Question:
Answer to Question: HERB5557 Pharmacognosy
Botanical name Vaccinium mertillus.
Other botanic terms that were historically used are Myrtillus niger Gilib or Myrtillus sylvaticus Drejer and Vaccinium Oreophilum Rydb. Vitis-idaea Myrtillus L. (Ritchie 56).Common Names- Whortleberry, myrtle whortleberry, myrtle blueberry, blueberry, huckleberry, bog berry (Chu, Cheung, Lau & Benzie, 2018).
Botanical description Vaccinium myrtillus belongs to the Ericaceae and is a shrub with a low growth rate.
It is also found in North America, Asia, and many other regions.
This plant is part the genus Vaccinum with other plants like Vaccinium macapon (cranberry), Vaccinium corymbosum (“blueberry”), and Vaccinium microcarpon (cranberry).
Vaccinium mertillus can be found in moist coniferous forests or meadows. The plant also prefers moderately shaded ground conditions.
American Herbal Products Association (AHA) has designated Vaccinium mertillus a “class I” herb. This means that they can be safely eaten and used correctly.
Vaccinium mythillus has no mutagenic or contraindications.
Vaccinium myrtillus flowers are bell-shaped and have a reddish or pink color.
The bright green and elliptical leaves grow from the alternating branch.
The fruit is small in size, between 5-9 cm in diameter, and contains purple flesh.
The plant blooms in the months April through June. The seed of the plant matures between July to September.
The hermaphrodite Vaccinium myrtillus can be pollinated by Lepidoptera flies and bees.
The plant is self-fertile.
The plant can grow in sandy soil or loamy soil.
Vaccinium mertillus prefers acidic soils, but will also grow well in neutral soils.
It prefers moist soils but can’t tolerate sea exposure (Koopphyto.org 2018, 2018).
Parts used Vaccinium mertillus Vaccinium myrtillus is made up of two parts: the ripe leaves and the fruits.
In certain cases, the root’s bark and roots can be used as well (Pfaf.org (2018)
Relevant Constituents – The Following Constituents Are Found in Vaccinium myrtillus
Anthocyanosides- Anthocyanosides, also known as glycosides or anthocyanins, are compounds found in plants.
The cyaniding glycosides are important anthocyanins. Most of them are found as pigments in the fruits.
Although the anthocyanins can be found in Vaccinium anthocyanins, they are not present in ripe fruits. However, Vaccinium myrtillus has the highest concentration of anthocyanins.
A ripe fruit contains approximately 300 to 700g of anthocyanins in Vaccinium mertillus.
Noting that the anthocyanins are subject to variation depending on the geographic area, the average fruit’s dry weight varies between 19 and 38 mg.
The anthocyanin total content is only about 24 percent in the concentrated extracts made from bilberry juice extracts.
European Pharmacopoeia 8.0 has estimated that a dry Vaccinium myrtillus extract contains between 32 and 39 percent anthocyanin. The extract is expressed in cyanide 3-Oglucoside-chloride.
Studies have shown that Vaccinium mertillus is rich in 14-15 anthocyanins.
Canter and Ernst (2004) discovered that 15 anthocyanins can be found in bilberry juice, fruit, and extract.
Structure of cyanide 3-Oglucoside Chloride
Flavan-3, and Proanthocyanidins are the main polyphenols found within bilberry.
The ripening of the fruit has an inverse relationship with the content of polyphenols.
Other identified polyphenols include cathechin dimer A-3 and Epicatechin dimer 2 (Fariaet al.2005).
Structure of Proanthocyanidins
Flavonoids- about 14 mg of flavonoid sugarsides is found within 100g fruits.
As the fruit ripens the content of the flavonoids begins to decrease.
Kaemferol chrysoroil luteolin, and apigenin are all reported to be present in bilberry (Riihinen und al., 2008).
Kaemferol’s Structure
Alkaloids – A alkaloid called Quinzilizidine was discovered, but the source is unknown (Slosse&Hootele, 1981).
Structure of quinolizidine
Tannins: The tannins are available in condensed and hydrolyzable forms.
The tannins found in dried fruits is around 1%. This is known as pyrogallol. (Moss & Parkinson 1976).
Structure of Pyrogallol
Vitamins- Fresh fruits include the nicotinamide (Pantothenic Acid) and vitamin C,B1 (Prioret al., 1997).
Structure of pantothenic alkali
Preparation of Form
The standardization of anthocyanidin at 25% is used in the preparation of commercial bilberry product. This is equivalent with the 36%.
But, this percentage is variable.
The medications are available in pharmaceutical form and contain about 100 mg anthocyanosidic. There is also 5 mg beta carotene.
The soft capsules of Vaccinium mertillus contain 70 mg.
Historical Information
Culpeper describes Vaccinium Myrtillus’ qualities as sour. It is also drying. Cold and astringent.
Culpeper (2006) says that Vaccinium mertillus may have a slightly binding action on the stomach or liver which can prevent loathing and vomiting.
The medicinal properties found in the leaves of Vaccinium Myrtillus have similar medicinal qualities to Urva ursi.
Vaccinium Myrtillus is used for the treatment of ulceration.
Tea made from the leaves, if consumed for longer times, can help with diabetes treatment (Talbott& Hughes 2007).
The dried bilberry was traditionally used to treat diarrhoea.
Traditional uses for dry fruits include: scurvy; gastrointestinal inflammation; haemorrhoids; dysentery; peripheral vascular disorders; haemorrhoids.
The bilberry is traditionally used to treat chronic vein insufficiency, increased fragility condition of the blood vessels, and other conditions (Madhavi. 1998).
Folklore mentions — Anecdotal explanations date back as far as the second world war, when British pilots used the bilberry fruits to improve night vision.
Bilberry are the main element in Lughnasa the Celtic festival honouring the gods of laugh. A vent is called bilberry Sunday and takes place in parts of Ireland. (Botanical.com (2018)).
Medicinal Activities (Contemporary Usage).
Both the human and veterinary medical uses of Vaccinium myrtillus’ leaves and fruits are therapeutic.
The active components found in the leaves act as hypoglycaemic, astringent, and bacteriostatic.
This treatment is highly recommended for the treatment rheumatism, diarrhoea (diarrhoea), blood ureas, urinary tract infection, diabetes, and diarrhoea.
The active ingredients in fruits play a key role in diabetes management.
Anti-diarrheal. Urinary and intestinal antiseptics.Vaccinium myrtillus leaf and fruit extracts are recommended externally in the treatment of wounds bleeding, eczema, fungal infection, thrush, stomatitis, pharyngitis (Greenlifeuniverse.com, 2018).
Medicinal indications (Contemporary Usage).
Bilberry is rich in anthocyanosides, which are potent antioxidants. These help to strengthen the blood vessels’ capillary walls, lower cholesterol and stabilize collagen tissues like cartilage, ligaments, tendons and other connective tissue.
It also increases the levels of retinal pigments which allow the eye to take in light.
The fruit extracts improve your night vision, prevents the formation of cataracts, slows down muscular aging and reduces muscle degeneration.
Oral bilberry extracts may be used for the prevention and treatment of chronic vein insufficiency.
It occurs when the valves of the veins which carry blood back from the heart become damaged or weak.
The dried bilberries, which contain tannins and act as an astringent in the treatment diarrhoea, are used.
Recent researches show that bilberry oil has anti-ulcer properties and is both preventive and curative.
The anti-cancerous properties of bilberry extracts were demonstrated in animal experiments.
A daily intake of bilberry juice has been proven to improve vision by strengthening the blood vessels.Pharmacokinetics
An experiment was performed to examine the pharmacokinetic profiles of the bilberry anthocyanidins. Also, the study measured the glucose transporters using a validated LC/ESI/MS method.
This study showed that the bioavailability of 15 anthocyanins is different.
Importantly, the PK profile was also significantly affected by the sugar moiety in addition to the aglycone.
The observed difference in behavior can be explained by examining the glucose transporters involvement, as previously demonstrated in CACO-2 cells.
This conclusion was supported by integrated PK analysis and computational study. Baron et.al. 2017 also found a significant correlation between the relative absorptions of each anthocyanin and the molecular recognization of GLUT2 & sGLT1.
Pharmacodynamics
In vitro experiments- Vasoactive characteristics: A study was conducted using isolated thoracic venous calf preparations containing Vaccinium myrtillus Extract. It was found that it reduced the contractions induced from 5-HT.
The effects were more noticeable when ascorbic acids was added.
The pretreatment with lysine-acetylsalicylate/indomethacin (Ema.europa.eu 2018, 2018) resulted in a decrease or nullification of the relaxing effect.
In vivo experiments were performed to examine the effects of bilberry in rats.
For 3 weeks, the wistar rodents were fed a diet without flavonoids.
After peritoneal injecting bilberry extract, the capillary fragility data was analyzed. It was found that there was a marked difference in capillary resistance between the bilberry extract-treated and control mice (Ema.europa.eu (2018)).
Relevance Of Pharmacodynamics Research To Modern Usage
The clinical studies did not provide sufficient information to assess the pharmacological, efficacy and safety of bilberry.
Majority of the information is derived through in vitro and animal studies. This information is based on knowledge of the key constituents found in the herb.
The majority of research is based upon the pharmacology of a drug. This includes the focus on the anthocyanosides and anthocyanins of the Vaccinium Myrtillus.
Caution
Anthocyanins present in the drug might prevent blood from clotting following an injury. However, this could increase bleeding chances if the bilberry supplements are taken along with blood thinners.
This includes fresh fruit, aspirin, and even aspirin.
Patients with diabetes should not consume bilberry extracts. The bilberry juices have been shown to lower blood sugar and could increase the effect of diabetic medicines.
Hypoglycaemia can also occur if bilberry supplements are taken together with garlic and other fenugreek, ginger, ginseng, and ginseng.
The long term consumption of the leaves is dangerous and toxic.
Long-term consumption of bilberry fruit with a dose of 180 mg/kg the anthocyanosides was safe for 6 months.Contradictions-
The antiplatelet aggregating abilities of bilberry extracts mean that very high doses must be administered to patients with haemorrhagic diseases (Alternative Medicine Review Volume Volume 2001).Dosage-
The type of bilberry consumed determines the dosage.
Fresh berries can be consumed from 55 to 115g three times daily.
You can eat dried berries every day, as they only contain a small amount flavonoids.
The bilberry liquid extracts can be taken in 80 to 160 mg daily.
The daily recommended intake of anthocyanosides amounts to approximately 20-40mg. It can be taken for up to three times daily.
The standardized capsules, which contain 25 percent of standardized Anthocyanosides, can be taken between 80 and 160 mg three times per day.
The chronic toxicity of 1.5g/kg/day, which is the maximum daily dose for anthocyanins in 2017 makes the leaves not suitable for long-term usage (Anthocyanins).
References
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The role of glucose transporters and the pharmacokinetic profile for bilberry and anthocyanins, in rats: LC/MS/MS as well as computational studies.
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