Bergaptol, a mechanism-based inactivation of CYP2C9

In this study, BGT was found to induce time-, concentration-, and NADPH-dependent irreversible inhibition of CYP2C9. A GSH co njugate was detected in an incubation mixture containing CYP2C9, BGT, NADPH, and GSH. Further mechanistic investigation revealed that a γ-ketoenal metabolite was responsible for the enzyme inactivation. The obtained data indicate that BGT was a mechanism-based inactivator of CYP2C9. The study would facilitate the understanding of the mechanistic insight into fruit–drug interactions mediated by grapefruits.

Source: Medicinal Chemistry Research - May 25, 2020 Category: Chemistry Source Type: research