Betulinic acid

472-15-1

456.70

DMSO : 35.71 mg/mL (78.19 mM; Need ultrasonic); H2O : < 0.1 mg/mL (insoluble)

Apoptosis; Cell Cycle/DNA Damage; Autophagy; Anti-infection; NF-kappaB; Autophagy; Metabolic Enzyme/Protease

Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 uM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties. Betulinic acid acts as a new activator of NF-kB.
IC50 & Target: IC50: 5 uM (eukaryotic topoisomerase I)

EC50: 1.4 uM (HIV-1)
In Vitro: Betulinic acid is a eukaryotic topoisomerase I inhibitor, with an IC50 of 5 uM, and prevents topoisomerase I-DNA interaction. Betulinic acid (10, 20, 40, 80, and 160 uM) significantly suppresses MDA-MB-231 cell viability in a time- and dose-dependent manner after treatment for 24 or 48 h. Betulinic acid (20, 40 uM) causes decrease in Bcl-2 expression of MDA-MB-231 cells. Betulinic acid also induces morphological changes of MDA-MB-231 cells at 20 uM, and leads to ultrastructure changes of MDA-MB-231 cells at 40 uM. Betulinic acid shows anti-HIV activities, with an EC50 of 1.4 uM in acutely infected H9 lymphocytes.
In Vivo: Betulinic acid (10 and 30 mg/kg, p.o.) significantly abrogates colon shortening, and reduces malondialdehyde (MDA) and lipid hydroperoxide levels in dextran sulfate sodium (DSS)-induced colitis in mice. Betulinic acid (30 mg/kg, p.o.) restores superoxide dismutase (SOD), catalase activity and glutathione (GSH) content to control levels in DSS-induced colitis in mice. Betulinic acid (30 mg/kg, p.o.) also inhibits the DSS-induced increase in inflammatory markers. Betulinic acid (3, 10, 30 mg/kg, p.o.) suppresses acetic acid-induced writhing responses and mustard oil (MO)-induced visceral nociception in mice.