BBA reportActive transport of dimethialium (cas 15659-74-2) in isolated rat hepatocytes

Add time:09/01/2019    Source:sciencedirect.com

The uptake of dimethialium (cas 15659-74-2), a thiamine analog having a methyl group in place of the hydroxyethyl group in the thiazole moiety, was studied in freshly isolated rat hepatocytes. In an Na+-medium, dimethialium at 10 μM was accumulated rapidly by the cells and an almost steady intra- to extracellular distribution ratio of 4.2 was attained in 5 min of incubation. The Kt and the Vmax for the saturable component were estimated to be 27 μM and 19 pmol/105 cells per min, respectively. In a K+ medium, the uptake of dimethialium was decreased to 58% of that of control. Ouabain and 2,4-dinitrophenol significantly lowered the rate of dimethialium uptake. Both phenylthiazinothiamine and oxythiamine were inhibitory on the uptake of dimethialium, which uptake was also inhibited by choline. These data indicate that dimethialium transport in liver cells proceeds via a carrier-mediated active process dependent on Na+ and biological energy. Furthermore, these results also suggest that thiamine transport in liver is dissociable from thiamine phosphorylation.

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