Prostaglandin phospholipid conjugates with unusual biophysical and cytotoxic properties |
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Authors: | Palle J Pedersen Sidsel K Adolph Thomas L Andresen Mogens W Madsen Robert Madsen Mads H Clausen |
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Institution: | 1. Department of Chemistry, Technical University of Denmark, Kemitorvet, Building 201, DK-2800 Kgs. Lyngby, Denmark;2. LiPlasome Pharma A/S, Technical University of Denmark, Diplomvej 378, DK-2800 Kgs. Lyngby, Denmark;3. Department of Micro- and Nanotechnology, Technical University of Denmark, DK-4000 Roskilde, Denmark |
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Abstract: | The synthesis of two secretory phospholipase A2 IIA sensitive 15-deoxy-Δ12,14-prostaglandin J2 phospholipid conjugates is described and their biophysical and biological properties are reported. The conjugates spontaneously form particles in the liposome size region upon dispersion in an aqueous buffer and both phospholipids are hydrolyzed by phospholipase A2, but with different conversion rates and extent of hydrolysis. The cytotoxicity was evaluated in HT-29 and Colo205 cells and the conjugates induced cell death in the presence of phospholipase A2 and surprisingly also in the absence of the enzyme. |
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