THDP17 Decreases Ammonia Production through Glutaminase Inhibition. A New Drug for Hepatic Encephalopathy Therapy
Figure 5
Metformin inhibits glutaminase activity in a dose dependent manner: from 17.5% at 10 mM up to 68% at 100 mM (A) (* p<0.05).
This effect, analyzed by Dixon plot, showed competitive inhibition kinetics, with a Ki of 14.28 mM (B). In Caco2 cells, metformin 20 mM showed 24% inhibition of glutaminase activity at 72 hours compared to control cultures (p<0.05) (glutamate production was decreased from 26.85±0.74 µM to 19.9±2.05 µM; p<0.05) (C).