What is Betulin?

Betulin is a pentacyclic triterpenoid compound extracted from birch bark. It has anti-inflammatory, antibacterial, antioxidant and anticancer effects, and has many benefits for human health. Betulin is a hydrophobic compound that can be easily obtained by solvent extraction. In order to improve the water solubility of Betulin and expand its application areas and scope, researchers have fabricated its nanostructures and used arabinogalactan as a component of the drug delivery structure (nanostructure). The betulin and allobetulin formate prepared in this way have procoagulant properties (hemolysis degree less than 2%) and can be used to manufacture materials with anticoagulant activity, such as sponges and gels.

Benefits of Betulin

Enhanced Osteogenesis

Studies have shown that Betulin can increase mineralization (calcium accumulation) of two human osteoblasts (hFOB 1.19 and Saos-2 cells) under osteogenic conditions; increase the mRNA levels of osteoblast differentiation markers (except ALP in Saos-2 cells) under osteoinductive conditions, accompanied by increased matrix mineralization. Furthermore, the osteoinductive activity of Betulin in hFOB 1.19 cells may be mediated by the activation of MAPK (JNK and ERK1/2) and mTOR, as specific inhibitors of these kinases abolished Betulin-induced osteoblast differentiation. These results suggest that Betulin has the potential to enhance osteogenic effects.

Antioxidant and antibacterial effects

Btulin/MβCD inclusion complex nanofibers (Betulin/MβCD-IC-NF) were prepared by methyl-β-cyclodextrin (MβCD) inclusion and electrospinning technology. DPPH free radical scavenging experiments and antibacterial experiments showed that Betulin/MβCD-IC-NF had good antioxidant and antibacterial properties.

Improvement of acute ethanol-induced fatty liver

In vitro and in vivo studies showed that supplementation with betulinic acid (BA) or betulin (BT) may improve acute ethanol-induced fatty liver through TLR4 and STAT3, becoming a promising drug for the treatment of ethanol-induced fatty liver. Supplementation with BA or BT significantly inhibited the ethanol-induced increase in serum ALT and AST, as well as the increase in serum TG; inhibited ethanol-induced eosinophilic necrosis, increased hepatocyte nuclei, and matrix inflammatory infiltration; significantly reduced ethanol-induced CYP2E1 activity and SREBP-1 and TLR4 expression (but lower doses of BA or BT had little effect on CYP2E1 and SREBP-1 expression), and increased STAT3 phosphorylation.

Anticancer

Betulin is a relatively safe and effective anticancer agent that has been shown to have anticancer and anti-inflammatory properties against pancreatic, gastric, lung, ovarian, melanoma cells, and nervous system cancers. Most importantly, it has less cytotoxic effects on normal cells than cancer cells. It is of great help in the treatment of most malignancies by inducing apoptotic pathways within cancer cells while sparing normal cells, and can be used alone or in combination with radiotherapy or chemotherapy drugs. For example, when Betulin is used in combination with a γ-cyclodextrin derivative in melanoma B164A5 cells, the combination therapy can reduce cell proliferation and induce differentiation and cell death.