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Titolo:
Selective inhibition of human erythrocyte Na+/K+ ATPase by cardiac glycosides and by a mammalian digitalis like factor
Autore:
Balzan, S; DUrso, G; Ghione, S; Martinelli, A; Montali, U;
Indirizzi:
CNR, Ist Fisiol Clin, I-56126 Pisa, Italy CNR Pisa Italy I-56126CNR, Ist Fisiol Clin, I-56126 Pisa, Italy Univ Pisa, Dipartimento Sci Uomo & Ambiente, Pisa, Italy Univ Pisa Pisa Italy isa, Dipartimento Sci Uomo & Ambiente, Pisa, Italy Univ Pisa, Dipartimento Sci Farmaceut, Pisa, Italy Univ Pisa Pisa ItalyUniv Pisa, Dipartimento Sci Farmaceut, Pisa, Italy
Titolo Testata:
LIFE SCIENCES
fascicolo: 16, volume: 67, anno: 2000,
pagine: 1921 - 1928
SICI:
0024-3205(20000908)67:16<1921:SIOHEN>2.0.ZU;2-A
Fonte:
ISI
Lingua:
ENG
Soggetto:
ENDOGENOUS OUABAIN; COMPOUND; PLASMA; SODIUM; BLOOD; PUMP;
Keywords:
cardiac glycosides; endogenous digitalis-like factor; Na+/K(+)ATPase; human red blood cells;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
21
Recensione:
Indirizzi per estratti:
Indirizzo: Balzan, S CNR, Ist Fisiol Clin, Via Savi 8, I-56126 Pisa, Italy CNR Via Savi 8 Pisa Italy I-56126 a Savi 8, I-56126 Pisa, Italy
Citazione:
S. Balzan et al., "Selective inhibition of human erythrocyte Na+/K+ ATPase by cardiac glycosides and by a mammalian digitalis like factor", LIFE SCI, 67(16), 2000, pp. 1921-1928

Abstract

Na+/K(+)ATPase is a transport membrane protein which contains the functional receptor for digitalis compounds, In this work we compare the inhibitioncurves of Na+/K(+)ATPase measured by the inhibition of Rb-86 uptake in human red blood cells by cardiac glycosides and by an endogenous digitalis like factor (EDLF) extracted from human newborn cord blood. The curves of Na+/K(+)TPase inhibition show a monophasic shape for ouabain, strophantidin, digitoxin, proscillaridin and EDLF whereas a biphasic shape for ouabagenin, digoxin, digoxigenin and digitoxigenin. All the drugs are potent inhibitors of erythrocyte Na+/K(+)ATPase with an IC50 ranging from 1.8x10(-9)M to 1.4x10(-11)M for the higher affinity binding site and from 1.8X10(-6)M to 5.5X10(-9)M for the lower affinity site. Digitoxigenin is the most active showing the higher active site at 1.4X10(-11)M. Ouabain and digoxin have higher affinity compared with their corresponding genins, while digitoxigenin showsa binding site with higher affinity than the respective cardiac glycosides, The increased affinity of the drugs to Na+/K(+)ATPase may be related to alipophilic region in correspondence of the carbons 10, 9, 11, 12, 13 of the steroid nucleus, situated in the opposite side with respect of the C-OH-14. The comparison of the inhibition curves and the HPLC profile of newborn EDLF and of the investigated cardenolides suggest that EDLF may be a compound identical or very similar to ouabain. (C) 2000 Elsevier Science Inc. Allrights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 27/11/20 alle ore 22:29:20