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• W1582548374 abstract "Ellipticine and some of its derivatives constitute an interesting class of substances displaying an antitumoral activity against both experimental and human tumors. We have recently shown that some of these molecules were able to interact rapidly and strongly with acidic phospholipids. In the present report, amphiphilic ellipticine and 9-methoxyellipticine were tested against synthetic dilauroyl phosphatidylglycerol and dipalmitoylphosphatidylglycerol as well as a sample of phosphatidyl-glycerol with methyl-branched fatty acids, to investigate the stoichiometry of these interactions and their consequences on the organization of the lipid phase. Through surface pressure and surface potential measurements, carried out at the air-water interface, it is shown that the two drugs strongly interact with phosphatidylglycerols, whatever the film surface pressure or the nature and physical state of the lipid acyl chains may be. Such interactions bring about large film expansions and a complete modification of the phase properties of the lipids. These interactions achieve, at saturation, drug/lipid associations near the 1/1 molar ratio, stabilized by both electrostatic and hydrophobic forces. The drug molecules can be viewed as inserted between the lipid molecules, the—NH+ group interacting with the phosphate function and the aromatic moiety being in contact with the lipid acyl chains. From compression isotherms of 1/1 drug/lipid mixtures, it can be inferred that the two drugs cause a large condensing effect on both the dilauroyl and dipalmitoyl derivatives of phosphatidyl-glycerol, as compared to the behaviour of the lipids alone when ionized. In the mixed films, both lipids would exist in a very similar and rather condensed state, intermediate between the liquid-expanded and gel states in which these two lipids can respectively exist on pure water. The possibility of membranes being one of the sites of action of ellipticines is discussed." @default.
• W1582548374 created "2016-06-24" @default.
• W1582548374 creator A5026669603 @default.
• W1582548374 creator A5065870348 @default.
• W1582548374 date "1980-04-01" @default.
• W1582548374 modified "2023-09-27" @default.
• W1582548374 title "Interactions between Ellipticine and Phospholipids. Effect of Ellipticine and 9-Methoxyellipticine on the Phase Behaviour of Phosphatidylglycerols. A Monolayer Study" @default.
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• W1582548374 doi "https://doi.org/10.1111/j.1432-1033.1980.tb04537.x" @default.
• W1582548374 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/7371647" @default.
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