product name Betulinic acid
Description: Betulinic acid (also known as ALS-357) is a natural pentacyclic triterpenoid from Syzigium claviflorum that displays anti-HIV and antitumor activity Betulinic acid is a inhibitor of HIV-1 with EC50 of 1.4 μ M. Betulinic acid selectively induces apoptosis in tumor cells by directly activating the mitochondrial pathway of apoptosis through a p53- and CD95-independent mechanism. Betulinic acid also displays TGR5 agonist activity (EC50 =1.04 μM).
References: Planta Med. 1998 Oct;64(7):655-7; J Nat Prod. 1994 Feb;57(2):243-7.
456.7
Formula
C30H48O3
CAS No.
472-15-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (43.8 mM)
Water: <1 mg/mL
Ethanol: 10 mg/mL (21.9 mM)
Solubility (In vivo)
Synonyms
ALS-357
other peoduct :
| In Vitro |
In vitro activity: 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. Betulinic acid also acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 μM. In addition, Betulinic acid inhibits eukaryotic topoisomerase I activity with IC50 of 5 μM and can be exploited as a strong candidate for anti-tumor drug. Kinase Assay: Annealed 25-mer duplex of oligonucleotide-1 and oligonicleotide-2 is incubated with 25 or 50 units of rat liver topoisomerase I at 8 °C for 15 min in the presence or absence of betulinic acid in binding buffer. After incubation the reaction mixtures are electrophoresed in 7% non-denaturing polyacrylamide gel at 4 °C in 0.167 × TBE buffer and DNA bands are stained with ethidium bromide. Cell Assay: |
|---|---|
| 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. |
| Animal model | LNCaP tumor xenograft model |
| Formulation & Dosage | Diluted in corn oil containing 1% DMSO; 10, 20 mg/kg/d; p.o. administration |
| References | Planta Med. 1998 Oct;64(7):655-7; J Nat Prod. 1994 Feb;57(2):243-7. |
