Demethyleneberberine

Demethyleneberberine is an isoquinoline alkaloid that has been found in P. chinensis and has diverse biological activities.^1,2,3,4,5 It is also an active metabolite of berberine (Item No. 10006427).^1,2 Demethyleneberberine is formed from berberine by cytochrome P450 (CYP) isoforms CYP2D6, CYP1A2, and CYP3A4.² It reduces viability, colony formation, and migration and invasion in A549 and H1299 lung cancer cells when used at a concentration of 40 µM.³ Demethyleneberberine (40 mg/kg per day) increases hepatic mitochondrial levels of glutathione (GSH) and glutathione peroxidase 4 (Gpx4), reduces hepatic mitochondrial levels of thiobarbituric acid reactive substances (TBARS), decreases hepatic swelling of mitochondria, and increases serum activity of alanine transaminase (Alt) in a mouse model of ethanol-induced oxidative liver damage.⁴ It decreases hepatic levels of inducible nitric oxide synthase (iNos) and triglycerides in the same model at the same dose. Demethyleneberberine (10 mg/kg per day) reduces hepatic collagen levels and increases survival in a mouse model of thioacetamide-induced hepatic fibrosis.⁵

WARNING This product is not for human or veterinary use.

1. Cao, S., Zhou, Y., Xu, P., et al. Berberine metabolites exhibit triglyceride-lowering effects via activation of AMP-activated protein kinase in Hep G₂ cells. J. Ethnopharmacol. 149(2), 576-582 (2013).

2. Li, Y., Ren, G., Wang, Y.X., et al. Bioactivities of berberine metabolites after transformation through CYP450 isoenzymes. J. Transl. Med. 9, 62 (2011).

3. Liu, J., Huang, X., Liu, D., et al. Demethyleneberberine induces cell cycle arrest and cellular senescence of NSCLC cells via c-Myc/HIF-1α pathway. Phytomedicine 91:153678, (2021).

4. Zhang, P., Qiang, X., Zhang, M., et al. Demethyleneberberine, a natural mitochondria-targeted antioxidant, inhibits mitochondrial dysfunction, oxidative stress, and steatosis in alcoholic liver disease mouse model. J. Pharmacol. Exp. Ther. 352(1), 139-147 (2015).

5. Wang, Y., Zhao, Z., Yan, Y., et al. Demethyleneberberine protects against hepatic fibrosis in mice by modulating NF-κB signaling. Int. J. Mol. Sci. 17(7), 1036 (2016).