TABLE 2

The IC50 values for the inhibition of danshen components on CYP enzymes activities


Danshen Components

IC50
CYP1A2
CYP2C9
CYP2D6
CYP3A4a
CYP3A4b
μM
Hydrophilic components
Protocatechuic acid >200 >200 >200 >200 >200
Protocatechuic aldehyde >200 >200 >200 130 160
Danshensu 110 50 >200 >200 >200
Salvianolic acid B 105 >200 >200 >200 >200
Lipophilic components
Tanshinone I 0.75 >200 120 >200 >200
Tanshinone IIA 1.3 >200 >200 >200 >200
Cryptotanshinone 0.75 33 75 >200 >200
Positive controlc
0.63
0.3
0.12
0.05
0.045
  • a Testosterone 6β-hydroxylation

  • b Midazolam 1-hydroxylation

  • c The positive controls were specific inhibitors of P450 (furafylline for CYP1A2, sulfaphenazole for CYP2C9, quinidine for CYP2D6, and ketoconazole for CYP3A4)