Jump to ContentJump to Main Navigation
Show Summary Details
More options …

Biological Chemistry

Editor-in-Chief: Brüne, Bernhard

Editorial Board: Buchner, Johannes / Lei, Ming / Ludwig, Stephan / Thomas, Douglas D. / Turk, Boris / Wittinghofer, Alfred

IMPACT FACTOR 2018: 3.014
5-year IMPACT FACTOR: 3.162

CiteScore 2018: 3.09

SCImago Journal Rank (SJR) 2018: 1.482
Source Normalized Impact per Paper (SNIP) 2018: 0.820

See all formats and pricing
More options …
Volume 381, Issue 2


Structure-Dependent Effects of Glucose-Containing Analogs of Platelet Activating Factor (PAF) on Membrane Integrity

Andre Wiese / Thomas Wieder / Michael Mickeleit / Susanne Reinöhl / Christoph C. Geilen / Ulrich Seydel / Werner Reutter
Published Online: 2005-06-01 | DOI: https://doi.org/10.1515/BC.2000.019


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.

About the article

Published Online: 2005-06-01

Published in Print: 2000-02-15

Citation Information: Biological Chemistry, Volume 381, Issue 2, Pages 135–144, ISSN (Print) 1431-6730, DOI: https://doi.org/10.1515/BC.2000.019.

Export Citation

Citing Articles

Here you can find all Crossref-listed publications in which this article is cited. If you would like to receive automatic email messages as soon as this article is cited in other publications, simply activate the “Citation Alert” on the top of this page.

A. Hildmann, T. Kairaliyeva, K. Danker, V. Shmanai, V.B. Fainerman, and R. Miller
Colloids and Surfaces A: Physicochemical and Engineering Aspects, 2017
Annette Hildmann and Kerstin Danker
European Journal of Lipid Science and Technology, 2014, Volume 116, Number 9, Page 1108
Geo Semini, Annette Hildmann, Andreas Klein, Lothar Lucka, Margarete Schön, Michael P. Schön, Vadim Shmanai, and Kerstin Danker
Biochemical Pharmacology, 2014, Volume 87, Number 3, Page 477
Kerstin Danker, Werner Reutter, and Geo Semini
British Journal of Pharmacology, 2010, Volume 160, Number 1, Page 36
M Potier, A Chantome, V Joulin, A Girault, S Roger, P Besson, M-L Jourdan, J-Y LeGuennec, P Bougnoux, and C Vandier
British Journal of Pharmacology, 2011, Volume 162, Number 2, Page 464
Geo Semini, Andreas Klein, and Kerstin Danker
Pharmacogenetics and Genomics, 2011, Volume 21, Number 7, Page 375
Geo Semini, Annette Hildmann, Hans-Ulrich Reissig, Werner Reutter, and Kerstin Danker
Biochemical Pharmacology, 2011, Volume 81, Number 8, Page 985
Clarissa von Haefen, Jana Wendt, Geo Semini, Marco Sifringer, Claus Belka, Silke Radetzki, Werner Reutter, Peter T. Daniel, and Kerstin Danker
Apoptosis, 2011, Volume 16, Number 6, Page 636
Annette Fischer, Dieter Müller, Martin Zimmermann-Kordmann, Burkhard Kleuser, Michael Mickeleit, Stephan Laabs, Werner Löwe, Frédéric Cantagrel, Werner Reutter, and Kerstin Danker
ChemBioChem, 2006, Volume 7, Number 3, Page 441
Faustino Mollinedo
Expert Opinion on Therapeutic Patents, 2007, Volume 17, Number 4, Page 385

Comments (0)

Please log in or register to comment.
Log in