Betulin Powder CAS 473-98-3

Betulin (BE) is a rich pentacyclic triterpenoid and secondary metabolite found in the outer bark of birch trees (Betulaceae sp.), with a wide range of biological and pharmacological properties, among which anti-cancer and chemopreventive activities are of great concern. Moreover, naturally high-purity Betulin powder can serve as a precursor for compounds with more biological functions, such as betulinic acid (carboxylic acid groups replacing alcohol groups).

What are the results of anti-cancer research on Betulin?

Betulin and its natural and synthetic derivatives have specific effects on cancer cells and low cytotoxicity on normal cells. Although the anti-tumor mechanism of betulin is not clear, researchers have proved its anti-tumor effect through some experiments.
We know that the use of compounds from natural plants is considered as a new aspect of treating human tumor diseases. Natural plant-derived substances are relatively easy to obtain because they are ubiquitous in nature, and seem to constitute a group of promising anticancer or chemopreventive agents, and play a key role in developing drugs or supplements for treating several human cancers.
For example, at present, the most widely used anti-cancer products in clinic are taxane (including Paclitaxel isolated from Taxus brevifolia) and vinca alkaloids extracted from plants.

According to the latest research, natural betulin powder can induce anti-cancer properties by inhibiting the growth of cancer cells. Its cytotoxicity and anti-proliferation potential have been studied in several established cancer cell lines, primary tumor cell cultures and cancer xenotransplantation models.

According to different cancer cell types, betulin showed different anti-proliferation activities, ranging from weak inhibition on human erythroleukemia cell line (K562) to strong inhibition on human neuroblastoma cell line (SK-N-AS), with the most obvious effect. In addition, betulin was also found to have significant cytotoxicity on primary cancer cell cultures isolated from tumor samples of patients with ovarian cancer, cervical cancer and glioblastoma, and its IC50 value ranged from 2.8 to 3.4 μM, which was significantly lower than that of established cell lines.

In addition, betulin has also been proved to have anti-proliferative activity against cancer in human digestive system. At the concentrations of 21.09 μM and 18.74 μM, betulin inhibited the proliferation of pancreatic cancer (EPP85-181) and human gastric cancer (EPG85-257) by 50%, respectively. MGC-803, another gastric cancer cell line, has a proliferation inhibition rate of 43.7% and 45.1% at the concentration of 20 μM, respectively. Betulin has been studied for its anti-proliferation potential on human colorectal cancer, DLD-1, HT-29, Col2 and SW707 cells. Its inhibitory effect on cell proliferation is highly dependent on cell lines. The BE IC50 values of DLD-1 and HT-29 colon cancer cells are equivalent, which are 6.6 μM and 4.3 μM, respectively, far lower than those of Col2 cells (45.2 μM) and SW707 cells (51.7 μM). On the contrary, betulin has no effect on HT-29 cells, and its IC50 value is higher than 250 μM m..

Because betulin has multi-target activity on cancer cells, it can be used in combination with common chemotherapy drugs in clinical application, and the synergistic effect is helpful to eliminate cancer cells including drug-resistant cells. In addition, another new method of its application in cancer treatment is chemical modification with various ligands to obtain enhanced cytotoxicity to tumor cells or better solubility and bioavailability than the parent compound. Therefore, betulin powder is an important precursor to synthesize new betulin derivatives with better anticancer and pharmacokinetic properties.

Besides anticancer application, what other physiological functions does betulin have?

Betulinic acid can improve T cell proliferation, NK cell activity and INF level, and the anti-tumor mechanism may be related to directly or indirectly enhancing the body's anti-tumor immunity. In addition to this excellent performance, betulin is cheap and widely available in nature, and its content in birch bark is as high as 30% of dry weight, but this resource has not been fully utilized. Because, in previous studies, it was considered that betulin had no definite medicinal value, and the extraction cost was relatively high. At present, Betulinic acid is mainly made from betulinic alcohol. At present, Betulinic acid has been proved to have antimalarial, anti-inflammatory, anti-melanoma and other tumors, anti-HIV and other effects. Recently, Polish scholars proposed that betulin has obvious protective effect on alcohol-induced liver cell injury.
1. Antitumor activity
As I said earlier, the effective experimental data of renting and renting has made a solid endorsement for the application of betulin in anticancer. According to the latest research, the active substance of Betulin powder can directly cause some types of tumor cells to start a self-destructive apoptosis program, and can slow down the growth of several types of tumor cells.

2. Anti-HIV activity
Betulin and its derivatives, as biological agents, show great potential in the treatment of HIV and cancer, which works by interfering with the later stage of the virus life cycle, which is related to the entry, growth and maturity of the virus. The mechanism study shows that although betulin and its derivatives do not inhibit HIV-1 reverse transcriptase, they can inhibit the formation of nucleosome when the concentration is higher than IC50. Therefore, the researchers concluded that these betulin derivatives acted by interfering with the later stage of the virus life cycle.

3. Anti-inflammatory effect
Most five-membered triterpenoids have anti-inflammatory properties, including betulinic acid and betulin. The anti-inflammatory properties of these two compounds have been verified in a large number of in vitro and in vivo model systems. The results show that betulin and betulinic acid have mild anti-inflammatory properties at high concentrations, and their anti-inflammatory properties are mainly attributed to the inhibition of non-neural gene pathways.

4. Others
Betulin can inhibit the maturation of sterol regulatory element binding protein (SBERPs) in vivo, thus reducing the biosynthesis of cholesterol, triglycerides and fatty acids. Relieve diet-induced obesity, reduce lipid content in serum and tissues, and then effectively prevent obesity and atherosclerosis; Betulin can also improve insulin sensitivity and has a good effect on type ⅱ diabetes. Betulin has antibacterial, antiviral, inhibiting protein dissolution in hair fibers, improving damaged hair luster, and promoting hair growth.

To sum up, betulin is a kind of chemical medicine, plant extract and Chinese herbal medicine extract. It has mild anticancer, antibacterial, antiviral and other biological activities, and can also be used as a precursor for the synthesis of betulin derivatives and betulinic acid and corresponding derivatives. At present, betulin is mainly used as a pharmaceutical intermediate. It can also be used in industries such as food and cosmetics.

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