The Role of Turmerones on Curcumin Transportation and P-Glycoprotein Activities in Intestinal Caco-2 Cells
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AbstractThe rhizome of Curcuma longa (turmeric) is often used in Asia as a spice and as a medicine. Its most well-studied component, curcumin, has been shown to exhibit poor bioavailability in animal studies and clinical trials. We hypothesized that the presence of lipophilic components (e.g., turmerones) in turmeric extract would affect the absorption of curcumin. The effects of turmerones on curcumin transport were evaluated in human intestinal epithelial Caco-2 cells. The roles of turmerones on P-glycoprotein (P-gp) activities and mRNA expression were also evaluated. Results showed that in the presence of alpha-and aromatic turmerones, the amount of curcumin transported into the Caco-2 cells in 2 hours was significantly increased. a-Turmerone and verapamil (a P-gp inhibitor) significantly inhibited the efflux of rhodamine-123 and digoxin (i.e., inhibited the activity of P-gp). It is interesting that aromatic turmerone significantly increased the rhodamine-123 efflux and Pgp (MDR1 gene) mRNA expression levels. The effects of alpha-and aromatic turmerones on curcumin transport as well as P-gp activities were shown here for the first time. The presence of turmerones did affect the absorption of curcumin in vitro. These findings suggest the potential use of turmeric extract (including curcumin and turmerones), rather than curcumin alone, for treating diseases.
All Author(s) ListYue GGL, Cheng SW, Yu H, Xu ZS, Lee JKM, Hon PM, Lee MYH, Kennelly EJ, Deng G, Yeung SK, Cassileth BR, Fung KP, Leung PC, Lau CBS
Journal nameJournal of Medicinal Food
Detailed descriptionTo ORKTS: DOI:10.1089/jmf.2011.1845.
Volume Number15
Issue Number3
Pages242 - 252
LanguagesEnglish-United Kingdom
KeywordsCaco-2 cells; Curcuma longa; curcumin; P-glycoprotein; turmerone
Web of Science Subject CategoriesChemistry, Medicinal; CHEMISTRY, MEDICINAL; Food Science & Technology; FOOD SCIENCE & TECHNOLOGY; Nutrition & Dietetics; NUTRITION & DIETETICS; Pharmacology & Pharmacy

Last updated on 2022-12-01 at 00:05