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Title

Spectroscopic Detection of Endovesiculation by Large Unilamellar Phosphatidylcholine Vesicles: Effects of Chlorpromazine, Dibucaine, and Safingol

Authors
Tedesco, Maureen M.
Published in Bioorganic & Medicinal Chemistry. 1999, vol. 7, no. 7, p. 1373-1379
Abstract Endovesiculation by large unilamellar vesicles (LUVs) induced by cationic amphiphiles is described in this work. A recent procedure to monitor phagocytosis of vesicles by macrophages by determining the amount of the simultaneously internalized water-soluble fluorescent dye HPTS with external quencher was adapted to LUVs (Daleke, D. L.; Hong, K.; Papahadjopoulos, D. Biochim. Biophys. Acta 1990, 1024, 352). Compared to dibucaine and safingol, the local anesthetic chlorpromazine (CPZ) was found to be the most efficient inducer of HPTS-internalization by LUVs. Control experiments using LUVs with entrapped HPTS indicated that the observed dye-internalization does not originate from transient lysis. A strong increase in activity above the critical micelle concentration of CPZ implies the importance of CPZ-micelles for endovesiculation. The significantly less efficient CPZ-induced HPTS-internalization by LUVs with 68 nm compared to 176 nm diameter further diminishes the likelihood of a micelle/bilayer fusion mechanism and supports the presence of ‘zipper-type' endovesiculation by LUVs with diameters as small as 68 nm.
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TEDESCO, Maureen M., MATILE, Stefan. Spectroscopic Detection of Endovesiculation by Large Unilamellar Phosphatidylcholine Vesicles: Effects of Chlorpromazine, Dibucaine, and Safingol. In: Bioorganic & Medicinal Chemistry, 1999, vol. 7, n° 7, p. 1373-1379. https://archive-ouverte.unige.ch/unige:7889

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