Abstract
Cell membranes play a fundamental role in protecting the cell from its surroundings, in addition to hosting many proteins with fundamental biological tasks. A study of drug/lipid interactions is a necessary and important step in fully clarifying the role and action mechanism of active ingredients, and shedding light on possible complications caused by drug overdosage. In this paper, the influence of benzocaine and propranolol drugs on the structure of l-α-phosphatidylcholine-based membranes has been investigated by means of neutron reflectivity, grazing incidence small angle neutron scattering, and small/ultra-small angle neutron scattering. Investigations allowed discovering a stiffening of the membranes and the formation of stalks, caused by the presence of benzocaine. On the other hand, disordered bilayers (lamellar powders) and highly curved structures were found in the presence of propranolol. The results obtained may be rationalized in terms of the molecular structures of drugs and may serve as a starting point for explaining the toxic behavior in long-term and overdosage scenarios.
Highlights
Cell membranes consist mainly of lipid bilayers as their structural unit.[1]
The influence of benzocaine and propranolol drugs on the structure of L-a-phosphatidylcholine-based membranes has been investigated by means of neutron reflectivity, grazing incidence small angle neutron scattering, and small/ultra-small angle neutron scattering
Part of its selectivity is due to the presence of different proteins that are embedded in the lipid bilayer
Summary
Cell membranes consist mainly of lipid bilayers as their structural unit.[1] In turn, these bilayers are composed of phospholipids, amphiphilic molecules formed by a functionalized hydrophilic phosphate head esterified with two fatty acid chains. The main task of a cell membrane is essentially to protect the cell from its surroundings, acting as a selective barrier between the internal cytoplasm and the extracellular environment.[2] Part of its selectivity is due to the presence of different proteins (known as membrane proteins) that are embedded in the lipid bilayer. The biological functions of these proteins include the possibilities of activating cell signaling, triggering intracellular signaling pathways, and interacting with external substances, including active ingredients.[3] To this aim, most of the drugs designed or used in pharmacological therapies target membrane proteins,[4] like channel blockers or protein binding inhibitors.[5]
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