Betulinic acid

Betulinic acid is a natural pentacyclic triterpenoid, acts as a eukaryotic topoisomerase I inhibitor, with an IC₅₀ of 5 μM, and possesses anti-HIV, anti-malarial, anti-inflammatory and anti-tumor properties^[1][2][3][4]. Betulinic acid can cross the blood-brain barrier^[5]. IC50 & Target:IC50: 5 μM (eukaryotic topoisomerase I)^[1]
EC50: 1.4 μM (HIV-1)^[4] In Vitro:Betulinic acid is a eukaryotic topoisomerase I inhibitor, with an IC₅₀ of 5 μM, and prevents topoisomerase I-DNA interaction^[1]. Betulinic acid (10, 20, 40, 80, and 160 μM) 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 μM) causes decrease in Bcl-2 expression of MDA-MB-231 cells. Betulinic acid also induces morphological changes of MDA-MB-231 cells at 20 μM, and leads to ultrastructure changes of MDA-MB-231 cells at 40 μM^[2]. Betulinic acid shows anti-HIV activities, with an EC₅₀ of 1.4 μM in acutely infected H9 lymphocytes^[4]. 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^[3].