Molecules 2013, 18(9), 10681-10693; doi:10.3390/molecules180910681
Article

Effect of Honokiol on Cytochrome P450 and UDP-Glucuronosyltransferase Enzyme Activities in Human Liver Microsomes

Received: 15 August 2013; in revised form: 28 August 2013 / Accepted: 28 August 2013 / Published: 3 September 2013
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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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MDPI and ACS Style

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.

AMA Style

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.

Chicago/Turabian Style

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.

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