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Screening for the Drug–Phospholipid Interaction: Correlation to Phospholipidosis
Author(s) -
Alakoskela JuhaMatti,
Vitovič Pavol,
Kinnunen Paavo K. J.
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200900052
Subject(s) - phospholipidosis , phospholipid , drug , amphiphile , chemistry , phospholipid scramblase , cationic polymerization , biophysics , lipid bilayer , absorption (acoustics) , membrane , biochemistry , organic chemistry , pharmacology , materials science , biology , copolymer , polymer , composite material , phosphatidylserine
Phospholipid bilayers represent a complex, anisotropic environment fundamentally different from bulk oil or octanol, for instance. Even “simple” drug association to phospholipid bilayers can only be fully understood if the slab‐of‐hydrocarbon approach is abandoned and the complex, anisotropic properties of lipid bilayers reflecting the chemical structures and organization of the constituent phospholipids are considered. The interactions of drugs with phospholipids are important in various processes, such as drug absorption, tissue distribution, and subcellular distribution. In addition, drug–lipid interactions may lead to changes in lipid‐dependent protein activities, and further, to functional and morphological changes in cells, a prominent example being the phospholipidosis (PLD) induced by cationic amphiphilic drugs. Herein we briefly review drug–lipid interactions in general and the significance of these interactions in PLD in particular. We also focus on a potential causal connection between drug‐induced PLD and steatohepatitis, which is induced by some cationic amphiphilic drugs.