Εξειδίκευση τύπου :	Άρθρο σε επιστημονικό περιοδικό
Τίτλος:	Development of a CP P-31 NMR Broadline Simulation Methodology for Studying the Interactions of Antihypertensive AT(1) Antagonist Losartan with Phospholipid Bilayers
Δημιουργός/Συγγραφέας:	Fotakis, Charalambos Christodouleas, Dionisios Chatzigeorgiou, Petros [EL] Ζερβού, Μαρία[EN] Zervou, Maria Benetis, Nikolas-Ploutarch Viras, Kyriakos [EL] Μαυρομούστακος, Θωμάς[EN] Mavromoustakos, Thomas
Εκδότης:	Biophysical Society
Τόπος έκδοσης:	CAMBRIDGE
Ημερομηνία:	2009-03-18
Γλώσσα:	Αγγλικά
ISSN:	0006-3495
DOI:	10.1016/j.bpj.2008.11.057
Περίληψη:	A cross-polarization (CP) P-31 NMR broadline simulation methodology was developed for studying the effects of drugs in phospholipids bilayers. Based on seven-parameter fittings, this methodology provided information concerning the conformational changes and dynamics effects of losartan in the polar region of the dipalmitoylphosphatidylcholine bilayers. The test molecule for this study was losartan, an anti hypertensive drug known to exert its effect on AT(1) transmembrane receptors. The results were complemented and compared with those of differential scanning calorimetry, solid-state C-13 NMR spectroscopy, Raman spectroscopy, and electron spin resonance. More specifically, these physical chemical methodologies indicated that the amphipathic losartan molecule interacts with the hydrophilic-head zone of the lipid bilayers. The CP P-31 NMR broadline simulations showed that the lipid molecules in the bilayers containing losartan displayed greater collective tilt compared to the tilt displayed by the load-free bilayers, indicating improved packing. The Raman results displayed a decrease in the trans/gauche ratio and increased intermolecular interactions of the acyl chains in the liquid crystalline phase. Additional evidence, suggesting that losartan possibly anchors in the realm of the headgroup, was derived from upfield shift of the average chemical shift sigma(iso) of the P-31 signal in the presence of losartan and from shift of the observed peak at 715 cm(-1) attributed to C-N stretching in the Raman spectra.
Τίτλος πηγής δημοσίευσης:	Biophysical Journal
Τόμος/Κεφάλαιο:	96
Τεύχος:	6
Σελίδες:	2227-2236
Θεματική Κατηγορία:	[EL] Φυσική[EN] Physics
Λέξεις-Κλειδιά:	Biophysics
Αξιολόγηση από ομότιμους (peer reviewed):	Ναι
Ηλεκτρονική διεύθυνση περιοδικού (link) :	http://www.biophysj.org
ΙΒΦΧΒ: αρχειακή συλλογή:	Ινστιτούτο Οργανικής και Φαρμακευτικής Χημείας (ΙΟΦΧ) (έως 2012)
Εμφανίζεται στις συλλογές:	Ινστιτούτο Χημικής Βιολογίας - Επιστημονικό έργο