| Name | Betulinic acid |
| Description | Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase. |
| Kinase Assay | Topoisomerase I-DNA interaction: 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 bromid |
| In vitro | In LNCaP cell cultures of athymic nude mice, Betulinic acid inhibits the growth of prostate cancer cells and tumors (xenografts). This inhibitory effect is partly due to the downregulation of protease-dependent Sp1/3/4 and several SP-regulated genes. |
| In vivo | As an anti-melanoma agent, Betulinic acid inhibits the activity of aminopeptidase N (IC50: 7.3 μM). It exhibits anti-HIV properties by blocking HIV replication in H9 lymphocytes (EC50: 1.4 μM) and inhibiting the growth of uninfected H9 cells (IC50: 13 μM). Moreover, Betulinic acid shows potential as an anti-cancer candidate, suppressing the activity of eukaryotic topoisomerase I (IC50: 5 μM). |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | Ethanol : 10 mg/mL (21.89 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 33.3 mg/mL (72.98 mM), Sonication is recommended.
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| Keywords | Human immunodeficiency virus | HIV | Mitophagy | Nuclear factor-kappaB | Autophagy | Endogenous Metabolite | inhibit | Nuclear factor-κB | ALS357 | Topoisomerase | NF-κB | Inhibitor | Mitochondrial Autophagy | Betulinic acid | Apoptosis | ALS 357 |
| Inhibitors Related | Sucrose | Tributyrin | Glycerol | Thymidine |
| Related Compound Libraries | Anti-Parasitic Compound Library | Selected Plant-Sourced Compound Library | Natural Product Library | Drug Repurposing Compound Library | Miao medicine Compound Library | Inhibitor Library | Anti-Aging Compound Library | Anti-Cancer Drug Library |
United States
