Interaction of four local anesthetics with phospholipid bilayer membranes: permeability effects and possible mechanisms

1980 ◽  
Vol 58 (10) ◽  
pp. 815-821 ◽  
Author(s):  
Michael A. Singer ◽  
Mahendra K. Jain
Keyword(s):  
Local Anesthetics ◽  
Temperature Curve ◽  
Phospholipid Bilayer ◽  
Lipid Phase ◽  
Lipid Phase Transition ◽  
Bilayer Membranes ◽  
Multilamellar Liposomes ◽  
Preferential Binding ◽  
Lower Temperature ◽  
Dicetyl Phosphate

Sodium 22 efflux was measured, at various temperatures, in the presence of different local anesthetics (dibucaine, tetracaine, benzocaine, procaine) in multilamellar liposomes composed of saturated phosphatidylcholines and dicetyl phosphate. These liposomes display a permeability maximum in the temperature region of their respective phase transitions. Local anesthetics cause this permeability maximum to occur at a lower temperature and also increase its magnitude. Binding of the anesthetics to these liposomes displays a biphasic temperature curve with a maximum in the vicinity of the transition temperature. In addition there appears to be a linear relationship between aqueous anesthetic concentrations causing equal permeability effects and corresponding membrane concentrations. All of the anesthetics decrease the cooperativity of the lipid phase transition and this is probably an important factor underlying induced permeability effects. However several observations suggest that additional factors are also important and we have postulated that one such factor is the preferential binding of the anesthetics to phase boundary regions.

Interaction of Amphotericin B and Nystatin with Phospholipid Bilayer Membranes: Effect of Cholesterol

1975 ◽  
Vol 53 (6) ◽  
pp. 1072-1079 ◽  
Author(s):  
Michael A. Singer
Keyword(s):  
Membrane Fluidity ◽  
Amphotericin B ◽  
Local Anesthetics ◽  
Cholesterol Content ◽  
Phospholipid Bilayer ◽  
High Cholesterol ◽  
Na Transport ◽  
Bilayer Membranes ◽  
Multilamellar Liposomes ◽  
Transmembrane Channels

Sodium-22 efflux was measured in multilamellar liposomes, exposed to one of the two polyene antibiotics amphotericin B or nystatin. Polyene mediated 22Na transport progressively rises with membrane sterol concentrations up to about 20 mol %, but falls with higher cholesterol concentrations. The polyene induced 22Na movement in cholesterol rich liposomes could be 'restored' by the addition of either dibucaine or propranolol (two local anesthetics) to the aqueous solution. These observations are interpreted in terms of the model of De Kruijff and Demel (Biochim. Biophys. Acta, 339, 57–70, 1974). In this model, nystatin and amphotericin B first complex with cholesterol and then these complexes aggregate to form transmembrane channels. It is here proposed that the aggregation of these complexes is inhibited by a high cholesterol content (decreased membrane fluidity) but that the two local anesthetics, by disrupting phospholipid–sterol interactions (increased membrane fluidity), can 'restore' this process of aggregation.

Determination of Lipid Phase Transition Temperatures in Hybrid Bilayer Membranes

Langmuir ◽  
2006 ◽  
Vol 22 (20) ◽  
pp. 8333-8336 ◽  
Author(s):  
Neil A. Anderson ◽  
Lee J. Richter ◽  
John C. Stephenson ◽  
Kimberly A. Briggman
Keyword(s):  
Phase Transition ◽  
Lipid Phase ◽  
Transition Temperatures ◽  
Lipid Phase Transition ◽  
Bilayer Membranes ◽  
Phase Transition Temperatures ◽  
Hybrid Bilayer Membranes

Fatty acyl chain structure, orientational order, and the lipid phase transition in Acholeplasma laidlawii B membranes. A review of recent 19F nuclear magnetic resonance studies

1984 ◽  
Vol 62 (11) ◽  
pp. 1134-1150 ◽  
Author(s):  
P. M. Macdonald ◽  
B. D. Sykes ◽  
R. N. McElhaney
Keyword(s):  
Phase Transition ◽  
Fatty Acids ◽  
Nuclear Magnetic Resonance ◽  
Acyl Chain ◽  
Orientational Order ◽  
Membrane Lipid ◽  
Fatty Acyl ◽  
Fatty Acyl Chain ◽  
Lipid Phase ◽  
Lipid Phase Transition

The orientational order parameters of monofluoropalmitic acids biosynthetically incorporated into membranes of Acholeplasma laidlawii B in the presence of a large excess of a variety of structurally diverse fatty acids have been determined via 19F nuclear magnetic resonance (19F NMR) spectroscopy. It is demonstrated that these monofluoropalmitic acids are relatively nonperturbing membrane probes based upon physical (differential scanning calorimetry), biochemical (membrane lipid analysis), and biological (growth studies) criteria. 19F NMR is shown to convey the same qualitative and quantitative picture of membrane lipid order provided by 2H-NMR techniques and to be sensitive to the structural characteristics of the membrane fatty acyl chains, as well as to the lipid phase transition. Representatives of each naturally occurring class of fatty acyl chain structures, including straight-chain saturated, methyl-branched, monounsaturated, and alicyclic-ring-substituted fatty acids, were studied and the 19F-NMR order parameters were correlated with the lipid phase transitions (determined calorimetrically). The lipid phase transition was the prime determinant of overall orientational order regardless of fatty acid structure. Effects upon orientational order attributable to specific structural substituents were discernible, but were secondary to the effects of the lipid phase transition. In the gel state, relative overall order was directly proportional to the temperature of the particular lipid phase transition. Not only the overall order, but also the order profile across the membrane was sensitive to the presence of particular structural substituents. In particular, in the gel state specific fatty acyl structures demonstrated a characteristic disordering effect in the membrane order profile. These various observations can be merged to provide a unified picture of the manner in which fatty acyl chain chemistry modulates the physical state of membrane lipids.

scholarly journals Fusion of phospholipid vesicles with planar phospholipid bilayer membranes. II. Incorporation of a vesicular membrane marker into the planar membrane.

1980 ◽  
Vol 75 (3) ◽  
pp. 251-270 ◽  
Author(s):  
F S Cohen ◽  
J Zimmerberg ◽  
A Finkelstein
Keyword(s):  
Divalent Cations ◽  
Phospholipid Bilayer ◽  
Phospholipid Vesicles ◽  
Osmotic Gradient ◽  
Bilayer Membranes ◽  
Fusion Procedure ◽  
Vesicular Membrane ◽  
Membrane Contact ◽  
Planar Membrane ◽  
Planar Membranes

Fusion of multilamellar phospholipid vesicles with planar phospholipid bilayer membranes was monitored by the rate of appearance in the planar membrane of an intrinsic membrane protein present in the vesicle membranes. An essential requirement for fusion is an osmotic gradient across the planar membrane, with the cis side (the side containing the vesicles) hyperosmotic to the opposite (trans) side; for substantial fusion rates, divalent cation must also be present on the cis side. Thus, the low fusion rates obtained with 100 mM excess glucose in the cis compartment are enhanced orders of magnitude by the addition of 5-10 mM CaCl2 to the cis compartment. Conversely, the rapid fusion rates induced by 40 mM CaCl2 in the cis compartment are completely suppressed when the osmotic gradient (created by the 40 mM CaCl2) is abolished by addition of an equivalent amount of either CaCl2, NaCl, urea, or glucose to the trans compartment. We propose that fusion occurs by the osmotic swelling of vesicles in contact with the planar membrane, with subsequent rupture of the vesicular and planar membranes in the region of contact. Divalent cations catalyze this process by increasing the frequency and duration of vesicle-planar membrane contact. We argue that essentially this same osmotic mechanism drives biological fusion processes, such as exocytosis. Our fusion procedure provides a general method for incorporating and reconstituting transport proteins into planar phospholipid bilayer membranes.

scholarly journals High Pressure Bioscience. Phospholipid Bilayer Membranes under High Pressure.

1999 ◽  
Vol 9 (3) ◽  
pp. 213-220 ◽  
Author(s):  
Shoji KANESHINA ◽  
Hitoshi MATSUKI ◽  
Hayato ICHIMORI
Keyword(s):  
High Pressure ◽  
Phospholipid Bilayer ◽  
Bilayer Membranes
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