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Study of the cholesterol extraction capacity of β-cyclodextrin and its derivatives, relationships with their effects on endothelial cell viability and on membrane models

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Abstract

Endothelial cells (HUVEC) were treated with β-cyclodextrin and hydroxypropylated or methylated derivatives solutions in order to quantify their cholesterol extraction capacity. Non-toxic concentrations of cyclodextrins (CDs) were determined following methyl thiazol tetrazolium (MTT) assays, total protein measurements, morphological observations and trypan blue assays. The residual cholesterol content of cells was measured and the extraction power of CDs compared to results obtained by phase solubility diagrams. Cholesterol was extracted with a dose-response relationship, the lowest residual cholesterol content being obtained with β-CD at 10 mM. Low substituted derivatives (Crysmeb® and hydroxypropyl-β-CD) maintained liposomes integrity (as shown before), were the less cytotoxic and presented the lowest affinity for cholesterol contrary to methylated derivatives with degrees of substitution around 2.

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Acknowledgement

This work has been supported financially by the Fonds Spéciaux pour la recherche from the University of Liège.

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Authors and Affiliations

  1. Laboratory of Pharmaceutical Technology, Department of Pharmacy, Drug Research Center, University of Liège, 1 av. de l’Hôpital, 4000, Liège, Belgium

    Delphine Castagne, Luc Delattre, Brigitte Evrard & Géraldine Piel

  2. Laboratory of Analytical Pharmaceutical Chemistry, Department of Pharmacy, Drug Research Center, University of Liège, 1 av. de l’Hôpital, 4000, Liège, Belgium

    Marianne Fillet

  3. Laboratory of Connective Tissues Biology, University of Liège, 3 av. de l’Hôpital, 4000, Liège, Belgium

    Betty Nusgens

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  1. Delphine Castagne
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Correspondence to Delphine Castagne.

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Castagne, D., Fillet, M., Delattre, L. et al. Study of the cholesterol extraction capacity of β-cyclodextrin and its derivatives, relationships with their effects on endothelial cell viability and on membrane models. J Incl Phenom Macrocycl Chem 63, 225–231 (2009). https://doi.org/10.1007/s10847-008-9510-9

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