Preferential location of lidocaine and etidocaine in lecithin bilayers as determined by EPR, fluorescence and H-2 NMR

dc.creatorde Paula, E
dc.creatorSchreier, S
dc.creatorJarrell, HC
dc.creatorFraceto, LF
dc.date2008
dc.dateJAN
dc.date2014-11-17T20:41:31Z
dc.date2015-11-26T17:42:08Z
dc.date2014-11-17T20:41:31Z
dc.date2015-11-26T17:42:08Z
dc.date.accessioned2018-03-29T00:24:00Z
dc.date.available2018-03-29T00:24:00Z
dc.identifierBiophysical Chemistry. Elsevier Science Bv, v. 132, n. 1, n. 47, n. 54, 2008.
dc.identifier0301-4622
dc.identifierWOS:000251496700007
dc.identifier10.1016/j.bpc.2007.10.004
dc.identifierhttp://www.repositorio.unicamp.br/jspui/handle/REPOSIP/80934
dc.identifierhttp://www.repositorio.unicamp.br/handle/REPOSIP/80934
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/80934
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1287208
dc.descriptionWe have examined the effect of the uncharged species of lidocaine (LDC) and etidocaine (EDC) on the acyl chain moiety of egg phosphatidylcholine liposomes. Changes in membrane organization caused by both anesthetics were detected through the use of EPR spin labels (5, 7 and 12 doxyl stearic acid methyl ester) or fluorescence probes (4, 6, 10, 16 pyrene-fatty acids). The disturbance caused by the LA was greater when the probes were inserted in more external positions of the acyl chain and decreased towards the hydrophobic core of the membrane. The results indicate a preferential insertion of LDC at the polar interface of the bilayer and in the first half of the acyl chain, for EDC. Additionally, 2 H NMR spectra of multilamellar liposomes composed by acyl chain-perdeutero DMPC and EPC (1:4 mol%) allowed the determination of the segmental order (S-mol) and dynamics (T-1) of the acyl chain region. In accordance to the fluorescence and EPR results, changes in molecular orientation and dynamics are more prominent if the LA preferential location is more superficial, as for LDC while EDC seems to organize the acyl chain region between carbons 2-8, which is indicative of its positioning. We propose that the preferential location of LDC and EDC inside the bilayers creates a 'transient site', which is related to the anesthetic potency since it could modulate the access of these molecules to their binding site(s) in the voltage-gated sodium channel. (C) 2007 Elsevier B.V. All rights reserved.
dc.description132
dc.description1
dc.description47
dc.description54
dc.languageen
dc.publisherElsevier Science Bv
dc.publisherAmsterdam
dc.publisherHolanda
dc.relationBiophysical Chemistry
dc.relationBiophys. Chem.
dc.rightsfechado
dc.rightshttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dc.sourceWeb of Science
dc.subjectlocal anesthetic
dc.subjectmembrane
dc.subjectfluorescence
dc.subjectmagnetic resonance
dc.subjectliposomes
dc.subjectNuclear Magnetic-resonance
dc.subjectAnesthetic-membrane Interaction
dc.subjectLocal-anesthetics
dc.subjectPhospholipid-bilayers
dc.subjectLipid-membranes
dc.subjectModel Membranes
dc.subjectMolecular Determinants
dc.subjectPartition-coefficients
dc.subjectPhase-separation
dc.subjectNa+ Channels
dc.titlePreferential location of lidocaine and etidocaine in lecithin bilayers as determined by EPR, fluorescence and H-2 NMR
dc.typeArtículos de revistas


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