myrtillus.

If taken for longer durations, tea made with the leaves may help to reduce diabetes risk (Talbott, Hughes, 2007).

The dried bilberry fruit is used to treat diarrhoea. It can also be used to treat mild infections in the mucous membranes and throat.

Traditional uses for dry fruits include: scurvy; gastrointestinal inflammation; haemorrhoids; dysentery; peripheral vascular disorders; haemorrhoids.

The traditional use of bilberry fruits is to treat chronic venous conditions, increased fragility of the blood vessels (Madhavi and co., 1998).

Folklore mentions: Anecdotal explanations go back to World War 2. The British pilots used bilberry fruit before bed to improve night vision.

Bilberry are the main features of Lughnasa’s Celtic festival (honouring God of Laughter), and they influence a vent that is known as bilberry sunday. It occurs in the last Sunday of July in Ireland (Botanical.com 2018).

Medicinal Actions (Contemporary Usage).

Both the leaves and fruits of Vaccinium Myrtillus are therapeutic in human and veterinary medicine.

The active ingredients found in the leaves can be used to treat bacteriostatic, astringent, and hypoglycaemic conditions.

This can be used for the treatment of rheumatism and diarrhoea.

The active ingredients in fruits are important in diabetes treatment. They act as photoreceptors sensitizers, activate retinal regeneration, protect the body against radiation, and help in cardiovascular regulation.

Anti-diarrheal, antibacterial, anti-inflammatory, and urinal antiseptic.

Medicinal Indications: Contemporary Usage

The anthocyanosides found in Bilberry are powerful antioxidants. This helps to strengthen blood vessels and lower cholesterol. It also stabilizes collagen tissues like cartilage, ligaments, and the tendons.

The concentration of the retinal colors in bilberry increases, which makes it easier for the eye to withstand light.

The fruit extracts improve night vision and prevent cataracts. They also slow down muscle degeneration.

Chronic venous sufficiency is preventable and can be treated by oral bilberry extracts.

This is when the valves that deliver blood back to your heart are damaged or weakened.

Dried bilberries can be used for diarrhoea because they contain tannins. They also act as an astringent to the treatment the gastrointestinal tract.

Recent research has demonstrated that bilberry extract has anti-ulcer activity. It is also curative and preventive.

Some animal experiments have shown that bilberry extracts are anti-cancerous.

Bilberry tea can be used daily to improve your vision. It strengthens the blood vessels, retina and eyesight (Herbwisdom.com 2018).

In order to determine the pharmacokinetic profile for bilberry anthocyanins, a rate model was developed. The method also allowed us to measure the glucose transporters with a validated LC–ESI–MS method.

This study identified 15 anthocyanins with different bioavailabilities.

Notable is the fact that the PK profile was affected by both sugar moiety (aglycone) and the sugar moiety (sugar moiety).

It is possible to explain the difference in behaviour by looking at the glucose transporters involvement, as was done previously in CACO-2 cells.

This correlation was confirmed by integrated PK studies and computational analysis. Baron et.al., 2017, also found that the relative absorptions for each anthocyanin were significantly affected by the molecular recognition of GLUT2 or sGLT1.

Pharmacodynamics

In vitro experiment – Vasoactive properties: This study was conducted on isolated thoracic venous calf preparations of Vaccinium Myrtillus extract. The results showed that it reduces the contractions induced in the thoracic by 5-HT.

When ascorbic acid is added, the effect becomes more apparent.

The pre-treatment of lysine acetylsalicylate and indomethacin (Ema.europa.eu (2018)) decreased or nullified this relaxing effect.

In vivo experiments were performed to examine the effects of bilberry in rats who had been denied of dietary flavonoids.

Three weeks of a diet that was devoid in flavonoids was fed to the wistar rats.

After peritoneal injections, the capillary fragility of the rats was determined. The data revealed a large difference in capillary resistance between the controls and those with bilberry extract (Ema.europa.eu 2018, 2018).

Relevance Of Pharmacodynamics Studies To Current Usage

In clinical trials, bilberry’s pharmacological and efficacy properties and efficiency have not been extensively studied.

Most of the information comes from clinical studies that were derived from animal models and in vitro tests. These are based on knowledge of key constituents of the herb.

Research on the pharmacology is the most important aspect of drug research. It focuses on the anthocyanoside as well as the anthocyanin content in Vaccinium myrtillus.

Cautions

Anthocyanins found in the drug could prevent blood clotting. If bilberry extracts with blood thinners are taken together, this may increase the risk of bleeding.

This includes fresh fruits and aspirin.

Because bilberry extracts can reduce blood sugar and may cause diabetes, it is not recommended for diabetic patients.

The hypoglycaemia could be caused by bilberry extracts being taken together with garlic, ginger, fenugreek or ginseng.

The long-term use of the leaves is unsuitable and may prove to be toxic if it is continued for more than 1.5g/kg/day.

Consumption of bilberry fruits in long term doses of 180 mg/kg of anthocyanosides, for a duration of six months, produced no toxic effects (Vaccinium Myrtillus Bilberry, Whortleberry PFAF, Plant Database, 2017).

Because of their antiplatelet-aggregating properties, very high dosages of the bilberry extraits must be taken with caution in patients suffering from haemorrhagic disorder (Alternative Medicine Review Volume Volume, 2001).

The recommended daily intake of bilberries depends on the form that they are consumed.

Three times daily, fresh berries weighing between 55-115 grams can also be taken.

Dried berries can be eaten every day as they contain very little flavonoids.

The bilberry extracts can be taken at 80 to 160 mg daily, if they have been standardized to 25 percent of the anthocyanosides.

The anthocyanosides are approximately 20-40mg and can be taken up to three times per day.

Take 80-160mg of the standardized capsules with 25 percent standardized anthocyanosides daily.

The chronic toxicity of 1.5g/kg/day in the leaves makes them unsuitable for long term consumption (Anthocyanins 2017).

References

Alternative Medicine Review Volume 6, Issue 5, Page 502.

Monograph. Vaccinium myrtillus.

Pharmacokinetic profile in rats of bilberry cyanins and the role glucose transporters: LC/MS/MS and computational research.

Journal of pharmaceutical and biological analysis, 144: 112-121.

Anthocyanosides in Vaccinium myrtillus (bilberry), for nightvision–a systematic review and analysis of placebo-controlled studies.

Survey of ophthalmology 49(1), 38-50.

(2018). Bilberry (Vaccinium mertillus).

Culpeper’s English & herbal doctor.

Applewood Books.

(2018).

Preparated blueberry extracts (Vaccinium myrtillus), have antioxidant properties.

Journal of Agricultural and Food Chemistry. 53 (17), 6896 – 6902.

Medicinal Actions and Uses

Bilberry Benefits & Information Vaccinium Myrtillus.

(2018).

Isolation of bioactive compounds from Vaccinium mertillus (bilberry). Fruits and cell cultures.

The digestion of bulbs (Polygonum viviparum Lem.) and berries. (Vaccinium myrtillus and Empetrum sp.

Captive ptarmigan (Lagopus muus)

British Journal of Nutrition, 33(2). 197-206.

(2018).

Antioxidant capacities as influenced by anthocyanin and total phenolic content, maturity, and variety Vaccinium species.

Journal of agricultural chemistry and food chemistry 46(7) 2686–2693.

(2008).

Food chemistry 110(1), 156–160.

Vaccinium myrtillus (L.) The Journal of Ecology. 291-299.

Myrtine and Epimyrtine, quinolizidinealkaloids from Vaccinium mertillus.

The guide for health professionals on dietary supplements.

Whortleberry PFAF plant database, Vaccinium myrtillus Bilberry.