Russian Journal of Bioorganic Chemistry, Vol. 24, No. 10, 1998, đ . 676

The Transport of Cytotoxic Liposomes to Malignant Cells by Means of Carbohydrate Determinants

E. L. Vodovozova, S. V. Khaidukov, G. P. Gaenko, T. N. Bondarchuk, I. I. Mikhalev, I. V. Grechishnikova, and Jul. G. Molotkovsky 1

Shemyakin–Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences,ul. Miklukho-Maklaya 16/10, GSP-7 Moscow , 117871 Russia

Abstract: A method for the synthesis of lipophilic glycoconjugates (vectors) was developed based on a polyethylene glycol-containing detergent. It was shown by flow cytofluorimetry that fluorescent labeled liposomes with the -galactosyl conjugate are bound to human leukemia HL-60 cells more effectively than liposomes embedded with the -glucosyl conjugate or vector-free liposomes. N-rac-1,2-Dioleoylglycero-3-oxalyl)rubomycin, a new lipid derivative of the antitumor drug rubomycin, was synthesized. Liposomes loaded with this lipid derivative and equipped with the galactosyl vector showed the greatest cytotoxic activity in vitro.

Key words: tumor cells, lectins, neoglycoconjugates, liposomes, cytotoxic drugs, lipid derivatives