engleski

Entrapment of peptidoglycan monomer and its derivative Boc-L-tyrosil-peptidoglycan monomer into the liposomes

Peptidoglycan monomer (PGM, -D-GlcNAc-(1→4)-MurNAc-L-Ala-D-isoGln-meso-A2pm (εNH2)-D-Ala-D-Ala is a repeating unit of Brevibacteruim divaricatum cell wall peptidoglycan. It exhibits strong immunomodulating, antitumor and antimetatastic activity. In an effort to enhance or influence the biological activity of PGM, its derivative Boc-L-tyrosyl-peptidoglycan monomer was prepared. Although the structure of original PGM molecule has been considerably changed by introduction sixth amino acid, the new sinthetic derivative exhibited wery similar biological activity to the activity of PGM. Liposomes, or lipid vesicles, are spherical, self-closed structure composed of curved lipid bilayers which entrap part of the solvent into their interior. The unique properties of liposomes have triggered numerous applications of liposomes in various fields of science and tehnology, from basic studies of the shape of cells and membrane mechanisms to application such as drug delivery sistems and cosmetics. In this work we examined the incorporation of the PGM and its derivative into the liposomes in order to possibly increase and optimize their therapeutic efficacy. The large multilamellar negatively charged vesicles using egg lecithin were prepared. The liposome dispersions were chromatographed on the Sephadex G-50 or centrifuged in ultracentrifuge. The entrapment of peptidoglycans and stability of respective preparations was followed in two ways: a) by the use of 14C-labelled peptidoglycans or b) by HPLC Regardless of the experimental conditions and the procedure used, only up to 14% of studied peptidoglycans could be entrapped into liposomes or incorporated into the lipid bilayer.

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