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Plos One : Complexation of C6-ceramide with Cholesteryl Phosphocholine – a Potent Solvent-free Ceramide Delivery Formulation for Cells in Culture, Volume 8

By Siskind, Leah, J.

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Book Id: WPLBN0003945765
Format Type: PDF eBook :
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Reproduction Date: 2015

Title: Plos One : Complexation of C6-ceramide with Cholesteryl Phosphocholine – a Potent Solvent-free Ceramide Delivery Formulation for Cells in Culture, Volume 8  
Author: Siskind, Leah, J.
Volume: Volume 8
Language: English
Subject: Journals, Science, Medical Science
Collections: Periodicals: Journal and Magazine Collection (Contemporary)
Historic
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Publisher: Plos

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Siskind, L. J. (n.d.). Plos One : Complexation of C6-ceramide with Cholesteryl Phosphocholine – a Potent Solvent-free Ceramide Delivery Formulation for Cells in Culture, Volume 8. Retrieved from http://www.nationalpubliclibrary.info/


Description
Description : Ceramides are potent bioactive molecules in cells. However, they are very hydrophobic molecules, and difficult to deliver efficiently to cells. We have made fluid bilayers from a short-chain D-erythro-ceramide (C6-Cer) and cholesteryl phosphocholine (CholPC), and have used this as a formulation to deliver ceramide to cells. C6-Cer complexed with CholPC led to much larger biological effects in cultured cells (rat thyroid FRTL-5 and human HeLa cells in culture) compared to C6- Cer dissolved in dimethyl sulfoxide (DMSO). Inhibition of cell proliferation and induction of apoptosis was significantly more efficient by C6-Cer/CholPC compared to C6-Cer dissolved in DMSO. C6-Cer/CholPC also permeated cell membranes and caused mitochondrial Ca2+ influx more efficiently than C6-Cer in DMSO. Even though CholPC was taken up by cells to some extent (from C6-Cer/CholPC bilayers), and was partially hydrolyzed to free cholesterol (about 9%), none of the antiproliferative effects were due to CholPC or excess cholesterol. The ceramide effect was not limited to D-erythro-C6-Cer, since L-erythro-C6-Cer and D-erythro-C6-dihydroCer also inhibited cell priolifereation and affected Ca2+ homeostasis. We conclude that C6-Cer complexed to CholPC increased the bioavailability of the short-chain ceramide for cells, and potentiated its effects in comparison to solvent-dissolved C6-Cer. This new ceramide formulation appears to be superior to previous solvent delivery approaches, and may even be useful with longer-chain ceramides

 

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