HERB5557 Pharmacognosy

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Answer:

Botanical name- Vaccinium mertillus.

Other botanic names are Myrtillus niger Gilib and Myrtillus sylvaticus Drejer.

Botanical description: Vaccinium myrtillus, a member the Ericaceae plant family, is a shrub that grows low in the Northern Europe.

It can be found in North America and several other parts of Asia.

It is part of the genus Vaccinum, which also includes Vaccinium macrocarpon (cranberry), and Vaccinium coermbosum (blueberry).

Vaccinium myrtillus is a plant that grows in moist coniferous forests and meadows. It prefers moderately humid ground conditions with moderate shade.

The American Herbal Products Association has declared Vaccinium myrtillus a class I herb. This means that the fruits are safe to eat and can be used correctly.

There has been no evidence of mutagenic activity or contraindications to Vaccinium myrtillus’s use.

The bell-shaped flowers of Vaccinium Myrtillus have a pink or reddish colour and are bell-shaped.

Bright green, elliptical leaves emerge from the alternating branches.

The purple or blue-black fruit has purple flesh and is small in diameter (5-9 inches) (Pfaf.org 2018, 2018).

The plant blooms between April and June, and the seeds ripen between July and September.

Vaccinium myrtillus, which is a hermaphrodite, is pollinated by Lepidoptera and flies as well as bees.

The plant is still self-fertile.

The soil should be sandy and loamy.

Vaccinium myrtillus prefers acidic soil, but can grow in any soil.

It is tolerant to maritime exposure but prefers moist soil (Koop-phyto.org 2018).

Parts used – The ripe fruits, and the leaves of the plant Vaccinium mertillus are edible and can be used medicinally.

In some cases, the bark and root can also be used (Pfaf.org 2018, 2018).

Relevant Constituents – These Constituents are Found in Vaccinium Myrtillus

Anthocyanosides – Anthocyanosides refer to the compounds found in plants as glycosides (anthocyanins).

The cyaniding glycosides, which are the most important anthocyanins, are the ones that are present in fruits as a pigment.

The anthocyanins in Vaccinium species are found in the ripe fruit, but the majority of anthocyanins in Vaccinium myrtillus are found in the Vaccinium myrtillus.

A ripe fruit’s anthocyanin total weight is approximately 300-700 grams in Vaccinium mertillus.

It is important to remember that anthocyanin content varies by geographical location. They can range from 19 to 38 mg/g dry fruit weight.

The total anthocyanin content in concentrated extracts from bilberry extracts is nearly 24 percent.

European Pharmacopoeia 8.0 estimated that a dry extract from Vaccinium myrtillus contains 32 percent to 39 per cent of anthocyanin. It is expressed as cyanide 3-Oglucoside chloride (European Pharmacopoeia 2018, 2018).

Studies have shown that Vaccinium mertillus has 14 to 15 anthocyanins.

The fruit, juice, and extract of bilberry have 15 different anthocyanins (Canter & Ernest, 2004).

Structure of 3-O-glucoside chloride cyanide

Polyphenols – The main polyphenols found in bilberries are Flavan-3-ols and Proanthocyanidins.

The ripening time of the fruit affects the amount of polyphenols.

Other polyphenols that have been identified include Epicatechin-dimer-dimer-b-3 and cathechin-dimer-dimer-b-2 (Faria, et al. 2005).

Structure of Proanthocyanidins

Flavonoids- Around 14 mg of flavonoid glycosides can be found in 100g of fruits.

As the fruit ripens, the concentration of flavonoids drops.

Kaemferol (Riihinen and co., 2008) are the flavonoids reported from bilberry.

Kaemferol Structure

Alkaloids- A quinolizidine alkaloid is found. However, the source of these alkaloids has not been confirmed (Slosse and Hootele 1981).

Structure of quinolizidine

Tannins- The tannins can be found in both the hydrolyzable or condensed forms.

The tannins in dry fruits are about 1%. This is called pyrogallol by Moss & Parkinson 1975.

Structure of pyrogallol

Vitamins- The fresh fruits contain the nicotinamide and pantothenic acids as well as vitamin C, B1(Prior et.al., 1998).

Structure of pantothenic Acid

Preparation Form

Standardizing anthocyanidin at 25 percents is what’s used to prepare commercial bilberry products. This is equivalent to the 36 percent of anthocyanins.

This percentage can vary greatly.

The anthocyanosidic is 100mg and the beta-carotene 5 mg in the pharmaceutical form.

Soft capsules contain 70 mg of Vaccinium myrtillus. They also contain 70 percent methanol V/V, which contains 36 percent anthocyanosides. (Ema.europa.eu (2018)).

Historical Information

Culpeper described Vaccinium myrtillus as having the characteristics of being sour, dry, cold, and astringent.

Culpeper (2006) also states that Vaccinium myrtillus has a slight binding effect on the stomach, liver and stomach which helps to prevent nausea and vomiting.

The medicinal properties of Vaccinium myrtillus leaves are similar to those of Urva ursi. They are particularly found in the bark and leaves.

The treatment of ulceration in the throat and mouth is done with Vaccinium myrtillus.

Tea made from leaves can be used to treat diabetes if it is consumed for longer periods of time (Talbott and Hughes, 2007).

The treatment for diarrhoea was done with dried bilberry fruits. Mild infection of the mucous membranes in the throat and mouth can also be treated with it.

The dry fruits were traditionally used to treat scurvy and other conditions such as scurvy, oral infection, haemorrhoids, dysentery and peripheral vascular disorders.

Traditional bilberry fruit treatment is for chronic venous insufficiency and increased fragility conditions within the blood vessels (Madhavi, 1998).

Folklore mentions – Anecdotal explanations date back at the World War 2, when British pilots used to eat bilberry fruits before nightfall to improve their night vision.

Bilberry is the main feature of Lughnasa, a Celtic festival honoring the god of laughter. This influences a vent known as bilberry Saturday. It takes place in some parts of Ireland on the last Sunday in July (Botanical.com 2018, 2018).

Medicinal actions (Contemporary Usage).

Both the human and veterinary medicine have great therapeutic value for the fruits and leaves of Vaccinium myrtillus.

The active ingredients in the leaves play the roles of bacteriostatic and astringent.

This herb is used to treat gout, diarrhoea, blood urea and urinary tract infections.

Active ingredients found in fruits can be used to treat diabetes. They activate the retinal regeneration, stimulate the photoreceptors and protect the body from radiation.

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

Medicinal Indications (Contemporary Usage).

Anthocyanosides in bilberry are potent antioxidants. They help strengthen the blood vessels’ capillary walls, lower cholesterol, and stabilize collagen tissues such as cartilage, ligaments, and tendons.

It increases the amount of retinal pigments, which allows the eye to tolerate light.

Fruit extracts improve night vision, prevent cataracts, and slow down muscular degeneration.

Chronic venous insufficiency can be prevented and treated with oral bilberry extracts.

This happens when the valves in the veins that return blood to the heart get damaged or weakened.

Because it contains tannins, dried bilberries can be used to treat diarrhoea.

Recent research has shown that bilberry extract can be used to treat and prevent ulcers.

Certain animal studies have demonstrated that bilberry extracts can prevent the development of cancer.

Daily intake of bilberry tea has been shown to improve vision by strengthening blood vessels and retina (Herbwisdom.com 2018, 2018).

The rate model was used to evaluate the pharmacokinetic profile and to measure glucose transporters using a validated LC–ESI-MS method.

The study revealed that 15 anthocyanins behave differently in terms of bioavailability.

The PK profile was significantly affected by both the sugar moiety as well as the aglycone.

This is evident and can be explained by the assessment of the involvement of glucose transporters, which was previously observed in CACO-2 cells.

This was also confirmed by integrated PK and computational studies. Baron et. al. 2017, 2017 found a strong correlation between the relative absorptions of each anthocyanin and the molecular recognitions of GLUT2 & GLUT2.

Pharmacodynamics

In vitro experiment – Vasoactive qualities: An in vitro study was done on isolated thoracic vein calf preparations from Vaccinium myrtillus extract. It was found to decrease the contractions that were induced by 5-HT.

Ascorbic acid was also found to increase the effect.

Pre-treatment with indomethacin or lysine Acetylsalicylate (Ema.europa.eu 2018) reduced or nullified the relaxing effect.

In vivo experiments were conducted to determine the effects of bilberry on rats that had been deficient in dietary flavonoids.

For three weeks, the wistar rats were given a diet devoid of flavonoids.

After peritoneal injection, the data showed a significant difference in the capillary fragility between the control and the diet with bilberry extract (Ema.europa.eu 2018).

Relevance of Pharmacodynamics Research to Contemporary Useage

Clinical studies have not been able to determine the pharmacological effects and efficiency of bilberry.

The majority of information is gathered through clinical studies that are derived using an animal model and in vitro testing. All of these are based upon the knowledge of key constituents in the herb.

Most of the research done is based on the pharmacology and is primarily focused on the anthocyanoside or anthocyanin content in the Vaccinium myrtillus.

Caution

Anthocyanins in the drug can prevent blood from clotting after an injury. This can lead to increased bleeding risk if bilberry extracts and blood thinners are combined.

This includes fresh fruit and aspirin.

The bilberry extracts may be harmful to diabetic patients. They can lower blood sugar levels and increase the effectiveness of diabetic medication.

This could also be a contributing factor to hypoglycaemia if the bilberry extracts were taken with garlic, fenugreek and ginseng.

Long term use of the leaves can prove toxic and dangerous.

The toxic effects of long-term consumption of bilberry fruits at 180 mg/kg anthocyanosides over a 6-month period was not observed (Vaccinium myrtillus, Whortleberry PFAF plant Database, 2017).

High doses of bilberry extracts should be avoided in combination with haemorrhagic conditions due to their antiplatelet aggregating qualities (Alternative Medicine Review Volume 2001).

The form of the bilberry that is being consumed will determine the recommended dosage.

Fresh berries between 55 and 115g can be eaten three times per day.

Because it only contains a small amount of flavonoids, dried berries can still be eaten daily.

You can consume bilberry aqueous extracts standardized to 25 percent anthocyanosides at a dose of 80-160 mg three times per day.

Anthocyanosides can be taken three times daily at a dose of 20-40 mg.

You can take 80 to 160 mg of the standardized capsules containing 25 percent of standard anthocyanosides three times daily.

The chronic toxicity of 1.5g/kg/day is enough to make the leaves unsuitable for long-term use (Anthocyanins 2017, 2017).

Refer to

Alternative Medicine Review Volume 6, No 5, Page 502.

Monograph on Vaccinium myrtillus, Bilberry.

The pharmacokinetic profile and role of glucose transporters in bilberry anthocyanins: LC-MS/MS, computational studies.

Journal of pharmaceutical analysis and biomedical analysis, 14(4), 112-121.

Anthocyanosides from Vaccinium myrtillus, (bilberry), for night vision–a systematic analysis of placebo-controlled trials.

Survey of Ophthalmology, 49(1): 38-50.

(2018). Bilberry (Vaccinium myrtillus) L.

Culpeper’s English and herbal physician.

Applewood Books.

(2018).

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

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

Health.

(2018). Bilberry Benefits & Information (Vaccinium Mirtillus).

(2018).

Isolation and culture of bioactive components from Vaccinium myrtillus (bilberry), fruits and cells.

(1975).

By a captive ptarmigan, Lagopus mutus.

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

(2018).

The total phenolic and anthocyanin levels, maturity and the variety of Vaccinium species influence antioxidant capacity.

Journal of agricultural and Food Chemistry, 46(7): 2686-2693.

Organ-specific distributions of phenolic compounds (Vaccinium myrtillus and ‘northblue)blueberry (Vaccinium Corymbosum. x V. Angustifolium).

Food Chemistry, 110(1): 156-160.

Vaccinium myrtillus, L. The Journal of Ecology 291-299.

Myrtine and epimyrtine are quinolizidine alkaloids obtained from Vaccinium myrtillus.

Guide for health professionals to dietary supplements.

Whortleberry PFAF plant database, Vaccinium myrtillus Bilberry.

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