Korean J Physiol Pharmacol.
2012 Dec;16(6):413-422. 10.4196/kjpp.2012.16.6.413.
The Effect of Lidocaine.HCl on the Fluidity of Native and Model Membrane Lipid Bilayers
- Affiliations
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- 1Department of Dental Pharmacology and Biophysics, College of Pharmacy, Chung-Ang University, Seoul 156-756, Korea. iyun@pusan.ac.kr, jho9612@pusan.ac.kr
- 2Department of Oral and Maxillofacial Surgery and Clinical Pharmacology, College of Pharmacy, Chung-Ang University, Seoul 156-756, Korea.
- 3Department of Pharmacology, College of Pharmacy, Chung-Ang University, Seoul 156-756, Korea.
- 4Department of Oral Physiology and Molecular Biology, School of Dentistry and Research Institute for Oral Biotechnology, Yangsan Campus of Pusan National University, Yangsan 626-870, Korea. mkbae@pusan.ac.kr
- KMID: 2285450
- DOI: http://doi.org/10.4196/kjpp.2012.16.6.413
Abstract
- The purpose of this study is to investigated the mechanism of pharmacological action of local anesthetic and provide the basic information about the development of new effective local anesthetics. Fluorescent probe techniques were used to evaluate the effect of lidocaine.HCl on the physical properties (transbilayer asymmetric lateral and rotational mobility, annular lipid fluidity and protein distribution) of synaptosomal plasma membrane vesicles (SPMV) isolated from bovine cerebral cortex, and liposomes of total lipids (SPMVTL) and phospholipids (SPMVPL) extracted from the SPMV. An experimental procedure was used based on selective quenching of 1,3-di(1-pyrenyl)propane (Py-3-Py) and 1,6-diphenyl-1,3,5-hexatriene (DPH) by trinitrophenyl groups, and radiationless energy transfer from the tryptophans of membrane proteins to Py-3-Py. Lidocaine.HCl increased the bulk lateral and rotational mobility of neuronal and model membrane lipid bilayes, and had a greater fluidizing effect on the inner monolayer than the outer monolayer. Lidocaine.HCl increased annular lipid fluidity in SPMV lipid bilayers. It also caused membrane proteins to cluster. The most important finding of this study is that there is far greater increase in annular lipid fluidity than that in lateral and rotational mobilities by lidocaine.HCl. Lidocaine.HCl alters the stereo or dynamics of the proteins in the lipid bilayers by combining with lipids, especially with the annular lipids. In conclusion, the present data suggest that lidocaine, in addition to its direct interaction with proteins, concurrently interacts with membrane lipids, fluidizing the membrane, and thus inducing conformational changes of proteins known to be intimately associated with membrane lipid.
Keyword
MeSH Terms
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Anesthetics, Local
Cell Membrane
Cerebral Cortex
Diphenylhexatriene
Energy Transfer
Lidocaine
Lipid Bilayers
Liposomes
Membrane Lipids
Membrane Proteins
Membranes
Neurons
Phospholipids
Proteins
Tryptophan
Anesthetics, Local
Diphenylhexatriene
Lidocaine
Lipid Bilayers
Liposomes
Membrane Lipids
Membrane Proteins
Phospholipids
Proteins
Tryptophan
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