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Inhibitory effect of tanshinones on rat CYP3A2 and CYP2C11 activity and its structure-activity relationship

Author:
Wang, Xin, Yeung, John H.K.
Source:
Fitoterapia 2011 v.82 no.4 pp. 539-545
ISSN:
0367-326X
Subject:
liver, rats, structure-activity relationships
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=199–243μM) and CYP2C11 inhibitors (Kᵢ=91–118μM). Dihydrotanshinone was not only a noncompetitive inhibitor of CYP3A2 (Kᵢ=110μM), but also a competitive CYP2C11 inhibitor (Kᵢ=55μM). 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.
Agid:
497830