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Effect of Honokiol on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes
College of Pharmacy, the Catholic University of Korea, Bucheon 420-743, Korea
Huons Co., Ltd., Ansan 426-791, Korea
* Author to whom correspondence should be addressed.
Received: 15 August 2013; in revised form: 28 August 2013 / Accepted: 28 August 2013 / Published: 3 September 2013
Abstract: Honokiol is a bioactive component isolated from the medicinal herbs Magnolia officinalis and Magnolia grandiflora that has antioxidative, anti-inflammatory, antithrombotic, and antitumor activities. The inhibitory potentials of honokiol on eight major human cytochrome P450 (CYP) enzymes 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4, and four UDP-glucuronosyltransferases (UGTs) 1A1, 1A4, 1A9, and 2B7 in human liver microsomes were investigated using liquid chromatography-tandem mass spectrometry. Honokiol strongly inhibited CYP1A2-mediated phenacetin O-deethylation, CYP2C8-mediated amodiaquine N-deethylation, CYP2C9-mediated diclofenac 4-hydroxylation, CYP2C19-mediated [S]-mephenytoin 4-hydroxylation, and UGT1A9-mediated propofol glucuronidation with Ki values of 1.2, 4.9, 0.54, 0.57, and 0.3 μM, respectively. Honokiol also moderately inhibited CYP2B6-mediated bupropion hydroxylation and CYP2D6-mediated bufuralol 1'-hydroxylation with Ki values of 17.5 and 12.0 μM, respectively. These in vitro results indicate that honokiol has the potential to cause pharmacokinetic drug interactions with other co-administered drugs metabolized by CYP1A2, CYP2C8, CYP2C9, CYP2C19, and UGT1A9.
Keywords: honokiol; cytochrome P450 inhibition; UDP-glucuronosyltransferase inhibition; human liver microsomes; drug-drug interaction
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Jeong, H.-U.; Kong, T.Y.; Kwon, S.S.; Hong, S.-W.; Yeon, S.H.; Choi, J.-H.; Lee, J.Y.; Cho, Y.Y.; Lee, H.S. Effect of Honokiol on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes. Molecules 2013, 18, 10681-10693.
Jeong H-U, Kong TY, Kwon SS, Hong S-W, Yeon SH, Choi J-H, Lee JY, Cho YY, Lee HS. Effect of Honokiol on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes. Molecules. 2013; 18(9):10681-10693.
Jeong, Hyeon-Uk; Kong, Tae Y.; Kwon, Soon S.; Hong, Sung-Woon; Yeon, Sung H.; Choi, Jun-Ho; Lee, Jae Y.; Cho, Yong Y.; Lee, Hye S. 2013. "Effect of Honokiol on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes." Molecules 18, no. 9: 10681-10693.