Modulation of hepatic drug metabolizing enzymes by the natural polyphenol curcumin

Rhonda J. Rosengren, Shuli Chen

Abstract


Curcumin, the yellow pigment found in turmeric, has potent chemopreventative properties towards cancer in both in vivo and in vitro models. Phase I cytochrome P450 (CYP) enzymes and phase II conjugation enzymes play a critical role in carcinogen metabolism and hence could be an important target for cancer chemoprevention and treatment. Various studies have been undertaken to evaluate the effects of curcumin on the activity of phase I and phase II enzymes. Phase I enzymes are functionalization enzymes and Phase II enzymes perform conjugative reactions. This review summarizes the studies on curcumin modulation of phase I and II activities in the last decade. Various studies have shown that curcumin inhibits the  activity of different CYPs including CYP1A1 and CYP1B1 CYP1A1, CYP1A2, CYP2A6, CYP3A4, CYP2B1 and CYP2E1 in vitro and in vivo. However, a few studies have also reported the induction of CYPs. Curcumin also modulates the activity of phase II enzymes. Phase II enzymes have attracted much less attention than CYPs, especially in clinical pharmacology. Most studies focus on the inhibition or induction of glutthione S-transferase (GST). Also modulating of sulfotransferases (SULTs) and glucuronosyltransferases (UGTs) has been reported. However, more studies in humans following oral adminstration of curcumin are required in order to fully elucidate the potential for curcumin to be used as an effective potential chemopreventative.


Keywords


cur cumin; phase II enzymes; CYP450s; inhibition; in vitro

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References


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DOI: http://dx.doi.org/10.18103/imr.v3i11.631

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