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First published on March 10, 2008; DOI: 10.1124/dmd.107.019612

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Received for publication November 2, 2007.
Revised March 3, 2008.
Accepted for publication March 5, 2008.

Identification and characterization of potent CYP2B6 inhibitors in Woohwangcheongsimwon suspension, an herbal preparation used in the treatment and prevention of apoplexy in Korea and China

Hyunmi Kim 1, Kwon-Bok Kim 1, Hei-Young Ku 1, Soo Jin Park 1, Hoon Choi 2, Joon-Kwan Moon 2, Byeoung-Soo Park 2, Jeong-Han Kim 2, Sung Su Yea 1, Choong-Hwan Lee 3, Hye Suk Lee 4, Jae-Gook Shin 1, Kwang-Hyeon Liu 1*

1 Inje University College of Medicine 2 Seoul National University 3 Konkuk University 4 Wonkwang University

* Address correspondence to: E-mail: dstlkh{at}inje.ac.kr

Abstract

Woohwangcheongsimwon is a traditional medicine for treating hypertension, arteriosclerosis, coma, and stroke in China and Korea. To assess potential interactions of herb and drug metabolism, commercially available Woohwangcheongsimwon suspensions were examined for their potential to inhibit the activity of nine human cytochrome P450 enzymes. The Woohwangcheongsimwon suspensions showed strong inhibition of CYP2B6 activity. To identify individual constituents with inhibitory activity, the suspension was partitioned using hexane, ethyl acetate, and dichloromethane, and each fraction was tested for its inhibitory effect on CYP2B6-catalyzed bupropion hydroxylation. The hexane fraction possessed inhibitory activity, and GC/MS analysis identified borneol and isoborneol as major constituents of the hexane fraction. These two terpenoids moderately inhibited CYP2B6-catalyzed bupropion hydroxylase activity in a competitive manner,with Ki values of 9.5 and 5.9 µM, respectively, as well as efavirenz 8-hydroxylase activity, with Ki values of 22 and 26 µM respectively. Additionally, reconstituted mixtures of borneol and isoborneol, at the same concentrations as in the Woohwangcheongsimwon suspension, had comparable potency in inhibiting bupropion hydroxylation. These in vitro data indicate that Woohwangcheongsimwon preparations contain constituents that can potently inhibit the activity of CYP2B6 and suggest that these preparations should be examined for potential pharmacokinetic drug interactions in vivo.


Key words: CYP inhibition, cytochrome P450, drug interactions


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A. J. Lau and T. K. H. Chang
Inhibition of Human CYP2B6-Catalyzed Bupropion Hydroxylation by Ginkgo biloba Extract: Effect of Terpene Trilactones and Flavonols
Drug Metab. Dispos., September 1, 2009; 37(9): 1931 - 1937.
[Abstract] [Full Text] [PDF]


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