Synthesis and biological evaluation of ceramide analogues with substituted aromatic rings or an allylic fluoride in the sphingoid moiety

J Med Chem. 2000 Nov 2;43(22):4189-99. doi: 10.1021/jm000939v.

Abstract

The biological activity of synthetic ceramide analogues, having modified sphingoid and N-acyl chains, as well as fluorine substituents in the allylic position, was investigated in hippocampal neurons. Their influence on axonal growth was compared to that of C(6)-N-acyl analogues of natural ceramides. D-erythro-Ceramides with a phenyl group in the sphingoid moiety and a short N-acyl chain were able to reverse the inhibitory effect of fumonisin B(1) (FB(1)), but not of D-threo-1-phenyl-2-decanoylamino-3-morpholino-1-propanol (PDMP), on accelerated axonal growth in hippocampal neurons. Moreover, we demonstrated that a ceramide analogue with an aromatic ring in the sphingoid moiety is recognized as a substrate by glucosylceramide synthase, which suggests that the observed biological effects are mediated by activation of the ceramide analogue via glucosylation. Introduction of a methyl, pentyl, fluoro, or methoxy substituent in the para position of the phenyl ring in the sphingoid moiety yielded partly active compounds. Likewise, substitution of the benzene ring for a thienyl group did not abolish the ability to reverse the inhibition of accelerated axonal growth by FB(1). Both D-erythro- and L-threo-ceramide analogues, having an allylic fluorine substituent, partly reversed the FB(1) inhibition.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Allyl Compounds / chemical synthesis*
  • Allyl Compounds / chemistry
  • Allyl Compounds / pharmacology
  • Animals
  • Axons / drug effects
  • Axons / physiology
  • Carboxylic Acids / antagonists & inhibitors
  • Cells, Cultured
  • Ceramides / chemical synthesis*
  • Ceramides / chemistry
  • Ceramides / pharmacology
  • Fumonisins*
  • Glucosyltransferases / metabolism
  • Golgi Apparatus / enzymology
  • Hippocampus / ultrastructure
  • Liver / ultrastructure
  • Rats
  • Rats, Wistar
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Allyl Compounds
  • Carboxylic Acids
  • Ceramides
  • Fumonisins
  • fumonisin B1
  • Glucosyltransferases
  • ceramide glucosyltransferase