Curcumin pharmacokinetics and pharmacodynamics

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Adv Exp Med Biol. 2007;595:453-70.

Pharmacokinetics and pharmacodynamics of curcumin.

Sharma RA, Steward WP, Gescher AJ.

Radiation Oncology & Biology, University of Oxford, Churchill

Hospital, UK.

Curcuma spp. contain turmerin, essential oils, and curcuminoids,

including curcumin. Curcumin [1,7-bis-(4-hydroxy-3-methoxyphenyl)-

1,6-heptadiene-3,5-dione] is regarded as the most biologically

active constituent of the spice turmeric and it comprises 2-8% of

most turmeric preparations. Preclinical data from animal models and

phase I clinical studies performed with human volunteers and

patients with cancer have demonstrated low systemic bioavailability

following oral dosing. Efficient first-pass metabolism and some

degree of intestinal metabolism, particularly glucuronidation and

sulfation of curcumin, might explain its poor systemic availability

when administered via the oral route.

A daily oral dose of 3.6 g of curcumin is compatible with detectable

levels of the parent compound in colorectal tissue from patients

with cancer. The levels demonstrated might be sufficient to exert

pharmacological activity. There appears to be negligible

distribution of the parent drug to hepatic tissue or other tissues

beyond the gastrointestinal tract. Curcumin possesses wide-ranging

anti-inflammatory and anticancer properties.

Many of these biological activities can be attributed to its potent

antioxidant capacity at neutral and acidic pH, its inhibition of

cell signaling pathways at multiple levels, its diverse effects on

cellular enzymes, and its effects on cell adhesion and angiogenesis.

In particular, curcumin's ability to alter gene transcription and

induce apoptosis in preclinical models advocates its potential

utility in cancer chemoprevention and chemotherapy. With regard to

considerable public and scientific interest in the use of

phytochemicals derived from dietary components to combat or prevent

human diseases, curcumin is currently a leading agent.