What is Betulin?
Betulin is an SREBP inhibitor with IC50 of 14.5 μM in K562 cells.
Bioactivity
Target:IC50: 14.5 μM (SREBP, K562 cell), 74.1 μM (SREBP, HeLa cell), 17.1 μM (SREBP, GOTO cell)[1], 21.09 μM (SREBP, 181P cell), 20.62 μM (SREBP, HeLa cell)
In vitro studies: Betulin (BE) has a wide range of biological and pharmacological properties, of which anticancer and chemopreventive activities have attracted most of the attention. BE has been shown to elicit anticancer properties by inhibiting cancer cell growth. Depending on the cancer cell type, BE has shown a rather different range of antiproliferative activities, ranging from weak inhibition of proliferation in human erythroleukemia cell line (K562) cells to strong inhibition in human neuroblastoma cells (SK-N-AS), where The most obvious effect. In addition, BE was also found to express significant cytotoxicity against primary cancer cell cultures isolated from tumor samples obtained from patients with ovarian, cervical and glioblastoma, with IC50 values ranging from 2.8 to 3.4 μM, comparable to significantly lower than that.
established cell lines . Comparison of crude birch bark extract and purified betulin and betulinic acid in human gastric cancer (EPG85-257) and human pancreatic cancer (EPP85-181) drug susceptibility and resistance (daunorubicin and mitoxantrone) cells cytotoxic activity of the line. showed significant differences in sensitivity between cell lines, depending on the compound used, suggesting that both betulin and betulinic acid could be considered promising leads for the treatment of cancer.
In vivo studies :Betulin can improve glucose intolerance and improve basic learning performance. Betulin treatment can significantly restore hippocampal SOD activity and reduce MDA content. Betulin also significantly reduced the levels of inflammatory cytokines in serum and hippocampus. Furthermore, the administration of BE effectively upregulated the expression of Nrf2, HO-1 and blocked the phosphorylation of IκB, NF-κB. In conclusion, BE may have a protective effect on STZ-induced cognitive decline in diabetic rats via the HO-1/Nrf-2/NF-κB pathway
Solubility:In vitro:10mM in DMSO
Stock solution:
1 mM 2.2588 mL 11.2938 mL 22.5876 mL
5 mM 0.4518 mL 2.2588 mL 4.5175 mL
10 mM 0.2259 mL 1.1294 mL 2.2588 mL
Cellular assays: Chemoresistance was tested using a proliferation assay based on sulforhodamine B staining. Briefly, 800 cells per well were seeded in 96-well plates in triplicate. After 24 hours of attachment, substances were added in a dilution series for 5 days of incubation before SRB staining. Incubation was terminated by replacing the medium with 10% trichloroacetic acid, followed by a further incubation at 4°C for 1 hour. Subsequently, the plates were washed five times with water and stained by adding 100 μL of 0.4% SRB in 1% acetic acid for 10 min at room temperature. Unbound dye was removed by soaking the plate five times with 1% acetic acid. Absorbance was read at 562 nm after air drying and redissolving of protein-binding dye in 10 mM Tris-HCl (pH = 8.0)
Animal experiments :Rats:;Rats were randomly divided into 5 groups (n = 10): control group, STZ group, STZ + betulin (20 mg/kg) group, STZ + betulin (40 mg/kg) group. Diabetes was induced for 4 weeks using STZ (30 mg/kg, ip) dissolved in citrate buffer (pH 4.4, 0.1 M) using a 1 mL syringe, while control rats received an equal volume of citrate buffer. Thereafter, diabetic rats were treated with betulin (20 mg/kg, 40 mg/kg) for an additional 4 weeks.
Shipping:room temperature; may vary
Pysical and chemical propertities
Density | 1.0±0.1 g/cm3 |
Boiling point | 522.3±23.0 °C at 760 mmHg |
Melting point | 256-257 °C(lit.) |
Molecular formula | C30H50O2 |
Molecular weight | 442.717 |
Flash point | 210.9±17.2 °C |
Exact mass | 442.381073 |
PSA | 40.46000 |
LogP | 9.01 |
Appearance | white crystalline powder |
Vapor Pressur | 0.0±3.1 mmHg at 25°C |
Refractive index | 1.525 |
Storage conditions | Store in an airtight, dry place at 2-8°C to avoid contact with other oxides |
stability | Used and stored as specified, will not decompose, avoid contact with oxides |
Specification
98%
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