Allosteric Activation of Glabridin towards Propofol Glucuronidation

The allosteric regulation effect is the regulation of an enzyme through binding an effector molecule at the enzyme's allosteric site. The allosteric inhibition of drugs or herbal components towards the glucuronidation of clinical hypnotic/amnestic agent propofol has been frequently reported, and the relatively few examples were given for the allosteric activation towards propofol glucuronidation. The present study reported the allosteric activation role of glabridin towards the glucuronidation of propofol. Human liver microsomes (HLMs) incubation system was used in the present study. Glabridin showed no effects towards propofol glucuronidation at 10 mu M of glabridin, and 100 mu M of glabridin increased the activity of propofol glucuronidation by 300%. Furthermore, the formation rate of propofol glucuronide was determined at multiple concentrations of glabridin and propofol. Concentration-dependent activation of glabridin towards propofol glucuronidation was observed. In conclusion, all these data indicated the potential influence of glabridin towards the serum concentration of propofol due to the allosteric activation of glabridin towards propofol glucuronidation.