Journal
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Volume 53, Issue -, Pages 55-61Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2013.12.003
Keywords
Cytochrome P450 inhibition; Hops; Isoxanthohumol; 8-Prenylnaringenin; Drug-botanical interactions
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Funding
- NIH from the Office of Dietary Supplements [P50 AT00155]
- National Center for Complementary and Alternative Medicine
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As hops (Humulus lupulus L.) are used in the brewing of beer and by menopausal women as estrogenic dietary supplements, the potential for hop extracts and hop constituents to cause drug-botanical interactions by inhibiting human cytochrome P450 enzymes was investigated. Inhibition of major human cytochrome P450 enzymes by a standardized hop extract and isolated hop prenylated phenols was evaluated using a fast and efficient assay based on ultrahigh pressure liquid chromatography-tandem mass spectrometry. The hop extract at 5 mu g/mL inhibited CYP2C8 (93%), CYP2C9 (88%), CYP2C19 (70%), and CYP1A2 (27%) with IC50 values of 0.8, 0.9, 3.3, and 9.4 mu g/mL, respectively, but time-dependent inactivation was observed only for CYP1A2. Isoxanthohumol from hops was the most potent inhibitor of CYP2C8 with an IC50 of 0.2 mu M, whereas 8-prenylnaringenin was the most potent inhibitor of CYP1A2, CYP2C9 and CYP2C19 with IC50 values of 1.1 mu M, 1.1 mu M and 0.4 mu M, respectively. Extracts of hops contain prenylated compounds such as the flavanones isoxanthohumol and 8-prenylnaringenin and the chalcone xanthohumol that can inhibit CYP450s, especially the CYP2C family, which may affect the efficacy and safety of some CYP2C substrate drugs when co-administered. (C) 2013 Elsevier B.V. All rights reserved.
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