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Effects of Curcuma Extracts and Curcuminoids on Expression of P-glycoprotein and Cytochrome P450 3A4 in the Intestinal Cell Culture Model LS180

Graber-Maier, Angelika and Büter, Karin Berger and Aeschlimann, Julia and Bittel, Claudia and Kreuter, Matthias and Drewe, Juergen and Gutmann, Heike. (2010) Effects of Curcuma Extracts and Curcuminoids on Expression of P-glycoprotein and Cytochrome P450 3A4 in the Intestinal Cell Culture Model LS180. Planta medica, Vol. 76, H. 16. pp. 1866-1870.

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Official URL: http://edoc.unibas.ch/dok/A6001406

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Abstract

CURCUMA LONGA L. is a widely used spice. Its main ingredients, the curcuminoids, are used in the treatment of inflammatory diseases and cancer. Bioavailability of curcuminoids is low, and huge amounts remain in the intestine. We therefore aimed to investigate their interaction potential with the ABC-transporter P-glycoprotein (P-gp, product of the MDR1/ABCB1 gene) and cytochrome P450 3A4 (CYP3A4) in an intestinal cell line (LS180). Intestinal P-gp and CYP3A4 play a major role in drug absorption, and consequently changes in their expression level could lead to interactions. The intestinal LS180 cell line was incubated with different CURCUMA extracts, the single curcuminoids (curcumin, demethoxycurcumin, and bisdemethoxycurcumin), as well as a curcuminoid mixture. Changes in mRNA expression of MDR1 and the cytochrome CYP3A4 were measured by real-time RT-PCR. MDR1 mRNA expression was significantly but not relevantly downregulated by the curcuminoids, whereas the extracts had no significant effect on it. CYP3A4 mRNA expression did not alter significantly after treatment. CURCUMA extracts, the single curcuminoids, and a curcuminoid mixture had no relevant effect on MDR1 and CYP3A4 mRNA expression in our intestinal cell system. Further studies are required to evaluate their effects IN VIVO.
Faculties and Departments:03 Faculty of Medicine > Departement Biomedizin > Former Units at DBM > Clinical Pharmacology (Drewe)
03 Faculty of Medicine > Departement Biomedizin > Former Units at DBM > Gastroenterology (Beglinger)
03 Faculty of Medicine > Bereich Medizinische Fächer (Klinik) > Klinische Pharmakologie > Klinische Pharmakologie (Krähenbühl)
03 Faculty of Medicine > Departement Klinische Forschung > Bereich Medizinische Fächer (Klinik) > Klinische Pharmakologie > Klinische Pharmakologie (Krähenbühl)
UniBasel Contributors:Gutmann, Heike and Drewe, Jürgen
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Hippokrates-Verl.
ISSN:0032-0943
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:07 Dec 2012 13:03
Deposited On:07 Dec 2012 13:02

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