Lipoprotein Distribution of a Novel Endotoxin Antagonist, E5531, in Plasma from Human Subjects with Various Lipid Levels
Author(s) -
Kishor M. Wasan,
Frank W. Strobel,
Steven C. Parrott,
Melvyn Lynn,
William J. Christ,
Lynn D. Hawkins,
Daniel P. Rossignol
Publication year - 1999
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.43.10.2562
Subject(s) - lipoprotein , triglyceride , antagonist , endocrinology , medicine , high density lipoprotein , distribution (mathematics) , low density lipoprotein , chemistry , low density lipoprotein receptor related protein 8 , plasma protein binding , cholesterol , very low density lipoprotein , biology , biochemistry , receptor , mathematical analysis , mathematics
The purpose of this study was to determine the distribution profile of a novel endotoxin antagonist, [14 C]E5531, at 1 μg/ml in plasma samples obtained from fasted human subjects with various lipid and protein concentrations. Our findings suggest that the majority of E5531 binds with high-density lipoproteins (HDLs) independently of plasma lipid and protein levels tested. Furthermore, it appears that an increase in triglyceride-rich lipoprotein (TRL) lipid and protein levels and an increase in low-density lipoprotein (LDL) lipid levels significantly increase TRL plus LDL binding of E5531. However, only an increase in HDL protein levels significantly increases HDL binding of E5531.
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