Inhibition of human recombinant cytochrome P450s by curcumin and curcumin decomposition products.

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Appiah-Opong R, Commandeur JN, van Vugt-Lussenburg B, Vermeulen NP

Inhibition of human recombinant cytochrome P450s by curcumin and curcumin decomposition products.

Toxicology. 2007 Jun 3;235(1-2):83-91. doi: 10.1016/j.tox.2007.03.007. Epub 2007 Mar 15.

PubMed ID

17433521 [ View in PubMed

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Abstract

Curcumin (diferuloylmethane) is a major yellow pigment and dietary component derived from Curcuma longa. It has potent anti-inflammatory, anticarcinogenic, antioxidant and chemoprotective activities among others. We studied the interactions of curcumin, a mixture of its decomposition products, and four of its individually identified decomposition products (vanillin, vanillic acid, ferulic aldehyde and ferulic acid) on five major human drug-metabolizing cytochrome P450s (CYPs). Curcumin inhibited CYP1A2 (IC(50), 40.0 microM), CYP3A4 (IC(50), 16.3 microM), CYP2D6 (IC(50), 50.3 microM), CYP2C9 (IC(50), 4.3 microM) and CYP2B6 (IC(50), 24.5 microM). Curcumin showed a competitive type of inhibition towards CYP1A2, CYP3A4 and CYP2B6, whereas a non-competitive type of inhibition was observed with respect to CYP2D6 and CYP2C9. The inhibitory activity towards CYP3A4, shown by curcumin may have implications for drug-drug interactions in the intestines, in case of high exposure of the intestines to curcumin upon oral administration. In spite of the significant inhibitory activities shown towards the major CYPs in vitro, it remains to be established, whether curcumin will cause significant drug-drug interactions in the liver, given the reported low systemic exposure of the liver to curcumin. The decomposition products of curcumin showed no significant inhibitory activities towards the CYPs investigated, and therefore, are not likely to cause drug-drug interactions at the level of CYPs.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Curcumin sulfate	Cytochrome P450 1A2	Protein	Humans	Unknown	Inhibitor	Details
Curcumin sulfate	Cytochrome P450 2B6	Protein	Humans	Unknown	Inhibitor	Details