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Analysis of drug interactions with very low density lipoprotein by high-performance affinity chromatography.


ABSTRACT: High-performance affinity chromatography (HPAC) was utilized to examine the binding of very low density lipoprotein (VLDL) with drugs, using R/S-propranolol as a model. These studies indicated that two mechanisms existed for the binding of R- and S-propranolol with VLDL. The first mechanism involved non-saturable partitioning of these drugs with VLDL, which probably occurred with the lipoprotein's non-polar core. This partitioning was described by overall affinity constants of 1.2 (±0.3) × 10(6) M(-1) for R-propranolol and 2.4 (±0.6) × 10(6) M(-1) for S-propranolol at pH 7.4 and 37 °C. The second mechanism occurred through saturable binding by these drugs at fixed sites on VLDL, such as represented by apolipoproteins on the surface of the lipoprotein. The association equilibrium constants

SUBMITTER: Sobansky MR 

PROVIDER: S-EPMC4167910 | biostudies-literature | 2014 Oct

REPOSITORIES: biostudies-literature