Betulinic acid is a natural pentacyclic triterpenoid compound, which is an inhibitor of eukaryotic cell topoisomerase I with IC50 value of 5 μM. It has anti-inflammatory, anti-malaria, anti-AIDS and anti-tumor activities. Betulinic acid(Betulinic acid) is also an agonist of 20S proteasome. EC50=5.5μmol/L, Betulinic acid can specifically enhance cT-L activity of 20S proteasome.
| Cell Experiment | |
|---|---|
| Cell lines | H9 lymphocytes |
| Preparation method | Incubating H9 lymphocytes ( 1 ×107 cells/ml) in the presence or absence of HIV-1 (IIIB isolate) for 1 h at 37 °C. Washing cells thoroughly to remove unadsorbed virions and resuspending in culture medium. Adding betulinic acid (diluted in test medium) to the culture medium. After incubation for 3 days at 37 °C, the cell densities of uninfected cultures are determined to assess toxicity of betulinic acid. Using a p24 antigen capture assay to determine the level of HIV infection in HIV-treated culture |
| Concentrations | |
| Incubation time | 3 days |
| Animal Experiment | |
|---|---|
| Animal models | LNCaP tumor xenograft model |
| Formulation | Diluted in corn oil containing 1% DMSO |
| Dosages | 10 and 20 mg/kg/d |
| Administration | Orally |
| Molecular Weight | 456.7 |
| Formula | C30H48O3 |
| CAS Number | 472-15-1 |
| Solubility (25°C) | DMSO 30 mg/mL |
| Storage | 2-8°C, protect from light, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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