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KMID : 0369819910210010043
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Jorunal of Korean Pharmaceutical Sciences
1991 Volume.21 No. 1 p.43 ~ p.50
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Characterization of the Hepatic Uptake of 1 - Anilino - 8 - naphthalene sulfonate ( ANS ) by Isolated Rat Hepatocytes : Is Serum Protein Essential for Hepatic Uptake of ANS in the Liver ?
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정연복/Chung YB
육동연/한건/Yuk DY/Han K
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Abstract
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The hepatic uptake of an anionic fluorescence probe, l-anilino-8-naphthalene sulfonate (ANS) was characterized using isolated rat hepatocytes. The initial uptake rate of ANS by isolated hepatocytes was determined. The uptake process of ANS was fitted well to the Michaelis-Menten equation with a saturable component. The Vmax and Km values were 2.9±0.1nmol/min/mg protein and 29.1±3.2μM, respectively. The uptake clearance (CLup) based on the ratio of Vmax to Km was 11.7 ml/min/g liver, revealing the good coincidence with that assessed from the analysis of the plasma disappearance curve in previous report. Furthermore, the effect of serum protein on the hepatic uptake of ANS into isolated hepatocytes was investigated. The permeability clearances (PSinf) of ANS uptake were much higher than those predicted based on the unbound fractions in the presence of serum. These suggested that the hepatic uptake of extensively serum protein-bound ANS is mediated not only by the unbound form of ligand but also by the serum protein-mediated uptake mechanism.
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KEYWORD
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Hepatic uptake, 1-anilino-8-naphthalene sulfonate (ANS), protein-mediated uptake, isolated rat hepatocytes, serum protein
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