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Titolo:
THE ANTICANCER DRUG TAMOXIFEN INDUCES CHANGES IN THE PHYSICAL-PROPERTIES OF MODEL AND NATIVE MEMBRANES
Autore:
CUSTODIO JBA; ALMEIDA LM; MADEIRA VMC;
Indirizzi:
UNIV COIMBRA,FAC FARM,BIOQUIM LAB,COURACA APOSTOLOS 51 P-3000 COIMBRAPORTUGAL UNIV COIMBRA,CTR NEUROCIENCIAS P-3400 COIMBRA PORTUGAL
Titolo Testata:
Biochimica et biophysica acta
fascicolo: 2, volume: 1150, anno: 1993,
pagine: 123 - 129
SICI:
0006-3002(1993)1150:2<123:TADTIC>2.0.ZU;2-5
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROTEIN-KINASE-C; SARCOPLASMIC-RETICULUM MEMBRANES; PHASE-TRANSITION; LIPID BILAYERS; BREAST-CANCER; INTRAMOLECULAR EXCIMERIZATION; FLUORESCENT-PROBE; FLUIDITY; INHIBITION; MOLECULES;
Keywords:
TAMOXIFEN; ANTICANCER DRUG; BREAST CANCER; MEMBRANE-LIPID INTERACTION; MEMBRANE FLUIDITY; FLUORESCENT PROBE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
46
Recensione:
Indirizzi per estratti:
Citazione:
J.B.A. Custodio et al., "THE ANTICANCER DRUG TAMOXIFEN INDUCES CHANGES IN THE PHYSICAL-PROPERTIES OF MODEL AND NATIVE MEMBRANES", Biochimica et biophysica acta, 1150(2), 1993, pp. 123-129

Abstract

The interactions of tamoxifen with lipid bilayers of model and nativemembranes were investigated by fluorescence polarization of 1,6-diphenyl-1,3,5-hexatriene (DPH) and by intramolecular excimer formation of 1,3-di(1-pyrenyl)propane (Py(3)Py). The effects of TAM on liposomes ofDMPC, DPPC and DSPC are temperature dependent. In the fluid phase, TAM reduces dynamics of the upper bilayer region as observed by Py(3)Py and has no effect on the hydrophobic region as detected by DPH. In thegel phase, the effects of TAM evaluated by Py(3)Py are not discernible for DMPC and DPPC bilayers, whereas DSPC bilayers become more fluid. However, DPH detects a strong fluidizing effect of TAM in the hydrophobic region of the above membrane systems, where DPH distributes, as compared with the small effects detected by Py(3)Py. TAM decreases the main phase transition temperature but does not extensively broaden thetransition thermotropic profile of pure lipids, except for bilayers of DMPC where TAM induces a significant broadening detected with the two probes. In fluid liposomes of sarcoplasmic reticulum lipids and native membranes, TAM induces an ordering effect, as evidenced by Py(3)Py,failing DPH to detect any apparent effect as observed for the fluid phase of liposomes of pure lipid bilayers. These findings confirm the hydrophobic nature of tamoxifen and suggest that the localization and effects of TAM are modulated by the order and fluidity of the bilayer. These changes in the dynamic properties of lipids and the non-specificinteractions with membrane lipids, depending on the order or fluidityof the biomembrane, may be important for the multiple cellular effects and action mechanisms of tamoxifen.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 10/07/20 alle ore 14:36:26