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Molecules 2014, 19(5), 5748-5760; doi:10.3390/molecules19055748

In Vitro Inhibitory Effects of Scutellarin on Six Human/Rat Cytochrome P450 Enzymes and P-glycoprotein

Department of Pharmacy, Shanghai Jiao Tong University Affiliated Sixth People's Hospital, No. 600 Yishan Road, Shanghai 200233, China
Department of Pharmacy, Wuhan University, Renmin Hospital, No.238 Jiefang Road, Wuchang disctrict, Wuhan 430060, China
Shanghai University of Traditional Chinese Medicine, No. 1200 Cailun Road, Shanghai 201203, China
Author to whom correspondence should be addressed.
Received: 15 March 2014 / Revised: 25 April 2014 / Accepted: 25 April 2014 / Published: 5 May 2014
(This article belongs to the Section Natural Products)
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Inhibition of cytochrome P450 (CYP) and P-glycoprotein (P-gp) are regarded as the most frequent and clinically important pharmacokinetic causes among the various possible factors for drug-drug interactions. Scutellarin is a flavonoid which is widely used for the treatment of cardiovascular diseases. In this study, the in vitro inhibitory effects of scutellarin on six major human CYPs (CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and six rat CYPs (CYP1A2, CYP2C7, CYP2C11, CYP2C79, CYP2D4, and CYP3A2) activities were examined by using liquid chromatography-tandem mass spectrometry. Meanwhile, the inhibitory effects of scutellarin on P-gp activity were examined on a human metastatic malignant melanoma cell line WM-266-4 by calcein-AM fluorometry screening assay. Results demonstrated that scutellarin showed negligible inhibitory effects on the six major CYP isoenzymes in human/rat liver microsomes with almost all of the IC50 values exceeding 100 μM, whereas it showed values of 63.8 μM for CYP2C19 in human liver microsomes, and 63.1 and 85.6 μM for CYP2C7 and CYP2C79 in rat liver microsomes, respectively. Scutellarin also showed weak inhibitory effect on P-gp. In conclusion, this study demonstrates that scutellarin is unlikely to cause any clinically significant herb-drug interactions in humans when co-administered with substrates of the six CYPs (CYP1A2, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4) and P-gp. View Full-Text
Keywords: scutellarin; cytochrome P450; P-glycoprotein; herb-drug interactions scutellarin; cytochrome P450; P-glycoprotein; herb-drug interactions

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MDPI and ACS Style

Han, Y.-L.; Li, D.; Yang, Q.-J.; Zhou, Z.-Y.; Liu, L.-Y.; Li, B.; Lu, J.; Guo, C. In Vitro Inhibitory Effects of Scutellarin on Six Human/Rat Cytochrome P450 Enzymes and P-glycoprotein. Molecules 2014, 19, 5748-5760.

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