Europium coordination complexes as potential anticancer drugs: their partitioning and permeation into lipid bilayers as revealed by pyrene fluorescence quenching.
The present study was undertaken to evaluate the membrane-associating properties of a series of novel antitumor agents, Eu(III) coordination complexes (EC), using the pyrene fluorescence quenching as an analytical instrument. Analysis of EC-induced decrease in pyrene fluorescence intensity in terms of partition and solubility-diffusion models allowed us to evaluate the partition and permeation coefficients of the examined compounds into the lipid vesicles prepared from zwitterionic lipid phosphatidylcholine (PC) and its mixtures with cholesterol (Chol) and anionic lipid cardiolipin (CL). The drug-lipid interactions were found to have the complex nature determined by both EC structure and lipid bilayer composition. High values of the obtained partition and permeation coefficients create the background for the development of EC liposomal formulations.
Department of Nuclear and Medical Physics, V.N. Karazin Kharkov National University, 4 Svobody Sq., Kharkov 61077, Ukraine. valtrusova@yahoo.com
Valeriya
V
Trusova
Andrey
A
Yudintsev
Ludmila
L
Limanskaya
Galyna
G
Gorbenko
Todor
T
Deligeorgiev
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry*; D002462:Cell Membrane / Q000737:chemistry; D005063:Europium / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D008051:Lipid Bilayers / Q000737:chemistry*; D009942:Organometallic Compounds / Q000737:chemistry*; D010539:Permeability; D011721:Pyrenes / Q000737:chemistry*; D013050:Spectrometry, Fluorescence
D000970:Antineoplastic Agents; D008051:Lipid Bilayers; D009942:Organometallic Compounds; D011721:Pyrenes; D005063:Europium; C030984:pyrene