Betulinic Acid Raw Materials Betulinic Acid powder

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Betulinic Acid Powder Usage and Synthesis.

Betulinic acid is a pentacyclic triterpenoid and its derivatives possess significant anti-tumour and anti-HIV activities.

Recently, phase II clinical trials of betulinic acid derivatives against HIV have been successful, and as a result, betulinic acid is considered to be one of the most promising drug lead compounds.

The main source of Betulinic acid is extracted and purified from the bark of the birch tree, but since the compound is found in the bark of the birch tree at a very low content of about a few ten thousandths of a percent, and about 230,000 tonnes of birch bark are consumed annually for the Chinese market, the prolonged logging has led to a serious shortage of birch resources, which has seriously impacted on the development and utilisation of Betulinic acid.

In terms of drug development, researchers based on nuclear factor κB receptor activating factor ligand and macrophage colony-stimulating factor jointly induced osteoclast differentiation system, from dozens of amino-substituted pyrazole and betulinic acid derivatives screened to obtain the osteoclast differentiation inhibitory activity and low cytotoxicity of the compound.

Although the number of enterprises in China's Betulinic Acid industry is relatively large, the scale is generally small, mostly belonging to small and medium-sized enterprises. The overall technical level of China's betulinic acid industry is relatively backward, and although the number of related enterprises is large, most of them are still in the stage of imitation and customised production.

Uses of Betulinic Acid.

1.Anti-inflammatory effects

Most pentacyclic triterpenoids have anti-inflammatory activity. The anti-inflammatory effect of betulinic acid has been verified in ex vivo and in vivo model systems in model systems. It can inhibit PGE2 production and reduce the inflammatory response.

2. Bacteriostatic effect

It can inhibit a variety of bacteria, including Escherichia coli, Bacillus subtilis, Staphylococcus aureus and Staphylococcus epidermidis.

3. Antiviral effect has more prominent antiviral activity, especially anti-HIV activity, but also in the anti-hepatitis C virus, anti-simple rash virus, anti-Echovirus, anti-influenza virus and so on have an effective effect.

4. Antihyperlipidemic effect

It has been found that Betulinic acid and its derivatives can regulate adipokines, reduce lipogenesis, lower triacylglycerol and total cholesterol levels and other mechanisms to play the role of anti-hyperlipidemia.

5. Antidiabetic effect

In the treatment of diabetes mellitus has shown good efficacy, which is mainly through the inhibition of α-amylase and α-glucosidase to reduce the hydrolysis of polysaccharides and promote glycogen synthesis of two aspects of treatment.

6.Antioxidant

Stress-active BA has a protective effect on normal cells and organisms, and this effect is related to anti-oxidative stress. For example, Betulinic acid has a protective effect on ischemia-reperfusion injury of brain, kidney and heart, etc. BA has a protective effect on ischemia-reperfusion brain injury in mice through anti-oxidative stress, anti-nitrogenation stress and increased blood flow.

7.Other

DiseasesNow there are also some studies found that it has a certain improvement effect on Alzheimer's disease. Its protective effect is mainly through attenuating neurobehavioural and cognitive dysfunction, reducing pro-inflammatory cytokines in the hippocampus, and reducing oxidative and nitrosative reactions. Betulinic acid has also been reported in the literature to have some anxiolytic effects, and its components have been used in some anxiolytic drugs.

Preparation of Betulinic Acid.

The microbial transformation method uses enzymes produced by organisms during metabolism to catalyse the reaction on the substrate to obtain the target product.

Compared with chemical synthesis methods, microbial transformation has high stereoselectivity, mild reaction conditions, low pollution and low cost, and this method has the potential for industrialisation.Feng et al. catalysed birch alcohol by culturing ArmillarialuteovirensZJUQH100-6, Cunninghamellablakesleeana cells to directly microbial transformation to produce BA.

In addition, a study was conducted for the first time to improve the yield of BA using biotechnology for induced production of BA from healing tissues of Ocimum species, which provided a new approach for the preparation of BA as well as other anticancer triterpene, etc.

Recently, a study reported the successful synthesis of BA using microorganisms by substituting the entire metabolic pathway of BA in plants into yeast cells.

It was found that the balance of metabolic flow in the fatty acid and terpene precursor synthesis pathways had a significant effect on BA synthesis, and the BA yield was significantly increased by the synergistic expression of the key regulatory genes in these two metabolic pathways (HFA1, HMG1, and ERG9), and the engineered bacterium was able to synthesise milligrams per litre of medium, thus, the preparative synthesis of BA was elevated to a new level.

Produt Method of Betulinic Acid.

Firstly, it is obtained by extraction and separation from natural plants. This way consumes a large amount of solvent, low yield, impurities are not easy to separate, so it is rarely used;

Secondly, betulinic acid is obtained by organic synthesis with betulinol as precursor. This method has been applied to industrial production, can get industrial scale betulinic acid, is now the main source of betulinic acid on the market;

Thirdly, using betulinol as precursor and generating betulinic acid through microbial conversion. This approach represents a new direction for the future of the plant extraction industry, but there are still many technical difficulties that cannot be solved.

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