Pharmacokinetics and Metabolism of 4-O-Methylhonokiol in Rats
- Authors
- Yu, Hyung Eun; Oh, Soo Jin; Ryu, Je Kyung; Kang, Jong Soon; Hong, Jin Tae; Jung, Jae-Kyung; Han, Sang-Bae; Seo, Seung-Yong; Kim, Young Heui; Park, Song-Kyu; Kim, Hwan Mook; Lee, Kiho
- Issue Date
- Apr-2014
- Publisher
- WILEY
- Keywords
- pharmacokinetics; 4-O-methylhonokiol; metabolism; honokiol; neolignan
- Citation
- PHYTOTHERAPY RESEARCH, v.28, no.4, pp.568 - 578
- Journal Title
- PHYTOTHERAPY RESEARCH
- Volume
- 28
- Number
- 4
- Start Page
- 568
- End Page
- 578
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/12714
- DOI
- 10.1002/ptr.5033
- ISSN
- 0951-418X
- Abstract
- The purpose of this study was to characterize the pharmacokinetics and metabolism of 4-O-methylhonokiol in rats. The absorption and disposition of 4-O-methylhonokiol were investigated in male Sprague-Dawley rats following a single intravenous (2 mg/kg) or oral (10 mg/kg) dose. Its metabolism was studied in vitro using rat liver microsomes and cytosol. 4-O-Methylhonokiol exhibited a high systemic plasma clearance and a large volume of distribution. The oral dose gave a peak plasma concentration of 24.1 +/- 3.3 ng/mL at 2.9 +/- 1.9 h and a low estimated bioavailability. 4-O-Methylhonokiol was rapidly metabolized and converted at least in part to honokiol in a concentration-dependent manner by cytochrome P450 in rat liver microsomes, predicting a high systemic clearance consistent with the pharmacokinetic results. It was also shown to be metabolized by glucuronidation and sulfation in rat liver microsomes and cytosol, respectively. 4-O-Methylhonokiol showed a moderate permeability with no apparent vectorial transport across Caco-2 cells, suggesting that intestinal permeation process is not likely to limit its oral absorption. Taken together, these results suggest that the rapid hepatic metabolism of 4-O-methylhonokiol could be the major reason for its high systemic clearance and low oral bioavailability. Copyright (c) 2013 John Wiley & Sons, Ltd.
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