Amiodarone induced modifications of the phospholipid physical state. A fluorescence polarization study

Biochemical Pharmacology
P ChatelainJ M Ruysschaert

Abstract

The effects of an antiarrhythmic and antianginal drug, amiodarone, on the physical state of membrane phospholipids was investigated by means of fluorescence polarization using the apolar probe 1,6 diphenyl-1,3,5-hexatriene incorporated in the hydrocarbon core. Multilamellar vesicles were prepared from neutral phospholipids (egg phosphatidylcholine, synthetic saturated phosphatidylcholine) alone or mixed with cholesterol or various lipids representative of the main lipid classes. Amiodarone reduces the temperature of the gel to liquid-crystalline phase transition and either increases or decreases lipid mobility in the gel or liquid-crystalline phase. In the gel state, the lipid mobility depends on drug concentration, degree of ionization and the length of the lipid acyl chains. In the liquid-crystalline state, the decreased lipid mobility which is concentration-dependent is essentially due to hydrophobic interactions. Amiodarone increases the lipid order parameter to the same extent as cholesterol. The data suggested that amiodarone is a rigid molecule deeply buried in the hydrocarbon core of the lipid and that amiodarone-lipid interactions are mainly hydrophobic.

References

Dec 1, 1979·Proceedings of the National Academy of Sciences of the United States of America·F Jähnig
Apr 1, 1979·Chemistry and Physics of Lipids·M Lyte, M Shinitzky
Apr 16, 1976·Biochimica Et Biophysica Acta·M Shinitzky, M Inbar
May 31, 1985·Biochemical and Biophysical Research Communications·P ChatelainM Gillard
Sep 1, 1966·Clinica Chimica Acta; International Journal of Clinical Chemistry·K Itaya, M Ui
Jun 1, 1984·The Journal of Pharmacy and Pharmacology·M R LallozR L Himsworth
Mar 1, 1982·Journal of Cardiovascular Pharmacology·E RivaA Guaitani
Feb 15, 1981·Biochemical Pharmacology·P Chatelain, J M Ruysschaert
Jan 1, 1984·Annual Review of Pharmacology and Toxicology·D B Goldstein
Apr 1, 1983·European Journal of Clinical Investigation·N M DebbasP Puech
Jul 21, 1981·Biochemistry·I YuliM Shinitzky

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Citations

Dec 15, 1989·Biochemical Pharmacology·S A BeddowsS S Nussey
Dec 11, 1991·Biochemical Pharmacology·J M Antonini, M J Reasor
Jan 1, 1995·Pharmacology & Therapeutics·B Fromenty, D Pessayre
Mar 3, 1995·International Journal of Cardiology·M C Antunes-MadeiraV V Madeira
Feb 1, 1993·Biophysical Chemistry·S Barghouthi, M R Eftink
Oct 24, 1996·European Journal of Pharmacology·J P MontenezM P Mingeot-Leclercq
Jun 29, 2001·British Journal of Pharmacology·D LapennaF Cuccurullo
Nov 16, 2001·Antimicrobial Agents and Chemotherapy·M P Mingeot-LeclercqR Brasseur
Nov 15, 2014·Archives of Toxicology·Paul JenningsJeffrey S Wiseman
May 31, 1985·Biochemical and Biophysical Research Communications·P ChatelainM Gillard
May 1, 1994·Journal of Pharmaceutical Sciences·P ChatelainR Laruel
Aug 2, 2003·Journal of Cardiovascular Electrophysiology·Nathalie LalevéeSylvain Richard
Jul 1, 1996·Journal of Cardiovascular Pharmacology·S U YasudaR L Woosley
Jun 19, 1991·International Journal of Cancer. Journal International Du Cancer·W T van der GraafN H Mulder
May 9, 1990·Biochimica Et Biophysica Acta·G L JendrasiakR S Porter
Jan 1, 1989·Progress in Cardiovascular Diseases·B N SinghR Kannan
May 29, 2007·Biochemical Pharmacology·Domenico LapennaFranco Cuccurullo

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