| In vitro metabolism and disposition of honokiol in rat and human livers. | |
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MedLine Citation:
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PMID: 21404278 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The biotransformation of honokiol, a major constituent of the bark of Magnolia officinalis, was investigated in rat and human livers. When isolated, rat livers were perfused with 10 µM honokiol and two metabolites, namely hydroxylated honokiol conjugated with glucuronic and sulfuric acid (M1) and honokiol monoglucuronide (M2), were quantified in bile and perfusate by high-performance liquid chromatography. The hepatic extraction ratio and clearance of honokiol was very high in rat liver (E: 0.99 ± 0.01 and 35.8 ± 0.04 mL/min, respectively) leading to very low bioavailability (F = 0.007 ± 0.001). M2 formation was also highly efficient in human liver microsomes [V(max) /K(m) = 78.1 ± 6.73 µL/(min mg)], which appeared to be catalyzed mainly by UDP-glucuronosyltransferases 1A1, A3, 1A8, and 1A10, indicating hepatic and extrahepatic glucuronidation. Monosulfation of honokiol to the minor metabolite honokiol monosulfate [V(max) /K(m) = 27.9 ± 4.33 µL/(min mg)] by human liver cytosol was less pronounced and is mediated by sulfotransferases 1A1* 1, 1A1* 2, 1A2, 1A3, 1B1, and 1E1. P450-mediated oxidation of honokiol by liver microsomes, however, was below detection limit. In summary, this study established that glucuronidation and sulfation are the main metabolic pathways for honokiol in rat and human liver, suggesting their major contribution to clearance in vivo. © 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci. |
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Authors:
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Michaela Böhmdorfer; Alexandra Maier-Salamon; Barbara Taferner; Gottfried Reznicek; Theresia Thalhammer; Steffen Hering; Antje Hüfner; Wolfgang Schühly; Walter Jäger |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-3-14 |
Journal Detail:
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Title: Journal of pharmaceutical sciences Volume: - ISSN: 1520-6017 ISO Abbreviation: - Publication Date: 2011 Mar |
Date Detail:
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Created Date: 2011-3-15 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 2985195R Medline TA: J Pharm Sci Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Wiley-Liss, Inc. |
Affiliation:
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Department of Clinical Pharmacy and Diagnostics, University of Vienna, A-1090 Vienna, Austria. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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