Betulinic acid 是从白桦树皮中分离出来的一种五环三萜类天然产物，是真核细胞拓扑异构酶 I 的抑制剂，IC50值为 5 μM，具有抗逆转录病毒、抗疟疾、抗癌和抗炎特性。

Betulinic acid 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.

在无胸腺裸鼠LNCaP细胞中,Betulinic acid对前列腺癌细胞和肿瘤(异种移植)的生长有抑制效果,该作用部分是由于蛋白酶依赖性Sp1/3/4及一些SP-调节基因的下调.

作为抗黑色素瘤剂,Betulinic acid可抑制氨肽酶N的活性（IC50：7.3 μM）。通过阻断H9淋巴细胞中HIV复制（EC50：1.4 μM）和未感染的H9细胞生长（IC50：13 μM）的抑制,Betulinic acid产生抗HIV活性。Betulinic acid还是十分有潜力的抗肿瘤候选药物,对真核生物拓扑异构酶I的活性有抑制作用（IC50：5 μM）。

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

472-15-1

C30H48O3

456.711

Lupatic acid;桦木酸;ALS-357;白桦脂酸;Betulic acid

DMSO:16 mg/mL (35 mM)
Ethanol:10 mg/mL (21.89 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years