Localization of Ellipticine Derivatives Interacting with Membranes
The interaction with membranes of three anti‐cancer drugs of the ellipticine family was studied by fluo‐ rescence quenching of membrane probes. The fluorescence of three probes, located at different levels in mem‐ branes, was quenched by addition of two types of ellipticine derivatives, one amphiphi...
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| Published in | European journal of biochemistry Vol. 133; no. 2; pp. 349 - 354 |
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| Main Authors | , , |
| Format | Journal Article |
| Language | English |
| Published |
Oxford, UK
Blackwell Publishing Ltd
01.06.1983
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| Online Access | Get full text |
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| Summary: | The interaction with membranes of three anti‐cancer drugs of the ellipticine family was studied by fluo‐ rescence quenching of membrane probes. The fluorescence of three probes, located at different levels in mem‐ branes, was quenched by addition of two types of ellipticine derivatives, one amphiphilic drug (9‐methoxy‐ ellipticine) and two dipolar molecules (9‐aminoellipticine and 9‐hydroxyellipticine). By comparing the quenching curves obtained, the following can be proposed.
a) 9‐Methoxyellipticine can penetrate deeper in the lipid layers than 9‐aminoellipticine and 9‐hydroxy‐ ellipticine can.
b) The three drugs are able to penetrate at least between the first methylene groups of the acyl chains of lipids in liposomes.
c) In an isolated bacterial membrane, only 9‐methoxyellipticine can be located in the region of the first methylene groups of lipids, the two dipolar drugs being adsorbed on the membrane surface.
It was also shown that cholesterol hindered the penetration of 9‐methoxyellipticine in the bilayer of liposomes. |
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| ISSN: | 0014-2956 1432-1033 |
| DOI: | 10.1111/j.1432-1033.1983.tb07469.x |