Local anesthetics destabilize lipid membranes by breaking hydration shell: infrared and calorimetry studies

Ueda, I.; Chiou, Jang-Shing; Prasad, Krishna; Kamaya, Hiroshi

doi:10.1016/0005-2736(94)90103-1

Cited by 54 publications

(36 citation statements)

References 44 publications

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“…It is also known that the membrane area could be artificially expanded, decreasing membrane tension that subsequently facilitates membrane resealing [27]. Furthermore, it has also been reported that anesthetics expand the lipid membrane by the spatial displacement of lipid molecules with the presence of anesthetic molecules [23]. It is therefore possible to hypothesize that lidocaine facilitates membrane fluidity making the plasma membrane easily permeable by sonication and that, at the same time, it decreases membrane tension by expanding it, facilitating membrane repair.…”

Section: Discussionmentioning

confidence: 98%

“…Therefore, the enhancement was probably due to the increase in the number of transfected cells and that was confirmed by visualization of individual transfected cells using the GFP expression vector, as shown in Figure 7. Local anesthetics have been shown to destabilize the lipid membranes by breaking the hydration shell and fluidizing lipid membranes [23]. In this study, we used lidocaine and it was shown to facilitate membrane fluidity dose-dependently.…”

Section: Discussionmentioning

confidence: 99%

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Enhancement of ultrasound‐mediated gene transfection by membrane modification

Nozaki

Ogawa

Feril

et al. 2003

The Journal of Gene Medicine

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

Enhancement of ultrasound‐mediated gene transfection by membrane modification

Nozaki

Ogawa

Feril

et al. 2003

The Journal of Gene Medicine

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“…This temperature corresponds to the liquid crystalline structure of the neat DMPC bilayer. It was known from earlier studies that addition of local anesthetics decreases the temperature of the transition to the gel phase in lipid bilayers [39]. That is why the bilayer remains in the liquid crystalline phase upon addition of articaine molecules.…”

Section: Simulation Detailsmentioning

confidence: 97%

“…This also was suggested as a possible mechanism for the anesthetic action of drug molecules [39]. Several hydrogen bonding patterns have been investigated: between articaine and lipid molecules, between articaine and water and also between lipids and water.…”

Section: Hydrogen Bondsmentioning

confidence: 99%

Molecular dynamics simulations of local anesthetic articaine in a lipid bilayer

Mojumdar

Lyubartsev

2010

Biophysical Chemistry

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In order to investigate structural and dynamical properties of local anesthetic articaine in a model lipid bilayer, a series of molecular dynamics simulations have been performed. Simulations were carried out for neutral and charged (protonated) forms of articaine inserted in fully hydrated dimyristoylphosphatidylcholine (DMPC) lipid bilayer. For comparison purpose, a fully hydrated DMPC bilayer without articaine was also simulated. The length of each simulation was 200 ns. Various properties of the lipid bilayer systems in the presence of both charged and uncharged forms of articaine taken at two different concentrations have been examined: membrane area per lipid, mass density distributions, order parameters, radial distribution functions, head group tilt, diffusion coefficients, electrostatic potential, etc, and compared with results of previous simulations of DMPC bilayer in presence of lidocaine. It was shown that addition of both charged and neutral forms of articaine causes increase of the dipole electrostatic potential in the membrane interior.

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“…By perturbing the electrostatic interactions among polar heads and the properties of the layer of bound water, an increase of the area per polar head occurs and bilayer interdigitation takes place. Surface adsorption and anesthetic-anesthetic interaction have already been suggested to explain infrared and calorimetric results concerning the interaction of the local anesthetics lidocaine and dibucaine with DPPC multilayers [33] and the effects of tetracaine on lipid bilayers [34]. The plot of P, vs. tem -p e r a t u r e ( F i g .…”

Section: Resultsmentioning

confidence: 99%

Procain interaction with DPPC multilayers: an ESR spin label investigation

et al. 1998

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A spin label electron spin resonance (ESR) study has been carried out on the interaction between the local anesthetic procaine (PRC) and multilamellar dispersions of di-palmitoylphosphatidylcholine (DPPC). The investigation has been performed either in the gel or in the liquid crystal phase of DPPC varying the anesthetic/DPPC molar ratio as well as the pH of the dispersion medium and using spin labeled DPPC molecules (5-and 16-PCSL) and the di-tert-butyl nitroxide (DTBN) spin probe. On increasing the anesthetic concentration in the dispersion medium up to PRC/DPPC molar ratio of 33 mol.%, a lyotropic transition of the bilayer from the lamellar gel phase Lp , to the interdigitated Lp; one is observed either at pH 5.0 or at pH 10.0. At intermediate pH values, about pH 7.0, such a PRC concentration dependent transition is absent. A decrease of the partition of the DTBN molecules between the dispersion medium and the fluid hydrophobic phase of DPPC multilayers is observed at pH 5.0 with anesthetic concentration, while an opposite behaviour is evidenced at pH 10.0. The pre-and main-phase transition temperatures of the DPPC multilayers are also affected although to different extent. These results are interpreted in terms of adsorption of the PRC molecules at the surface of the model membrane at the extreme pH values investigated, while at about neutral pH values they intercalate among the DPPC molecules. The protonation state of procaine plays an important role as it determines the way of surface adsorption of the PRC molecules in the neutral form at the high pH value and in the charged cationic form at pH 5.0.

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Local anesthetics destabilize lipid membranes by breaking hydration shell: infrared and calorimetry studies

Cited by 54 publications

References 44 publications

Enhancement of ultrasound‐mediated gene transfection by membrane modification

Enhancement of ultrasound‐mediated gene transfection by membrane modification

Molecular dynamics simulations of local anesthetic articaine in a lipid bilayer

Procain interaction with DPPC multilayers: an ESR spin label investigation

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