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Title 

Pharmacokinetics and metabolism of 4-O-methylhonokiol in rats

Authors 

Hyung-En YuSoo Jin OhJe Kyung RyuJong Soon KangJ T HongJ K JungS B HanS Y SeoY H KimS K ParkH M KimK Lee

Publisher 

Wiley-Blackwell

Issue Date 

2014

Citation 

Phytotherapy Research, vol. 28, no. 4, pp. 568-578

Keywords 

4-O-methylhonokiolhonokiolmetabolismneolignanpharmacokinetics

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.

ISSN 

0951-418X

Link 

http://dx.doi.org/10.1002/ptr.5033

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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