Pharmacokinetics of Curcumin Conjugate Metabolites in Healthy Human Subjects

Abstract

Background: Curcumin is a polyphenol, found in the spice turmeric, that has promising anticancer properties, but previous studies suggest that absorption of curcumin may be limited. Methods: This study examined the pharmacokinetics of a curcumin preparation in healthy human volunteers 0.25 to 72 h after a single oral dose. Curcumin was administered at doses of 10 g (n = 6) and 12 g (n = 6). Subjects were randomly allocated to dose level for a total of six subjects at each dose level. Serum samples were assayed for free curcumin, for its glucuronide, and for its sulfate conjugate. The data were fit to a onecompartment absorption and elimination model. Results: Using a high-performance liquid chromatography assay with a limit of detection of 50 ng/mL, only

Curcumin and its allied analogues: epigenetic and health perspectives - a review

“…Sharma et al (2004) investigated the curcumin not only in plasma, but also in urine, at lower concentrations, whereas curcumin in serum is undetectable below oral doses of 4 grams. Vareed et al (2008) determined that glucuronides are curcumin conjugates produced by human metabolism and detectable in plasma at higher concentrations than free curcumin with a peak at 4 h after oral dosing. The considered safe dose of dietary spice has been consumed up to 0.01 g/day for centuries.…”

Oxidative Stress and Cardiovascular Dysfunction Associated with Cadmium Exposure: Beneficial Effects of Curcumin and Tetrahydrocurcumin

“…curcumin-glucuronoside, dihydrocurcumin-glucuronoside, tetrahyfrocurcumin-glucuronoside), and tetrahydrocurcumin is major metabolite of curcumin in vivo. In human and rat intestine, curcumin is metabolized into curcumin glucuronide, curcumin sulphate, tetrahydrocurcumin, hexahydrocurcumin and octahydrocurcumin (Ireson et al 2002;Sharma et al 2004;Vareed et al 2008). The systemic clearance of curcumin from the body is also an important factor, which determines its relative biological activity.…”

Therapeutic actions of curcumin in bone disorders

“…9 Finally, curcumin also alters the expression of numerous cytokines (tumor necrosis factor-a, interleukin-1 (IL-1), IL-6 and chemokines), receptors (epidermal growth factor receptor, low-density lipoprotein receptor and estrogen receptor-a) and cell surface adhesion molecules. 1,[5][6][7] Consequently, curcumin displays both anti-oxidant and antiinflammatory properties and found to suppress tumor initiation, promotion and metastasis. 10 For example, curcumin was shown to induce apoptosis in MCF-7 breast cancer cells (25 mM for 24 h), 11 human leukemia HL 60 cells (10-40 mM for 16-24 h) 12 and human melanoma cells (30-60 mM for 24 h).…”

“…As previously mentioned, curcumin has poor water solubility, stability and in general short elimination half-life from body. 7 To overcome these pharmacokinetic limits, smart approches have been developed to improve curcumin delivery into the body. As it has been demonstrated with various therapeutical agents, delivering drugs directly in situ considerably improves both efficiency and tolerance of treatment.…”

“…For instance, it was shown that the plasmatic concentration of curcumin remained low (nanomolar range) even after high oral doses (that is, 10-12 g per day) were administered. 7 Approximately 65% of the orally administered curcumin undergoes rapid clearance and is eliminated from body mainly in the feces.…”