title: Interaction of a β-lactam calixarene derivative with a model eukaryotic membrane affects the activity of PLA2.
abstract: In this research, the interaction between a membrane phospholipid, 1,2-dilauroyl-sn-glycero-3-phosphocholine (DLPC), and a p-tert-butylcalix[4]arene derivative bearing 6-aminopenicillanic acid (Calix), conceived as a possible drug carrier, was studied. The Langmuir film balance technique was used to measure surface pressure and electrical surface potential of pure and mixed Calix/DLPC monolayers spread on water at different temperatures. Phospholipase A2 (PLA2) activity was used as well to detect the impact of the calixarene derivative on the monolayer properties. Interaction between the molecules in mixed monolayers has been described quantitatively using thermodynamic functions. Interestingly, low amounts of Calix introduce ordering in the lipid film. This effect may be analogous to that of cholesterol interacting with phospholipids. A lower activity of PLA2 observed with the Calix/DLPC films compared to pure DLPC may be related to structural modifications of the mixed systems.
authors.affiliation: Department of Physical Chemistry and Electrochemistry, Faculty of Chemistry, Jagiellonian University, ul. R. Ingardena 3, 30-060 Krakow, Poland. bkorch@chemia.uj.edu.pl
authors.forename: Beata
authors.initials: B
authors.lastname: Korchowiec
authors.forename: Marcelina
authors.initials: M
authors.lastname: Gorczyca
authors.forename: Adel
authors.initials: A
authors.lastname: Ben Salem
authors.forename: Jean-Bernard
authors.initials: JB
authors.lastname: Regnouf de Vains
authors.forename: Ewa
authors.initials: E
authors.lastname: Rogalska
mesh_terms: D000818:Animals; D055162:Biocatalysis; D047250:Calixarenes / Q000737:chemistry / Q000378:metabolism*; D002462:Cell Membrane / Q000201:enzymology*; D005057:Eukaryotic Cells / Q000166:cytology* / Q000201:enzymology*; D006868:Hydrolysis; D007700:Kinetics; D008066:Lipolysis; D008954:Models, Biological; D008958:Models, Molecular; D010713:Phosphatidylcholines / Q000737:chemistry / Q000378:metabolism; D054467:Phospholipases A2 / Q000378:metabolism*; D034421:Sus scrofa; D013696:Temperature; D047090:beta-Lactams / Q000737:chemistry / Q000378:metabolism*
chemical_list: D010713:Phosphatidylcholines; D047090:beta-Lactams; D047250:Calixarenes; C015153:1,2-dilauroylphosphatidylcholine; D054467:Phospholipases A2