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© 2003 The American Society for Nutritional Sciences J. Nutr. 133:2607-2611, August 2003


Nutrient Metabolism

Choline Uptake in Human Intestinal Caco-2 Cells Is Carrier-Mediated

Amrita V. Kamath, Inger M. Darling and Marilyn E. Morris3

Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, University at Buffalo, The State University of New York, Amherst, NY 14260

3To whom correspondence should be addressed. E-mail: memorris{at}buffalo.edu.

The objective of the current investigation was to examine the transport characteristics of choline, an endogenous quaternary ammonium compound, into human intestinal Caco-2 cells; the transport of choline has not been characterized in human intestine. The cellular accumulation of choline was independent of an inwardly directed Na+ gradient and demonstrated temperature dependence and saturability. Using the initial uptake rates, choline accumulation was best characterized by a Michaelis-Menten equation and a diffusion component with a Km and Vmax of 110 ± 3 µmol/L and 2800 ± 250 pmol/(mg protein · 10 min), respectively. Choline uptake was significantly inhibited by an excess of choline itself and by hemicholinium-3, a structural analog of choline. However other hydrophilic organic cations, such as tetraethylammonium (TEA) and N-methylnicotinamide (NMN), did not affect choline uptake in Caco-2 cells. Additionally, two typical p-glycoprotein substrates, daunomycin and verapamil, both inhibited choline accumulation. However the opposite was not true: choline did not inhibit DNM accumulation in Caco-2 cells. These results indicate the presence of a carrier-mediated transport system for choline in Caco-2 cells. The substrate specificity of this carrier is unlike that seen in the rat intestinal epithelium, and the human transport protein is distinct from those for TEA and NMN. P-glycoprotein substrates may inhibit choline uptake through specific or nonspecific interactions with the choline transporter.


KEY WORDS: • Caco-2 • human intestine • transport • choline




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