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Amiodarone-liposome interaction: a multinuclear NMR and X-ray diffraction study.

G L Jendrasiak¹, T J McIntosh, A Ribeiro

¹Department of Radiation Oncology, East Carolina University, Greenville, NC 27858-4354.

Biochimica Et Biophysica Acta

|May 9, 1990

Summary

Amiodarone, an antiarrhythmic drug, interacts with lipid bilayers, affecting their structure and properties. This study reveals amiodarone

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Area of Science:

Cardiology
Biophysics
Pharmacology

Background:

Amiodarone is a key antiarrhythmic medication.
Its effects and side effects are linked to lipids.
Understanding its interaction with cell membranes is crucial.

Purpose of the Study:

To investigate the interaction of amiodarone with lipid bilayers.
To elucidate the structural consequences of amiodarone incorporation.

Main Methods:

Multinuclear Nuclear Magnetic Resonance (NMR) spectroscopy.
X-ray diffraction analysis.
Studies conducted on egg phosphatidylcholine (EPC) liposomes and multilayers.

Main Results:

Amiodarone alters lipid headgroup signals (NMR) and methylene group signals (NMR).

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It decreases bilayer thickness and increases interfacial electron density (X-ray diffraction).

Iodine atoms are near the hydrocarbon/water interface; the tertiary amine is in the headgroup region.

Conclusions:

Amiodarone perturbs the structure of lipid bilayers.
Its molecular location within the bilayer is determined.
Provides insights into amiodarone's mechanism of action and lipid-related side effects.