In vitro proguanil activation to cycloguanil is mediated by CYP2C19 and CYJP3A4 in adult Chinese liver microsomes

摘要

The kinetic be- haviors of CG formation were described well by a single- enzyme Michaelis-Menten equation in five livers. The apparent K-m and V_max were(82±47)μmol.L~-1 and(8 ±6)pmol.min~-1.mg~-1 protein, respectively). Howev- er, the remaining one displayed a two-enxyme kinetic be- havior. The Involved in PG activation to CG in adult Chinese liver Microsomes. CYP2C19 played an important role in the Clearance of PG at a substrate concentrations close to in Vivo therapeutic concentrations, while CYP3A4 gradually Made a dominant contribution with the increase of PG Concentration.