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Cupiennin 1a exhibits a remarkably broad, non-stereospecific cytolytic activity on bacteria, protozoan parasites, insects, and human cancer cells

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Abstract

Cupiennin 1a, a cytolytic peptide isolated from the venom of the spider Cupiennius salei, exhibits broad membranolytic activity towards bacteria, trypanosomes, and plasmodia, as well as human blood and cancer cells. In analysing the cytolytic activity of synthesised all-d- and all-l-cupiennin 1a towards pro- and eukaryotic cells, a stereospecific mode of membrane destruction could be excluded. The importance of negatively charged sialic acids on the outer leaflet of erythrocytes for the binding and haemolytic activity of l-cupiennin 1a was demonstrated. Reducing the overall negative charges of erythrocytes by partially removing their sialic acids or by protecting them with tri- or pentalysine results in reduced haemolytic activity of the peptide.

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Acknowledgments

We thank Dr. Heather Murray for critical comments on the manuscript, and the Swiss National Science Foundation for funding.

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Authors and Affiliations

  1. Institute of Ecology and Evolution, University of Bern, Baltzerstrasse 6, 3012, Bern, Switzerland

    Lucia Kuhn-Nentwig & Wolfgang Nentwig

  2. Department of Medicine Laboratory of Biochemistry, Interdisciplinary Research Centre, K.U. Leuven, Campus Kortrijk, 8500, Kortrijk, Belgium

    Jean Willems

  3. Institute of Cell Biology, University of Bern, Baltzerstrasse 4, 3012, Bern, Switzerland

    Thomas Seebeck

  4. Children’s Hospital Zürich, University Children’s Clinic, Steinwiesstrasse 75, 8032, Zurich, Switzerland

    Tarek Shalaby

  5. Swiss Tropical Institute, Socinstrasse 57, P.O. Box 4002, Basel, Switzerland

    Marcel Kaiser

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  1. Lucia Kuhn-Nentwig
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  2. Jean Willems
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  4. Tarek Shalaby
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  6. Wolfgang Nentwig
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Correspondence to Lucia Kuhn-Nentwig.

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Kuhn-Nentwig, L., Willems, J., Seebeck, T. et al. Cupiennin 1a exhibits a remarkably broad, non-stereospecific cytolytic activity on bacteria, protozoan parasites, insects, and human cancer cells. Amino Acids 40, 69–76 (2011). https://doi.org/10.1007/s00726-009-0471-0

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  • DOI: https://doi.org/10.1007/s00726-009-0471-0

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