Uptake Mechanism of Trientine by Rat Intestinal Brush-border Membrane Vesicles

• Published in: Journal of pharmacy and pharmacology Vol. 48; no. 5; pp. 517 - 521
• Main Authors: TANABE, RYOU, KOBAYASHI, MICHIYA, SUGAWARA, MITSURU, ISEKI, KEN, MIYAZAKI, KATSUMI
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01-05-1996; Pharmaceutical Press
• Subjects: Animals; Biological and medical sciences; Chromatography, High Pressure Liquid; Diffusion; Intestine, Small - metabolism; Intestine, Small - ultrastructure; Male; Medical sciences; Microvilli - metabolism; Miscellaneous; Pharmacology. Drug treatments; Potassium - metabolism; Rats; Rats, Wistar; Spermidine - pharmacology; Spermine - pharmacology; Temperature; Time Factors; Trientine - metabolism; Valinomycin - pharmacology; Polyamine; Rat; Digestive system; Biological transport; Rodentia; Gut; In vitro; Uptake; Vertebrata; Brush border; Mammalia; Absorption; Spermine; Animal; Spermidine; Chelating agent; Copper; Comparative study
• ISSN: 0022-3573; 2042-7158
• DOI: 10.1111/j.2042-7158.1996.tb05965.x

The uptake characteristics of trientine by rat intestinal brush‐border membrane vesicles were studied.
The uptake characteristics of trientine were similar to those of the physiological polyamines with respect to the excessive accumulation in vesicles, the pH dependency, the temperature dependency and the ineffectiveness of K+ diffusion potential (inside negative). The initial uptake of trientine was saturable with a Km value of 1.13 mM, which was larger than that of spermine and spermidine. Furthermore, the uptake rate of trientine was dose‐dependently inhibited by spermine and spermidine. Spermine competitively inhibited the uptake of trientine with a Ki value of 18.6 μM, and it was close to the Km value for spermine (30.4 μM).
These data suggested that the uptake of trientine was similar to that of spermine and spermidine in rat small intestinal brush‐border membrane vesicles, and these polyamines seem to inhibit the absorption of trientine from the gastrointestinal tract.