Abstract
This study investigated the effect of tanshinones on rat liver microsomal CYP3A2 and 2C11 activity and explored the structure-activity relationship of tanshinones with CYP3A activity. Cryptotanshinone, tanshinone I and tanshinone IIA were competitive CYP3A2 inhibitors ( K i = 199–243 μM) and CYP2C11 inhibitors ( K i = 91–118 μM). Dihydrotanshinone was not only a noncompetitive inhibitor of CYP3A2 ( K i = 110 μM), but also a competitive CYP2C11 inhibitor ( K i = 55 μM). The structural difference between dihydrotanshinone and tanshinone I at C-15 position of furan ring resulted in the different modes of inhibition on CYP3A activity.
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