Toviy Lovitz Russian chemist
who discovered betulin
About Betulin
Betulin – а birch extract, a crystalline organic matter discovered by Johann Tobias Lowitz.
Chemical
formula of betulin
С36Н60О3
Betulin was discovered by T.E. Lovitz in birch water. It is also contained in birch tar. It is a white tar-like substance which fills
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IUPAC Name: (1R,3aS,5aR,5bR,7aR,9S,11aR,11bR,13aR,13bR)-3a-(hydroxymethyl)-5a,5b,8, 8,11a-pentamethyl-1-prop-1-en-2-yl-1,2,3,4,5,6,7,7a,9,10,11,11b,12,13,13a,13b-hexadecahydrocyclopenta[a]chrysen-9-ol

Betulin (lup-20(29)-ene-3β,28-diol) is an abundant, naturally occurring triterpene. It is commonly isolated from the bark of birchtrees where it forms up to 30% of the dry weight of the extractive [1] and is found in birch sap as well.[2] The purpose of the compound in the bark is not known. It can be converted to betulinic acid (the alcohol group replaced by a carboxylic acid group), which is biologically more active than betulin itself.

Betulin contains betulinic acid, which possesses a wide spectrum of biological and pharmacological activities. Betulinic acid has antimalarial and anti-inflammatory activities. Betulinic acid and its derivatives have especially shown anti-HIV activity and cytotoxicity against a variety of tumor cell lines comparable to some clinically used drugs. A new mechanism of action has been confirmed for some of the most promising anti-HIV derivatives, which makes them potentially useful additives to the current anti-HIV therapy. Betulinic acid is specifically cytotoxic to several tumor cell lines by inducing apoptosis in cells. Moreover, it is non-toxic up to 500 mg/kg body weight in mice. The literature concerning derivatization of betulin for structure-activity relationship (SAR) studies and its pharmacological properties is reviewed.

Betulin is characterized by broad spectrum of benefits mostly assigned to the dermatology area: anti-inflammatory, antipruritic, it promotes differentiation of skin cells (keratinocytes), promotes wound healing and help to build the impugned protective barrier of the skin. In short, they harmonize and normalize disturbed skin functions such as exist inter alia in atopic dermatitis, psoriasis, contact dermatitis or extremely dry skin. Moreover betuline has a very good skin compatibility and according to present knowledge evokes no allergies. Other pharmacological effects of Betuline, such as antiviral, antimicrobial, antioxidant, anti-tumor, tissue-protecting and its usefulness for the medical world are the subject of research.

The very compound that makes the birch “shine bright white” has been tentatively linked to treatment for such devastating human ailments as some melanomas or cancer, several forms of herpes and even for AIDS.

Betulin, a powdery substance in the outer bark of a birch tree, has been shown to help wounds heal faster and cut inflammation. Many cosmetic companies, touting it as a skin toner and restorer, add birch bark extract to various products. And a birch bark compound, betulinic acid, is being tested as a treatment for melanoma and other serious diseases.

Betulin contains betulinic acid, which possesses a wide spectrum of biological and pharmacological activities. Betulinic acid has antimalarial and anti-inflammatory activities. Betulinic acid and its derivatives have especially shown anti-HIV activity and cytotoxicity against a variety of tumor cell lines comparable to some clinically used drugs. A new mechanism of action has been confirmed for some of the most promising anti-HIV derivatives, which makes them potentially useful additives to the current anti-HIV therapy. Betulinic acid is specifically cytotoxic to several tumor cell lines by inducing apoptosis in cells. Moreover, it is non-toxic up to 500 mg/kg body weight in mice. The literature concerning derivatization of betulin for structure-activity relationship (SAR) studies and its pharmacological properties is reviewed.

Fields of application

  1. Raw material for pharmaceutical production;
  2. In biologically active food supplements for prevention and tretament of liver porblems includng hepatitis C, cancer and HIV.
  3. As a main active ingredient in parfumery-cosmetic products especially for skin care application ;

It has been known since ancient times that white part of birch bark possesses strong antiseptic properties: birch bark is applied to wounds for faster healing, tar and activated carbon is made also from it. Ancient Russian medicinal manuals, recommended grinded birch bark for treating purulent wounds, prolongedly unhealing ulcers: "so that the rotten meat from the ulcer was eaten away, grinded birch crust should be poured into the rotten wound ". A rim made from the white part of birch bark "removes" headache. It is possible to say that in nature there is no other tree so many parts of which (crust, leaves, buds, juice, wood and phytopathogenic parasitic fungus - chaga), so frequently were used in folk medicine.

Especially successfully (in 3-10 min) the bactericides of white part of a birch bark manage to eliminate pathogens of typhoid fever, tuberculosis and diphtheria. Unique therapeutic properties are given to white part of birch bark thanks to BETULIN - substance from the class of triterpenoids (triterpenovy diatomic alcohol of lupan). White part of a birch bark remains white even when the tree itself has completely rotted. The resistance of the white part of a birch bark to harmful microflora is attributed to betulin.

The studies, carried out during recent years, showed that betuline has valuable pharmacological properties: antioxidant, antitumorigenic, hepatoprotective, antiviral, immunomodulator, antibacterial, that regenerate, antipyretic, bile-expelling. Betulinic acid has been explored as a potential treatment for skin cancer for more than a decade. Betulin, its derivatives and other birch bark compounds also are being tested for effectiveness in treating HIV, the virus that causes AIDS, and respiratory syncytial virus (RSV), which can cause severe cold-like symptoms and pneumonia.

In the white part of a birch bark there are other medical substances: betulinic acid, b - sitosterol, flavonoids, lupeleol and other. Examinations conducted in Russian institute of pharmacology, showed that the complex of substances forming the white part of a birch bark possesses high antimutagenic activity, capable of lowering the number of mutations in the chromosomes and the genes, the frequency of the appearance of hereditary changes in the organism. The antimutagenic action of the substances of white part of a birch bark is connected with their capability for the suppression of free-radical oxidation, and in the ability of white part of a birch bark to induce the production of interferons, which, as it’s known, positively influence the processes of reparation of DNA.The substances contained in white part of a birch bark contribute to the decrease of hypoxia and to increase of the stability of organism to the oxygen deficiency, being antihypoxant correcting the metabolism of cells.

Treatment of liver diseases is directed, mainly, to protect cells of liver from damages caused by different chemical substances. Application of medical plants and herbs appear to be an important component in treatment and rehabilitation of patients undergoing antitumor therapy with radiation and surgery.

Unique biological activity of substances of those isolated by white part of a birch bark contributes to the decrease of adverse toxic actions of chemo - and radiation therapy on the organism. The antioxidant activity of betuline is connected with its direct effect on the enzyms of the antioxidant protection, whose basic functional role consists of decomposition of organic peroxides, first of all - peroxides of lipids, which play paramount role in the disturbance of normal structure of biological membranes. Substances forming betulin possess high hepatoprotective and detoxifying property. Betulin normalizes bile secretion, reduces cholesterol level in blood. Statistics testifies that in the regions, where white part of birch bark is traditionally used in household articles such as caskets, boxes and ducts for storing food products, people live longer and the index of oncologic diseases has been recorded as very low.

Clinical Evidence

of betulin health benefits
Cell Metabolism

The unexpectedness of the discovery is that the presence of betulin in an organism changes the mechanism of lipid digestion by liver. This leads to reduction of cholesterol in blood and consequently to reduction of “atherosclerotic plaques” in vessels. It also helps prevent obesity and increases sensitivity to insulin.

Химия в интересах устойчивого развития

The unexpectedness of the discovery is that the presence of betulin in an organism changes the mechanism of lipid digestion by liver. This leads to reduction of cholesterol in blood and consequently to reduction of “atherosclerotic plaques” in vessels. It also helps prevent obesity and increases sensitivity to insulin.
Bao - Liang Song

Бао-Лян Сонг (Bao-Liang Song)

Betulin has 15 health benefits

Спектр полезных свойств бетулина взаимосвязан,
многие вытекают одно из другого
Antiviral effect
Betulin induces synthesis of interferon when delivered orally. It is important to fight viral infections such as avian influenza, influenzavirus A, herpes simplex, hepatitis C, HIV-1
Hepatoprotective effect
Betulin being a natural hepatoprotector is effective in case of acute and chronic liver injuries with different aetiology as well as injuries complicated by cholestasis
Neuroprotective effect
Beulin allows to provide the most effective treatment of patients suffering from cerebral ischemia and to prevent development of serious and inconvertible injury of brain neurons
Antiseptic
Acceleration of the wound healing process
Hypocholesteremic
Lowering of cholesterol and reduction of the number of “atherosclerotic plagues” in vessels
Hypolipidemic
Normalization of bialation, reduction of the amount of tryglycerides in blood, improvement of vessels state
Antihypoxant
Improvement of organism resistance to alkaline environment
Choleractic
Imrovement of bile outflow
Antilithogenous
Prevention of gallstone formation and cholecystitis
Antimutagentic
Protection from mutagens — chemical substances causing changes in human genetic apparatus
Immunomodulatory
Strong immune system modulation in case of immunodeficiency, viral pathologies and antineoplastic therapy
Antioxidant
Free radicals neutralization as the main cause of senescence
Gasoprotective
Reinforcement of the defenses of gastric mucosa against effect of aggressive factors of gastric acid
Anti-inflammatory
Tissue repair after inflammatory process
Antineoplastic
Protective care of neoplasms
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