Hepatoprotective activity, lipid-lowering properties, anti-atherosclerotic properties
Model:
In vitro with the use of biotest system on the basis of a key enzyme of rat liver cytochrome P-450 microsomal system

Result, opinion:  
The studied birch bark extract drugs containing various concentrations of betulin have hepatoprotective and detoxifying activity as they activate rat liver cytochrome P-450 microsomal system with respect to substrates 1 and type 2; aniline and dimethylaniline.



Source:
“Birch World” Ltd.
"The results of the study of hepatoprotective and detoxifying activity of betulin drugs using biotest systems of rat liver cytochrome P-450 microsomes"
M. Mineeva  , L. Strelkova





Model:
Experimental hepatitis model of rats.

Result, opinion:  
As a result of experimental research of birch bark extract's influence on intact rats' bile secretion and functional activity of rat liver with tetrachloromethanic hepatitis established the following:
-Birch bark extract exhibits a pronounced detoxifying activity, as evidenced by the positive effect of the drug on the detoxification system in the liver of animals on the background of CCI4- hepatitis
-Increased activity of biotransformation enzymes
-Cytochrome P450 and glutathione transferase

Source:
“Birch World” Ltd.
“The protocol of experimental pharmacological study of choleretic and hepatoprotective properties”
ARSRI of Medicinal and Aromatic Plants (VILAR), Russian Academy of Agricultural Sciences
A. Baginskaya, M. Mineeva and etc.

Model:
Determination of BED's affinity to a biological membrane using the method of fluorescent probes

Result, opinion:  
Research suggests membrane-acting of dry birch bark extract in relation to the microsomal membrane. Dry birch bark extract in vitro and in vivo is a substance that competes for binding sites with the MBA probe improves its permeability, increasing the polarity of deep membrane layers.



Source:
“Birch World” Ltd.
“Research report on dry birch bark extract's membrane-acting in relation to the intact membranes of rat liver microsomes and at course administeration of betulin to rats with chronic hepatitis”
Under the leadership of M. Mineeva.


Model: in vivo

Result, opinion:  
The experiments indicate diverse pharmacological activity of triterpene substances. In this case we can say that betulenol has the lipid-lowering effect to the greatest extent and its acetylation does not increase the lipid-lowering effect; the most effective doses are 75 and 150 mg/kg. Choleretic activity is inherent in approximately equal extent in the amount of triterpenoids and betulenol and is even more pronounced in betulenol diacetate. However anti-lithogenic activity to the greatest extent is inherent to betulenol. Substances in doses of 10 and 75 mg/kg have approximately the same effect. The greatest effect of normalizing toxic in hepatitis have triterpenoids in a dose of 10 mg/kg. Wherein has betulenol the greatest impact on ALT (a measure of cytolysis) and triterpenoids amount - on the activity of alkaline phosphatase (an indicator of cholestasis); all substances (amount of triterpenoids, betulenol and its diacetate) have a positive effect on lipophanerosis of the liver.



Findings: The amount of triterpenoids from birch bark, individual triterpenoid betulin and its diacetate have hypolipidemic, choleretic,  hepatoprotective and anti-lithogenic activity and reduce cholesterol in the aorta. The pharmacological activity of triterpenoids depends on their compound and dose and exceeds the effect of a number of official drugs Роlysponinum , Cetamiphenum , Saparalum and Glycyram.



Source:
“Pharmacological properties of birch bark triterpenoids”
Department of Biochemistry (head – professor Y. Vasilenko) and Drug Technology (head – professor Y. Pshukov) of Pyatigorsk Pharmaceutical Institute.
Chapter 7.
The study of biological activity of triterpenoids from birch bark and roots of false licorice.

The thesis for the degree of Doctor of Pharmacy V. Semchenko, Pyatigorsk, 1993.


Model: in vivo
Result, opinion:  
Betulin reduces obesity when fed a high-fat diet by increasing energy expenditure, while lovastatin (known statin) by reducing lipid absorption/increasing excretion.
Betulin improves lipid parameters of blood, liver and adipose tissue of mice. Betulin interacts with proteins that bind sterol regulatory element - SREBPs (sterol regulatory element-binding proteins) – with transcription factors, which as is known, are important for activation of the expression of genes involved in the biosynthesis of cholesterol , fatty acids and triglycerides. In studies on cells scientists have confirmed that betulin lowers the activity of usually activated SREBPs genes and lipid levels.
Inhibition of SREBP may be a useful strategy for the treatment of type II diabetes and atherosclerosis. Betulin can serve as a lead compound for the pharmacological control of metabolic disorders.

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It can be concluded that the sum of triterpenoids from birch bark is an effective bacteriostatic agent against microorganisms such as Staphylococcus aureus, Bacillus antracoides, Eschericha coli and Salmonella typhimurium, and also retards the growth of dermatophyte fungi Candida albicans and Aspergillus niger. High activity against Aspergillus niger in prospective opens  possibilities for the use of birch triterpenoids in veterinary with regard to frequent contamination of farm animals with these microorganisms.
Glucose tolerance and insulin resistance significantly improve when using betulin.
Based on the original natural compounds of betulenol (1) and betulinolic acid (2) with relatively low anti- HIV activity, by their chemical modification a number of highly active compounds have been found. The most promising semi-synthetic derivative of Lupane series include amides, dipeptides and esters of  betulenolic and betulinic acids.