Design and facile synthesis of neoglycolipids as lactosylceramide mimetics and their transformation into glycoliposomes

Biosci Biotechnol Biochem. 2005 Jan;69(1):166-78. doi: 10.1271/bbb.69.166.

Abstract

Neoglycolipids composed of disaccharide glycoside and phospholipid were designed and prepared as mimetics of lactosylceramide. The lactosyl- and N-acetyllactosaminyl-phospholipids (Lac-DPPA and LacNAc-DPPA) were enzymatically synthesized from lactose and LacNAc respectively by cellulase-mediated condensation with 1,6-hexanediol, followed by conjugation of the resulting glycosides and dipalmitoylphosphatidyl choline (DPPC) mediated by Streptomyces phospholipase D. Alternatively, allyl beta-lactoside was ozonolyzed to give an aldehyde, which was condensed with dipalmytoyl phosphatidyl ethanolamine to afford a second type of glycolipid (Lac-DPPE). NMR spectroscopy indicated that the neoglycolipids behave differently in different solvent systems. X-ray diffraction clearly showed that multilamellar vesicles (MLVs) of Lac-DPPE and Lac-DPPA-MLV are in the bilayer gel phase at 20 degrees C, whereas those of Lac-DPPE-MLV were in the lamellar liquid-crystalline phase at 50 degrees C. Differential scanning calorimetry showed that Lac-DPPE-MLV had complex thermotropic behavior depending on the incubation conditions. After a long incubation at 10 degrees C, endothermic transitions are observed at 39.6, 42.3 degrees C, and 42.9 degrees C. These neoglycolipids have the ability to trap calcein, a chelating derivative of fluorescein, in MLVs and showed specific binding to lectin in plate assays using fluorescently labeled compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calorimetry, Differential Scanning
  • Glycolipids / chemical synthesis*
  • Glycolipids / chemistry
  • Lactosylceramides / chemistry
  • Lectins / chemistry
  • Liposomes / chemistry*
  • Molecular Structure
  • X-Ray Diffraction

Substances

  • Glycolipids
  • Lactosylceramides
  • Lectins
  • Liposomes