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Titolo:
The amphiphilic drug flufenamic acid can induce a hexagonal phase in DMPC:a solid state P-31- and F-19-NMR study
Autore:
Grage, SL; Gauger, DR; Selle, C; Pohle, W; Richter, W; Ulrich, AS;
Indirizzi:
Univ Jena, Inst Mol Biol, D-07745 Jena, Germany Univ Jena Jena Germany D-07745 ena, Inst Mol Biol, D-07745 Jena, Germany Univ Jena, Inst Ultrastrukturforsch, D-07743 Jena, Germany Univ Jena Jena Germany D-07743 ltrastrukturforsch, D-07743 Jena, Germany
Titolo Testata:
PHYSICAL CHEMISTRY CHEMICAL PHYSICS
fascicolo: 20, volume: 2, anno: 2000,
pagine: 4574 - 4579
SICI:
1463-9076(2000)2:20<4574:TADFAC>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
X-RAY-DIFFRACTION; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; CALCIUM INFLUX; MEMBRANE; NMR; HYDRATION; MIXTURES; LECITHIN; BILAYER; PHOSPHATIDYLCHOLINE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Physical, Chemical & Earth Sciences
Citazioni:
43
Recensione:
Indirizzi per estratti:
Indirizzo: Ulrich, AS Univ Jena, Inst Mol Biol, Winzerlaer Str 10, D-07745 Jena, Germany Univ Jena Winzerlaer Str 10 Jena Germany D-07745 Jena, Germany
Citazione:
S.L. Grage et al., "The amphiphilic drug flufenamic acid can induce a hexagonal phase in DMPC:a solid state P-31- and F-19-NMR study", PHYS CHEM P, 2(20), 2000, pp. 4574-4579

Abstract

Established solid state P-31-NMR and novel F-19-NMR experiments are used in a complementary approach to describe the behaviour of a fluorinated drug,flufenamic acid (FFA), in phospholipid model membranes. The non-steroidal anti-inflammatory agent FFA was dissolved at 5% (w/w) in dimyristoylphosphatidylcholine (DMPC), and the system was investigated at low hydration (3 H2O per lipid) where morphological transitions of the lipid are strongly affected by additives. It is demonstrated that FFA induces a fluid H-II phase in DMPC at ambient temperatures, i.e. much below its regular chain-melting transition which occurs around 50 degrees C at low hydration. The guest molecules are preferentially accommodated in the hexagonal phase of the lipid, which coexists with the usual crystalline state of pure DMPC. The peculiar transition sequence L-C --> H-II --> L-alpha with increasing temperature isexplained by a re-distribution of FFA in the lipid matrix and a concomitant phase separation under conditions of limiting hydration. Small-angle X-ray diffraction and freeze-fracture electron microscopy are used to confirm the existence of the hexagonal and bilayer phases, and to determine their respective dimensions. When the drug FFA dissolves in the bilayer, its structural effect on the surrounding lipid molecules may be related to its pharmacological activity in membranes. For example, FFA is known to modulate ion channel function, and it has been suggested that it inhibits phospholipase activity by accelerating the transbilayer flip-flop of lipids.

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Documento generato il 26/01/21 alle ore 04:47:22