Inhibitory effect of tanshinones on rat CYP3A2 and CYP2C11 activity and its structure-activity relationship |
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| Authors: | Wang Xin Yeung John H K |
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| Institution: | a School of Biomedical Sciences, Faculty of Medicine, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong SAR, China |
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| 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 (Ki = 199-243 μM) and CYP2C11 inhibitors (Ki = 91-118 μM). Dihydrotanshinone was not only a noncompetitive inhibitor of CYP3A2 (Ki = 110 μM), but also a competitive CYP2C11 inhibitor (Ki = 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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| Keywords: | Tanshinones CYP3A2 CYP2C11 Structure– activity Inhibition |
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