Ibuprofen and the Phosphatidylcholine Bilayer : Membrane Water Permeability in the Presence and Absence of Cholesterol

The interactions between drugs and cell membranes can modulate the structural and physical properties of membranes. The resultant perturbations of the membrane integrity may affect the conformation of the proteins inserted within the membrane, disturbing the membrane-hosted biological functions. In...

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Veröffentlicht in:Langmuir : the ACS journal of surfaces and colloids. - 1985. - 37(2021), 15 vom: 20. Apr., Seite 4468-4480
1. Verfasser: Wood, Megan (VerfasserIn)
Weitere Verfasser: Morales, Michael, Miller, Elizabeth, Braziel, Samuel, Giancaspro, Joseph, Scollan, Patrick, Rosario, Juan, Gayapa, Alyssa, Krmic, Michael, Lee, Sunghee
Format: Online-Aufsatz
Sprache:English
Veröffentlicht: 2021
Zugriff auf das übergeordnete Werk:Langmuir : the ACS journal of surfaces and colloids
Schlagworte:Journal Article Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, Non-P.H.S. Lipid Bilayers Phosphatidylcholines Water 059QF0KO0R Cholesterol 97C5T2UQ7J Ibuprofen WK2XYI10QM
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520 |a The interactions between drugs and cell membranes can modulate the structural and physical properties of membranes. The resultant perturbations of the membrane integrity may affect the conformation of the proteins inserted within the membrane, disturbing the membrane-hosted biological functions. In this study, the droplet interface bilayer (DIB), a model cell membrane, is used to examine the effects of ibuprofen, a nonsteroidal anti-inflammatory drug (NSAID), on transbilayer water permeability, which is a fundamental membrane biophysical property. Our results indicate that the presence of neutral ibuprofen (pH 3) increases the water permeability of the lipid membranes composed of 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC). When cholesterol is present with the DOPC, however, the water permeability is not influenced by addition of ibuprofen, regardless of the cholesterol content in DOPC. Given the fact that cholesterol is generally considered to impact packing in the hydrocarbon chain regions, our findings suggest that a potential competition between opposing effects of ibuprofen molecules and cholesterol on the hydrocarbon core environment of the phospholipid assembly may influence the overall water transport phenomena. Results from confocal Raman microspectroscopy and interfacial tensiometry show that ibuprofen molecules induce substantial structural and dynamic changes in the DOPC lipid bilayer. These results, demonstrating that the presence of ibuprofen increases the water permeability of pure DOPC but not that of DOPC-cholesterol mixtures, provide insight into the differential effect of a representative NSAID on heterogeneous biological membranes, depending upon the local composition and structure, results which will signal increased understanding of the gastrointestinal damage and toxicity induced by these molecules 
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650 4 |a Research Support, Non-U.S. Gov't 
650 4 |a Research Support, U.S. Gov't, Non-P.H.S. 
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700 1 |a Morales, Michael  |e verfasserin  |4 aut 
700 1 |a Miller, Elizabeth  |e verfasserin  |4 aut 
700 1 |a Braziel, Samuel  |e verfasserin  |4 aut 
700 1 |a Giancaspro, Joseph  |e verfasserin  |4 aut 
700 1 |a Scollan, Patrick  |e verfasserin  |4 aut 
700 1 |a Rosario, Juan  |e verfasserin  |4 aut 
700 1 |a Gayapa, Alyssa  |e verfasserin  |4 aut 
700 1 |a Krmic, Michael  |e verfasserin  |4 aut 
700 1 |a Lee, Sunghee  |e verfasserin  |4 aut 
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