1178583-19-1

GL-V9 is an AMPK activator, protecting against colitis-associated colorectal cancer by limiting NLRP3 inflammasome through autophagy.

GL-V9 inhibits proliferation of HepG2 cell (IC50 is 35.2 μM) through induction of apoptosis and cell cycle arrest at G2/M phase. GL-V9 regulates mitochondrial membrane potential and increases the production of intracellular reactive oxygen species. GL-V9 inhibits the pentose phosphate pathway (PPP), enhances fatty acid oxidation (FAO) through activation of AMPK, and thus inhibits the metastasis of cancer cells. GL-V9 exhibits antitumor efficacy in mouse model[1][2].

[1] Li L, et al., GL-V9, a newly synthetic flavonoid derivative, induces mitochondrial-mediated apoptosis and G2/M cell cycle arrest in human hepatocellular carcinoma HepG2 cells. Eur J Pharmacol. 2011 Nov 16;670(1):13-21. DOI:10.1016/j.ejphar.2011.08.054
[2] Yang L, et al., Regulation of AMPK-related glycolipid metabolism imbalances redox homeostasis and inhibits anchorage independent growth in human breast cancer cells. Redox Biol. 2018 Jul;17:180-191. DOI:10.1016/j.redox.2018.04.016