Research Article
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Published Online: 4 September 2007

Improving the Solubility and Pharmacological Efficacy of Curcumin by Heat Treatment

Publication: ASSAY and Drug Development Technologies
Volume 5, Issue Number 4

Abstract

Lipid peroxidation has been implicated in a variety of diseases. 4-Hydroxy-2-nonenal (HNE), a major oxidation by-product, is cytotoxic, mutagenic, and genotoxic, being involved in disease pathogenesis. Naturally occurring pharmacologically active small molecules are very attractive as natural nonsteroidal anti-inflammatory agents. Interest has greatly increased recently in the pharmacotherapeutic potential of curcumin, the yellow pigment found in the rhizomes of the perennial herb Curcuma longa (turmeric). Curcumin is efficacious against colon cancer, cystic fibrosis, and a variety of other disorders. Curcumin's full pharmacological potential is limited owing to its extremely limited water solubility. We report here that the water solubility of curcumin could be increased from 0.6 μg/ml to 7.4 μg/ml (12-fold increase) by the use of heat. Spectrophotometric (400–700 nm) and mass spectrometric profiling of the heat-extracted curcumin displays no significant heat-mediated disintegration of curcumin. Using an enzyme-linked immunosorbent assay that employed HNE modification of solid-phase antigen, we found that the heat-solubilized curcumin inhibited HNE-protein modification by 80%. Thus, inhibition of HNE modification may be a mechanism by which curcumin exerts its effect. We also report a simple assay to detect curcumin spectrophotometrically. Curcumin was solubilized in methanol and serially diluted in methanol to obtain a set of standards that were then read for optical density at 405 nm. Curcumin in the heat-solubilized samples was determined from this standard. Heat-solubilized curcumin should be considered in clinical trials involving curcumin, especially in the face of frustrating results obtained regarding curcumin-mediated correction of cystic fibrosis defects.

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cover image ASSAY and Drug Development Technologies
ASSAY and Drug Development Technologies
Volume 5Issue Number 4August 2007
Pages: 567 - 576
PubMed: 17767425

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Published online: 4 September 2007
Published in print: August 2007

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Biji T. Kurien
Arthritis and Immunology Program, Oklahoma Medical Research Foundation, Oklahoma City, OK.
Anil Singh
Department of Biochemistry and Molecular Biology, Oklahoma City, OK.
Hiroyuki Matsumoto
Department of Biochemistry and Molecular Biology, Oklahoma City, OK.
R. Hal Scofield
Arthritis and Immunology Program, Oklahoma Medical Research Foundation, Oklahoma City, OK.
Department of Medicine, University of Oklahoma Health Sciences Center, Oklahoma City, OK.
Department of Veterans Affairs Medical Center, Oklahoma City, OK.

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