engleski

ADAMANTYLTRIPEPTIDES ENTRAPPED INTO LIPOSOMES STUDIED BY SPIN LABELLING OF LIPOSOMES

The peptides of particular interest for pharmaceutical applications are those which exhibit immunological activity. Compounds comprising the elements of bacterical peptidoglycan structure have been recognized as an important group of immunomodulators. Synthetic adamantyltripeptides, D- and L-(adamant-2-yl)-Gly-L-Ala-D-isoGln (AdTP1 and AdTP2) comprise adamantyl moiety linked to dipeptide L-Ala-D-isoGln which is a structural element of natural peptidoglycans, were shown to exhibit versatile biological activity [1, 2]. We have been examinig their encapsulation into liposomes with the aim to increase and optimize their therapeutic effect. Adamantyltripeptides were studied entrapped into large multilamelar liposomes. In order to show how the examined peptides incorporated into liposomes affect membrane properties, electron spin resonance, a spin labelling method was used. The multilamelar liposomes were spin labelled with n-doxyl stearic acid (n=5, 7, 12, 16) and dynamic properties of the nitroxide label were studied as a function of the entrapped adamantyltripeptides. [1] Vranešić, B., Tomašić, J., Smerdel, S., Kantoci, D., Benedetti, F., Helv. Chim. Acta 76 (1993) 1752. [2] Tomašić, J., Hanzl-Dujmović, I., Špoljar, B., Vranešić, B., Šantak, M., Jovičić, A., Vaccine 8 (2000) 1236.

adamantiltripeptidi; liposomi; ESR

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