| Inhibitory effects of curcumenol on human liver cytochrome P450 enzymes. | |
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MedLine Citation:
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PMID: 20148399 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Curcumenol, one of the major components of Zedoary turmeric oil, has been widely used to treat cancer and inflammation. As an antibiotic or anticancer drug, curcumenol is highly likely to be used in combination with various synthetic drugs in most cases, thus it is necessary to evaluate potential pharmacokinetic drug-drug interactions induced by curcumenol. In this study, the inhibitory effects of curcumenol on seven CYP isoforms were investigated, and the results demonstrated that only CYP3A4 was strongly inhibited (IC(50) = 12.6 +/- 1.3 microM). Kinetic analysis showed the inhibition type was competitive with K(i) value of 10.8 microM. Time- and NADPH-dependent inhibitions were also investigated to show curcumenol is not a mechanism-based inhibitor. Employing these in vitro data and maximum plasma concentration of curcumenol in human predicted from beagle dog's in vivo pharmacokinetic data, the change in AUC of victim drugs was predicted to be 0.4%, which suggested that curcumenol may be safely used without inducing metabolic drug-drug interaction through P450 inhibition. Nevertheless, due to the limited pharmacokinetic data available for curcumenol in humans, it is still not possible to evaluate its potential clinical effects on human patients from in vitro data. Thus, the magnitude of drug-drug interaction (DDI) induced by curcumenol warrants further investigation. |
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Authors:
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Dong-Xue Sun; Zhong-Ze Fang; Yan-Yan Zhang; Yun-Feng Cao; Ling Yang; Jun Yin |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Phytotherapy research : PTR Volume: 24 ISSN: 1099-1573 ISO Abbreviation: Phytother Res Publication Date: 2010 Aug |
Date Detail:
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Created Date: 2010-07-26 Completed Date: 2010-09-23 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8904486 Medline TA: Phytother Res Country: England |
Other Details:
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Languages: eng Pagination: 1213-6 Citation Subset: IM |
Copyright Information:
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Copyright (c) 2010 John Wiley & Sons, Ltd. |
Affiliation:
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School of Traditional Chinese Medicine, Shenyang Pharmaceutical University, Shenyang 110016, China. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Area Under Curve Curcuma / chemistry* Cytochrome P-450 CYP3A / antagonists & inhibitors* Dogs Drug Interactions Enzyme Inhibitors / pharmacokinetics* Female Humans Inhibitory Concentration 50 Liver / enzymology Male Microsomes, Liver / drug effects, enzymology* Sesquiterpenes / pharmacokinetics* |
| Chemical | |
Reg. No./Substance:
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0/Enzyme Inhibitors; 0/Sesquiterpenes; 0/curcumenol; EC 1.14.13.67/CYP3A4 protein, human; EC 1.14.14.1/Cytochrome P-450 CYP3A |
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