Structure-Dependent Effects of Glucose-Containing Analogs of Platelet Activating Factor (PAF) on Membrane Integrity
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Andre Wiese
Abstract
Synthetic cholinecontaining phospholipids comprise a new class of compounds with antineoplastic properties. We have investigated the effect of recently synthesized glucosecontaining analogs of lysophosphatidylcholine (glyceroglucophospholipid, GlcPC) and of lysoplatelet activating factor (GlcPAF) and its C16, C14 and C12 derivatives (ET-16, ET-14, and ET-12) on proliferation of immortalized human keratinocyte (HaCaT) cells. The data were compared to the ability of the compounds to intercalate into phosphatidylserine liposomes and to form lesions in planar bilayer membranes. A correlation between bioactivity and membrane activity was found. The number of molecules that intercalated into phosphatidylserine liposomes depended on the chemical structure of the compounds and was in the order GlcPAF [almost equal to] ET-16 [almost equal to] ET-14 [greater than] GlcPC [greater than] ET-12. All compounds induced membrane lesions, and the lesion forming activity was in the same order. Similar activity rankings were found for the release of lactate dehydrogenase from HaCaT cells as a measure of lytic activity and for the influence on cell number as a measure of proliferation. In the latter test, however, proliferation was already inhibited at nontoxic concentrations. From these findings, it may be concluded that the intercalation of the compounds at toxic concentrations leads to the formation of membrane lesions and finally results in membrane rupture leading to cell death.
Copyright © 2000 by Walter de Gruyter GmbH & Co. KG
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Articles in the same Issue
- The Twin-Arginine Translocation System: A Novel Means of Transporting Folded Proteins in Chloroplasts and Bacteria
- De Novo DNA Methylation at Nonrandom Founder Sites 5' from an Unmethylated Minimal Origin of DNA Replication in Latent Epstein-Barr Virus Genomes
- Trichostatin A Modulates Expression of p21waf1/cip1, Bcl-xL, ID1, ID2, ID3, CRAB2, GATA-2, hsp86 and TFIID/TAFII31 mRNA in Human Lung Adenocarcinoma Cells
- Effects of the Active Aldehyde Group Generated by RNA N-Glycosidase in the Sarcin/Ricin Domain of Rat 28S Ribosomal RNA on Peptide Elongation
- Responses to Peroxynitrite in Yeast: Glyceraldehyde-3-Phosphate Dehydrogenase (GAPDH) as a Sensitive Intracellular Target for Nitration and Enhancement of Chaperone Expression and Ubiquitination
- Enhancing the T R Transition of Insulin by Helix-Promoting Sequence Modifications at the N-Terminal B-Chain
- Structure-Dependent Effects of Glucose-Containing Analogs of Platelet Activating Factor (PAF) on Membrane Integrity
- Two Different Mechanisms for Activation of Cyclic PIP Synthase: by a G Protein or by Protein Tyrosine Phosphorylation
- 3-Hydroxybenzoate:Coenzyme A Ligase from Cell Cultures of Centaurium erythraea: Isolation and Characterization
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- Immunolabeling of CD3-Positive Lymphocytes with a Recombinant Single-Chain Antibody/Alkaline Phosphatase Conjugate
- Phage Display of RNase A and an Improved Method for Purification of Phages Displaying RNases
