Abstract
The interactions of drugs with cell membranes are of primary importance for several processes involved in drugs activity. However, these interactions are very difficult to study due to the complexity of biological membranes. Lipid model membranes have been developed and used to gain insight into drug–membrane interactions. In this study, the interaction of protocatechuic acid ethyl ester, showing radical-scavenging activity, antimicrobial, antitumor and anti-inflammatory effects, with model membranes constituted by multilamellar vesicles and monolayers made of DMPC and DSPC, has been studied. Differential scanning calorimetry and Langmuir–Blodgett techniques have been used. Protocatechuic acid ethyl ester interacted both with MLV and monolayers. However, a stronger interaction of the drug with DMPC-based model membranes has been obtained. The finding of this study could help to understand the protocatechuic acid ethyl ester action mechanism.
Highlights
Studies on the interactions of cell membranes with drugs are of interest to understanding the action of molecular mechanisms
Phosphatidylcholine derivatives (DMPC and DSPC) were used to prepare a biological membrane model represented by multilamellar vesicles (MLV) and to evaluate their interactions with protocatechuic acid ethyl ester (PCAEE)
Protocatechuic acid ethyl ester caused the disappearance of the DMPC MLV pre-transition peak at all the used molar fractions, indicating that the compound localized in the polar region of the lipid bilayers [29,30]; upon increasing the compound molar fraction, a gradual shift of the main peak towards lower temperatures and a concomitant broadening occurred
Summary
Studies on the interactions of cell membranes with drugs are of interest to understanding the action of molecular mechanisms. PCAEE has higher radical-scavenging activity by a better location at the lipid/aqueous phase interface where the oxidation occurs, and higher antimicrobial, antitumor, and anti-inflammatory effects [10,11] Most of these actions take place in phospholipid bilayers or inside the cells, so it is essential to have information on the interaction of PCAEE with biological membranes. Compounds, interacting with the phospholipid bilayers, can modificate the lipid chain packing, that causes the variation of the transition thermodynamic parameters [16–19] This behaviour can be analysed by the van’t Hoff model of the freezing-point depression of solutions [20,21]; Langmuir–Blodgett (LB) is commonly used to study the interaction between drugs and phospholipid monolayers, which represents a useful model for biomembranes. The results can give indications on the ability of PCAEE to dissolve in the biomembrane models
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