Betulinic acid is a pentacyclic triterpene which induces apoptosis and antiangiogenic responses in tumors derived from multiple tissues. Betulinic acid shows anti-HIV activity by blocking HIV replication in H9 lymphocytes with an EC50 value of 1.4 μM and inhibiting uninfected H9 cell growth with an IC50 value of 13 μM. In vivo, Betulinic acid inhibits prostate cancer cell and tumor (xenograft) growth in athymic nude mice bearing LNCaP cells and this is due, in part, to proteasome-dependent downregulation of Sp1, Sp3, Sp4 and several Sp-regulated genes.
|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|
|Incubation time||3 days|
|Animal models||LNCaP tumor xenograft model|
|Formulation||Diluted in corn oil containing 1% DMSO|
|Dosages||10 and 20 mg/kg/d|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
Betulinic acid inhibits prostate cancer growth through inhibition of specificity protein transcription factors.
Chintharlapalli S, et al. Cancer Res. 2007 Mar 15;67(6):2816-23. PMID: 17363604.
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